Academic literature on the topic 'Peptidic synthesis'

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Journal articles on the topic "Peptidic synthesis"

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Collar, Aarón Gutiérrez, and Tanja Gulder. "Peptidic catalysts for macrocycle synthesis." Science 366, no. 6472 (December 19, 2019): 1454. http://dx.doi.org/10.1126/science.aaz9325.

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Chronopoulou, Laura, Silvia Lorenzoni, Giancarlo Masci, Mariella Dentini, Anna Rita Togna, Giuseppina Togna, Federico Bordi, and Cleofe Palocci. "Lipase-supported synthesis of peptidic hydrogels." Soft Matter 6, no. 11 (2010): 2525. http://dx.doi.org/10.1039/c001658f.

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Surís-Valls and Voets. "Peptidic Antifreeze Materials: Prospects and Challenges." International Journal of Molecular Sciences 20, no. 20 (October 17, 2019): 5149. http://dx.doi.org/10.3390/ijms20205149.

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Necessitated by the subzero temperatures and seasonal exposure to ice, various organisms have developed a remarkably effective means to survive the harsh climate of their natural habitats. Their ice-binding (glyco)proteins keep the nucleation and growth of ice crystals in check by recognizing and binding to specific ice crystal faces, which arrests further ice growth and inhibits ice recrystallization (IRI). Inspired by the success of this adaptive strategy, various approaches have been proposed over the past decades to engineer materials that harness these cryoprotective features. In this review we discuss the prospects and challenges associated with these advances focusing in particular on peptidic antifreeze materials both identical and akin to natural ice-binding proteins (IBPs). We address the latest advances in their design, synthesis, characterization and application in preservation of biologics and foods. Particular attention is devoted to insights in structure-activity relations culminating in the synthesis of de novo peptide analogues. These are sequences that resemble but are not identical to naturally occurring IBPs. We also draw attention to impactful developments in solid-phase peptide synthesis and ‘greener’ synthesis routes, which may aid to overcome one of the major bottlenecks in the translation of this technology: unavailability of large quantities of low-cost antifreeze materials with excellent IRI activity at (sub)micromolar concentrations.
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Dood, Dharmpal S., Alan P. Kozikowski, Bernadette Cusack, and Elliott Richelson. "Synthesis of partially non-peptidic neurotensin mimetics." Bioorganic & Medicinal Chemistry Letters 4, no. 10 (May 1994): 1241–46. http://dx.doi.org/10.1016/s0960-894x(01)80338-3.

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Bird, Michael J., Anthony P. Silvestri, and Philip E. Dawson. "Expedient on-resin synthesis of peptidic benzimidazoles." Bioorganic & Medicinal Chemistry Letters 28, no. 16 (September 2018): 2679–81. http://dx.doi.org/10.1016/j.bmcl.2018.04.062.

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Baell, Jonathan B., Peter J. Duggan, and Y. Phei Lok. "ω-Conotoxins and Approaches to Their Non-Peptide Mimetics." Australian Journal of Chemistry 57, no. 3 (2004): 179. http://dx.doi.org/10.1071/ch03242.

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ω-Conotoxins are an interesting class of naturally occurring peptides that induce dramatic effects on the central nervous system (CNS). They have been shown to interfere with the normal function of neuronal calcium channels and can act as non-addictive analgesics. The usual problems associated with the delivery of peptidic therapeutics have led to efforts to produce non-peptidic mimetics of ω-conotoxins. Identification of the key amino-acid residues responsible for the physiological effects of the ω-conotoxins MVIIA and GVIA has allowed the design and synthesis of compounds that bind to neuronal calcium channels at low micromolar concentrations. These mimics bear the side chains of three amino acids that project from central scaffolds in similar ways to critical side chains of the conotoxins they simulate. Several useful leads have been identified, some of which show selectivity for N-type calcium channels.
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Albin, John S., and Bradley L. Pentelute. "Efficient Flow Synthesis of Human Antimicrobial Peptides." Australian Journal of Chemistry 73, no. 4 (2020): 380. http://dx.doi.org/10.1071/ch20043.

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Organisms from all kingdoms of life have evolved a vast array of peptidic natural products to defend against microbes. These are known collectively as antimicrobial peptides (AMPs) or host defence peptides, reflecting their abilities not only to directly kill microbes, but also to modulate host immune responses. Despite decades of investigation, AMPs have yet to live up to their promise as lead therapeutics, a reality that reflects, in part, our incomplete understanding of these diverse agents in their various physiological contexts. Towards improving our understanding of AMP biology and the ways in which this can be best leveraged for therapeutic development, we are interested in large-scale comparisons of the antimicrobial and immunological activities of human AMPs, an undertaking that requires an efficient workflow for AMP synthesis and subsequent characterization. We describe here the application of flow chemistry and reverse-phase flash chromatography to the generation of 43AMPs, approaches that, when combined, significantly expedite synthesis and purification, potentially facilitating more systematic approaches to downstream testing and engineering.
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Keen, Stephen P., Cameron J. Cowden, Brian C. Bishop, Karel M. J. Brands, Antony J. Davies, Ulf H. Dolling, David R. Lieberman, and Gavin W. Stewart. "Practical Asymmetric Synthesis of a Non-Peptidic αvβ3Antagonist." Journal of Organic Chemistry 70, no. 5 (March 2005): 1771–79. http://dx.doi.org/10.1021/jo048082n.

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Ciapetti, Paola, André Mann, Angèle Schoenfelder, Maurizio Taddei, Elisabeth Trifilieff, Isabelle Canet, and Jean Louis Canet. "Design and synthesis of chiral peptidic nucleic acids." Letters in Peptide Science 4, no. 4-6 (December 1997): 341–49. http://dx.doi.org/10.1007/bf02442898.

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Peddie, Victoria, Raymond J. Butcher, Ward T. Robinson, Matthew C. J. Wilce, Daouda A. K. Traore, and Andrew D. Abell. "Synthesis and Conformation of Fluorinated β-Peptidic Compounds." Chemistry - A European Journal 18, no. 21 (April 19, 2012): 6655–62. http://dx.doi.org/10.1002/chem.201200313.

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Dissertations / Theses on the topic "Peptidic synthesis"

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Jaulent, Agnes Marianne. "Design, synthesis and biological assay of peptidic protease inhibitors." Thesis, Imperial College London, 2005. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.416585.

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Rihakova, Lenka. "New peptidic angiotensin II analogues : their synthesis and pharmacological characterization." Thèse, Sherbrooke : Université de Sherbrooke, 2001. http://savoirs.usherbrooke.ca/handle/11143/4154.

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Sood, Geeta. "Base modified peptidic nucleic acids: synthesis and crystallographic analysis of intermediates." Thesis, Aston University, 1998. http://publications.aston.ac.uk/10967/.

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Peptidic Nucleic Acids (PNAs) are achiral, uncharged nucleic add mimetics, with a novel backbone composed of N-(2-aminoethyl)glycine units attached to the DNA bases through carboxymethylene linkers. With the aim of extending and improving upon the molecular recognition properties of PNAs, the aim of this work was to synthesjse PNA building block intermediates containing a series of substituted purine bases for subsequent use in automated PNA synthesis. Four purine bases: 2,6~diaminopurine (D), isoGuanine (isoG), xanthine (X) and hypoxanthine (H) were identified for incorporation into PNAs targeted to DNA, with the promise of increased hybrid stability over extended pH ranges together with improvements over the use of adenine (A) in duplex formation, and cytosine (C) in triplex formation. A reliable, high-yielding synthesis of the PNA backbone component N -('2- butyloxycarbonyl-aminoethyl)glycinate ethyl ester was establishecl. The precursor N~(2-butyloxycarbonyl)amino acetonitrile was crystallised and analysed by X-ray crystallography for the first time. An excellent refinement (R = 0.0276) was attained for this structure, allowing comparisons with known analogues. Although chemical synthesis of pure, fully-characterised PNA monomers was not achieved, chemical synthesis of PNA building blocks composed of diaminopurine, xanthine and hypoxanthine was completely successful. In parallel, a second objective of this work was to characterise and evaluate novel crystalline intermediates, which formed a new series of substituted purine bases, generated by attaching alkyl substituents at the N9 or N7 sites of purine bases. Crystallographic analysis was undertaken to probe the regiochemistry of isomers, and to reveal interesting structural features of the new series of similarly-substituted purine bases. The attainment of the versatile synthetic intermediate 2,6-dichloro~9- (carboxymethyl)purine ethyl ester, and its homologous regioisomers 6-chloro~9- (carboxymethyl)purine ethyl ester and 6-chloro-7-(carboxymethyl)purine ethyl ester, necessitated the use of X-ray crystallographic analysis for unambiguous structural assignment. Successful refinement of the disordered 2,6-diamino-9-(carboxymethyl) purine ethyl ester allowed comparison with the reported structure of the adenine analogue, ethyl adenin-9-yl acetate. Replacement of the chloro moieties with amino, azido and methoxy groups expanded the internal angles at their point of attachment to the purine ring. Crystallographic analysis played a pivotal role towards confirming the identity of the peralkylated hypoxanthine derivative diethyl 6-oxo-6,7-dihydro-3H-purlne~3,7~djacetate, where two ethyl side chains were found to attach at N3 and N7.
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Mulani, Amina. "Synthesis and Evaluation of Peptidic Probes for Tissue Transglutaminase and Factor XIIIa." Thesis, Université d'Ottawa / University of Ottawa, 2014. http://hdl.handle.net/10393/31224.

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Transglutaminases (TGases) are a group of enzymes that catalyze the formation of an amide bond between the γ-carboxamide group of a glutamine residue and an amine donor, usually an ε-amino group of the lysine residue, leading to the formation of ε-(γ-glutamyl)lysine crosslinks. Owing to the roles that transglutaminases such as tissue transglutaminase (TG2) and Factor XIIIa (FXIIIa) have been found to play in a wide range of disease states, efforts have been directed towards the study of these proteins. The study of enzymes to better understand their function and mode of action is facilitated through the use of tools such as protein labelling, enzyme inhibition, and substrate analogue kinetic studies among others. Transition state analogues have been effective inhibitors in the study of enzyme activity. Sulfoxide inhibitors can efficiently mimic transition states leading to the tetrahedral intermediate of an acyl transfer reaction and we discuss the synthesis towards sulfoxide transition state analogue inhibitors of TG2 in chapter 2. Novel sulfoxide compounds were synthesized, though the desired target compounds proved difficult to isolate due to their instability. Fluorescent probes are effective in protein labelling as a means of discerning activity. This technique was applied in order to elucidate intracellular TG2 activity, which is a topic of controversy. To that end, the synthesis of a fluorescent, TG2-specific, cell permeable probe is discussed in chapter 3. However, preliminary in vivo results show that while the probe is cell permeable and fluorescent, it was not TG2-specific. Molecular modelling suggests that the hexa-arginine tag, designed to improve cell permeability, decreases the affinity of the probe for its intended target. Finally, FXIIIa has become a new addition to the study of transglutaminases in the Keillor group. Given our interest in this enzyme, we had three goals for this work as explained in chapter 4. Firstly, owing to the anticipated high demand for FXIIIa required for later experiments, our primary aim was the development of an optimized method for the expression and purification of recombinant FXIIIA. After evaluating different conditions for FXIIIA expression, the Studier auto-induction ZYP media1 at 20 °C for 24 h was found to provide the optimal conditions for the expression of recombinant GST-tagged FXIIIA, typically giving a total of 1.5 mg of protein/L of culture. Secondly, a variety of different peptides were synthesized and tested using a glutamate dehydrogenase (GDH)-based assay to identify a high affinity sequence for a substrate of FXIIIa. The two peptides with the highest affinity for FXIIIa were Ac-DQMMMAF-OH and Ac-DQMML-OH. Testing with TG2 displayed negligible reactivity, confirming their use as orthogonal peptides, results reinforced by modelling studies of the peptides with both FXIIIa and TG2. This discovery represents the first time peptides orthogonal to TG2 with affinity for FXIIIa have been kinetically characterized with both transglutaminase enzymes. Lastly, our work towards a fluorogenic activity assay by incorporating a coumarin ester through attachment to a glutamic acid residue into a peptide sequence recognized by FXIIIa, will be discussed.
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Hernandez, Maria Luisa Escudero. "Enzymatic desymmetrization of prochiral cyclohexanones : synthesis of a non-peptidic NK2 antagonist." Thesis, University of Liverpool, 2000. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.343757.

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Willems, Hendrika Maria Gerarda. "The design and synthesis of non-peptidic α-helix and β-turn mimetics." Thesis, University of Cambridge, 1996. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.627463.

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Lamm, Matthew S. "Molecular self-assembly design, synthesis, and characterization of peptidic materials for bio- and nano-technologies /." Access to citation, abstract and download form provided by ProQuest Information and Learning Company; downloadable PDF file, 136 p, 2008. http://proquest.umi.com/pqdweb?did=1456296191&sid=2&Fmt=2&clientId=8331&RQT=309&VName=PQD.

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Remesic, Michael Vincent, and Michael Vincent Remesic. "The Design, Synthesis, and Biological Evaluation of Novel Peptidic Ligands for the Treatment of Chronic Neuropathic Pain." Diss., The University of Arizona, 2017. http://hdl.handle.net/10150/625593.

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Chronic neuropathic pain is a disease that impacts the livelihood of millions of people in the United States with no effective pain treatments and limited information pertaining to the underlying mechanisms. Opioid therapy is considered the gold standard for pain therapeutics, but chronic use of these medications brings about serious side effects such as tolerance, addiction, and respiratory depression which limit their overall therapeutic potential. Herein, two approaches are discussed to circumvent these issues: i) a multifunctional approach using N-phenyl-N-piperidin-4-yl-propionamide (Ppp) coupled to various endogenous opioid ligand scaffolds, and ii) non-opioid dynorphin A (DYN A) ligands at the Bradykinin-2 receptor (B2R). The μ-opioid receptor (MOR) upon agonist stimulation provides analgesia and concomitant activation of the δ-opioid receptor (DOR) leads to an increased antinociceptive effect. Chronic activation of the MOR has been correlated with an upregulation of the κ-opioid receptor (KOR) and KOR associated side effects such as anxiety and depression. The discovery of a new class of opioid receptor (OR) ligands that have the biological profile of MOR/DOR agonists and KOR antagonists would be beneficial considering they would have an increased analgesic effect, leading to a lower dosage being administered and thus lower overall side effects, and block symptoms elicited from KOR stimulation. Discussed are various structure activity relationships (SARs) of numerous scaffolds that present novel biological profiles. Ultimately, we discovered a compound that, to our knowledge, is the 1st MOR/DOR agonist and KOR antagonist. DYN A is the endogenous ligand for the KOR and its [des-Tyr1]-DYN A fragment interacts with the B2R, but not the KOR, promoting hyperalgesia. Peptidomimetic non-opioid DYN A analogues were synthesized and evaluated at the B2R. A minimum pharmacophore was identified and antagonists with both improved biological stability and affinity were discovered.
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Minta, Ewelina. "Synthesis and structure-activity relationship of peptidic analogues of omega-agatoxin IVB, pharmacological toll in cognition studies : towards calcium channel modulators." Montpellier 2, 2006. http://www.theses.fr/2006MON20072.

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Ce manuscript décrit la synthèse et l'évaluation biologique d'analogues de l'w-agatoxine IV B dans le but de trouver de nouveaux outils pour l'étude de l'activité de canaux calciques. L'w-agatoxine IV B est une neurotoxine peptidique isolée du venin d'araignée Agelenopsis aperta qui à ce jour est l'inhibiteur spécifique et sélectif des canaux calciques de type P (avec l'w-agatoxine IV A). Les canaux calciques de type P sont les canaux dépendant du voltage impliqués dans la neurotransmission dépendante du Glutamate dans le système nerveux central. La synthèse de structures peptidiques simplifiées, en comparaison avec celle de la toxine native, est décrite. L'étude du choix de la cible biologique, avec une approche modélisation moléculaire et la méthodologie de synthèse de differents analogues linéaires et cycliques de cette neurotoxine sont présentées. Les composes sont synthétisés par synthèse peptidique en phase solide (SPPS) en stratégie Fmoc avec une étude particulière sur les conditions de cyclisation et le choix de groupements protecteurs appropriés pour cette réaction de cyclisation. Les modifications des peptides naturels pour obtenir de nouveaux composés biologiquement actifs incluent les modifications des chaines latérales et l'insertion d'aminoacides non naturels (7-azatryptophane, D-Trp-OH, analogue phosphonique du Trp). Les peptides synthétisés ont été testés par des méthodes électrophysiologiques (patch Clamp); les activités biologiques des peptides linéaires et cycliques sont corrélées à l'aids d'analyses structurales par RMN
This dissertation concerns the synthesis and biological evaluation of w-agatoxin IV B mimetics in order to find a new tool for studying calcium channel's activity. W-Agatoxin IVB is one of the neurotoxins extracted from American funnel web spider Agelenopsis aperta, which is to date the only (along with w-agatoxin IVA) very selective gating inhibitor of the P-type calcium channels. Voltage-gated P-type Ca2+ channels are closely involved in glutamate-dependant neurotransmission in mammalian central nervous system (CNS). The syntheses of structurally simplified peptides, in comparison with native toxin, but still with retention of activity, are described. Then, the studies on choice of the biological target, including molecular modelling approach and the methodology of synthesis of different - linear and cyclic - analogues of w-AGA IVB are presented. The compounds were synthesized using solid phase peptide chemistry (SPPS) and Fmoc strategy, with particular consideration for the cyclisation conditions and the insight into selection of protective groups used for peptide cyclisation. Modifications of naturally occurring peptides in order to obtain biologically active components are taken into consideration, which include, among others, side chain modifications and non-natural amino acid insertion (7-AzaTrp, D-Trp, phosphonic analogue of tryptophan). The synthesized peptides were tested using neurophysiological techniques (patch clamp); the biological activity is correlated with NMR structures of cyclic and linear peptides
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Caporale, Andrea. "Function-structure relationship of PHT(1-11) analogues." Doctoral thesis, Università degli studi di Padova, 2008. http://hdl.handle.net/11577/3425540.

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Parathyroid hormone (PTH) is an 84 amino acid peptide hormone produced in the parathyroid glands. It acts primarily on bone and kidney to maintain extracellular calcium levels within normal limits. It has been shown that the 1-34 N-terminal fragment of PTH is sufficient to bind and activate the PTH type I receptor (PTH1R). The study of reduced-size PTH agonist and antagonist analogues has been the subject of extensive research for the development of bone anabolic drugs. Recent investigations focusing on the interaction of N-terminal fragments of PTH with PTH1R showed that some modifications can increase signalling potency in peptides as short as 11 amino acid residues (e.g. S3→A3, N10→Q10, L11→R11). This work of PhD thesis represents our effort to investigate the role of side chains and structural characteristics of N-terminal domain of PTH(1-11). We applied the hierarchical approach and some peptidomimetics concepts to synthesize specific libraries of peptide to obtain information about hormone/receptor interaction. With these information, we have been able to project a first example of peptidomimetic of PTH. The strategical role of Val2 in the interaction with the PTH1R receptor was demonstrated and confirmed. We have observed that guanidine group in C-terminus has a specific role in the binding to the receptor for the shortest PTH(1-11) fragment. We have shown that substitutions with alpha-MeNle at positions 8 can increase helix stability which can be also stabilized and promoted through a bridge between 6 and 10 positions. We synthesized a group of active analogues which are characterized by a stable alpha-helix in all peptide sequences and have the correct orientation of essential esidues 2, 5, 8 and 11.
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Books on the topic "Peptidic synthesis"

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The chemical synthesis of peptides. Oxford: Clarendon Press, 1991.

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Labsystems Research Symposium on Synthetic Peptides in Biology and Medicine (1985 Hämeenlinna, Finland). Synthetic peptides in biology and medicine: Proceedings of the Labsystems Research Symposium on Synthetic Peptides in Biology and Medicine held in Hämeenlinna, Finland, on June 6-8, 1985. Edited by Alitalo Kari, Partanen Paul, Vaheri Antti, and Labsystems (Firm). Amsterdam: Elsevier Science Publishers, 1985.

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D, Fricker Lloyd, ed. Peptide biosynthesis and processing. Boca Raton: CRC Press, 1991.

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Peptide synthesis and applications. 2nd ed. New York: Humana Press, 2013.

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Hussein, Waleed M., Mariusz Skwarczynski, and Istvan Toth, eds. Peptide Synthesis. New York, NY: Springer US, 2020. http://dx.doi.org/10.1007/978-1-0716-0227-0.

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1949-, Basava Channa, and Anantharamaiah G. M. 1947-, eds. Peptides: Design, synthesis, and biological activity. Boston: Birkhäuser, 1994.

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Pennington, Michael W., and Ben M. Dunn. Peptide Synthesis Protocols. New Jersey: Humana Press, 1994. http://dx.doi.org/10.1385/0896032736.

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Enzymatic peptide synthesis. Boca Raton, FL: CRC Press, 1987.

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W, Pennington Michael, and Dunn Ben M, eds. Peptide synthesis protocols. Totowa, N.J: Humana Press, 1994.

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Bodanszky, M. Principles of peptide synthesis. 2nd ed. Berlin: Springer-Verlag, 1993.

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Book chapters on the topic "Peptidic synthesis"

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Baumann, Michael, Delf Schmid, Hilmar Bischoff, Christoph Königs, Ursula Dietrich, and Christian Griesinger. "Combinatorial Synthesis, Screening and Testing of Peptidic RNA-Ligands." In Peptides: The Wave of the Future, 204–5. Dordrecht: Springer Netherlands, 2001. http://dx.doi.org/10.1007/978-94-010-0464-0_91.

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Meldal, Morten. "Organozymes: Molecular Engineering and Combinatorial Selection of Peptidic Organo- and Transition-Metal Catalysts." In Organic Synthesis and Molecular Engineering, 333–60. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2013. http://dx.doi.org/10.1002/9781118736449.ch12.

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Mathieu, Marc N., John D. Wade, Yean-Yeow Tan, Roger J. Summers, and Geoffrey W. Tregear. "Design, synthesis and biological activity of template-assembled peptidic mimetics of rat relaxin." In Relaxin 2000, 241–42. Dordrecht: Springer Netherlands, 2001. http://dx.doi.org/10.1007/978-94-017-2877-5_38.

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Wisniewski, Kazimierz, Robert Galyean, Hiroe Taki, Sudar Alagarsamy, Glenn Croston, Regent Laporte, Claudio D. Schteingart, and Pierre J.-M. Rivière. "Synthesis and in vitro Pharmacological Profile of Potent and Selective Peptidic V1a Receptor Agonists." In Advances in Experimental Medicine and Biology, 507–8. New York, NY: Springer New York, 2009. http://dx.doi.org/10.1007/978-0-387-73657-0_220.

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Mérette, Sandrine A. M., Christopher A. Goodwin, Michael F. Scully, and John J. Deadman. "N to C Solid Phase Organic Synthesis of Peptidic and Peptidomimetic Derivatives Using 9-Fluorenylmethyl Esters." In Peptides: The Wave of the Future, 279–80. Dordrecht: Springer Netherlands, 2001. http://dx.doi.org/10.1007/978-94-010-0464-0_127.

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Otvos, Laszlo, Philippe Bulet, Istvan Varga, and Ralf Hoffmann. "Antibacterial insect glycopeptides: Synthesis, structure and activity." In Peptides Frontiers of Peptide Science, 703–4. Dordrecht: Springer Netherlands, 2002. http://dx.doi.org/10.1007/0-306-46862-x_307.

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Nishio, Hideki, Tatsuya Inui, Yuji Nishiuchi, Edward G. Rowan, Alan L. Harvey, Terutoshi Kimura, and Shumpei Sakakibara. "Solution synthesis and structure revision of dendrotoxin I." In Peptides Frontiers of Peptide Science, 593–94. Dordrecht: Springer Netherlands, 2002. http://dx.doi.org/10.1007/0-306-46862-x_257.

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Schmid, Holger, Sjouke Hoving, Stefan Vetter, Thomas Vorherr, and Ernesto Carafoli. "Synthesis and purification of unphosphorylated and phosphorylated Phospholamban." In Peptides Frontiers of Peptide Science, 709–10. Dordrecht: Springer Netherlands, 2002. http://dx.doi.org/10.1007/0-306-46862-x_310.

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Kalle, Kilk, and lo Langel. "Cellular Delivery of Peptide Nucleic Acid by Cell-Penetrating Peptides." In Peptide Synthesis and Applications, 131–41. Totowa, NJ: Humana Press, 2005. http://dx.doi.org/10.1385/1-59259-877-3:131.

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Kitaguchi, H. "Peptide synthesis." In Enzymatic Reactions in Organic Media, 224–43. Dordrecht: Springer Netherlands, 1996. http://dx.doi.org/10.1007/978-94-011-0611-5_8.

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Conference papers on the topic "Peptidic synthesis"

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Liet,, Benjamin, Eugénie Laigre, Claire Tiertant, Didier Boturyn, Nathalie Berthet, and Olivier Renaudet. "Design, synthesis and study of multimeric peptidic conjugates for a new approach of antitumoral immunotherapy." In 35th European Peptide Symposium. Prompt Scientific Publishing, 2018. http://dx.doi.org/10.17952/35eps.2018.043.

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Gonzalez, Janet, Anna Babinska, Ebenezer L. V. Ewul, Edem Timpo, Alhassan Jallow, Zhiyong Qiu, Radoslaw Bednarek, et al. "Structure-Based Design, Synthesis and Evaluation of Novel Peptidic Inhibitors of Thrombin-Induced Activation of Platelets Aggregation." In The 24th American Peptide Symposium. Prompt Scientific Publishing, 2015. http://dx.doi.org/10.17952/24aps.2015.174.

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Premnath, Padmavathy N., Joshua K. Bolger, Shu Liu, and McInnes Campbell. "Abstract 1351: Computational design and synthesis of non-peptidic inhibitors targeting the cyclin binding groove of CDK2/Cyclin A." In Proceedings: AACR 102nd Annual Meeting 2011‐‐ Apr 2‐6, 2011; Orlando, FL. American Association for Cancer Research, 2011. http://dx.doi.org/10.1158/1538-7445.am2011-1351.

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Mikheeva, N. A., E. P. Drozhdina, and N. A. Kurnosova. "Morphofunctional features of proliferating cells exposed to PSMA peptide." In VIII Vserossijskaja konferencija s mezhdunarodnym uchastiem «Mediko-fiziologicheskie problemy jekologii cheloveka». Publishing center of Ulyanovsk State University, 2021. http://dx.doi.org/10.34014/mpphe.2021-142-144.

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The effect of the synthetic PSMA peptide on dividing cells of laboratory animals was studied. The experiment was carried out on male white laboratory mice of the BALB/c-line. The toxic effect of PSMA peptidi was evaluated at therapeutic (1.4 μg / kg of animal weight or 0.04 μg / animal) and subtoxic (140 μg / kg of animal weight or 4.0 μg / animal) doses. The cytotoxic effect of PSMA peptide on red bone marrow cells and cambial intestinal cells of the of laboratory mice was determined. A decrease in the proliferative activity of the colon crypt cells was revealed upon administration of a subtoxic dose of the PSMA peptide and there were no signs of toxic damage to the red bone marrow cells of animals. Key words: toxicity, proliferation, synthetic peptides, mitotic index, micronucleus test.
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Stüber, W., H. Pelzer, and N. Heimburger. "INDUCTION OF ANTITHROMBIN III (AT III) ANTIBODIES BY IMMUNIZATION WITH SYNTHETIC PEPTIDES." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1644355.

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The primary structure of AT III was examined in respect of potential antigenic sites. The topics were the determination of the hydrophilicity, hydropathy, acrophilicity and the propensities for alpha-helices, B-turns and 13-sheets. The peptides AT III 21-34, 21-42, 129 - 140, 226 - 240 and 343 -363 were synthesized using the solid phase peptide synthesis methode. The subsequent purification of the crude peptides was achieved by h.p.I.e. or by ion exchange chromatography. The peptides were coupled to keyhole limpet hemocyanine (KLH) via thioether bonds. Antisera against KLH-peptides were raised in rabbits (n = 25) and tested with AT III-coated polystyrene tubes; bound antibodies were detected with anti-rabbit-IgG-peroxidase. Obtained antisera were further purified by immuno-adsorption using immobilized AT III. Polystyrene tubes were coated with purified peptide antibodies and binding of AT III was studied with enzyme immunoassay technique (EIA) using anti-AT III-peroxidase.As a result, immunoreactivity of rabbit antisera against synthetic peptides of AT III could be achieved. The obtained antibodies against the individual synthetic peptides as well as their mixtures exhibited specific binding to AT III when tested with EIA.
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Fulcher, C. A., R. A. Houghten, S. de Graaf Mahoney, J. R. Roberts, and T. S. Zimmerman. "SYNTHETIC PEPTIDE PROBES OF FACTOR VIII IMMUNOLOGY AND FUNCTION." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1644768.

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In order to develop specific immunologic reagents for mapping functionally important sites on FVIII, we have prepared rabbit polyclonal antibodies against synthetic peptides of FVIII derived from regions along the entire FVIII amino acid sequence. To date, a total of 70 peptides have been synthesized and characterized by amino acid and HPLC analysis. The peptides were coupled to keyhole limpet hemocyanin with glutaraldehyde as a linkage reagent and used to immunize rabbits. Antisera were tested by ELISA assay on polystyrene microtiter plates coated with either the peptide immunogen, or purified FVIII. The antisera were also tested for their ability to inhibit FVIII clotting activity and to react with separated FVIII polypeptides on immunoblots.Of the 70 peptides, all reacted with the peptide immunogen, 45 reacted with purified FVIII and 33 reacted with FVIII on immunoblots. Because we had obtained evidence that cleavage of the amino terminal region of the 80 kDa polypeptide may play a role in FVIII activation by thrombin, a series of partially overlapping peptides, 15 residues in length, were synthesized in this area. After affinity purifying these antibodies on columns of FVIII immobilized on agarose, adjusting the antibodies to equal antigen binding titers by dot immunoblotting and testing for inhibition of FVIII activity, only one antibody could strongly inhibit FVIII clotting activity. This inhibition could be blocked by the peptide itself at nanomolar concentrations and no significant inhibition could be shown by antibodies to partially overlapping peptides individually, or in combination. These data suggest that a site important to FVIII function can be localized to a 15 amino acid residue region of the 80 kDa polypeptide of FVIII. In addition, a second inhibitoryantibody was identified which was produced against a peptide in the carboxy terminal region of the 54 kDa thrombin fragment of FVIII and this area is currently being studied in a similar manner. In addition, two monoclonal anti-FVIII synthetic peptide antibodies have been produced which react with purified FVIII on immunoblots. One of these antibodies also functions as an immunoadsorbent when linked to agarose and FVII can be purified in this manner, using the synthetic peptide as eluant. It is evident that antibodies to synthetic peptides of FVIII can be useful probes of FVIII structure, function and interactions as well as being of use in FVIII purification.
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Fresslnaud, E., J. E. Sadler, J. P. Girma, H. R. Baumgartner, and D. Meyer. "SYNTHETIC RGD-CONTAINING PEPTIDES OF VON WILLEBRAND FACTOR INHIBIT PLATELET ADHESION TO COLLAGEN." In XIth International Congress on Thrombosis and Haemostasis. Schattauer GmbH, 1987. http://dx.doi.org/10.1055/s-0038-1643591.

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The Arg-Gly-Asp (RGD) sequence is common to fibrinogen (Fg), fibronectin (Fn) and von Willebrand Factor (vWF). RGD-containing peptides compete for binding of these adhesive proteins to platelet membrane GPIIb/IIIa and inhibit thrombin-induced platelet aggregation as does an unrelated dodecapeptide from the γ Fg COOH terminus (γFg 400-411). We compared in flowing blood the effect of γ Fg 400-411 and of 3 synthetic peptides derived from the sequence of human vWF upon platelet adhesion to collagen. The 3 vWF peptides (13 or 18 aminoacids) contained an RGD sequence in the NH2 (peptide 03), central (peptide 07) or COOH (peptide 02) portions. Collagen was coated onto plastic coverslips and exposed in a parallel-plate perfusion chamber to reconstituted human blood at a shear rate of 2,600 s™1 for 3 min at 37°C. Perfusates contained physiological concentrations of 51 Cr-platelets and red cells in either citrated autologous plasma or modified Tyrode buffer containing 4% human albumin ; in the latter case, the collagen-coated coverslips were preincubated with normal plasma or purified human vWF prior to perfusion. Platelet-collagen interactions were estimated by radioactivity counting and quantitative morphometry. RGD peptides 02, 03 and 07 inhibited platelet-collagen interactions in a dose-dependent manner. With peptide 07, deposition of 51 Cr-platelets decreased from 283.8 ± 32.5 × 105/cm2 (mean ± SEM, n = 3) with buffer to 169.6 ± 33.0 in the presence of 50 μM peptide (p < 0.05), 133.7 ± 26.4 with 150 uM (p <0.012) and 101.8 ± 27.1 with 300 uM (p <0.005). The inhibitory effect of γ Fg 400-411 upon platelet deposition was less significant than that of the RGD peptides at 50 and 150 uM concentrations (224.4 ± 39.8, N.S. and 139.5 ± 55.3, p < 0.05, respectively). RGD peptide 07 also inhibited in a dose-dependent way both platelet adhesion to collagen and thrombus growth. Similar results were observed with peptides 02 and 03, indicating that the position of the RGD sequence is not critical. No synergetic effect between RGD and γFg 400-411 peptides was observed. These results with vWF peptides confirm that GPIIb/IIIa is involved not only In platelet aggregation (thrombus growth) but also in vWF-mediated platelet adhesion to collagen.
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Biondi, Barbara, Silvia Millan, Fernando Formaggio, Alessandra Semenzato, and Cristina Peggion. "Synthesis and conformationof short peptides modeled after peptide LL-37." In 35th European Peptide Symposium. Prompt Scientific Publishing, 2018. http://dx.doi.org/10.17952/35eps.2018.195.

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Bjørlie, Mads, Rachel Irankunda, Jean-Michel Girardet, Sandrine Boschi-Müller, Betül Yesiltas, Charlotte Jacobsen, and Laetitia Canabady-Rochelle. "Screening of Metal-chelating Peptides and Hydrolysates Using Surface Plasmon Resonance and Switchsense." In 2022 AOCS Annual Meeting & Expo. American Oil Chemists' Society (AOCS), 2022. http://dx.doi.org/10.21748/zszk2778.

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Abstract: Lipid oxidation is, among other factors, catalyzed by the presence of metal ions and efficient metal chelators are therefore highly sought after in the food industry. Among these, natural metal chelators are gaining interest as opposed to their synthetic counterparts such as EDTA. Traditional screening for metal chelation capacity is time consuming and non-specific. The aim of this study was to screen potato protein hydrolysate and synthetic peptides derived from potato protein sequences for their metal-chelating capacity. Seven peptides and two hydrolysates (raw and ultra-filtrated) were studied. Peptides were selected using two different models: an empirical-based bioinformatics approach (AnOxPePred) and a theoretically based model for metal chelation. Surface Plasmon Resonance (SPR) is a label-free, optical technique used to determine the dissociation constant (KD) of a complex formed between immobilized Ni2+ and peptides. The SwitchSENSE technology is another approach used to study Ni2+/peptide affinity. It utilizes the quenching of fluorescence of a fluorophore upon Ni2+ immobilization and the inverse fluorescence increase upon peptide binding onto Ni2+. Both analyses were carried out at pH 7.4. In this study, we successfully determined the dissociation constants (KD) of two peptides (ASH and DHGPKIFEPS) using SPR. These values compare favourably with previous results indicating metal chelating potential. The association rate constant (kon) of all peptides were determined using switchSENSE. Yet, due to bad fitting of the kinetics data obtained with switchSENSE, the KDs of the hydrolysates were only determined with low accuracy.
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Lomakin, Aleksey, David B. Teplow, Daniel A. Kirschner, and George B. Benedek. "Nucleation and Growth of Amyloid β-Protein Fibrils: Detection of Nuclei and Quantitation of Rate Constants." In Photon Correlation and Scattering. Washington, D.C.: Optica Publishing Group, 1996. http://dx.doi.org/10.1364/pcs.1996.sab.3.

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Alzheimer's disease is a progressive, neurodegenerative disorder characterized by amyloid deposition in senile plaques in the cerebral parenchyma and vasculature.(1) These plaques are composed primarily of fibers of the amyloid β-protein, Aβ. A number of studies have provided information on the structure of fibrils formed both in vivo and in vitro, and on factors affecting fiber formation. Synthetic Aβ peptides also form fibers which are ultrastructurally indistinguishable from those isolated from the brain. These peptides have been utilized to examine how a variety of parameters, including temperature, pH, solvent composition, peptide concentration, and peptide sequence, influence the final structure of Aβ aggregates. What is substantially less understood, however, is the kinetics of Aβ fibril growth.
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Reports on the topic "Peptidic synthesis"

1

Vouros, Paul, and Terrance Black. Solid Phase Peptide Synthesis of Antimicrobial Peptides for cell Binding Studies: Characterization Using Mass Spectrometry. Fort Belvoir, VA: Defense Technical Information Center, November 2002. http://dx.doi.org/10.21236/ada412571.

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2

Atassi, M. Z. Synthesis and Activity of Oxygen-Carrying Heme Peptides. Fort Belvoir, VA: Defense Technical Information Center, November 2004. http://dx.doi.org/10.21236/ada428126.

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3

Atassi, M. Z. Design & Synthesis of Oxygen-Binding Heme Peptides. Fort Belvoir, VA: Defense Technical Information Center, July 1990. http://dx.doi.org/10.21236/ada224458.

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4

Judd, Amrit K. Active Antitoxic Immunization against Ricin Using Synthetic Peptides. Fort Belvoir, VA: Defense Technical Information Center, August 1989. http://dx.doi.org/10.21236/adb137490.

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Author, Not Given. [Synthetic adhesive peptides for clinical imaging]. Final report. Office of Scientific and Technical Information (OSTI), December 1994. http://dx.doi.org/10.2172/10130310.

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Bredesen, Dale. Novel Synthetic Hunter-Killer Peptides Target and Destroy Prostate Cancer. Fort Belvoir, VA: Defense Technical Information Center, September 1999. http://dx.doi.org/10.21236/ada384822.

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Altstein, Miriam, and Ronald Nachman. Rationally designed insect neuropeptide agonists and antagonists: application for the characterization of the pyrokinin/Pban mechanisms of action in insects. United States Department of Agriculture, October 2006. http://dx.doi.org/10.32747/2006.7587235.bard.

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The general objective of this BARD project focused on rationally designed insect neuropeptide (NP) agonists and antagonists, their application for the characterization of the mechanisms of action of the pyrokinin/PBAN (PK-PBAN) family and the development of biostable, bioavailable versions that can provide the basis for development of novel, environmentally-friendly pest insect control agents. The specific objectives of the study, as originally proposed, were to: (i) Test stimulatory potencies of rationally designed backbone cyclic (BBC) peptides on pheromonotropic, melanotropic, myotropic and pupariation activities; (ii) Test the inhibitory potencies of the BBC compounds on the above activities evoked either by synthetic peptides (PBAN, LPK, myotropin and pheromonotropin) or by the natural endogenous mechanism; (iii) Determine the bioavailability of the most potent BBC compounds that will be found in (ii); (iv) Design, synthesize and examine novel PK/PBAN analogs with enhanced bioavailability and receptor binding; (v) Design and synthesize ‘magic bullet’ analogs and examine their ability to selectively kill cells expressing the PK/PBAN receptor. To achieve these goals the agonistic and antagonistic activities/properties of rationally designed linear and BBC neuropeptide (NP) were thoroughly studied and the information obtained was further used for the design and synthesis of improved compounds toward the design of an insecticide prototype. The study revealed important information on the structure activity relationship (SAR) of agonistic/antagonistic peptides, including definitive identification of the orientation of the Pro residue as trans for agonist activity in 4 PK/PBANbioassays (pheromonotropic, pupariation, melanotropic, & hindgut contractile) and a PK-related CAP₂b bioassay (diuretic); indications that led to the identification of a novel scaffold to develop biostbiostable, bioavailable peptidomimetic PK/PBANagonists/antagonists. The work led to the development of an arsenal of PK/PBAN antagonists with a variety of selectivity profiles; whether between different PKbioassays, or within the same bioassay between different natural elicitors. Examples include selective and non-selective BBC and novel amphiphilic PK pheromonotropic and melanotropic antagonists some of which are capable of penetrating the moth cuticle in efficacious quantities. One of the latter analog group demonstrated unprecedented versatility in its ability to antagonize a broad spectrum of pheromonotropic elicitors. A novel, transPro mimetic motif was proposed & used to develop a strong, selective PK agonist of the melanotropic bioassay in moths. The first antagonist (pure) of PK-related CAP₂b diuresis in flies was developed using a cisPro mimetic motif; an indication that while a transPro orientation is associated with receptor agonism, a cisPro orientation is linked with an antagonist interaction. A novel, biostablePK analog, incorporating β-amino acids at key peptidase-susceptible sites, exhibited in vivo pheromonotropic activity that by far exceeded that of PBAN when applied topically. Direct analysis of neural tissue by state-of-the-art MALDI-TOF/TOF mass spectrometry was used to identify specific PK/PK-related peptides native to eight arthropod pest species [house (M. domestica), stable (S. calcitrans), horn (H. irritans) & flesh (N. bullata) flies; Southern cattle fever tick (B. microplus), European tick (I. ricinus), yellow fever mosquito (A. aegypti), & Southern Green Stink Bug (N. viridula)]; including the unprecedented identification of mass-identical Leu/Ile residues and the first identification of NPs from a tick or the CNS of Hemiptera. Evidence was obtained for the selection of Neb-PK-2 as the primary pupariation factor of the flesh fly (N. bullata) among native PK/PK-related candidates. The peptidomic techniques were also used to map the location of PK/PK-related NP in the nervous system of the model fly D. melanogaster. Knowledge of specific PK sequences can aid in the future design of species specific (or non-specific) NP agonists/antagonists. In addition, the study led to the first cloning of a PK/PBAN receptor from insect larvae (S. littoralis), providing the basis for SAR analysis for the future design of 2ⁿᵈgeneration selective and/or nonselective agonists/antagonists. Development of a microplate ligand binding assay using the PK/PBAN pheromone gland receptor was also carried out. The assay will enable screening, including high throughput, of various libraries (chemical, molecular & natural product) for the discovery of receptor specific agonists/antagonists. In summary, the body of work achieves several key milestones and brings us significantly closer to the development of novel, environmentally friendly pest insect management agents based on insect PK/PBANNPs capable of disrupting critical NP-regulated functions.
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Haynes, Barton F. Structural and Functional Studies of Experimental HIV Synthetic Peptide Immunogens. Fort Belvoir, VA: Defense Technical Information Center, October 1997. http://dx.doi.org/10.21236/ada333309.

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Kennedy, Ronald C. Use of Synthetic Peptides Anti-Idiotypes for Controlling Human Immunodeficiency Virus Infection. Fort Belvoir, VA: Defense Technical Information Center, August 1992. http://dx.doi.org/10.21236/ada269558.

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Hwu, Chia-Yu, and Daniel Harvey. Design, Synthesis and Study of Cell Adhesion Antagonists: Hydroxamate-Based Peptide Inhibitors of avb3 Integrin. Fort Belvoir, VA: Defense Technical Information Center, July 2000. http://dx.doi.org/10.21236/ada384216.

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