Elumalai, Nagarajan published the artcileNanomolar Inhibitors of the Transcription Factor STAT5b with High Selectivity over STAT5a, Formula: C10H10O6, the publication is Angewandte Chemie, International Edition (2015), 54(16), 4758-4763, database is CAplus and MEDLINE.
Src homol. 2 (SH2) domains play a central role in signal transduction. Although many SH2 domains have been validated as drug targets, their structural similarity makes development of specific inhibitors difficult. The cancer-relevant transcription factors STAT5a and STAT5b are particularly challenging small-mol. targets because their SH2 domains are 93% identical on the amino acid level. Here the authors present the natural product-inspired development of the low-nanomolar inhibitor I, as the first small mol. which inhibits the STAT5b SH2 domain (Ki=44 nM) with more than 50-fold selectivity over STAT5a. The binding site of the core moiety of I was validated by functional anal. of point mutants. A prodrug of I was shown to inhibit STAT5b with high selectivity over STAT5a in tumor cells. I provides the first demonstration that naturally occurring SH2 domains with more than 90% sequence identity can be selectively targeted with small organic mols.
Angewandte Chemie, International Edition published new progress about 5411-14-3. 5411-14-3 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ether, name is 2,2-(1,2-Phenylenebis(oxy))diacetic acid, and the molecular formula is C10H10O6, Formula: C10H10O6.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia