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Structure–activity relationships for the interactions of 2`- and 3`-(O)-(N-methyl)anthraniloyl-substituted purine and pyrimidine nucleotides with mammalian adenylyl cyclases

Pinto, Cibele S. ; Lushington, Gerald H. ; Richter, M. ; Gille, A. ; Geduhn, Jens ; König, Burkhard ; Mou, T.-C. ; Sprang, S. R. ; Seifert, Roland


Membranous adenylyl cyclases (ACs) play a key role in signal transduction and are promising drug targets. In previous studies we showed that 2',3'-(O)-(N-methylanthraniloyl) (MANT)-substituted nucleotides are potent AC inhibitors. The aim of this study was to provide systematic structure-activity relationships for 21 (M)ANT-substituted nucleotides at the purified catalytic AC subunit heterodimer ...


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