476371-64-9Relevant academic research and scientific papers
Design and evaluation of a series of pyrazolopyrimidines as p70S6K inhibitors
Bussenius, Joerg,Anand, Neel K.,Blazey, Charles M.,Bowles, Owen J.,Bannen, Lynne Canne,Chan, Diva S.-M.,Chen, Baili,Co, Erick W.,Costanzo, Simona,Defina, Steven C.,Dubenko, Larisa,Engst, Stefan,Franzini, Maurizio,Huang, Ping,Jammalamadaka, Vasu,Khoury, Richard G.,Kim, Moon H.,Klein, Rhett R.,Laird, Douglas,Le, Donna T.,Mac, Morrison B.,Matthews, David J.,Markby, David,Miller, Nicole,Nuss, John M.,Parks, Jason J.,Tsang, Tsze H.,Tsuhako, Amy L.,Wang, Yong,Xu, Wei,Rice, Kenneth D.
scheme or table, p. 2283 - 2286 (2012/05/04)
The 70-kDa ribosomal protein S6 kinase (p70S6K) is part of the PI3K/AKT/mTOR pathway and has been implicated in cancer. High throughput screening versus p70S6K led to the identification of aminopyrimidine 3a as active inhibitor. Lead optimization of 3a resulted in highly potent, selective, and orally bioavailable pyrazolopyrimidines. In this manuscript we report the structure-activity relationship of this series and pharmacokinetic, pharmacodynamic, and efficacy data of the lead compound 13c.
Inhibitor scaffolds as new allele specific kinase substrates
Kraybill, Brian C.,Elkin, Lisa L.,Blethrow, Justin D.,Morgan, David O.,Shokat, Kevan M.
, p. 12118 - 12128 (2007/10/03)
The elucidation of protein kinase signaling networks is challenging due to the large size of the protein kinase superfamily (>500 human kinases). Here we describe a new class of orthogonal triphosphate substrate analogues for the direct labeling of analog
