Article
Structural basis for the specific inhibition of heterotrimeric Gq protein by a small molecule.
Proceedings of the National Academy of Sciences of the United States of America - 3 Aug 2010
Nishimura Akiyuki, Kitano Ken, Takasaki Jun, Taniguchi Masatoshi, Mizuno Norikazu, Tago Kenji, Hakoshima Toshio, Itoh Hiroshi
Abstract excerpt
Heterotrimeric GTP-binding proteins (G proteins) transmit extracellular stimuli perceived by G protein-coupled receptors (GPCRs) to intracellular signaling cascades. Hundreds of GPCRs exist in humans and are the targets of a large percentage of the pharmaceutical drugs used today. Because G proteins are regulated by GPCRs, small molecules that directly modulate G proteins have the potential to become therapeutic...
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