Istvan J. Enyedy
Biogen Idec
75 Papers
722 Citations
Istvan J. Enyedy is an academic researcher from Biogen Idec. The author has contributed to research in topics: Kinase & Chemistry. The author has an hindex of 27, co-authored 71 publications. Previous affiliations of Istvan J. Enyedy include Novartis & Bayer.
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Papers
Discovery of Small-Molecule Inhibitors of Bcl-2 through Structure-Based Computer Screening
Istvan J. Enyedy,Yan Ling,Kassoum Nacro,York Tomita,Xihan Wu,Yeyu Cao,Ribo Guo,Bihua Li,Xiao-Feng Zhu,Ying Huang,Ya-Qiu Long,Peter P. Roller,Dajun Yang,Shaomeng Wang +13 more
TL;DR: It was found that compound 6 can be used as a valuable pharmacological tool to elucidate the function of Bcl-2 and also serves as a novel lead compound for further design and optimization of small-molecule inhibitors targeted at the BH3 binding pocket in B cl-2.
355
Small molecules inhibit the interaction of Nrf2 and the Keap1 Kelch domain through a non-covalent mechanism.
Douglas Marcotte,Weike Zeng,Jean-Christophe Hus,Andres McKenzie,C Hession,Ping Jin,Chris Bergeron,Alexey Lugovskoy,Istvan J. Enyedy,Hernan Cuervo,Hernan Cuervo,Deping Wang,Cédric Atmanene,Dominique Roecklin,Malgorzata M. Vecchi,Valérie Vivat,Joachim Kraemer,Dirk Winkler,Victor Hong,Victor Hong,Jianhua Chao,Matvey E. Lukashev,Laura Silvian +22 more
TL;DR: Several small molecule compounds that specifically bind to the Keap1 Kelch-DC domain are identified as measured by NMR, native mass spectrometry and X-ray crystallography and one compound upregulates Nrf2 response genes measured by a luciferase cell reporter assay.
217
Identification and Biochemical Characterization of Small-Molecule Inhibitors of Clostridium botulinum Neurotoxin Serotype A
Virginia I. Roxas-Duncan,Istvan J. Enyedy,Vicki A. Montgomery,Vanessa S. Eccard,Marco A. Carrington,Huiguo Lai,Nizamettin Gul,David C.H. Yang,Leonard A. Smith +8 more
TL;DR: The reduced toxicity and high potency demonstrated by these five compounds at the biochemical, cellular, and tissue levels are distinctive among the BoNT/A small-molecule inhibitors reported thus far.
95
Structure-based approach for the discovery of bis-benzamidines as novel inhibitors of matriptase
TL;DR: The results demonstrated that structure-based database screening is effective in the discovery of matriptase inhibitors and that bis-benzamidines represent a class of promising matript enzyme inhibitors that can be used for further drug design studies.
91
EC144 is a potent inhibitor of the heat shock protein 90.
Jiandong Shi,Ryan Van de Water,Kevin Hong,Ryan Lamer,Kenneth W Weichert,Cristina M Sandoval,Srinivas Rao Kasibhatla,Marcus F. Boehm,Jianhua Chao,Karen Lundgren,Noelito Timple,Rachel Lough,Gerardo Ibanez,Christina Boykin,Francis Burrows,Marilyn R. Kehry,Theodore J. Yun,Erin K Harning,Christine Ambrose,Jeffrey Thompson,Sarah A. Bixler,Anthone W. Dunah,Pamela A. Snodgrass-Belt,Joseph Arndt,Istvan J. Enyedy,Ping Li,Victor Hong,Andres McKenzie,Marco A. Biamonte +28 more
TL;DR: Alkyne 40 is a second generation inhibitor of heat shock protein 90 (Hsp90) and is substantially more potent in vitro and in vivo than the first generation inhibitor 14 (BIIB021) that completed phase II clinical trials.
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