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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Xehetasun bibliografikoak
Argitaratua izan da:ACS Med Chem Lett
Egile Nagusiak: 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.
Formatua: Artigo
Hizkuntza:Inglês
Argitaratua: American Chemical Society 2017
Sarrera elektronikoa: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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