Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor

[Image: see text] Inhibition of mutant IDH1 is being evaluated clinically as a promising treatment option for various cancers with hotspot mutation at Arg(132). Having identified an allosteric, induced pocket of IDH1(R132H), we have explored 3-pyrimidin-4-yl-oxazolidin-2-ones as mutant IDH1 inhibito...

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Publicat a:ACS Med Chem Lett
Autors principals: Cho, Young Shin, Levell, Julian R., Liu, Gang, Caferro, Thomas, Sutton, James, Shafer, Cynthia M., Costales, Abran, Manning, James R., Zhao, Qian, Sendzik, Martin, Shultz, Michael, Chenail, Gregg, Dooley, Julia, Villalba, Brian, Farsidjani, Ali, Chen, Jinyun, Kulathila, Raviraj, Xie, Xiaoling, Dodd, Stephanie, Gould, Ty, Liang, Guiqing, Heimbach, Tycho, Slocum, Kelly, Firestone, Brant, Pu, Minying, Pagliarini, Raymond, Growney, Joseph D.
Format: Artigo
Idioma:Inglês
Publicat: American Chemical Society 2017
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC5641959/
https://ncbi.nlm.nih.gov/pubmed/29057061
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.7b00342
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