Ontology highlight
ABSTRACT:
SUBMITTER: Elumalai N
PROVIDER: S-EPMC4471549 | biostudies-literature | 2015 Apr
REPOSITORIES: biostudies-literature
Elumalai Nagarajan N Berg Angela A Natarajan Kalaiselvi K Scharow Andrej A Berg Thorsten T
Angewandte Chemie (International ed. in English) 20150220 16
Src homology 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-molecule targets because their SH2 domains are 93% identical on the amino acid level. Here we present the natural product-inspired development of the low-nanomolar inhibitor Stafib-1, as th ...[more]