Allosteric IGF-1R Inhibitors.
Ontology highlight
ABSTRACT:
SUBMITTER: Heinrich T
PROVIDER: S-EPMC4007842 | biostudies-literature | 2010 Aug
REPOSITORIES: biostudies-literature
Publications
Allosteric IGF-1R Inhibitors.
Heinrich Timo T Grädler Ulrich U Böttcher Henning H Blaukat Andree A Shutes Adam A
ACS medicinal chemistry letters 20100518 5
Targeting allosteric protein sites is a promising approach to interfere selectively with cellular signaling cascades. We have discovered a novel class of allosteric insulin-like growth factor-I receptor (IGF-1R) inhibitors. 3-Cyano-1H-indole-7-carboxylic acid {1-[4-(5-cyano-1H-indol-3-yl)butyl]piperidin-4-yl}amide (10) was found with nanomolar biochemical, micromolar, cellular IGF-1R activity and no relevant interference with cellular insulin receptor signaling up to 30 μM. The allosteric bindin ...[more]
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