Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Colin V, Gegg"'
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
Autor:
Kevin Gaida, Xuxia Zhang, Robin Elliott, Benxian Liu, Andrea Itano, Cynthia Park, Justin K. Murray, Colin V. Gegg, Jennifer Aral, Les P. Miranda, Joseph G. McGivern, Hongyan Li, Anne Colombero, E. Allen Sickmier, Kevin Salyers, Michael Stenkilsson, Jonathan Werner, Steven Yu, Mark J. Rose, John K. Sullivan, Yi-Xin Qian, Peter Miu, Kristin L. Andrews
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
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
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
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
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
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
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
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
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)
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