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Journal articles on the topic 'Inhibitor'

Author: Grafiati

Published: 4 June 2021

Last updated: 25 July 2025

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1

Arita, Minetaro, Takaji Wakita, and Hiroyuki Shimizu. "Cellular kinase inhibitors that suppress enterovirus replication have a conserved target in viral protein 3A similar to that of enviroxime." Journal of General Virology 90, no. 8 (2009): 1869–79. http://dx.doi.org/10.1099/vir.0.012096-0.

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Previously, we identified a cellular kinase inhibitor, GW5074, that inhibits poliovirus (PV) and enterovirus 71 replication strongly, although its target has remained unknown. To identify the target of GW5074, we searched for cellular kinase inhibitors that have anti-enterovirus activity similar or related to that of GW5074. With this aim, we performed screenings to identify cellular kinase inhibitors that could inhibit PV replication cooperatively with GW5074 or synthetically in the absence of GW5074. We identified MEK1/2 inhibitors (SL327 and U0126), an EGFR inhibitor (AG1478) and a phosphat

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2

Shi, Qizhen, Erin L. Kuether, Jocelyn A. Schroeder, Crystal L. Perry, Scot A. Fahs, and Robert R. Montgomery. "Factor VIII Inhibitors: Von Willebrand Factor Makes A Difference In Vitro and In Vivo." Blood 116, no. 21 (2010): 709. http://dx.doi.org/10.1182/blood.v116.21.709.709.

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Abstract Abstract 709 The important association between von Willebrand factor (VWF) and factor VIII (FVIII) has been investigated for decades, but the effect of VWF on FVIII inhibitors is still controversial. Studies have demonstrated that some anti-FVIII inhibitory antibodies inhibit VWF-FVIII interaction, while others rely on the presence of VWF to inhibit FVIII activities. The influence of VWF on the Bethesda assay, which is routinely used in the clinic to determine the titer of FVIII-neutralizing inhibitors, is still uncertain because the plasma from hemophilia A patients with inhibitors c

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3

Moon, Hyun-Jung, Su-Hoon Lee, Hak-Bong Kim, Kyoung-A. Lee, Chi-Dug Kang, and Sun-Hee Kim. "SIRT1 Inhibitor Enhances Hsp90 Inhibitor-mediated Abrogation of Hsp90 Chaperone Function and Potentiates the Cytotoxicity of Hsp90 Inhibitor in Chemo-resistant Human Cancer Cells." Journal of Life Science 26, no. 7 (2016): 826–34. http://dx.doi.org/10.5352/jls.2016.26.7.826.

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4

Potempa, J., J. J. Enghild та J. Travis. "The primary elastase inhibitor (elastasin) and trypsin inhibitor (contrapsin) in the goat are serpins related to human α1-anti-chymotrypsin". Biochemical Journal 306, № 1 (1995): 191–97. http://dx.doi.org/10.1042/bj3060191.

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Two primary serine proteinase inhibitors in goat plasma have been isolated and characterized. The N-terminal sequence analysis of the purified proteins revealed that they are closely related to each other and are highly homologous to human alpha 1-anti-chymotrypsin rather than alpha 1-proteinase inhibitor. However, despite structural similarities the inhibitory specificity of the goat inhibitors differed from each other and from that of anti-chymotrypsin. In contrast with human anti-chymotrypsin, one of the goat inhibitors was shown to be a strong and specific inhibitor of trypsin (k(ass.) = 1

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Böhm, Martina, Manuela Krause, Charis Von Auer, Wolfgang Miesbach, and Inge Scharrer. "The Frequency and the Significance of ADAMTS-13 Neutralising Inhibitors in 62 Patients with Non-Familial Thrombotic Thrombocytopenic Purpura." Blood 104, no. 11 (2004): 3945. http://dx.doi.org/10.1182/blood.v104.11.3945.3945.

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Abstract Neutralising inhibitors against ADAMTS-13 are detected in 51–67% of patients with Thrombotic Thrombocytopenic Purpura (TTP). These ADAMTS-13 inhibitors have not been very well characterised and the diagnostic or the prognostic value of these inhibitors is not established. In the present study, we measured ADAMTS-13 activity and the corresponding inhibitor titer in 96 samples from 62 patients with TTP at various stages of their disease. All patients presented with non-familial TTP. For patients with severe ADAMTS-13 activity without detectable inhibitor heritable ADAMTS-13 deficiency w

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Cheng, Liwei, Limin Wang, Zhi Li, Bei Liu, and Guangjin Chen. "Inhibition Effect of Kinetic Hydrate Inhibitors on the Growth of Methane Hydrate in Gas–Liquid Phase Separation State." Energies 12, no. 23 (2019): 4482. http://dx.doi.org/10.3390/en12234482.

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The effect of kinetic hydrate inhibitors (KHIs) on the growth of methane hydrate in the gas–liquid phase separation state is studied at the molecular level. The simulation results show that the kinetic inhibitors, named PVP and PVP-A, show good inhibitory effects on the growth of methane hydrate under the gas–liquid phase separation state, and the initial position of the kinetic hydrate inhibitors has a major effect on the growth of methane hydrates. In addition, inhibitors at different locations exhibit different inhibition performances. When the inhibitor molecules are located at the gas–liq

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Luan, Hengjie, Mingkang Liu, Qinglin Shan, Yujing Jiang, Peng Yan, and Xiaoyu Du. "Experimental Study on the Effect of Mixed Thermodynamic Inhibitors with Different Concentrations on Natural Gas Hydrate Synthesis." Energies 17, no. 9 (2024): 2078. http://dx.doi.org/10.3390/en17092078.

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Natural gas hydrate (NGH) is a potential future energy resource. More than 90% of NGH resources exist in the pore medium of seafloor sediments. During the development of deep-sea oil and gas fields, wellbore pipelines are often clogged due to the synthesis of gas hydrates, and the addition of thermodynamic inhibitors is a common solution to prevent hydrate synthesis. In this paper, the effects of two single inhibitors, sodium chloride and ethylene glycol, as well as hybrid inhibitors combining these two inhibitors on the synthesis of methane hydrates were investigated using the self-developed

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8

Hays, Priya. "Personalized medicine in oncology: Small molecule inhibitors, biologics and immunotherapies." Open Access Government 46, no. 1 (2025): 120–21. https://doi.org/10.56367/oag-046-11897.

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Personalized medicine in oncology: Small molecule inhibitors, biologics and immunotherapies Priya Hays, PhD, CEO of Hays Documentation Specialists, discusses innovations and advancements in the development and evaluation of personalized cancer therapies. Advancements in cancer research have led to changes in the treatment of patients with cancer, resulting in novel personalized cancer therapies. The three major classes include small molecule inhibitors, biologics, and cancer immunotherapies. Standard first-line immunotherapies include anti-CTLA-4 inhibitor ipilimumab and anti-PD-1 inhibitor ni

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9

Savitri, Erna Noor, Putut Marwoto, and Sunyoto Eko Nugroho. "The Effectiveness of a Combination of Lime (Citrus aurantifolia.), Lerak (Sapindus rarak) and Jasmine Flower (Jasminum nudiflorum) Extracts as and Environmentally Friendly Corrosion Inhibitor." Jurnal Penelitian Pendidikan IPA 10, no. 3 (2024): 1019–24. http://dx.doi.org/10.29303/jppipa.v10i3.6364.

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Corrosion can also be defined as the forced destruction of metal by the surrounding medium which is usually a liquid (corrosive agent). Corrosion prevention processes can be carried out, including by coating the metal surface, cathodic protection, adding corrosion inhibitors and so on. Several types of inhibitors that have been widely used in industrial applications are synthetic chemical inhibitors. However, the compounds of inhibitors are environmentally unfriendly, toxic and expensive. To overcome this problem, it is necessary to develop an environmentally friendly alternative corrosion inh

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10

Sever, Natasa, Metka Filipic, Joze Brzin, and Tamara T. Lah. "Effect of Cysteine Proteinase Inhibitors on Murine B16 Melanoma Cell Invasion in vitro." Biological Chemistry 383, no. 5 (2002): 839–42. http://dx.doi.org/10.1515/bc.2002.088.

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Abstract Various types of proteinases are implicated in the malignant progression of human and animal tumors. Proteinase inhibitors may therefore be useful as therapeutic agents in antiinvasive and antimetastatic treatment. The aims of this study were (1) to estimate the relative importance of proteinases in B16 cell invasion in vitro using synthetic, classspecific proteinase inhibitors and (2) to assess the inhibitory effect of some naturally occurring cysteine proteinase inhibitors. Serine proteinase inhibitor reduced invasiveness by up to 24%, whereas inhibition of aspartic proteinases redu

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11

Milner, Malgorzata, Jadwiga Chroboczek, and Wlodzimierz Zagorski-Ostoja. "Engineered resistance against proteinases." Acta Biochimica Polonica 54, no. 3 (2007): 523–36. http://dx.doi.org/10.18388/abp.2007_3226.

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Exogenous proteinase inhibitors are valuable and economically interesting protective biotechnological tools. We examined whether small proteinase inhibitors when fused to a selected target protein can protect the target from proteolytic degradation without simultaneously affecting the function and activity of the target domain. Two proteinase inhibitors were studied: a Kazal-type silk proteinase inhibitor (SPI2) from Galleria mellonella, and the Cucurbita maxima trypsin inhibitor I (CMTI I). Both inhibitors target serine proteinases, are small proteins with a compact structure stabilized by a

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12

Jasim, Haider Hadi, Read Abd Al-Hussain, and Ahmed Shawqi Sadeq. "Evaluation the Efficiency of Various Types of Corrosion Inhibitors Used for Basrah Water Storage Tanks." Al-Nahrain Journal for Engineering Sciences 23, no. 3 (2020): 267–76. http://dx.doi.org/10.29194/njes.23030267.

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In this paper, the efficiency of six different types of corrosion inhibitors used in Basrah drinking water tanks was assessed using a potentiostatic test method. The mechanism of adsorption of silicate and phosphate inhibitors in AISI 316 stainless steel surfaces and the effects of different water components in inhibitors are discussed in detail. The values of corrosion rate obtained from the Potentiostatic test showed that the protection against corrosion in the presence of inhibitors is better compared to the case of absence of inhibitors. The results of the six types of corrosion inhibitors

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13

Mutlaq, Saud Khalaf, and Rahman Khudair Abdul Hussein Abdul. "Treating Crude Oil Pipelines from Corrosion by Using Heterocyclic and Nano-Carbon Polymers." Journal of Global Scientific Research 9, no. 4 (2024): 3431–46. https://doi.org/10.5281/zenodo.10916642.

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 ABSTRACT A study of steel corrosion rates was carried out and it was taken from Qayara fields - south of Mosul province in (0.1M) of sulfuric acid and potassium chloride with different temperatures (293,303,313,323,333) Kelvin in the absence and presence of polymeric inhibitors, inhibitory coatings were prepared at different proportions (1: 1). , (1: 2) and (2: 1) from nano-carbon and poly-pyrrole respectively. The highest inhibition efficiency in the acid medium was (91%) for inhibitor (A) and for inhibitor (B) was (78%) and inhibitor (C) was (65%) and inhibitor (D) was (100%) and inhib

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14

Umezawa, Koji, and Isao Kii. "Druggable Transient Pockets in Protein Kinases." Molecules 26, no. 3 (2021): 651. http://dx.doi.org/10.3390/molecules26030651.

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Drug discovery using small molecule inhibitors is reaching a stalemate due to low selectivity, adverse off-target effects and inevitable failures in clinical trials. Conventional chemical screening methods may miss potent small molecules because of their use of simple but outdated kits composed of recombinant enzyme proteins. Non-canonical inhibitors targeting a hidden pocket in a protein have received considerable research attention. Kii and colleagues identified an inhibitor targeting a transient pocket in the kinase DYRK1A during its folding process and termed it FINDY. FINDY exhibits a uni

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15

Na, Bon Hyang, Thi Xoan Hoang та Jae Young Kim. "Hsp90 Inhibition Reduces TLR5 Surface Expression and NF-κB Activation in Human Myeloid Leukemia THP-1 Cells". BioMed Research International 2018 (2018): 1–8. http://dx.doi.org/10.1155/2018/4319369.

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Tumors highly express active heat shock protein 90 (Hsp90), which is involved in tumor survival and progression. Enhanced Toll-like receptor (TLR) 5 expression and signaling were reported to be associated with acute myeloid leukemia. In the present study, we investigated the possible modulatory effects of Hsp90 inhibitors on TLR5 expression and signaling in the human myeloid leukemia cell line THP-1. Cells were pretreated with various concentrations of the Hsp90 inhibitor geldanamycin (GA) or the Hsp70 inhibitor VER155008, followed by stimulation with bacterial flagellin. Flagellin-induced nuc

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16

Domoney, C., and T. Welham. "Trypsin inhibitors in Pisum: variation in amount and pattern of accumulation in developing seed." Seed Science Research 2, no. 3 (1992): 147–54. http://dx.doi.org/10.1017/s0960258500001276.

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AbstractA survey of Pisum genotypes for seed trypsin inhibitors revealed a tenfold range in the extent of inhibition. Approximately 90% of trypsin inhibitory activity was associated with two albumin fractions in selected variant lines. The differences among extreme variants were consistent in three environments, between two sources of trypsin tested and whether expressed on a unit protein or dry weight basis.A study of the appearance of trypsin inhibitors during seed development in selected highand low-inhibitor lines showed differences in the accumulation pattern of active inhibitors. An endo

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17

Schmidt, Anja, Kerstin Brettschneider, Jörg Kahle, et al. "Neutralisation of factor VIII inhibitors by anti-idiotypes isolated from phage-displayed libraries." Thrombosis and Haemostasis 116, no. 07 (2016): 32–41. http://dx.doi.org/10.1160/th15-12-0925.

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SummaryFollowing replacement therapy with coagulation factor VIII (FVIII), up to 30 % of haemophilia A patients develop FVIII-specific inhibitory antibodies (FVIII inhibitors). Immune tolerance induction (ITI) is not always successful, resulting in a need for alternative treatments for FVIII inhibitor-positive patients. As tolerance induction in the course of ITI appears to involve the formation of anti-idiotypes specific for anti-FVIII antibodies, such anti-idiotypes might be used to restore haemostasis in haemophilia A patients with FVIII inhibitors. We isolated antiidiotypic antibody fragme

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18

Ganea, D., D. Cearlock, J. Minowada, and S. Dray. "A serine proteinase inhibitor produced by an HTLV I virus-transformed human T lymphocyte line." Journal of Immunology 138, no. 4 (1987): 1208–14. http://dx.doi.org/10.4049/jimmunol.138.4.1208.

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Abstract A previous report from our laboratory indicated that a proteinase inhibitor is produced by rabbit T lymphocytes. We now report that a human T cell line, C91/PL, produces a proteinase inhibitor which inhibits the enzymatic activity of trypsin and kallikrein. This newly identified proteinase inhibitor (LPI 1) did not inhibit the enzymatic activity of four other serine proteinases (thrombin, plasmin, chymotrypsin, or pancreatic elastase), a thiol proteinase (papain), or a carboxyl proteinase (pepsin). Active synthesis of LPI 1 by the C91/PL cell line was shown by the appearance of simila

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19

Suzuki, Suzuki, Morio Arai, Kagehiro Amano, Kazuhiko Kagawa, and Katsuyuki Fukutake. "Factor VIII Inhibitor Antibodies with C2 Domain Specificity Are Less inhibitory to Factor VIII Complexed with von Willebrand Factor." Thrombosis and Haemostasis 76, no. 05 (1996): 749–54. http://dx.doi.org/10.1055/s-0038-1650655.

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SummaryIn order to clarify the potential role of von Willebrand factor (vWf) in attenuating the inactivation of factor VIII (fVIII) by those antibodies with C2 domain specificity, we investigated a panel of 14 human antibodies to fVIII. Immunoblotting analysis localized light chain (C2 domain) epitopes for four cases, heavy chain (A2 domain) epitopes in five cases, while the remaining five cases were both light and heavy chains. The inhibitor titer was considerably higher for Kogenate, a recombinant fVIII concentrate, than for Haemate P, a fVIII/vWf complex concentrate, in all inhibitor plasma

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20

Yan, Daojing, Jiakun Xu, Xiang Wang, et al. "Spiro-Oxindole Skeleton Compounds Are Efficient Inhibitors for Indoleamine 2,3-Dioxygenase 1: An Attractive Target for Tumor Immunotherapy." International Journal of Molecular Sciences 23, no. 9 (2022): 4668. http://dx.doi.org/10.3390/ijms23094668.

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Indoleamine 2,3-dioxygenase 1 (IDO1) is an attractive heme enzyme for its significant function in cancer immunotherapy. Potent IDO1 inhibitors have been discovered for decades, whereas no clinical drugs are used for cancer treatment up to now. With the goal of developing medically valuable IDO inhibitors, we performed a systematic study of SAR405838 analogs with a spiro-oxindole skeleton in this study. Based on the expression and purification of human IDO1, the inhibitory activity of spiro-oxindole skeleton compounds to IDO1 was evaluated by IC50 and Ki values. The results demonstrated that in

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21

Liu, Jing, Bingqin Wang, Tianqi Chen, Lianjun Hao, Jun Wu, and Chao Liu. "The Effect of Corrosion Inhibitors on the Corrosion Behavior of Ductile Cast Iron." Metals 15, no. 1 (2025): 70. https://doi.org/10.3390/met15010070.

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Based on actual service environment parameters, this experiment investigated the change in the corrosion rate of nodular cast iron (DCI) in an environment containing organic (triethanolamine phosphate, PTEA) and inorganic (hexametaphosphate, SHMP) inhibitors, and analyzed the effects of both inhibitors and the pH value of the solution on the corrosion behavior of DCI. Additionally, a variable flow rate device was used to conduct immersion tests, enabling the accurate evaluation of the materials’ corrosion resistance in an actual service environment. After a certain period, the corrosion of the

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Weiler, Elmar, Farhad Khalil-Manesh, and Harvey C. Gonick. "Effects of Lead and a Low-Molecular-Weight Endogenous Plasma Inhibitor on the Kinetics of Sodium—Potassium-Activated Adenosine Triphosphatase and Potassium-Activated p-Nitrophenylphosphatase." Clinical Science 79, no. 2 (1990): 185–92. http://dx.doi.org/10.1042/cs0790185.

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1. Lead, ouabain and an endogenous plasma inhibitor were all found to be potent inhibitors of purified hog cerebral cortex sodium—potassium-activated adenosine triphosphatase and potassium-stimulated p-nitrophenylphosphatase. 2. The kinetic characteristics of inhibition of both enzymes by lead and the endogenous plasma inhibitor differed in several respects. For sodium—potassium-activated adenosine triphosphatase, lead and the endogenous plasma inhibitor were non-competitive inhibitors with respect to potassium; lead was competitive with respect to sodium, whereas the endogenous plasma inhibit

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Senggunprai, Laddawan, Kouichi Yoshinari, and Yasushi Yamazoe. "Inhibitory effects of kynurenic acid, a tryptophan metabolite, and its derivatives on cytosolic sulfotransferases." Biochemical Journal 422, no. 3 (2009): 455–62. http://dx.doi.org/10.1042/bj20090168.

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KYNA (kynurenic acid) is an endogenous metabolite of tryptophan in the kynurenine pathway and has been characterized as an antagonist of ionotropic glutamate receptors. In addition, we have reported this endogenous compound as a potent inhibitor of SULTs (cytosolic sulfotransferases). In the present study we characterized the inhibitory effects of KYNA on several human (h) and mouse (m) recombinant SULTs. No sulfate metabolite of KYNA was detected with mouse and human SULTs examined under the conditions used, suggesting that it is a bona fide inhibitor of SULTs. Among the mouse enzymes examine

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24

Han, Di, Huiqun Wang, Wei Cui, Beibei Zhang, and Bo-Zhen Chen. "Computational insight into the mechanisms of action and selectivity of Afraxis PAK inhibitors." Future Medicinal Chemistry 12, no. 5 (2020): 367–85. http://dx.doi.org/10.4155/fmc-2019-0273.

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Aim: The p21-activated kinases (PAKs) are involved in many important biological activity regulations. FRAX019, FRAX414, FRAX597, FRAX1036 and G-5555 were identified as PAKs inhibitors. Their detailed inhibitory mechanisms deserve further investigation. Results: Molecular dynamics simulations and further calculations for the PAK1/inhibitor and PAK4/inhibitor complexes indicate that their binding free energies are basically consistent with the trend of experimental activity data. Conclusion: The anchoring of residues Leu347PAK1 and Leu398PAK4 is the structural basis for designing Afraxis PAK inh

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NAKAMURA, K., N. YOKOYAMA, and I. IGARASHI. "Cyclin-dependent kinase inhibitors block erythrocyte invasion and intraerythrocytic development of Babesia bovis in vitro." Parasitology 134, no. 10 (2007): 1347–53. http://dx.doi.org/10.1017/s0031182007002831.

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SUMMARYCyclin-dependent kinases (CDKs) are essential for the regulation of the eukaryotic cell cycle. A number of chemicals, which selectively inhibit the CDK activities, have been synthesized for the development of anti-cancer drugs. This report describes the inhibitory effect of purine derivatives known to be CDK inhibitors on the asexual growth of Babesia bovis. The 4 compounds, roscovitine, purvalanol A, CGP74514A, and CDK2 Inhibitor II, showed significantly suppressive effects on the in vitro growth of B. bovis. Three (roscovitine, purvalanol A, and CDK2 Inhibitor II) showed an inhibitory

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KUMAR, Priyadarsini, and Donal A. WALSH. "A dual-specificity isoform of the protein kinase inhibitor PKI produced by alternate gene splicing." Biochemical Journal 362, no. 3 (2002): 533–37. http://dx.doi.org/10.1042/bj3620533.

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We have previously shown that the protein kinase inhibitor β (PKIβ) form of the cAMP-dependent protein kinase inhibitor exists in multiple isoforms, some of which are specific inhibitors of the cAMP-dependent protein kinase, whereas others also inhibit the cGMP-dependent enzyme [Kumar, Van Patten and Walsh (1997), J. Biol. Chem. 272, 20011–20020]. We have now demonstrated that the switch from a cAMP-dependent protein kinase (PKA)-specific inhibitor to one with dual specificity arises as a consequence of alternate gene splicing. We have confirmed using bacterially produced pure protein that a s

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27

Chuang, Fu-Cheng, Chih-Chun Wang, Jian-Han Chen, Tzer-Zen Hwang, Shyh-An Yeh, and Yu-Chieh Su. "PI3k inhibitors (BKM120 and BYL719) as radiosensitizers for head and neck squamous cell carcinoma during radiotherapy." PLOS ONE 16, no. 1 (2021): e0245715. http://dx.doi.org/10.1371/journal.pone.0245715.

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Approximately 500,000 new cases of head and neck squamous cell carcinoma (HNSCC) are reported annually. Radiation therapy is an important treatment for oral squamous cell carcinoma (OSCC). The survival rate of patients with HNSCC remained low (50%) in decades because of radiation therapy failure caused by the radioresistance of HNSCC cells. This study aimed to identify PI3K inhibitors that can enhance radiosensitivity. Results showed that pan-Phosphoinositide 3-kinases (PI3K) inhibitor BKM120 and class I α-specific PI3K inhibitor BYL719 dose-dependently reduced the growth of OSCC cells but not

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Du, Juan, Song Wang, Xinyue Zhang, Chang Liu, Yurou Zhang, and Hao Zhang. "The Inhibitory Mechanism of 7H-Pyrrolo[2,3-d]pyrimidine Derivatives as Inhibitors of P21-Activated Kinase 4 through Molecular Dynamics Simulation." Molecules 28, no. 1 (2023): 413. http://dx.doi.org/10.3390/molecules28010413.

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The overexpression of p21-activated kinase 4 (PAK4) is associated with a variety of cancers. In this paper, the binding modes and inhibitory mechanisms of four 7H-pyrrolo[2,3-d]pyrimidine competitive inhibitors of PAK4 were investigated at the molecular level, mainly using molecular dynamics simulations and binding free energy calculations. The results show that the inhibitors had strong interactions with the hinge region, the β-sheets, and the residues with charged side chains around the 4-substituent. The terminal amino group of the inhibitor 5n was different from the other three, which coul

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Mauser-Bunschoten, EP, HK Nieuwenhuis, G. Roosendaal, and HM van den Berg. "Low-dose immune tolerance induction in hemophilia A patients with inhibitors." Blood 86, no. 3 (1995): 983–88. http://dx.doi.org/10.1182/blood.v86.3.983.983.

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Abstract In patients with hemophilia A and inhibitory alloantibodies against factor VIII, various dosage schedules are used to obtain immune tolerance. In this study, we have evaluated the results of 13 years of low-dose immune tolerance induction and factors that are predictive of a positive result. The effect of immune tolerance induction in relation to age at inhibitor development, number of exposure days, age at start of therapy, maximum inhibitor titer, factor VIII products involved, and virologic status were determined. We evaluated 24 patients with severe hemophilia A and inhibitors who

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Mauser-Bunschoten, EP, HK Nieuwenhuis, G. Roosendaal, and HM van den Berg. "Low-dose immune tolerance induction in hemophilia A patients with inhibitors." Blood 86, no. 3 (1995): 983–88. http://dx.doi.org/10.1182/blood.v86.3.983.bloodjournal863983.

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In patients with hemophilia A and inhibitory alloantibodies against factor VIII, various dosage schedules are used to obtain immune tolerance. In this study, we have evaluated the results of 13 years of low-dose immune tolerance induction and factors that are predictive of a positive result. The effect of immune tolerance induction in relation to age at inhibitor development, number of exposure days, age at start of therapy, maximum inhibitor titer, factor VIII products involved, and virologic status were determined. We evaluated 24 patients with severe hemophilia A and inhibitors who were tre

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Korn, J. H., K. M. Brown, E. Downie, Z. H. Liao, and D. L. Rosenstreich. "Augmentation of IL 1-induced fibroblast PGE2 production by a urine-derived IL 1 inhibitor." Journal of Immunology 138, no. 10 (1987): 3290–94. http://dx.doi.org/10.4049/jimmunol.138.10.3290.

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Abstract IL 1, a monocyte-derived cytokine, has potent biologic effects in a variety of target tissues. The existence of naturally occurring inhibitors of IL 1 activity has been recently described; these inhibitors blocked one IL 1 effect: stimulation of thymocyte responses to mitogens. We examined the effect of one well-characterized inhibitor of IL 1, isolated from the urine of febrile patients, on a second IL 1 effect, stimulation of fibroblast PGE synthesis. In this system, purified preparations of the urinary inhibitor that completely blocked murine thymocyte proliferative responses to mi

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Rødland, Gro Elise, Sissel Hauge, Grete Hasvold, et al. "Differential Effects of Combined ATR/WEE1 Inhibition in Cancer Cells." Cancers 13, no. 15 (2021): 3790. http://dx.doi.org/10.3390/cancers13153790.

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Inhibitors of WEE1 and ATR kinases are considered promising for cancer treatment, either as monotherapy or in combination with chemo- or radiotherapy. Here, we addressed whether simultaneous inhibition of WEE1 and ATR might be advantageous. Effects of the WEE1 inhibitor MK1775 and ATR inhibitor VE822 were investigated in U2OS osteosarcoma cells and in four lung cancer cell lines, H460, A549, H1975, and SW900, with different sensitivities to the WEE1 inhibitor. Despite the differences in cytotoxic effects, the WEE1 inhibitor reduced the inhibitory phosphorylation of CDK, leading to increased CD

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Brewer, Jamie R., Sandra Harris, David Green, and Anaadriana Zakarija. "Significance of Factor VIII Inhibitors by ELISA in Patients with Hemophilia A." Blood 112, no. 11 (2008): 3398. http://dx.doi.org/10.1182/blood.v112.11.3398.3398.

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Abstract Background: The Bethesda assay traditionally has been used to detect Factor VIII inhibitors in patients with Hemophilia A, but recent evidence suggests that it is not sensitive to all inhibitors, particularly non-inhibitory or low-titer antibodies. Methods: Patients with Hemophilia A without prior history of inhibitor were recruited. Study questionnaire collected demographic and clinical information, bleeding history and factor usage over the preceding 6 months. Functional status was assessed by the Hemophilia Activities List (HAL). Factor VIII inhibitor was assessed by both the Bethe

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Prabhu, S. Arun, M. Syed Ali Padusha, and S. S. Syed Abuthahir. "Corrosion Inhibition Potential of Aqueous Extract of Bauhinia acuminata Linn Leaves on Carbon Steel in Hydrochloric Acid Medium." Asian Journal of Chemistry 36, no. 10 (2024): 2275–82. http://dx.doi.org/10.14233/ajchem.2024.32176.

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The corrosion of carbon steel in 1 N HCl was analyzed using an aqueous Bauhinia acuminata Linn (BaL) leaf extract. Weight loss method was used to determine the inhibitor efficaciousness and corrosion rate. When dissolved in water, a linneus plant leaf extract exhibit an inhibitory effect which is proportionate to the amount of inhibitors present. It is possible to speed up the corrosion process by increasing the inhibitors’ concentration. Studies have shown that the BaL leaves extract has a 97.30% inhibitory efficiency. By increasing the concentration of inhibitor solutions, a surface layer fo

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Shaker, Fatima Mahmood, and Dhifaf Jaafar Sadeqb. "Protecting Oil Flowlines from Corrosion Using 5-ACETYL-2-ANILINO-4-DIMETHYLAMINOTHIAZOLE." Pakistan Journal of Medical and Health Sciences 16, no. 6 (2022): 571–74. http://dx.doi.org/10.53350/pjmhs22166571.

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Oil flow lines are used to transport oil and its derivatives from a well over long distances, and because oil wells produce other potentially corrosive products, such as carbon dioxide and Hydrogen sulfide, it is necessary to take methods to protect the pipeline from corrosion. One of these methods is the use of corrosion inhibitors in this study. Prepare 5-acetyl-2-anilino-4-dimethylaminothiazole and test it as a corrosion inhibitor on a sample of the Rumaila flow line at a constant temperature 25°C in (3.5%) NaCl and (3.5%) KCl solution in the absence and presence of different concentrations

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ZHAN, JIN-HUI, XI ZHAO, XU-RI HUANG, and CHIA-CHUNG SUN. "MOLECULAR DYNAMICS AND FREE ENERGY ANALYSES OF ERK2–PYRAZOLYLPYRROLE INHIBITORS INTERACTIONS: INSIGHT INTO STRUCTURE-BASED LIGAND DESIGN." Journal of Theoretical and Computational Chemistry 08, no. 05 (2009): 887–908. http://dx.doi.org/10.1142/s0219633609005131.

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The extracellular signal-regulated protein kinase 2 (ERK2) is a pivotal member involving in Ras/Raf/MEK/ERK signal transduction pathway, acting as a central point where multiple signaling pathways coalesce to drive transcription. The pyrazolylpyrrole compounds as ATP competitive inhibitors of ERK2 can bind target with a special binding mode and have higher inhibitory potency than other ERK2-inhibitors. We investigated the interaction mode of ERK2-inhibitor using molecular dynamics simulation. The molecular mechanics Poisson–Boltzmann surface area approach is used to calculate the binding free

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El-latif, Ashraf Oukasha Abd. "Protease purification and characterization of a serine protease inhibitor from Egyptian varieties of soybean seeds and its efficacy against Spodoptera littoralis." Journal of Plant Protection Research 55, no. 1 (2015): 16–25. http://dx.doi.org/10.1515/jppr-2015-0003.

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Abstract Serine inhibitors have been described in many plant species and are universal throughout the plant kingdom. Trypsin inhibitors are the most common type. In the present study, trypsin and chymotrypsin inhibitory activity was detected in the seed flour extracts of four Egyptian varieties of soybean (Glycine max). The soybean variety, Giza 22, was found to have higher trypsin and chymotrypsin inhibitory potential compared to other tested soybean varieties. For this reason, Giza 22 was selected for further purification studies which used ammonium sulphate fractionation and DEAE-Sephadex A

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ALIAS, ZAZALI, and NORA ASYIKIN RAMLI. "PURIFICATION AND PARTIAL CHARACTERISATION OF A PROTEASE INHIBITOR FROM Mimosa diplotricha." Malaysian Applied Biology 51, no. 4 (2022): 169–75. http://dx.doi.org/10.55230/mabjournal.v51i4.26.

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Search for inhibitors to insect proteases is one of many strategies to control pests. Previous work has demonstrated successful purification of effective inhibitors from plant origin. Thus, the current study attempted to purify protease inhibitors from locally available medicinal plants. The study demonstrated that the ethanolic extracts of Mimosa diplotricha leaves caused a significant 80% reduction in bovine trypsin activity. The inhibitory property of the proteinaceous nature of the extract was reconfirmed through qualitative analysis using the detection of trypsin inhibitors on the SDS-PAG

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VARGA, Andrei, Camelia URDĂ, Ramona Dina GALBEN, et al. "Soybean Trypsin Inhibitor Activity - a review." Hop and Medicinal Plants 31, no. 1-2 (2023): 151–60. https://doi.org/10.15835/hpm.v31i1-2.14745.

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Soybean (Glycine max) is one of the most important source of protein for food and feed globally. Complete utilization of protein in human and animal digestion can be reduced by certain trypsin inhibitory (TI) substances present in fresh soybeans. Two classes of protease inhibitors (polypeptides) are found in soybeans: Kunitz trypsin inhibitor (KTI) and Bowman-Birk trypsin inhibitor (BBI). KTI is primarily responsible for its trypsin inhibitory activity, while BBI has been reported to have nutraceutical properties. The content of TI in soybean depends on the soybean genotype, environmental fact

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Shi, Qizhen, Erin L. Kuether, Jocelyn A. Schroeder, Scot A. Fahs, David A. Wilcox, and Robert R. Montgomery. "The Important Role of Von Willebrand Factor In Platelet-Derived FVIII Gene Therapy of Murine Hemophilia A In the Presence of Inhibitors." Blood 116, no. 21 (2010): 2201. http://dx.doi.org/10.1182/blood.v116.21.2201.2201.

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Abstract Abstract 2201 von Willebrand factor (VWF) is a carrier protein for FVIII and protects FVIII from protease degradation. Our previous studies have demonstrated that targeting FVIII expression to platelets results in FVIII storage together with VWF in platelet α-granules and that platelet-FVIII (2bF8) corrects murine hemophilia A phenotype even in the presence of high titer anti-FVIII inhibitory antibodies. While ectopic expression of FIX in platelets is also trafficked and stored in α-granules and corrects the bleeding diathesis in hemophilia B mice, the efficacy of platelet-FIX is limi

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E, Jingwen, Ye Liu, Shanshan Guan, et al. "How Different Substitution Positions of F, Cl Atoms in Benzene Ring of 5-Methylpyrimidine Pyridine Derivatives Affect the Inhibition Ability of EGFRL858R/T790M/C797S Inhibitors: A Molecular Dynamics Simulation Study." Molecules 25, no. 4 (2020): 895. http://dx.doi.org/10.3390/molecules25040895.

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Lung cancer is the most frequent cause of cancer-related deaths worldwide, and mutations in the kinase domain of the epidermal growth factor receptor (EGFR) are a common cause of non-small-cell lung cancers, which is a major subtype of lung cancers. Recently, a series of 5-methylpyrimidine-pyridinone derivatives have been designed and synthesized as novel selective inhibitors of EGFR and EGFR mutants. However, the binding-based inhibition mechanism has not yet been determined. In this study, we carried out molecular dynamic simulations and free-energy calculations for EGFR derivatives to fill

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Gouw, Samantha C., Johanna G. van der Bom, Günter Auerswald, Carmen Escuriola Ettinghausen, Ulf Tedgård, and H. Marijke van den Berg. "Recombinant versus plasma-derived factor VIII products and the development of inhibitors in previously untreated patients with severe hemophilia A: the CANAL cohort study." Blood 109, no. 11 (2007): 4693–97. http://dx.doi.org/10.1182/blood-2006-11-056317.

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Abstract It has been suggested that plasma-derived factor VIII products induce fewer inhibitors than recombinant factor VIII products. We investigated the relationship of factor VIII product type and switching between factor VIII products with the risk to develop inhibitors. This multicenter retrospective cohort study included 316 patients with severe hemophilia A born between 1990 and 2000. The outcome was clinically relevant inhibitor development, defined as the occurrence of at least 2 positive inhibitor titers with decreased recovery. The risk of inhibitor development was not clearly lower

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Batsuli, Glaivy, Courtney Cox, John F. Healey, Pete Lollar, and Shannon L. Meeks. "Anti-Factor VIII C1 Domain Antibodies Are Present in the Plasmas of Patients with Hemophilia and Inhibitors." Blood 124, no. 21 (2014): 1482. http://dx.doi.org/10.1182/blood.v124.21.1482.1482.

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Abstract Hemophilia A is an X-linked disorder characterized by a deficiency or absence of blood coagulation protein factor VIII (fVIII). Treatment involves replacement of fVIII through infusions for acute bleeding episodes or prevention of bleeding events. Approximately 30% of individuals with severe hemophilia A will develop antibodies to fVIII. Many studies have characterized the antigenic properties of the C2 and A2 domains as these domains are considered the predominant immunogenic domains of the fVIII protein. However, there is increasing evidence that the C1 domain contributes to fVIII f

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Potempa, J., J. K. Wunderlich, and J. Travis. "Comparative properties of three functionally different but structurally related serpin variants from horse plasma." Biochemical Journal 274, no. 2 (1991): 465–71. http://dx.doi.org/10.1042/bj2740465.

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Three structurally related but functionally different serpins from horse plasma were isolated and characterized. In spite of their identical N-terminal sequences, which show some similarity to that of human alpha 1-proteinase inhibitor, the reactive-centre loops of each of these proteins show extensive variation. Only inhibitor I, with a P1 methionine residue, resembles human alpha 1-PI with regard to (a) similarity of amino acid sequence in the vicinity of the reactive-site peptide bond, (b) broad inhibitory specificity, (c) sensitivity to oxidative inactivation and (d) high rate of reactivit

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Liao, Z., A. Haimovitz, Y. Chen, J. Chan, and D. L. Rosenstreich. "Characterization of a human interleukin 1 inhibitor." Journal of Immunology 134, no. 6 (1985): 3882–86. http://dx.doi.org/10.4049/jimmunol.134.6.3882.

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Abstract Human urine contains a specific inhibitor of interleukin 1 (IL 1) that is found in increased amounts during fever. This inhibitor was purified by using a sequence of ammonium sulfate fractionation, DEAE cellulose ion-exchange chromatography, molecular sieve chromatography on Sephacryl S-200, affinity chromatography on concanavalin A (Con A) Sepharose, and polyacrylamide gel electrophoresis. Two peaks of IL 1 inhibitory material were eluted from the polyacrylamide gels. One peak contained three proteins of 29, 32, and 67 kd, respectively, which could be visualized by silver staining. T

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Kubyshkin, A. V., and I. I. Fomochkina. "THE INFLUENCE OF INTRODUCTION OF PROTEINASE INHIBITORS ON EFFICIENCY FOR SUPPRESSION OF PROTEOLYTIC ACTIVATION OF PNEUMONIA." Fiziolohichnyĭ zhurnal 55, no. 1 (2009): 43–48. http://dx.doi.org/10.15407/fz55.01.043.

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We studied the influence of a way of introduction proteinase inhibitors on efficiency of suppression of proteolysis activation during pneumonia. Comparative study of efficiency of proteases inhibition in experimental pneumonia has shown higher efficacy of local introduction of drugs. Intravenous and intraperitoneal introduction of proteinase inhibitors exhibited inhibitory effect of a smaller degree on local and systemic proteases activation, did not decrease an acute phase of response of a-1-protease inhibitor in comparison with endotracheal instillation of Contrycal and Ingiprol. The study h

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Jang, Dong Man, Hyo Jin Lim, Hyunggu Hahn, Yeon Lee, Hark Kyun Kim, and Hyoun Sook Kim. "Structural Basis of Inhibition of DCLK1 by Ruxolitinib." International Journal of Molecular Sciences 22, no. 16 (2021): 8488. http://dx.doi.org/10.3390/ijms22168488.

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Given the functional attributes of Doublecortin-like kinase 1 (DCLK1) in tumor growth, invasion, metastasis, cell motility, and tumor stemness, it is emerging as a therapeutic target in gastrointestinal cancers. Although a series of specific or nonspecific ATP-competitive inhibitors were identified against DCLK1, different types of scaffolds that can be utilized for the development of highly selective inhibitors or structural understanding of binding specificities of the compounds remain limited. Here, we present our work to repurpose a Janus kinase 1 inhibitor, ruxolitinib as a DCLK1 inhibito

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Yamasaki, Tomohiro, Lumin Zhang, Tyrone Dowdy, Adrian Lita, Kazuhiko Kurozumi, and Mioara Larion. "TMET-15. THE COMBINATIONAL EFFECT OF INHIBITOR FOR A FATTY ACID DESATURASE AND A FATTY ACID TRANSPORTER ON GLIOMA GROWTH." Neuro-Oncology 25, Supplement_5 (2023): v275—v276. http://dx.doi.org/10.1093/neuonc/noad179.1059.

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Abstract BACKGROUND It is not well understood how much exogenous fatty acids uptake and de novo fatty acid synthesis affect the cell proliferation in glioma. In this study, we examined the combinational effect of inhibitor for a fatty acid desaturase (SCD) and a fatty acid transporter (CD36) on glioma growth. METHODS Normal human astrocytes (NHA) were used as glial cells, and U251 transfected with IDH wild-type or IDH mutant gene and patient-derived glioma cells (BT142, TS603, GSC923S) were used as glioma cells. The function of SCD was suppressed by SCD inhibitor and SCD siRNA, and Sulfo-N-suc

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Li, Qi, Hongyu Yang, Jun Mo, et al. "Identification by shape-based virtual screening and evaluation of new tyrosinase inhibitors." PeerJ 6 (January 26, 2018): e4206. http://dx.doi.org/10.7717/peerj.4206.

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Targeting tyrosinase is considered to be an effective way to control the production of melanin. Tyrosinase inhibitor is anticipated to provide new therapy to prevent skin pigmentation, melanoma and neurodegenerative diseases. Herein, we report our results in identifying new tyrosinase inhibitors. The shape-based virtual screening was performed to discover new tyrosinase inhibitors. Thirteen potential hits derived from virtual screening were tested by biological determinations. Compound 5186-0429 exhibited the most potent inhibitory activity. It dose-dependently inhibited the activity of tyrosi

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Naito, Y., and J. M. Lowenstein. "5′-Nucleotidase from rat heart membranes. Inhibition by adenine nucleotides and related compounds." Biochemical Journal 226, no. 3 (1985): 645–51. http://dx.doi.org/10.1042/bj2260645.

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ADP and ATP and their analogues were evaluated as inhibitors of 5′-nucleotidase purified from heart plasma membrane. ADP analogues are more powerful inhibitors than the corresponding ATP analogues. The most powerful inhibitor found is adenosine 5′-[alpha beta-methylene]diphosphate (AOPCP) for which the enzyme shows a Ki of 5 nM at pH 7.2. Measurements of pKi values for ADP and AOPCP as a function of pH indicate that the major inhibitory species of both nucleotides is the dianion. In the physiological range of pH values, AOPCP is a more powerful inhibitor than ADP principally because a higher p

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