Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Kevin, Salyers"'
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:
Christopher A. James, Ronya Primack, Kevin Salyers, Roger Pham, Marc W. Retter, Valerie Almon, James Meyer, Mylo Wagner, Marcus Soto, Manuel Ponce
Publikováno v:
Bioanalysis. 6:2135-2146
Background: AMG 517 or 1-aminobenzotriazole were quantified by LC–MS/MS from low blood/plasma volumes for rat pharmacokinetic (PK) characterization in order to qualify manual/automated dried blood spot (DBS) sampling and plasma separation capillary
Autor:
James Meyer, Kevin Salyers, Minghan Wang, Matthew P. Bourbeau, Yang Xu, Melissa Graham, Christopher H. Fotsch, John G. Allen, Wei Gu, Michael D. Bartberger, Mark R. Fielden, Murielle M. Véniant, Ki-Won Kim, James Busby, Aaron C. Siegmund, Renee Komorowski, Hong Shu
Publikováno v:
Journal of Medicinal Chemistry. 56:10132-10141
Acetyl-CoA carboxylase (ACC) is a target of interest for the treatment of metabolic syndrome. Starting from a biphenyloxadiazole screening hit, a series of piperazine oxadiazole ACC inhibitors was developed. Initial pharmacokinetic liabilities of the
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:
Ching He, Nancy Doyle, Erin Stevens, Padma K. Narayanan, Remi Jawando, Cen Xu, Nianyu Li, Madeline M. Fort, Kevin Salyers, Florence Poitout-Belissent, Riki Stevenson, Mai Phuong Nguyen, Katherine Sprugel, Vibha Jawa, Nancy E. Everds, Keith Bailey, Sam M Tran, Jacquelin Jolette
Publikováno v:
Toxicologic Pathology. 41:951-969
Cynomolgus monkeys dosed with a therapeutic monoclonal antibody (mAbY.1) at ≥50 mg/kg had unexpected acute thrombocytopenia (nadir ∼3,000 platelets/µl), sometimes with decreases in red cell mass. Increased activated macrophages, mitotic figures,
Autor:
Kevin Salyers, Yang Xu
Publikováno v:
ADME-Enabling Technologies in Drug Design and Development
Autor:
Yosup Rew, Hilary Plake Beck, Anne Y. Saiki, Steven H. Olson, Brian M. Fox, Kevin Salyers, Dongyin Yu, Michael DeGraffenreid, Stephen Schneider, John G. Allen, Jonathan D. Oliner, Qiuping Ye
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2752-2755
Human murine double minute 2 (MDM2) is a negative regulator of p53, which plays an important role in cell cycle and apoptosis. We report several optimizations to the synthesis of the chromenotriazolopyrimidine series of MDM2-p53 protein-protein inter
Autor:
Hugo M. Vargas, Yang Xu, Jerry Siu, Janet Buys, Michelle Horner, Jian Lin, Ashis Saha, Han Xu, Michele McElvain, Anurag Sharadendu, Scot Middleton, Roland Burli, Yael Marantz, Dalia Segal, Kevin Salyers, Mercedes Lobera, Dilara Mccauley, Srinivas Chereku, Xiang Yu, Nili Schutz, Michael Schrag
Publikováno v:
ACS Medicinal Chemistry Letters. 2:97-101
We have discovered novel benzofuran-based S1P1 agonists with excellent in vitro potency and selectivity. 1-((4-(5-Benzylbenzofuran-2-yl)-3-fluorophenyl)methyl) azetidine-3-carboxylic acid (18) is a potent S1P1 agonist with >1000× selectivity over S1
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:
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