307353-32-8Relevant articles and documents
Synthesis and evaluation of tiaprofenic acid-derived UCHL5 deubiquitinase inhibitors
Gurusingha Arachchige, Harshani S.,Herath Mudiyanselage, Poornima D.H.,VanHecke, Garrett C.,Patel, Kush,Cheaito, Hassan A.,Dou, Q. Ping,Ahn, Young-Hoon
supporting information, (2020/12/25)
The ubiquitin–proteasome system (UPS) plays an important role in maintaining protein homeostasis by degrading intracellular proteins. In the proteasome, poly-ubiquitinated proteins are deubiquitinated by three deubiquitinases (DUBs) associated with 19S re
Discovery of a potent class of PI3Kα inhibitors with unique binding mode via encoded library technology (ELT4)
Yang, Hongfang,Medeiros, Patricia F.,Raha, Kaushik,Elkins, Patricia,Lind, Kenneth E.,Lehr, Ruth,Adams, Nicholas D.,Burgess, Joelle L.,Schmidt, Stanley J.,Knight, Steven D.,Auger, Kurt R.,Schaber, Michael D.,Franklin, G. Joseph,Ding, Yun,Delorey, Jennifer L.,Centrella, Paolo A.,Mataruse, Sibongile,Skinner, Steven R.,Clark, Matthew A.,Cuozzo, John W.,Evindar, Ghotas
supporting information, p. 531 - 536 (2015/05/27)
In the search of PI3K p110α wild type and H1047R mutant selective small molecule leads, an encoded library technology (ELT) campaign against the desired target proteins was performed which led to the discovery of a selective chemotype for PI3K isoforms from a three-cycle DNA encoded library. An X-ray crystal structure of a representative inhibitor from this chemotype demonstrated a unique binding mode in the p110α protein.
AMIDE COMPOUNDS, COMPOSITIONS AND USES THEREOF
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Page/Page column 122-123, (2009/10/22)
Compounds are provided according to formula (1 ) : where A, B, W, X', L, R1, R3, R4b, and m' are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.