Výsledky vyhledávání - "Colin V, Gegg"

Discovery of the Migraine Prevention Therapeutic Aimovig (Erenumab), the First FDA-Approved Antibody against a G-Protein-Coupled Receptor

Autor: Brian Mingtung Chan, Kelly A Berry, David W. Brankow, Chadwick T. King, Sylvia Nai-Yu Hu, Nebojsa Kezunovic, Tom Boone, Licheng Shi, Cen Xu, Colin V. Gegg, Matt R. Kelley, Hsieng Sen Lu

Publikováno v: ACS Pharmacol Transl Sci

[Image: see text] In 2018, the United States Food and Drug Administration (FDA) approved Aimovig (erenumab) for the prevention of migraine. Erenumab is the first FDA approved antibody therapeutic against a G-protein-coupled receptor, the canonical re

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e0a97f4f56650c1bbf83553db82caa76
https://doi.org/10.1021/acsptsci.9b00061

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Pharmaceutical Optimization of Peptide Toxins for Ion Channel Targets: Potent, Selective, and Long-Lived Antagonists of Kv1.3

Publikováno v: Journal of Medicinal Chemistry. 58:6784-6802

To realize the medicinal potential of peptide toxins, naturally occurring disulfide-rich peptides, as ion channel antagonists, more efficient pharmaceutical optimization technologies must be developed. Here, we show that the therapeutic properties of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::49ed4b88835ea36a6e04bf82dabb3f1f
https://doi.org/10.1021/acs.jmedchem.5b00495

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Peptide antagonists of the calcitonin gene-related peptide (CGRP) receptor with improved pharmacokinetics and pharmacodynamics

Autor: Eileen Johnson, Jerry Ryan Holder, Barton H. Manning, Licheng Shi, Kevin Salyers, Michael Stenkilsson, Colin V. Gegg, Marie E. Wright, George Doellgast, Kenneth D. Wild, Les P. Miranda

Publikováno v: Biopolymers. 100:422-430

Antagonism of the calcitonin gene-related peptide (CGRP) receptor may be a useful approach for migraine treatment. Selective PEGylated peptide antagonists to the CGRP receptor are described, derived from CGRP(8-37) with polymer derivatization at an e

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1ea37007135bf79af7cc0c5558bc94bf
https://doi.org/10.1002/bip.22270

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Ligand-Binding Mass Spectrometry to Study Biotransformation of Fusion Protein Drugs and Guide Immunoassay Development: Strategic Approach and Application to Peptibodies Targeting the Thrombopoietin Receptor

Autor: Michael Hall, Hsieng Sen Lu, Christopher S. Spahr, Robert Ortiz, Steven Yu, Colin V. Gegg, Kenneth W. Walker, Jean W. Lee, Vimal Patel, Liana Zhang, Binodh DeSilva

Publikováno v: The AAPS Journal. 12:576-585

The knowledge of in vivo biotransformation (e.g., proteolysis) of protein therapeutic candidates reveals structural liabilities that impact stability. This information aids the development and confirmation of ligand-binding assays with the required s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::180ca94a2bdcef05a7dfaace19bdf26c
https://doi.org/10.1208/s12248-010-9218-9

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Investigation of the effects of altered receptor binding activity on the clearance of erythropoiesis-stimulating proteins: Nonerythropoietin receptor-mediated pathways may play a major role

Autor: Linda O. Narhi, Graham Molineux, Sameer Doshi, Balaji Agoram, Ken Aoki, Steve Elliott, Colin V. Gegg, Graham Richard Jang

Publikováno v: Journal of Pharmaceutical Sciences. 98:2198-2211

Erythropoietin (EPO) receptor-mediated endocytosis and degradation in the bone marrow has been hypothesized to be the major clearance pathway of erythropoiesis-stimulating agents (ESA). We investigated the role of this pathway in ESA clearance by det

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bdc79524cfce27766fb893c5f96987b8
https://doi.org/10.1002/jps.21578

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Interactions between PEG and type I soluble tumor necrosis factor receptor: Modulation by pH and by PEGylation at the N terminus

Autor: Giovanni B. Strambini, Margherita Gonnelli, Byeong S. Chang, Bruce A. Kerwin, Colin V. Gegg, Tiansheng Li

Publikováno v: Protein Science. 11:1825-1833

The effects of polyethylene glycol (PEG) on protein structure and the molecular details that regulate its association to polypeptides are largely unknown. These issues were addressed using type I soluble tumor necrosis factor receptor (sTNF-RI) as a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f06f1b5a4151a10a72e40a4e95edb13
https://doi.org/10.1110/ps.0208102

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An Acyl-Ghrelin-Specific Neutralizing Antibody Inhibits the Acute Ghrelin-Mediated Orexigenic Effects in Mice

Autor: David W. Brankow, Shu-Chen Lu, Jing Xu, Shuying Liu, Shirley Steavenson, Colin V. Gegg, Richard A. Lindberg, Wei Gu, Narumol Chinookoswong, Murielle M. Véniant

Publikováno v: Molecular Pharmacology. 75:901-907

Ghrelin is a 28-amino acid peptide secreted mainly by the stomach. Acyl-ghrelin, which binds to and activates the growth hormone secretagogue receptor type 1a (GHS-R1a), is considered to be the active form for its orexigenic effects. It has been demo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::295b85dcb2ee6b40eaa2abba9ecd4f50
https://doi.org/10.1124/mol.108.052852

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Identification of Potent, Selective, and Metabolically Stable Peptide Antagonists to the Calcitonin Gene-Related Peptide (CGRP) Receptor

Autor: Licheng Shi, Jennifer Aral, Richard S. Rogers, Violeta G. Valladares, Hongyan Li, Marie E. Wright, Kevin Salyers, Eileen Johnson, Jerry Ryan Holder, Les P. Miranda, Kenneth W. Walker, George Doellgast, Colin V. Gegg, Kenneth D. Wild, Brian D. Bennett

Publikováno v: Journal of Medicinal Chemistry. 51:7889-7897

Calcitonin gene-related peptide (CGRP) is a 37-residue neuropeptide that can be converted to a CGRP(1) receptor antagonist by the truncation of its first seven residues. CGRP(8-37), 1, has a CGRP(1) receptor K(i) = 3.2 nM but is rapidly degraded in h

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d6e67e4b147d3e6c1d74e860256269e
https://doi.org/10.1021/jm8009298

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Design and Synthesis of Conformationally Constrained Glucagon-Like Peptide-1 Derivatives with Increased Plasma Stability and Prolonged in Vivo Activity

Autor: Hongyan Li, Shanaka Stanislaus, Jennifer Aral, Mark Guido, Ankita Patel, Jingwen Zhang, Colin V. Gegg, Stephanie Diamond, Leszek Poppe, Jason Long, Les P. Miranda, Murielle M. Véniant, Mark J. Rose, Mark Ma, Katherine Ann Winters

Publikováno v: Journal of Medicinal Chemistry. 51:2758-2765

A series of conformationally constrained derivatives of glucagon-like peptide-1 (GLP-1) were designed and evaluated. By use of [Gly (8)]GLP-1(7-37)-NH2 (2) peptide as a starting point, 17 cyclic derivatives possessing i to i + 4, i to i + 5, or i to

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::98139b752b32b55aa26d08bc0a67b837
https://doi.org/10.1021/jm701522b

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Peptide antagonists of the calcitonin gene-related peptide (CGRP) receptor with improved pharmacokinetics and pharmacodynamics

Autor: Les P, Miranda, Licheng, Shi, Jerry R, Holder, Marie, Wright, Colin V, Gegg, Eileen, Johnson, Kenneth, Wild, Michael, Stenkilsson, George, Doellgast, Barton H, Manning, Kevin, Salyers

Publikováno v: Biopolymers. 100(4)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::a31b70dedf454786a35ff7d2eadd6074
https://pubmed.ncbi.nlm.nih.gov/23868210

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