Ontology highlight
ABSTRACT:
SUBMITTER: Law JM
PROVIDER: S-EPMC5066158 | biostudies-literature | 2016 Oct
REPOSITORIES: biostudies-literature
Law Jason M JM Stark Sebastian C SC Liu Ke K Liang Norah E NE Hussain Mahmud M MM Leiendecker Matthias M Ito Daisuke D Verho Oscar O Stern Andrew M AM Johnston Stephen E SE Zhang Yan-Ling YL Dunn Gavin P GP Shamji Alykhan F AF Schreiber Stuart L SL
ACS medicinal chemistry letters 20160818 10
Evidence suggests that specific mutations of isocitrate dehydrogenases 1 and 2 (IDH1/2) are critical for the initiation and maintenance of certain tumor types and that inhibiting these mutant enzymes with small molecules may be therapeutically beneficial. In order to discover mutant allele-selective IDH1 inhibitors with chemical features distinct from existing probes, we screened a collection of small molecules derived from diversity-oriented synthesis. The assay identified compounds that inhibi ...[more]