Zobrazeno 1 - 10
of 38
pro vyhledávání: '"Scott W. Martin"'
Autor:
Jeffrey W. Johannes, Fiona Pachl, Amber Balazs, Tieguang Yao, C. Larner, Lisa McWilliams, Marianne Schimpl, Scott W. Martin, Kevin J. Embrey, Tom D. Heightman, Paul Hemsley, Jonathan P. Orme, Derek Barratt, Giuditta Illuzzi, Andrew Madin, Paolo Di Fruscia, Avipsa Ghosh, Martin J. Packer, Scott D. Edmondson, Elisabetta Leo, Xiaolan Zheng, Matthew D. Chuba, Xiaohui Pei, Mark J. O'Connor, Verity Talbot, Ke Zhang, Stephen Fawell, Elizabeth Underwood, Anna Staniszewska, Lina Liu, Lin Xue, Sonja J. Gill, Anders Gunnarsson, Andrew Pike, Susan E. Critchlow, Jeffrey G. Varnes, Andrew X. Zhang, Sébastien L. Degorce, J. Lane, Sudhir M. Hande, Hongyao She, Sabina Cosulich, Michal Bista
Publikováno v:
Journal of Medicinal Chemistry. 64:14498-14512
Poly-ADP-ribose-polymerase (PARP) inhibitors have achieved regulatory approval in oncology for homologous recombination repair deficient tumors including BRCA mutation. However, some have failed in combination with first-line chemotherapies, usually
Publikováno v:
Drug Discovery Today. 25:1793-1800
Proteolysis-targeting chimeras (PROTACs) are an emerging therapeutic modality with the potential to open target space not accessible to conventional small molecules via a degradation-based mechanism; however, their bifunctional nature can result in p
Publikováno v:
Rapid Communications in Mass Spectrometry. 34
Rationale To capture all metabolites in metabolite identification studies, MS/MS information is required in both positive and negative ionization mode, usually involving several sample injections to gain all information about samples. A high-resoluti
Autor:
Michael Davies, Scott W. Martin, Tashinga E. Bapiro, Helen Rollison, James W.T. Yates, Andy Sykes, Matthias Hoch, Barry Jones
Publikováno v:
Drug Metabolism and Disposition. 46:1268-1276
AZD9496 ((E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic acid) is an oral selective estrogen receptor degrader currently in clinical development for treatment of estroge
Autor:
Jonathan Wills, Ian D. Wilson, Alan McCarthy, Huw B. Jones, Chris Page, Kerry Ratcliffe, Sunil Sarda, Tim Schulz-Utermoehl, Kathryn Pickup, Alison V. M. Rodrigues, Elizabeth A. Partridge, Scott W. Martin
Publikováno v:
Archives of Toxicology. 91:2643-2653
The distribution, metabolism, excretion and hepatic effects of the human hepatotoxin fenclozic acid were investigated following single oral doses of 10 mg/kg to normal and bile duct-cannulated male C57BL/6J mice. Whole body autoradiography showed dis
Autor:
David G. Temesi, Malcolm R. Clench, Alexandra L. Orton, Eva M. Lenz, Scott W. Martin, Robin Smith
Publikováno v:
Rapid Communications in Mass Spectrometry. 31:145-151
Rationale: The incubation of CPAQOP (1-[(2R)-2-[[4-[3-chloro-4-(2-pyridyloxy)anilino]quinazolin-5-yl]oxymethyl]-1-piperidyl]-2-hydroxy) with human liver microsomes generated several metabolites that highlighted the hydroxyacetamide side chain was a m
Autor:
Paul A. Dickinson, Kathryn Pickup, Mireille Cantarini, Jo Collier, Paul Frewer, Scott W. Martin, Peter Ballard
Publikováno v:
Drug Metabolism and Disposition. 44:1201-1212
Preclinical and clinical studies were conducted to determine the metabolism and pharmacokinetics of osimertinib and key metabolites AZ5104 and AZ7550. Osimertinib was designed to covalently bind to epidermal growth factor receptors, allowing it to ac
Autor:
Sébastien L. Degorce, Patrick Ple, Mickaël Maudet, Jennifer H. Pink, Rowena Callis, Andrew Bailey, Bryan Roberts, Chris De Savi, Richard A. Norman, Rémy Morgentin, Aurélien Péru, Richard Ducray, Scott W. Martin, James S. Scott, Gillian M. Lamont, Philip A. MacFaul
Publikováno v:
Journal of Medicinal Chemistry. 58:3522-3533
A novel estrogen receptor down-regulator, 7-hydroxycoumarin (5, SS5020), has been reported with antitumor effects against chemically induced mammary tumors. Here, we report on our own investigation of 7-hydroxycoumarins as potential selective estroge
Autor:
Zhong Yang, Jay O. Knipe, Susan B. Roberts, Yong Tu, Paul E. Morin, Ying-Kai Wang, John Wan, Andrew Nickel, Katharine A. Grant-Young, Piyasena Hewawasam, Sam T. Chao, Xiaoliang Zhuo, Bergstrom Carl P, Brett R. Beno, Qi Gao, Dianlin Xie, Chong-Hwan Chang, Dawn D. Parker, Mian Gao, Alicia Regueiro-Ren, Mengping Liu, Umesh Hanumegowda, Richard J. Colonno, Kathy Mosure, Nicholas A. Meanwell, Min Ding, Lenore A. Pelosi, John F. Kadow, Xiaofan Zheng, Steven Sheriff, Voss Stacey A, Alicia Ng, Kenneth S. Santone, Mark R. Witmer, Jung-Hui Sun, Robert G. Gentles, Bender John A, Min Gao, Yi Wang, Jeff Tredup, Daniel M. Camac, Scott W. Martin, Thomas W. Hudyma, Julie A. Lemm, Kap-Sun Yeung, Karen Rigat
Publikováno v:
Journal of Medicinal Chemistry. 57:1855-1879
Described herein are structure-activity relationship studies that resulted in the optimization of the activity of members of a class of cyclopropyl-fused indolobenzazepine HCV NS5B polymerase inhibitors. Subsequent iterations of analogue design and s
Autor:
Huw B. Jones, Sunil Sarda, Jonathan Wills, Scott W. Martin, Kathryn Pickup, Alison V. M. Rodrigues, Ian D. Wilson, Chris Page
Publikováno v:
Xenobiotica. 44:164-173
1. The distribution, metabolism, excretion and hepatic effects of fenclozic acid were investigated following a single oral dose of 10 mg/kg to hepatic reductase null (HRN) mice. 2. The majority of the [(14)C]-fenclozic acid was eliminated via the uri