J
James D. Winkler
Researcher at GlaxoSmithKline
Publications - 56
Citations - 7317
James D. Winkler is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Arachidonic acid & Phospholipase A2. The author has an hindex of 33, co-authored 55 publications receiving 6640 citations. Previous affiliations of James D. Winkler include Wake Forest University.
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Journal ArticleDOI
Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4
Jing Lu,Yimin Qian,Martha Altieri,Hanqing Dong,Jing Wang,Kanak Raina,John Hines,James D. Winkler,Andrew P. Crew,Kevin Coleman,Craig M. Crews +10 more
TL;DR: ARV-825 is designed, a hetero-bifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation ofBRD4 in all BL cell lines tested.
Journal ArticleDOI
The codependence of angiogenesis and chronic inflammation.
TL;DR: The codependence of chronic inflammation and angiogenesis is beginning to be understood, the potential benefits of targetingAngiogenesis in the treatment of chronicinflammation, and of targeting chronic inflammation to affect angiogenic research are begun.
Journal ArticleDOI
PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer.
Kanak Raina,Jing Lu,Yimin Qian,Martha Altieri,Deborah M. Gordon,Ann Marie Rossi,Jing Wang,Xin Chen,Hanqing Dong,Kam W. Siu,James D. Winkler,Andrew P. Crew,Craig M. Crews,Kevin Coleman +13 more
TL;DR: This study proves that ARV-771, a small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of CRPC as compared with BET inhibition.
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Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor.
Tammie C. Yeh,Vivienne Marsh,Bryan Bernat,Josh Ballard,Heidi Colwell,Ronald Evans,Janet Parry,Darin Smith,Barbara J. Brandhuber,Stefan Gross,Allison L. Marlow,Hurley Brian T,Lyssikatos Joseph P,Patrice Lee,James D. Winkler,Kevin Koch,Eli M. Wallace +16 more
TL;DR: ARRY-142886 is a potent and selective MEK1/2 inhibitor that is highly active in both in vitro and in vivo tumor models.
Journal ArticleDOI
Mammalian Chk2 is a downstream effector of the ATM-dependent DNA damage checkpoint pathway
Priya Chaturvedi,Wai K Eng,Yuan Zhu,Michael R. Mattern,Rubin Mishra,Mark R. Hurle,Xiaolong Zhang,Roland S. Annan,Quinn Lu,Leo F. Faucette,Gilbert F. Scott,Xiaotong Li,Steven A. Carr,Randall K. Johnson,James D. Winkler,Bin-Bing S. Zhou +15 more
TL;DR: Results suggest that Chk2 is a downstream effector of the ATM-dependent DNA damage checkpoint pathway and might not only delay mitotic entry, but also increase the capacity of cultured cells to survive after treatment with γ-radiation or with the topoisomerase-I inhibitor topotecan.