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Carl A. Machutta
Researcher at Stony Brook University
Publications - 12
Citations - 769
Carl A. Machutta is an academic researcher from Stony Brook University. The author has contributed to research in topics: Enzyme kinetics & Histone methyltransferase. The author has an hindex of 10, co-authored 12 publications receiving 660 citations. Previous affiliations of Carl A. Machutta include GlaxoSmithKline.
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Journal ArticleDOI
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
Sharad K. Verma,Xinrong Tian,Louis V. LaFrance,Celine Duquenne,Dominic Suarez,Kenneth A. Newlander,Stuart Paul Romeril,Joelle Lorraine Burgess,Seth W. Grant,Brackley James,Alan P. Graves,Daryl A. Scherzer,Art Shu,Christine Thompson,Heidi M. Ott,Glenn S. Van Aller,Carl A. Machutta,Elsie Diaz,Yong Jiang,Johnson Neil W,Steven D. Knight,Ryan G. Kruger,Michael T. McCabe,Dashyant Dhanak,Peter J. Tummino,Caretha L. Creasy,William H. Miller +26 more
TL;DR: This work has identified highly potent, selective, SAM-competitive, and cell-active EZH2 inhibitors, including GSK926 and GSK343, which are small molecule chemical tools that would be useful to further explore the biology of EZh2.
Journal ArticleDOI
Crystal Structure of Mycobacterium tuberculosis MenB, a Key Enzyme in Vitamin K2 Biosynthesis
James J. Truglio,Karsten Theis,Yuguo Feng,Ramona Gajda,Carl A. Machutta,Peter J. Tonge,Caroline Kisker +6 more
TL;DR: A catalytic mechanism in which MenB enables proton transfer within the substrate to yield an oxyanion as the initial step in catalysis is postulate.
Journal ArticleDOI
Crystal Structures of Mycobacterium Tuberculosis Kasa Show Mode of Action within Cell Wall Biosynthesis and its Inhibition by Thiolactomycin
TL;DR: This work determined the crystal structures of KasA, a key enzyme involved in the biosynthesis of long-chain fatty acids, in its apo-form and bound to the natural product inhibitor thiolactomycin, and identified a polyethylene glycol molecule that mimics a fatty acid substrate of approximately 40 carbon atoms length.
Journal ArticleDOI
Development and validation of reagents and assays for EZH2 peptide and nucleosome high-throughput screens
Elsie Diaz,Carl A. Machutta,Stephanie Chen,Yong Jiang,Christopher J. Nixon,Glenn A. Hofmann,Danielle Key,Sharon Sweitzer,Mehul Patel,Zining Wu,Caretha L. Creasy,Ryan G. Kruger,Louis V. LaFrance,Sharad K. Verma,Melissa B. Pappalardi,BaoChau Le,Glenn S. Van Aller,Michael T. McCabe,Peter J. Tummino,Andrew J. Pope,Sara H. Thrall,Benjamin Schwartz,Martin Brandt +22 more
TL;DR: The strategy to screen EZH2 with either a surrogate peptide or a natural substrate led to the identification of the same tractable series, which are reversible, reversible, are [3H]-S-adenosyl-L-methionine competitive, and display biochemical inhibition of H3K27 methylation.
Journal ArticleDOI
Prioritizing multiple therapeutic targets in parallel using automated DNA-encoded library screening.
Carl A. Machutta,Christopher S. Kollmann,Kenneth E Lind,Xiaopeng Bai,Pan F. Chan,Jianzhong Huang,Lluis Ballell,Svetlana L. Belyanskaya,Gurdyal S. Besra,David Barros-Aguirre,Robert H. Bates,Paolo A. Centrella,Sandy S. Chang,Jing Chai,Anthony E. Choudhry,Aaron Coffin,Aaron Coffin,Christopher P. Davie,Hongfeng Deng,Jianghe Deng,Yun Ding,Jason W. Dodson,David T. Fosbenner,Enoch Gao,Taylor L. Graham,Todd L. Graybill,Karen A. Ingraham,Walter P. Johnson,Bryan W. King,Christopher R. Kwiatkowski,Joël Lelièvre,Yue Li,Xiaorong Liu,Quinn Lu,Ruth Lehr,Alfonso Mendoza-Losana,John D. Martin,Lynn McCloskey,Patti McCormick,Heather O’Keefe,Thomas O’Keeffe,Christina S. Pao,Christina S. Pao,Christopher B. Phelps,Hongwei Qi,Keith Rafferty,Genaro S. Scavello,Matt S. Steiginga,Flora S. Sundersingh,Sharon Sweitzer,Lawrence M. Szewczuk,Lawrence M. Szewczuk,Amy N. Taylor,May Fern Toh,Juan Wang,Minghui Wang,Devan J. Wilkins,Devan J. Wilkins,Bing Xia,Gang Yao,Jean Zhang,Jingye Zhou,Jingye Zhou,Christine Patricia Donahue,Jeffrey A. Messer,David J. Holmes,Christopher C. Arico-Muendel,Andrew J. Pope,Jeffrey W. Gross,Ghotas Evindar +69 more
TL;DR: The findings demonstrate that parallel ELT selections can be used to assess ligandability and highlight opportunities for successful lead and tool discovery.