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Stephen W. Fesik
Researcher at Vanderbilt University
Publications - 298
Citations - 42613
Stephen W. Fesik is an academic researcher from Vanderbilt University. The author has contributed to research in topics: Nuclear magnetic resonance spectroscopy & Binding site. The author has an hindex of 95, co-authored 294 publications receiving 40006 citations. Previous affiliations of Stephen W. Fesik include Howard Hughes Medical Institute & Yale University.
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Journal ArticleDOI
Regulation of the Apaf-1/caspase-9 apoptosome by caspase-3 and XIAP.
Hua Zou,Ruomei Yang,Junshan Hao,Jean Wang,Chaohong Sun,Stephen W. Fesik,Joe C. Wu,Kevin J. Tomaselli,Robert C. Armstrong +8 more
TL;DR: It is found that cleavage of procaspase-9 at Asp330 to generate p35, p 10 or p37, p10 forms resulted in a significant increase in apoptosome activity compared with p35/p12, and the significance of this increase was demonstrated by the near complete loss of apoptosomesome-mediated caspasing-3 activity.
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A Novel MCL1 Inhibitor Combined with Venetoclax Rescues Venetoclax-Resistant Acute Myelogenous Leukemia.
Haley E. Ramsey,Melissa A. Fischer,Taekyu Lee,Agnieszka E. Gorska,Maria Pia Arrate,Londa Fuller,Kelli L. Boyd,Stephen A. Strickland,John Sensintaffar,Leah Hogdal,Gregory D. Ayers,Edward T. Olejniczak,Stephen W. Fesik,Michael R. Savona +13 more
TL;DR: VU661013 is described, a novel, potent, selective MCL1 inhibitor that destabilizes BIM/MCL1 association, leads to apoptosis in AML, and is active in venetoclax-resistant cells and patient-derived xenografts.
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Solution structure of the cyclosporin A/cyclophilin complex by NMR
Yves Thériault,Timothy M. Logan,Robert P. Meadows,Liping Yu,Edward T. Olejniczak,Thomas F. Holzman,Robert L. Simmer,Stephen W. Fesik +7 more
TL;DR: The solution structure of the cyclosporin A/cyclophilin complex obtained by heteronuclear three-dimensional NMR spectroscopy is presented and is analysed in terms of the binding interactions and structure/activity relationships for CsA analogues.
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Structure of the N-terminal RNA-binding domain of the SARS CoV nucleocapsid protein.
Qiulong Huang,Liping Yu,Andrew M. Petros,Angelo Gunasekera,Zhihong Liu,Nan Xu,Philip J. Hajduk,Jamey Mack,Stephen W. Fesik,Edward T. Olejniczak +9 more
TL;DR: The three-dimensional structure of the N-terminal domain of the SARS coronavirus (CoV) nucleocapsid protein is described, which consists of a five-stranded beta sheet with a folding topology distinct from other RNA-binding proteins.
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Discovery of a Potent, Selective Protein Tyrosine Phosphatase 1B Inhibitor Using a Linked-Fragment Strategy
Bruce G. Szczepankiewicz,Gang Liu,Philip J. Hajduk,Cele Abad-Zapatero,Zhonghua Pei,Zhili Xin,Thomas H. Lubben,James M. Trevillyan,Michael A. Stashko,Stephen J. Ballaron,Heng Liang,Flora Huang,Charles W. Hutchins,Stephen W. Fesik,Michael R. Jirousek +14 more
TL;DR: The modular approach to drug design described in this work should be applicable for the design of potent and selective inhibitors of other therapeutically relevant protein tyrosine phosphatases.