J
John Drewe
Researcher at Shire plc
Publications - 82
Citations - 4273
John Drewe is an academic researcher from Shire plc. The author has contributed to research in topics: Apoptosis & Caspase. The author has an hindex of 35, co-authored 82 publications receiving 3988 citations.
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Journal ArticleDOI
Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 1. Structure-activity relationships of the 4-aryl group.
William Kemnitzer,John Drewe,Songchun Jiang,Hong Zhang,Yan Wang,Jianghong Zhao,Shaojuan Jia,John Herich,Denis Labreque,Richard Storer,Karen Meerovitch,David Y. Bouffard,Rabindra Rej,Real Denis,Charles Blais,Serge Lamothe,Giorgio Attardo,Henriette Gourdeau,Ben Tseng,Shailaja Kasibhatla,Sui Xiong Cai +20 more
TL;DR: Results confirm that the cell-based caspase activation assay is a powerful tool for the discovery of potent apoptosis inducers and suggest that the 4-aryl-4H-chromenes have the potential to be developed into future anticancer agents.
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Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 2. Structure–activity relationships of the 7- and 5-, 6-, 8-positions
William Kemnitzer,Shailaja Kasibhatla,Songchun Jiang,Hong Zhang,Jianghong Zhao,Shaojuan Jia,Lifen Xu,Candace Crogan-Grundy,Real Denis,Nancy Barriault,Louis Vaillancourt,Sylvie Charron,Jennifer Dodd,Giorgio Attardo,Denis Labrecque,Serge Lamothe,Henriette Gourdeau,Ben Tseng,John Drewe,Sui Xiong Cai +19 more
TL;DR: It was found that a small hydrophobic group, such as NMe2, NH2, NHEt, and OMe, is preferred at the 7-position, and several 7-substituted and 7,8-di-subStituted analogs were found to have similar potencies as the lead compound MX58151 both as caspase activators and inhibitors of cell proliferation.
Journal Article
Antivascular and antitumor evaluation of 2-amino-4-(3-bromo-4,5-dimethoxy-phenyl)-3-cyano-4H-chromenes, a novel series of anticancer agents
Henriette Gourdeau,Lorraine Leblond,Bettina Hamelin,Clemence Desputeau,Kelly Dong,Irenej Kianicka,Dominique Custeau,Chantal Boudreau,Lilianne Geerts,Sui-Xiong Cai,John Drewe,Denis Labrecque,Shailaja Kasibhatla,Ben Tseng +13 more
TL;DR: The results identify MX-116407 as the lead candidate and strongly support its continued development as a novel anticancer agent for human use and the ability of these compounds to disrupt tumor vasculature and to induce tumor necrosis.
Journal ArticleDOI
Discovery, characterization and SAR of gambogic acid as a potent apoptosis inducer by a HTS assay.
Han-Zhong Zhang,Shailaja Kasibhatla,Yan Wang,John Herich,John Guastella,Ben Tseng,John Drewe,Sui Xiong Cai +7 more
TL;DR: The high potency of 2 as an inducer of apoptosis, its novel mechanism of action, easy isolation and abundant supply, as well as the fact that it is amenable to chemical modification, makes gambogic acid an attractive molecule for the development of anticancer agents.
Journal ArticleDOI
Discovery and Structure−Activity Relationship of 3-Aryl-5-aryl-1,2,4-oxadiazoles as a New Series of Apoptosis Inducers and Potential Anticancer Agents
Han-Zhong Zhang,Shailaja Kasibhatla,Jared Kuemmerle,William Kemnitzer,Kristin Ollis-Mason,Ling Qiu,Candace Crogan-Grundy,Ben Tseng,John Drewe,Sui Xiong Cai +9 more
TL;DR: The cell-based chemical genetics approach for the discovery of apoptosis inducers can identify potential anticancer agents as well as their molecular targets.