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Journal articles on the topic 'Bi-peptide'

Author: Grafiati
Published: 4 June 2021
Last updated: 17 February 2022

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1

Schiller, Peter W. "Bi- or multifunctional opioid peptide drugs." Life Sciences 86, no. 15-16 (April 2010): 598–603. http://dx.doi.org/10.1016/j.lfs.2009.02.025.

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2

Diaferia, Carlo, Francesca Netti, Moumita Ghosh, Teresa Sibillano, Cinzia Giannini, Giancarlo Morelli, Lihi Adler-Abramovich, and Antonella Accardo. "Bi-functional peptide-based 3D hydrogel-scaffolds." Soft Matter 16, no. 30 (2020): 7006–17. http://dx.doi.org/10.1039/d0sm00825g.

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3

Li, Yueting, Guangfu Yin, Ximing Pu, Xianchun Chen, Xiaoming Liao, and Zhongbing Huang. "Novel Bi-Functional 14-mer Peptides with Both Ovarian Carcinoma Cells Targeting and Magnetic Fe3O4Nanoparticles Affinity." Materials 12, no. 5 (March 5, 2019): 755. http://dx.doi.org/10.3390/ma12050755.

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Fe3O4 magnetic nanoparticles (Fe3O4-MNPs) have attracted much interest for their potential medical applications due to their desirable magnetic properties. However, their potential cytotoxicity, high RES clearance in circulation, and nonspecific distribution in tissue might be the main obstacles in practice. In the present study, a novel bi-functional 14-mer peptide with both ovarian carcinoma cells targeting and magnetic Fe3O4 nanoparticles affinity was designed and synthesized, and then a facile and effective modification method was developed to bestow the Fe3O4-MNPs with tumor-targeting capability via modification, using the bi-functional peptides. First, on the basis of a tumor-targeting 7-mer peptide QQTNWSL (Q-L) and another Fe3O4-MNPs-targeting 7-mer peptide TVNFKLY (T-Y)—screened by phage-displayed peptide libraries—two bi-functional 14-mer peptides sequenced as LSWNTQQ-YLKFNVT (abbreviated as LQ-YT) and QQTNWSL-YLKFNVT (QL-YT) were synthesized through combining the Q-L peptide and T-Y peptide in predetermined configurations. Their specificity for bonding with A2780 tumor cells and affinity for Fe3O4-MNPs were verified. Then the bi-functional 14-mer peptides were applied to modify the Fe3O4-MNPs. Results showed that both bi-functional 14-mer peptides could be conjugated to the Fe3O4-MNPs surface with high affinity. Immunofluorescence and Prussian blue staining assays indicated that the LQ-YT-modified Fe3O4-MNPs could specifically bond to A2780 tumor cells. In addition to our findings suggesting that more β-turns and random coils are conducive to increasing polypeptide surface area for binding and exposing the target group and bonding sites on LQ-YT to external targets, we demonstrated that the bi-functional 14-mer peptide has affinity for Fe3O4-MNPs, and that Fe3O4-MNPs, which was modified with a 14-mer peptide, could be bestowed with a targeting affinity for ovarian carcinoma cells.
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4

Chen, Ming, Shuanglong Wang, and Xihan Yu. "Cryptand-imidazolium supported total synthesis of the lasso peptide BI-32169 and its d-enantiomer." Chemical Communications 55, no. 23 (2019): 3323–26. http://dx.doi.org/10.1039/c8cc10301a.

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The first total synthesis of natural lasso peptide is reported, in which cryptand-imidazolium complex support manipulates the peptide chain to achieve a lasso peptide configuration of BI-32169. Moreover, the synthesis of d-enantiomeric lasso peptide via this new method opens up new horizons in the study of lasso peptides.
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5

Qiu, Yibo, Xinya Hemu, Ding Xiang Liu, and James P. Tam. "Selective Bi-directional Amide Bond Cleavage ofN-Methylcysteinyl Peptide." European Journal of Organic Chemistry 2014, no. 20 (June 6, 2014): 4370–80. http://dx.doi.org/10.1002/ejoc.201402261.

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6

Lee, So Youn, Eun Jae Jang, In-Ho Bae, Dae Sung Park, Doo Sun Sim, and MyungHo Jeong. "Efficacy of dextran and peptide-everolimus bi-directional stent." Journal of Biomaterials Applications 33, no. 9 (February 18, 2019): 1232–41. http://dx.doi.org/10.1177/0885328218822664.

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Everolimus inhibits stent restenosis and the WKYMV (fluorescein isothiocyanate) peptide promotes endothelial homing. Dextran is a natural polymer that is widely used as a pharmaceutical agent. The purpose of this study was to develop a double-drug-coated stent using a bidirectional coating system and to examine the surface shape with in vitro experiments. Stent length was 16 mm and strut thickness was 70 µm (Chonnam National University Hospital Tiger stent). Optical and scanning electron microscopy showed good coating without cracks or bubbles. Fluorescein isothiocyanate-peptide was dip-coated on the lumen and the abluminal surface was coated with everolimus and dextran. Stents were coated with dextran, everolimus, or everolimus–dextran. The radial force and flexibility were measured to determine the mechanical properties. Contact angle testing was performed in all groups. Dextran and peptide as hydrophilic substances and everolimus as a hydrophobic substance were each coated on cover glasses (cobalt–chromium). A10 and human umbilical vein endothelial cells were used in the experiments. Water and dimethyl sulfoxide served as a control, and three drug groups were tested: peptide–everolimus, everolimus–dextran, and peptide–everolimus–dextran. Immunocytochemistry was performed to assess cell adhesion. Light intensity was plotted according to the average on nuclear staining. Experiments were conducted using 5-bromo-2′-deoxyuridine to investigate A10 and human umbilical vein endothelial cell proliferation. Cell adhesion and proliferation of peptide–everolimus–dextran were inhibited at A10, and human umbilical vein endothelial cell was found to proliferate with cell adhesion. On conclusion, dextran and peptide–everolimus bidirectional stent is effective in re-endothelialization and inhibition of cell proliferation.
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7

Iijima, Kazutoshi, Hiroumi Nagahama, Akari Takada, Toshiki Sawada, Takeshi Serizawa, and Mineo Hashizume. "Surface functionalization of polymer substrates with hydroxyapatite using polymer-binding peptides." Journal of Materials Chemistry B 4, no. 21 (2016): 3651–59. http://dx.doi.org/10.1039/c6tb00624h.

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Polymer substrates were modified with hydroxyapatite (HAp) using two bi-functional peptides consists of polymer-binding peptide and triasparate for HAp mineralization in simulated body fluids and HAp-binding peptide for immobilization HAp nanoparticles.
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8

Lee, Geum-Hwa, Taeho Ahn, Do-Sung Kim, Seoung Ju Park, Yong Chul Lee, Wan Hee Yoo, Sung Jun Jung, et al. "Bax Inhibitor 1 Increases Cell Adhesion through Actin Polymerization: Involvement of Calcium and Actin Binding." Molecular and Cellular Biology 30, no. 7 (February 1, 2010): 1800–1813. http://dx.doi.org/10.1128/mcb.01357-09.

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ABSTRACT Bax inhibitor 1 (BI-1), a transmembrane protein with Ca2+ channel-like activity, has antiapoptotic and anticancer activities. Cells overexpressing BI-1 demonstrated increased cell adhesion. Using a proteomics tool, we found that BI-1 interacted with γ-actin via leucines 221 and 225 and could control actin polymerization and cell adhesion. Among BI-1−/− cells and cells transfected with BI-1 small interfering RNA (siRNA), levels of actin polymerization and cell adhesion were lower than those among BI-1+/+ cells and cells transfected with nonspecific siRNA. BI-1 acts as a leaky Ca2+ channel, but mutations of the actin binding sites (L221A, L225A, and L221A/L225A) did not change intra-endoplasmic reticulum Ca2+, although deleting the C-terminal motif (EKDKKKEKK) did. However, store-operated Ca2+ entry (SOCE) is activated in cells expressing BI-1 but not in cells expressing actin binding site mutants, even those with the intact C-terminal motif. Consistently, actin polymerization and cell adhesion were inhibited among all the mutant cells. Compared to BI-1+/+ cells, BI-1−/− cells inhibited SOCE, actin polymerization, and cell adhesion. Endogenous BI-1 knockdown cells showed a similar pattern. The C-terminal peptide of BI-1 (LMMLILAMNRKDKKKEKK) polymerized actin even after the deletion of four or six charged C-terminal residues. This indicates that the actin binding site containing L221 to D231 of BI-1 is responsible for actin interaction and that the C-terminal motif has only a supporting role. The intact C-terminal peptide also bundled actin and increased cell adhesion. The results of experiments with whole recombinant BI-1 reconstituted in membranes also coincide well with the results obtained with peptides. In summary, BI-1 increased actin polymerization and cell adhesion through Ca2+ regulation and actin interaction.
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9

Gungormus, Mustafa, Monica Branco, Hanson Fong, Joel P. Schneider, Candan Tamerler, and Mehmet Sarikaya. "Self assembled bi-functional peptide hydrogels with biomineralization-directing peptides." Biomaterials 31, no. 28 (October 2010): 7266–74. http://dx.doi.org/10.1016/j.biomaterials.2010.06.010.

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10

Liu, Min, Nan Liu, Yaxiong Yang, Bo Yang, and Xiaodong Liu. "Rational Design of Peptide Modulators Bi-Directionally Tuning Cav1.3 Channels." Biophysical Journal 106, no. 2 (January 2014): 332a. http://dx.doi.org/10.1016/j.bpj.2013.11.1904.

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11

Yeh, Y. C., G. Y. Hwang, and V. C. Yang. "Identification Of Scavenger Receptor Sr-Bi In The Endothelial Cells And The Smooth Muscle Cells Of Rat Aorta In Vitro." Microscopy and Microanalysis 5, S2 (August 1999): 1338–39. http://dx.doi.org/10.1017/s1431927600020018.

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The class B ,type I scavenger receptor (SR-BI) was the first molecularly well defined cell surface receptor which binds HDL and mediates the selective uptake of HDL cholesteryl ester. It is expressed primarily in liver and steroidogenic tissues. However, the recent studies also suggested a potentially important role of SR-BI in the initial steps of cholesterol efflux in the peripheral tissues. In this study, we have used immunoblotting and immunofluorescence microscopy to study the expression and subcellular localization of SR-BI in the cultured endothelial cells and the smooth muscle cells of rat aorta.A peptide containing residues 495 to 509 from mSR-BI plus an NH2-terminal cysteine was coupled to hemocyanin. Then the peptide was used to generate mSR-BI495 antiserum in New Zealand white rabbits. The cells from the aortic ring of 1-month-old Spraque-Dawly rats were grown in the dishes containing complete medium (Dulbecco's modified Eagle's medium with 10% fetal bovine serum) and incubated at 37°C in 95% air/ 10 % CO2 atmosphere for 3-4 days.
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12

Lu, Jingxiong, Hsin-Hui Shen, Zhangxiong Wu, Bo Wang, Dongyuan Zhao, and Lizhong He. "Self-assembly of bi-functional peptides on large-pore mesoporous silica nanoparticles for miRNA binding and delivery." Journal of Materials Chemistry B 3, no. 39 (2015): 7653–57. http://dx.doi.org/10.1039/c5tb01133g.

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13

Pham, Ngoc B., Wen Liu, Nathan R. Schueller, Ellen S. Gawalt, Yong Fan, and Wilson S. Meng. "Toward reducing biomaterial antigenic potential: a miniaturized Fc-binding domain for local deposition of antibodies." Biomaterials Science 7, no. 3 (2019): 760–72. http://dx.doi.org/10.1039/c8bm01220b.

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14

Arafat, Md Easin, Md Wakil Ahmad, S. M. Shovan, Abdollah Dehzangi, Shubhashis Roy Dipta, Md Al Mehedi Hasan, Ghazaleh Taherzadeh, Swakkhar Shatabda, and Alok Sharma. "Accurately Predicting Glutarylation Sites Using Sequential Bi-Peptide-Based Evolutionary Features." Genes 11, no. 9 (August 31, 2020): 1023. http://dx.doi.org/10.3390/genes11091023.

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Post Translational Modification (PTM) is defined as the alteration of protein sequence upon interaction with different macromolecules after the translation process. Glutarylation is considered one of the most important PTMs, which is associated with a wide range of cellular functioning, including metabolism, translation, and specified separate subcellular localizations. During the past few years, a wide range of computational approaches has been proposed to predict Glutarylation sites. However, despite all the efforts that have been made so far, the prediction performance of the Glutarylation sites has remained limited. One of the main challenges to tackle this problem is to extract features with significant discriminatory information. To address this issue, we propose a new machine learning method called BiPepGlut using the concept of a bi-peptide-based evolutionary method for feature extraction. To build this model, we also use the Extra-Trees (ET) classifier for the classification purpose, which, to the best of our knowledge, has never been used for this task. Our results demonstrate BiPepGlut is able to significantly outperform previously proposed models to tackle this problem. BiPepGlut achieves 92.0%, 84.8%, 95.6%, 0.82, and 0.88 in accuracy, sensitivity, specificity, Matthew’s Correlation Coefficient, and F1-score, respectively. BiPepGlut is implemented as a publicly available online predictor.
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15

Park, Byung-Wook, Rui Zheng, Kyoung-A. Ko, Brent D. Cameron, Do-Young Yoon, and Dong-Shik Kim. "A novel glucose biosensor using bi-enzyme incorporated with peptide nanotubes." Biosensors and Bioelectronics 38, no. 1 (October 2012): 295–301. http://dx.doi.org/10.1016/j.bios.2012.06.005.

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16

Hirsch, Jochen R., Nikola Skutta, and Eberhard Schlatter. "Signaling and distribution of NPR-Bi, the human splice form of the natriuretic peptide receptor type B." American Journal of Physiology-Renal Physiology 285, no. 2 (August 2003): F370—F374. http://dx.doi.org/10.1152/ajprenal.00049.2003.

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Recently, we described a splice variant of the human natriuretic peptide receptor type B (NPR-Bi) in human proximal tubule cells [immortalized human kidney epithelial cells (IHKE-1) that lacks a functional guanylate cyclase domain (Hirsch JR, Meyer M, Mägert HJ, Forssmann WG, Mollerup S, Herter P, Weber G, Cermak R, Ankorina-Stark I, Schlatter E, and Kruhøffer M. J Am Soc Nephrol 10: 472–480, 1999). Its signaling pathway does not include cGMP, cAMP, or Ca2+ but leads to inhibition of K+ channels. In patch-clamp experiments, effects of tyrosine kinase receptor blockers on C-type natriuretic peptide (CNP)-mediated depolarizations of membrane voltages ( Vm) of IHKE-1 cells were tested. The epidermal growth factor (EGF) receptor blocker genistein (10 μM) abolished the effect of CNP (0.2 ± 0.4 mV, n = 7), and comparable results were obtained with 10 μM daidzein ( n = 8). Aminogenistein (10 μM, n = 5) and tyrphostin AG1295 (10 μM, n = 5) had no significant effects. EGF (1 nM) hyperpolarized cells by –5.3 ± 0.8 mV ( n = 5). This effect was completely blocked by genistein or daidzein. The Cl– channel blocker NPPB (10 μM, n = 5) inhibited the EGF-mediated hyperpolarization. mRNA expression of NPR-B and NPR-Bi shows reversed patterns along the human nephron. NPR-B is highly expressed in glomeruli and proximal tubules, whereas NPR-Bi shows strong signals in the distal nephron. Expression of NPR-Bi in the cortical collecting duct was also confirmed with immunohistochemistry. In other human tissues, NPR-Bi shows strongest expression in pancreas and lung, whereas in the heart and liver NPR-B is the dominating receptor. In conclusion, CNP inhibits an apical K+ channel in IHKE-1 cells independently of cGMP and so far this effect can only be blocked by genistein and daidzein. Tyrosine phosphorylation might be the missing link in the signaling pathway of CNP/NPR-Bi.
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17

Chen, Ming, Shuanglong Wang, and Xihan Yu. "Correction: Cryptand-imidazolium supported total synthesis of the lasso peptide BI-32169 and its d-enantiomer." Chemical Communications 56, no. 63 (2020): 9040. http://dx.doi.org/10.1039/d0cc90330b.

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18

Pöhler, Alexander, Janine Faigle, and Roland F. Staack. "Evaluation of potential biotin interference in immunogenicity testing." Bioanalysis 11, no. 17 (September 2019): 1547–54. http://dx.doi.org/10.4155/bio-2019-0080.

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Aim: One-step bridging assays typically used for immunogenicity testing may be challenged by biotin interference (BI) caused by widely available dietary supplementation or medically prescribed high-dose therapies. We investigated BI in two one-step antidrug antibody assays. Results: Both assays showed biotin-related interference, with the peptide-based assay being less affected than the antibody-based assay. BI was reduced by minimum required dilution adaption from 10 to 1% and eliminated by a depletion-based sample pretreatment. Conclusion: Increased biotin levels have the potential to interfere with immunogenicity testing methods that use biotin technology. Since the extent of interference differs from assay to assay, assessment during development phase is recommended. Minimum required dilution adjustment or sample pretreatment are options to reduce or eliminate BI.
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19

Wen, Cui-jiao, Jia-yuan Gong, Ke-wei Zheng, Yi-de He, Jia-yu Zhang, Yu-hua Hao, and Zheng Tan. "Targeting nucleic acids with a G-triplex-to-G-quadruplex transformation and stabilization using a peptide–PNA G-tract conjugate." Chemical Communications 56, no. 48 (2020): 6567–70. http://dx.doi.org/10.1039/d0cc02102d.

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The synergy between two recognizing units in a bi-functional peptide–PNA G-tract conjugate recognizes a three guanine-tracts motif to form an extra stable bimolecular complex, resulting in highly potent and selective interference to DNA metabolism.
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20

Mirzaei, Mahmoud. "Formation of a peptide assisted bi-graphene and its properties: DFT studies." Superlattices and Microstructures 54 (February 2013): 47–53. http://dx.doi.org/10.1016/j.spmi.2012.11.006.

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21

Norenberg, J. P., B. J. Krenning, I. R. Konings, M. de Jong, A. Sri-nivasan, K. Garmestani, M. W. Brechbiel, and L. K. Kvols. "213Bi[Dota0, Tyr3]octreotide (Bi-DOTATOC) in peptide receptor radionuclide therapy (PRRT)." Nuclear Medicine Communications 20, no. 4 (April 1999): 383. http://dx.doi.org/10.1097/00006231-199904000-00081.

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22

Lingasamy, Prakash, Allan Tobi, Maarja Haugas, Hedi Hunt, Päärn Paiste, Toomas Asser, Tõnu Rätsep, Venkata Ramana Kotamraju, Rolf Bjerkvig, and Tambet Teesalu. "Bi-specific tenascin-C and fibronectin targeted peptide for solid tumor delivery." Biomaterials 219 (October 2019): 119373. http://dx.doi.org/10.1016/j.biomaterials.2019.119373.

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23

Diener, Hans-Christoph, Piero Barbanti, Carl Dahlöf, Uwe Reuter, Julia Habeck, and Jana Podhorna. "BI 44370 TA, an oral CGRP antagonist for the treatment of acute migraine attacks: Results from a phase II study." Cephalalgia 31, no. 5 (December 20, 2010): 573–84. http://dx.doi.org/10.1177/0333102410388435.

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Methods: Four hundred and sixty-one adult subjects with migraine were randomised to one of five treatments, the oral antagonist at the calcitonin gene-related peptide (CGRP) receptor BI 44370 TA (50 mg, 200 mg, 400 mg), active comparator eletriptan 40 mg or placebo. The analysis included 341 subjects who took study medication. Results: The primary endpoint, pain-free after two hours, was reached by significantly more subjects in the BI 44370 TA 400 mg (20/73 = 27.4%) and eletriptan 40 mg (24/69 = 34.8%) groups compared to placebo (6/70 = 8.6%, p = .0016), but not by subjects in the BI 44370 TA 200 mg group (14/65 = 21.5%). The effect of 50 mg BI 44370 TA (5/64 = 7.8%) was similar to that of placebo. Analysis of secondary endpoints supported the conclusion from the primary analysis. The frequency of adverse events was low in all groups. Conclusion: Efficacy of BI 44370 TA was shown in a dose-dependent manner in the treatment of acute migraine attacks.
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24

Stephenson, Rachel J., Fran Wolber, Paul G. Plieger, and David R. K. Harding. "Synthesis and Characterization of Bradykinin Derivatives Based on a β-Cyclodextrin Core." Australian Journal of Chemistry 69, no. 3 (2016): 328. http://dx.doi.org/10.1071/ch15460.

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Mono-6A-fluorenylmethyloxycarbonylamino-mono-6X-succinyl-β-cyclodextrin (1), an amino acid-based bi-functionalized derivative of β-cyclodextrin (β-CD), has been functionalized with the bioactive peptide, bradykinin and/or sulfonamides using fluorenylmethyloxycarbonyl (Fmoc) solid phase peptide synthesis (SPPS). The all-in-one molecule contains a carrier (cyclodextrin), targeting agent (bradykinin), and/or model drug (sulfonamide). Varying combinations of these bradykinin-focussed molecules have been synthesized using Fmoc SPPS on Rink amide resin. The positioning of the sulfonamide group, the bradykinin peptide and the cyclodextrin carrier are essential for biological activity. The inclusion of spacers is also important. Structure–activity studies performed on three cancer cell lines in vitro support these conclusions.
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25

Proudfoot, Sarah C., and Daisy Sahoo. "Proline residues in scavenger receptor-BI's C-terminal region support efficient cholesterol transport." Biochemical Journal 476, no. 6 (March 22, 2019): 951–63. http://dx.doi.org/10.1042/bcj20180831.

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Abstract High-density lipoproteins (HDLs) facilitate reverse cholesterol transport, a process in which HDL removes cholesterol from circulation and carries it to the liver for biliary excretion. Reverse cholesterol transport is also facilitated by HDL's high-affinity receptor, scavenger receptor-BI (SR-BI), by mechanisms that are not fully understood. To improve our understanding of SR-BI function, we previously solved the NMR (nuclear magnetic resonance) structure of a peptide encompassing amino acids 405–475 of SR-BI. This segment of SR-BI, that includes the functionally critical C-terminal transmembrane domain and part of the extracellular domain, also contains four conserved proline (Pro) residues. We hypothesized that these proline residues support SR-BI in a conformation that allows for efficient cholesterol transport. To test this, we generated individual Pro-to-alanine mutations in full-length SR-BI and transiently expressed the mutant receptors in COS-7 cells to measure the effects on SR-BI-mediated cholesterol transport functions. Our findings reveal that HDL cell association and uptake of HDL-cholesteryl esters are impaired by mutation of Pro-412, Pro-438, or the transmembrane proline kink residue (Pro-459). In addition, SR-BI-mediated cholesterol efflux and membrane cholesterol distribution are impaired by mutation of Pro-412 or Pro-438, indicating that these residues are essential for a fully functional SR-BI receptor. Furthermore, we demonstrate that Pro-408 is necessary for proper SR-BI expression, but mutation of Pro-408 does not cause SR-BI to become misfolded or rapidly degraded by the proteasome or the lysosome. We conclude that key proline residues play an important role in SR-BI function by allowing for the efficient transport of cholesterol between cells and HDL.
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Potterat, Olivier, Klaus Wagner, Gerd Gemmecker, Jürgen Mack, Carsten Puder, Regine Vettermann, and Rüdiger Streicher. "BI-32169, a Bicyclic 19-Peptide with Strong Glucagon Receptor Antagonist Activity fromStreptomycessp." Journal of Natural Products 67, no. 9 (September 2004): 1528–31. http://dx.doi.org/10.1021/np040093o.

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27

Chao, Celia, and Mark R. Hellmich. "Bi-directional Signaling between Gastrointestinal Peptide Hormone Receptors and Epidermal Growth Factor Receptor." Growth Factors 22, no. 4 (December 2004): 261–68. http://dx.doi.org/10.1080/08977190412331286900.

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28

de Koster, H. S., D. C. Anderson, and A. Termijtelen. "T cells sensitized to synthetic HLA-DR3 peptide give evidence of continuous presentation of denatured HLA-DR3 molecules by HLA-DP." Journal of Experimental Medicine 169, no. 3 (March 1, 1989): 1191–96. http://dx.doi.org/10.1084/jem.169.3.1191.

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T cell clones raised against a synthetic peptide, identical to the third hypervariable region of the DR3 BI chain, were tested for secondary proliferative responses against a panel of PBLs. All seven DR3 DPw3+ stimulators could induce proliferation. DR3- DPw3+ PBLs were recognized when the synthetic peptide was added to the cultures. Inhibition studies with mAbs showed that in both cases the HLA-DP molecule is involved in the recognition of both types of stimulators. We conclude that the clones recognize the DR3 peptide presented by HLA-DPw3. This stimulus can be obtained in two different ways: (a) by addition of synthetic peptide to DPw3+ PBLs or (b) by using DR3 DPw3+ stimulator cells where DR3 peptides are present in the culture as a product of denaturation of the DR3 molecule. Because all DR3 DPw3+ PBLs tested could stimulate the line and clones, we assume that the presentation of the DR3 peptide by DP is a naturally and continuously occurring phenomenon.
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MESSINA, CALOGERO S., HANS WEIHER, and INGO G. H. SCHMIDT-WOLF. "Targeting Prostate Cancer with a Combination of WNT Inhibitors and a Bi-functional Peptide." Anticancer Research 37, no. 2 (February 10, 2017): 555–60. http://dx.doi.org/10.21873/anticanres.11348.

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30

Yoshimatsu, Keiichi, Jason LeJeune, David A. Spivak, and Lei Ye. "Peptide-imprinted polymer microspheres prepared by precipitation polymerization using a single bi-functional monomer." Analyst 134, no. 4 (2009): 719. http://dx.doi.org/10.1039/b814967d.

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31

Sandra, Koen, Mahan Moshir, Filip D’hondt, Robin Tuytten, Katleen Verleysen, Koen Kas, Isabelle François, and Pat Sandra. "Highly efficient peptide separations in proteomicsPart 2: Bi- and multidimensional liquid-based separation techniques." Journal of Chromatography B 877, no. 11-12 (April 15, 2009): 1019–39. http://dx.doi.org/10.1016/j.jchromb.2009.02.050.

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32

Yang, Jingsong, Francesca Zappacosta, Roland S. Annan, Kelvin Nurse, Peter J. Tummino, Robert A. Copeland, and Zhihong Lai. "The catalytic role of INCENP in Aurora B activation and the kinetic mechanism of Aurora B/INCENP." Biochemical Journal 417, no. 1 (December 12, 2008): 355–60. http://dx.doi.org/10.1042/bj20081365.

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Aurora kinases are a family of serine/threonine protein kinases that play essential roles in mitosis and cytokinesis. AurB (Aurora B kinase) has shown a clear link to cancer and is being pursued as an attractive cancer target. Multiple small molecules targeting AurB have entered the clinic for the treatment of cancer. A protein cofactor, INCENP (inner centromere protein), regulates the cellular localization and activation of AurB. In the present study, we examined the effect of INCENP on the activation kinetics of AurB and also elucidated the kinetic mechanism of AurB-catalysed substrate phosphorylation. We have concluded that: (i) substoichoimetric concentrations of INCENP are sufficient for AurB autophosphorylation at the activation loop residue Thr232, and hence INCENP plays a catalytic role in AurB autophosphorylation; (ii) AurB/INCENP-catalysed phosphorylation of a peptide substrate proceeds through a rapid equilibrium random Bi Bi kinetic mechanism; and (iii) INCENP has relatively minor effects on the specific activity of AurB using a peptide substrate when compared with its role in AurB autoactivation. These results indicate that the effects of INCENP, and probably accessory proteins in general, may differ when enzymes are acting on different downstream targets.
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Lin, Kaiping, Qi Lv, Xiaoling Yang, Ting Lin, Min Feng, and Xiaxia Chen. "Glucagon-like peptide-1 receptor agonist versus basal insulin in type-2 diabetic patients: An efficacy and safety analysis." Tropical Journal of Pharmaceutical Research 19, no. 10 (November 26, 2020): 2213–17. http://dx.doi.org/10.4314/tjpr.v19i10.27.

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Purpose: To compare the effectiveness of glucagon-like peptide 1 receptor agonist with that of basal insulin in type 2 diabetes patients. Methods: Type-2 diabetes patients who were insensitive to metformin were treated with glucagon-like peptide 1 receptor agonist (GP cohort, n = 115) or basal insulin (BI cohort, n = 152) with metformin. Hemoglobin A1c (HbA1c) level and body weight were determined, and adverse effects also recorded. Results: After 16 weeks of treatment, glucagon-like peptide 1 receptor agonist did not significantly reduce HbA1c levels (7.45 ± 2.11 % vs. 7.01 ± 2.01, p = 0.107). In contrast, basal insulin significantly reduced the levels of HbA1c (7.91 ± 2.98 % vs. 7.13 ± 2.22 %, p = 0.010, q = 3.852). Glucagon-likepeptide 1 receptor agonist reduced the body weight of patients (65.25 ± 7.55 kg vs. 62.16 ± 6.15 kg, p = 0.0008, q = 5.121), unlike basal insulin (63.71 ± 6.15 vs. 62.65 ± 6.76 kg, p = 0.154). Conclusion: Glucagon-like peptide 1 receptor agonist and basal insulin + metformin produce identical effectiveness in the treatment of type-2 diabetic patients. Keywords: Glucagon-like peptide-1 receptor agonist, Glycemic control, Insulin, Metformin, Type-2 diabetes
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34

Cheung, B. M. Y., J. E. C. Dickerson, M. J. Ashby, M. J. Brown, and J. Brown. "Effects of Physiological Increments in Human α-Atrial Natriuretic Peptide and Human Brain Natriuretic Peptide in Normal Male Subjects." Clinical Science 86, no. 6 (June 1, 1994): 723–30. http://dx.doi.org/10.1042/cs0860723.

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1. Brain natriuretic peptide, closely related to atrial natriuretic peptide in structure, may be an important circulating hormone. Its physiological role is unclear. First, we studied the effects of incremental infusions of brain natriuretic peptide in six healthy men on plasma brain natriuretic peptide levels and the pharmacokinetics of brain natriuretic peptide. Synthetic human brain natriuretic peptide-32 was infused intravenously, at an initial rate of 0.4 pmol min−1 kg−1, doubling every 15 min until the dose rate reached 6.4 pmol min−1 kg−1, at which rate the infusion was maintained for 30 min. 2. The brain natriuretic peptide infusion raised the brain natriuretic peptide-like immunoreactivity from 1.4 ± 0.5 pmol/l to 21.4 ± 7.6 pmol/l. Brain natriuretic peptide-like immunoreactivity after the end of infusion was consistent with a bi-exponential decay, with half-lives of 2.1 min and 37 min. 3. Next, we studied the effects of low-dose infusion of brain natriuretic peptide to mimic physiological increments in the circulating levels in comparison with atrial natriuretic peptide. Six dehydrated male subjects received intravenous infusions of atrial natriuretic peptide and brain natriuretic peptide, separately and in combination, in a randomized double-blind, placebo-controlled, four-part cross-over design. Atrial natriuretic peptide and brain natriuretic peptide were given at the rate of 0.75 and 0.4 pmol min−1 kg−1, respectively, for 3 h. The control infusion consisted of the vehicle. 4. Analysis of variance showed that atrial natriuretic peptide and atrial natriuretic peptide plus brain natriuretic peptide, but not brain natriuretic peptide alone, increased urinary flow and decreased urinary osmolality significantly. However, urinary sodium excretion was significantly increased by atrial natriuretic peptide, brain natriuretic peptide and atrial natriuretic peptide plus brain natriuretic peptide. 5. None of the four infusates significantly altered the blood pressure, heart rate or glomerular filtration rate. 6. This study showed, for the first time, that physiological increments in brain natriuretic peptide, like those in atrial natriuretic peptide, are natriuretic. Although atrial natriuretic peptide and brain natriuretic peptide do not appear to interact synergistically, they are likely to act in concert in the physiological regulation of sodium balance.
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Song, Hui, Chao Liu, Yijun Wu, Honggang Hu, and Fang Yan. "Efficient Synthesis of Bicyclic Peptide BI-32169 Utilizing a Novel Aryl Boronate Ester Protecting Group." Acta Chimica Sinica 76, no. 2 (2018): 95. http://dx.doi.org/10.6023/a17100473.

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Rowinska-Zyrek, Magdalena, Daniela Valensin, Lukasz Szyrwiel, Zbigniew Grzonka, and Henryk Kozlowski. "Specific interactions of Bi(III) with the Cys-Xaa-Cys unit of a peptide sequence." Dalton Transactions, no. 42 (2009): 9131. http://dx.doi.org/10.1039/b913430a.

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37

Tang, Yng, Ryan Davis, Tanushree Ganguly, and Julie Sutcliffe. "Identification, Characterization, and Optimization of Integrin αvβ6-Targeting Peptides from a One-Bead One-Compound (OBOC) Library: Towards the Development of Positron Emission Tomography (PET) Imaging Agents." Molecules 24, no. 2 (January 16, 2019): 309. http://dx.doi.org/10.3390/molecules24020309.

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The current translation of peptides identified through the one-bead one-compound (OBOC) technology into positron emission tomography (PET) imaging agents is a slow process, with a major delay between ligand identification and subsequent lead optimization. This work aims to streamline the development process of 18F-peptide based PET imaging agents to target the integrin αvβ6. By directly identify αvβ6–targeting peptides from a 9-mer 4-fluorobenzoyl peptide library using the on-bead two-color (OBTC) cell-screening assay, a total of 185 peptide beads were identified and 5 beads sequenced for further evaluation. The lead peptide 1 (VGDLTYLKK(FB), IC50 = 0.45 ± 0.06 μM, 25% stable in serum at 1 h) was further modified at the N-, C-, and bi-termini. C-terminal PEGylation increased the metabolic stability (>95% stable), but decreased binding affinity (IC50 = 3.7 ± 1 μM) was noted. C-terminal extension (1i, VGDLTYLKK(FB)KVART) significantly increased binding affinity for integrin αvβ6 (IC50 = 0.021 ± 0.002 μM), binding selectivity for αvβ6-expressing cells (3.1 ± 0.8:1), and the serum stability (>99% stable). Our results demonstrate the challenges in optimizing OBOC-derived peptides, indicate both termini of 1 are sensitive to modifications, and show that further modification of 1 is necessary to demonstrate utility as an 18F-peptide imaging agent.
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Suthiram, Janine, Thomas Ebenhan, Biljana Marjanovic-Painter, Mike M. Sathekge, and Jan Rijn Zeevaart. "Towards Facile Radiolabeling and Preparation of Gallium-68-/Bismuth-213-DOTA-[Thi8, Met(O2)11]-Substance P for Future Clinical Application: First Experiences." Pharmaceutics 13, no. 9 (August 25, 2021): 1326. http://dx.doi.org/10.3390/pharmaceutics13091326.

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Substance P (SP) is a small peptide commonly known as a preferential endogenous ligand for the transmembrane neurokinin-1 receptor. Nuclear Medicine procedures currently involve radiolabeled SP derivatives in peptide radioligand endotherapy of inoperable glioblastoma. Promising clinical results sparked the demand for facile production strategies for a functionalized 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid-[Thi8, Met(O2)11]-SP to allow for rapid Gallium-68 or Bismuth-213 complexation. Therefore, we provide a simple kit-like radiotracer preparation method that caters for the gallium-68 activity eluted from a SnO2 generator matrix as well as preliminary results on the adaptability to produce [213Bi]Bi-DOTA-[Thi8, Met(O2)11]SP from the same vials containing the same starting material. Following a phase of radioanalysis for complexation of gallium-68 to DOTA-[Thi8, Met(O2)11]SP and assessing the radiolabeling parameters, the vials containing appropriate kit-prototype material were produced in freeze-dried batches. The facile radiolabeling performance was tested and parameters for future human application were calculated to meet the criteria for theranostic loco-regional co-administration of activity doses comprising [68Ga]Ga-DOTA-[Thi8, Met(O2)11]SP mixed with [213Bi]Bi-DOTA-[Thi8, Met(O2)11]SP. [68Ga]Ga-DOTA-[Thi8, Met(O2)11]SP was prepared quantitatively from lyophilized starting material within 25 min providing the required molar activity (18 ± 4 GBq/µmol) and activity concentration (98 ± 24 MBq/mL), radiochemical purity (>95%) and sustained radiolabeling performance (4 months at >95% LE) as well as acceptable product quality (>95% for 120 min). Additionally, vials of the same starting materials were successfully adapted to a labeling strategy available for preparation of [213Bi]Bi-DOTA-[Thi8, Met(O2)11]SP providing sufficient activity for 1–2 human doses. The resultant formulation of [68Ga]Ga-/[213Bi]Bi-DOTA-[Thi8, Met(O2)11]SP activity doses was considered of adequate radiochemical quality for administration. This investigation proposes a simple kit-like formulation of DOTA-[Thi8, Met(O2)11]SP—a first-line investigation into a user friendly, straightforward tracer preparation that would warrant efficient clinical investigations in the future. Quantitative radiolabeling was accomplished for [68Ga]Ga-DOTA-[Thi8, Met(O2)11]SP and [213Bi]Bi-DOTA-[Thi8, Met(O2)11]SP preparations; a key requirement when addressing the specific route of catheter-assisted co-injection directly into the intratumoral cavities.
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Norenberg, J. P., B. J. Krenning, I. R. Konings, M. de Jong, A. Srinivasan, K. Garmestani, M. W. Brechbiel, and L. K. Kvols. "213BI-[DOTA0,TYR3]OCTREOTIDE (Bi-DOTATOC) IN PEPTIDE RECEPTOR RADIONUCLIDE THERAPY (PRRT): RADIOLABELING, STABILITY, AND BIODISTRIBUTION." Clinical Nuclear Medicine 24, no. 3 (March 1999): 212. http://dx.doi.org/10.1097/00003072-199903000-00026.

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40

Li, Hao, Haona Xie, Nana Yang, Yue Huang, Lizhou Sun, and Genxi Li. "Design of a bi-functional peptide for protein assays: observation of cortactin expression in human placenta." Chemical Communications 49, no. 47 (2013): 5387. http://dx.doi.org/10.1039/c3cc42353k.

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41

Sharma, Gitanjali, Amit Modgil, Buddhadev Layek, Kanwardeep Arora, Chengwen Sun, Benedict Law, and Jagdish Singh. "Cell penetrating peptide tethered bi-ligand liposomes for delivery to brain in vivo: Biodistribution and transfection." Journal of Controlled Release 167, no. 1 (April 2013): 1–10. http://dx.doi.org/10.1016/j.jconrel.2013.01.016.

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42

Wang, Xiuli, Winnie Wong, Wen-Chung Chang, Don Diamond, Michael C. Jensen, Christine Brown, John Zaia, and Stephen J. Forman. "Enhanced Antitumor Efficacy of Adoptively Transferred CD19-Redirected CMV Specific Central Memory T Cells by CMV Vaccine." Blood 120, no. 21 (November 16, 2012): 3014. http://dx.doi.org/10.1182/blood.v120.21.3014.3014.

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Abstract Abstract 3014 Development of T cell products that have engineered specificity for CD19 has broad application to adoptive transfer therapy for B-lineage lymphoma and leukemia. Clinical studies have demonstrated the safety and feasibility of cloned and bulk T cell transfer as a therapy for patients. But potency of this strategy has proven challenging, primarily due to issues relating to a lack of persistence of the adoptively transferred cells in patients. In contrast, the adoptive transfer of viral specific T cells has shown efficient efficacy for preventing progressive viral infections and exhibited long term persistence in patients, in part due to the viral specific T cells received optimal co-stimulation after engagement of their native receptors. Conceptually, engineering CMV specific T cells with CD19CAR to provide them with a second specificity for a tumor antigen may enable the transferred T cells (bi-specific T cells) to persist or numerically expand in vivo by stimulation of the endogenous TCR by virus antigen. Moreover, bi-specific T cell can be used in treatment for B cell malignancies in allo-settings without causing GVHD due to the pre-defined non-alloreactive TCR specificity. In this study, we explored the use of CMVxCD19CAR bi-specific T cells in CD19+tumor bearing NSG mice and evaluated their antitumor activity in response to CMVpp65 antigen stimulation as a consequence of CAR transduced T cell expansion. CMV specific T cells derived from central memory T cells were selectively expanded by 2 rounds of stimulation with cGMP grade pp65 protein followed a rapid expansion containing OKT3 and feeder cells. The established CMV specific Tcm, in which majority of them are CMVpp65 tetramer positive, were then transduced with cGMP grade SIN lentivirus expressing CD19R:CD28:z/EGFRt. After stimulation with CD19 positive LCL, 40% of the resultant cells co-express pp65 tetramer and CAR as detected by EGFRt/Erbitux analysis. Functionally, the bi-specific T cells exhibit specific cytolytic activity and secret IFNg, IL2 and TNFα upon engagement with pp65 or CD19 antigen, indicating that the effector function of the bi-specific T cells can be induced through endogenous TCR or the introduced CAR. To evaluate the in vivo viral antigen driven anti-tumor efficacy of the adoptively transferred bi-specific T cells, CD19+LCL expressing GFPffluc were inoculated (i.v) into huIL-15 reconstituted NSG mice. Once the tumor engraftment was confirmed by in vivo imaging, bi-specific T cells were adoptively transferred (i.v) into the tumor bearing mice. Anti- tumor activity was observed 14 days post T cell infusion. As expected, this effect is transient and tumor re-progression occurred. In order to deliver CMV antigen for vaccine, we generated T-APC by loading CMVpp65 peptide into autologous T cells and injected the CMV T-APCs (I.v) into the bi-specific T cell treated mice, Influenza specific MP1 peptide pulsed autologous T cells were used as control T-APCs. CMV T-APC induced a second wave of antitumor activity 2 weeks post vaccine and mice survived for more than 2 months post adoptive transfer of T cells, while tumor grew vigorously when MP1-T-APCs were given as stimulators. The findings demonstrated that CD19CAR modified CMV specific T cells are capable of responding to viral antigen reactivation through their endogenous TCR, which could be used to magnify the antitumor activity of CAR transduced T cells in vivo. Disclosures: No relevant conflicts of interest to declare.
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Eldawoody, Hany A. Fikry, Mohammed Abdel Bari Mattar, Abeer Mesbah, Ashraf Zaher, and Mohammed Elsherif. "Can brain natriuretic peptide, S100b, and interleukin-6 prognosticate the neurological consequences in Egyptian patients presented with supratentorial intracerebral hemorrhage?" Surgical Neurology International 11 (December 22, 2020): 460. http://dx.doi.org/10.25259/sni_784_2020.

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Background: Biomarkers in supratentorial intracerebral hemorrhage (SICH) enhance the prognosis of the disease. This study aimed to assess the prognosticative grade of S100 calcium-binding protein B (S100B), interleukin-6 (IL-6), and the pro-brain natriuretic peptide (pro-BNP) in SICH outcome prediction. Methods: Blood samples of 50 SICH patients were analyzed for the biomarkers. The patients were classified into two groups with and without intraventricular hemorrhage (IVH). The following scales including Glasgow Coma Score (GCS), the Barthel index (BI), intracerebral hemorrhage (ICH) score, ICH volume, National Institutes of Health Stroke Scale (NIHSS), Modified Rankin Score (mRS), and length of stay were used to evaluate the severity. Results: The severity scores (NIHSS, GCS, BI, mRI) were significantly higher in SICH patients with IVH versus SICH patients without IVH (P = 0.002, 0.008, 0.001, and 0.03, respectively). Serum levels for a pro-BNP and S100b are significantly higher in SICH patients with IVH versus SICH patients without IVH (P = 0.02 and 0.027, respectively). Multivariate correlations between demographic (age), biomarkers panel (IL-6, S100b, and proBNP), and clinical and severity scores (ICH score, ICH volume, length of hospital stay [LOS], BI, mRS, GCS, and NIHSSS) in all studied patients showed a highly significant correlation between ICH score and pro-BNP (P = 0.04). There was a highly significant correlation between LOS and IL-6 (P = 0.003). Conclusion: Pro-BNP, IL-6, and S100b are greatly associated with the presence of IVH that, in turn, correlated well with poor clinical outcome measures.
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Lotfy, Mohamed, Huba Kalasz, Gyorgy Szalai, Jaipaul Singh, and Ernest Adeghate. "Recent Progress in the Use of Glucagon and Glucagon Receptor Antago-nists in the Treatment of Diabetes Mellitus." Open Medicinal Chemistry Journal 8, no. 1 (December 31, 2014): 28–35. http://dx.doi.org/10.2174/1874104501408010028.

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Glucagon is an important pancreatic hormone, released into blood circulation by alpha cells of the islet of Langerhans. Glucagon induces gluconeogenesis and glycogenolysis in hepatocytes, leading to an increase in hepatic glucose production and subsequently hyperglycemia in susceptible individuals. Hyperglucagonemia is a constant feature in patients with T2DM. A number of bioactive agents that can block glucagon receptor have been identified. These glucagon receptor antagonists can reduce the hyperglycemia associated with exogenous glucagon administration in normal as well as diabetic subjects. Glucagon receptor antagonists include isoserine and beta-alanine derivatives, bicyclic 19-residue peptide BI-32169, Des-His1-[Glu9] glucagon amide and related compounds, 5-hydroxyalkyl-4-phenylpyridines, N-[3-cano-6- (1,1 dimethylpropyl)-4,5,6,7-tetrahydro-1-benzothien-2-yl]-2-ethylbutamide, Skyrin and NNC 250926. The absorption, dosage, catabolism, excretion and medicinal chemistry of these agents are the subject of this review. It emphasizes the role of glucagon in glucose homeostasis and how it could be applied as a novel tool for the management of diabetes mellitus by blocking its receptors with either monoclonal antibodies, peptide and non-peptide antagonists or gene knockout techniques.
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Wang, Jianhao, Jingyan Li, Yiwan Teng, Yanhua Bi, Wei Hu, Jinchen Li, Cheli Wang, Lin Qiu, and Pengju Jiang. "Charge Effect on the Quantum Dots-Peptide Self-Assembly Using Fluorescence Coupled Capillary Electrophoresis." Journal of Nanoscience and Nanotechnology 16, no. 4 (April 1, 2016): 4035–39. http://dx.doi.org/10.1166/jnn.2016.11898.

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We present a molecular characterization of metal-affinity driven self-assembly between CdSe–ZnS quantum dots and a series of hexahistidine peptides with different charges. In particular, we utilized fluorescence coupled capillary electrophoresis to test the self-assembly process of quantum dots with peptides in solution. Four peptides with different charges can be efficiently separated by fluorescence coupled capillary electrophoresis. The migration time appeared to be influenced by the charges of the peptide. In addition, the kinetics of self-assembly process of quantum dots with one of the peptides manifested a bi-phasic kinetics followed by a saturating stage. This work revealed that there exist two types of binding sites on the surface of quantum dots for peptide 1: one type termed “high priority” binding site and a “low priority” site which is occupied after the first binding sites are fully occupied. The total self-assembly process finishes in solution within 80 s. Our work represents the systematic investigation of the details of self-assembly kinetics utilizing high-resolution fluorescence coupled capillary electrophoresis. The charge effect of peptide coating quantum dots provides a new way of preparing bioprobes.
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Lelièvre, Dominique, David Daguet, and André Brack. "On-line solid-phase synthesis of a peptide bi-derivatized with biotin and 4-azido salicylic acid." Tetrahedron Letters 36, no. 51 (December 1995): 9317–20. http://dx.doi.org/10.1016/0040-4039(95)02029-o.

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Kiselyov, Vladislav V., Shizhong Li, Vladimir Berezin, and Elisabeth Bock. "Insight into the structural mechanism of the bi-modal action of an NCAM mimetic, the C3 peptide." Neuroscience Letters 452, no. 3 (March 2009): 224–27. http://dx.doi.org/10.1016/j.neulet.2009.01.080.

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48

Lityńska, Anna, Ewa Pocheć, Dorota Hoja-Lukowicz, Elzbieta Kremser, Piotr Laidler, Angela Amoresano, and Chiara Monti. "The structure of the oligosaccharides of alpha3beta1 integrin from human ureter epithelium (HCV29) cell line." Acta Biochimica Polonica 49, no. 2 (June 30, 2002): 491–500. http://dx.doi.org/10.18388/abp.2002_3808.

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There is a growing line of evidence that glycosylation of alpha and beta subunits is important for the function of integrins. Integrin alpha3beta1, from human ureter epithelium cell-line HCV29, was isolated by affinity chromatography on laminin GD6 peptide. Characterization of its carbohydrate moieties was carried out using sodium dodecyl sulfate/polyacrylamide gel electrophoresis followed by Western blotting on Immobilon P and on-blot deglycosylation with peptide N-glycosidase-F. Profiles of N-glycans for each subunit were obtained by matrix-assisted laser desorption/ionization mass spectrometry. Our findings demonstrated, in both subunits of integrin alpha3beta1, the presence of complex type oligosaccharides with a wide heterogeneity. Bi- tri- and tetraantennary structures were the most common, while high-mannose type structures were minor. Also the presence of short poly-N-acetyllactosamine entities was shown. These results show that while the predominant oligosaccharides of both subunits are identical, some slight differences between them do exist.
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Jarry, Marie, Mickaël Diallo, Céline Lecointre, Laurence Desrues, Tursonjan Tokay, David Chatenet, Jérôme Leprince, et al. "The vasoactive peptides urotensin II and urotensin II-related peptide regulate astrocyte activity through common and distinct mechanisms: involvement in cell proliferation." Biochemical Journal 428, no. 1 (April 28, 2010): 113–24. http://dx.doi.org/10.1042/bj20090867.

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UII (urotensin II) and its paralogue URP (UII-related peptide) are two vasoactive neuropeptides whose respective central actions are currently unknown. In the present study, we have compared the mechanism of action of URP and UII on cultured astrocytes. Competition experiments performed with [125I]UII showed the presence of very-high- and high-affinity binding sites for UII, and a single high-affinity site for URP. Both UII and URP provoked a membrane depolarization accompanied by a decrease in input resistance, stimulated the release of endozepines, neuropeptides specifically produced by astroglial cells, and generated an increase in [Ca2+]c (cytosolic Ca2+ concentration). The UII/URP-induced [Ca2+]c elevation was PTX (pertussis toxin)-insensitive, and was blocked by the PLC (phospholipase C) inhibitor U73122 or the InsP3 channel blocker 2-APB (2-aminoethoxydiphenylborane). The addition of the Ca2+ chelator EGTA reduced the peak and abolished the plateau phase, whereas the T-type Ca2+ channel blocker mibefradil totally inhibited the Ca2+ response evoked by both peptides. However, URP and UII induced a mono- and bi-phasic dose-dependent increase in [Ca2+]c and provoked short- and long-lasting Ca2+ mobilization respectively. Similar mono- and bi-phasic dose-dependent increases in [3H]inositol incorporation into polyphosphoinositides in astrocytes was obtained, but the effect of UII was significantly reduced by PTX, although BRET (bioluminescence resonance energy transfer) experiments revealed that both UII and URP recruited Gαo-protein. Finally, UII, but not URP, exerted a dose-dependent mitogenic activity on astrocytes. Therefore we described that URP and UII exert not only similar, but also divergent actions on astrocyte activity, with UII exhibiting a broader range of activities at physiological peptide concentrations.
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Doekel, Sascha, Katrin Eppelmann, and Mohamed A. Marahiel. "Heterologous expression of nonribosomal peptide synthetases inB. subtilis: construction of a bi-functionalB. subtilis/E. colishuttle vector system." FEMS Microbiology Letters 216, no. 2 (November 2002): 185–91. http://dx.doi.org/10.1111/j.1574-6968.2002.tb11434.x.

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