Biochemical Pharmacology volume 78, issue 1, P62-69 2009 DOI: 10.1016/j.bcp.2009.03.023 View full text
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Cibele Pinto, Melanie Hübner, Andreas Gille, Mark Richter, Tung-Chung Mou, Stephen R. Sprang, Roland Seifert

Abstract: The diterpene forskolin (FS) binds to, and activates, mammalian membranous adenylyl cyclase (AC) isoforms I–VIII. Diterpenes without C1-OH group do not activate ACs. The C1-OH group forms a hydrogen bond with the backbone oxygen of Val506 of the C1 catalytic subunit of AC (isoform V numbering). To better understand the mechanism of AC activation we examined the interactions of FS and eight FS analogs with purified catalytic AC subunits C1 (AC V) and C2 (AC II) by fluorescence spectroscopy, using 2′,3′-O-(N-me…

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