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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. and Seifert, Roland (2011) Structure–activity relationships for the interactions of 2`- and 3`-(O)-(N-methyl)anthraniloyl-substituted purine and pyrimidine nucleotides with mammalian adenylyl cyclases. Biochemical Pharmacology 82 (4), pp. 358-370.

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Abstract

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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Item type:Article
Date:2011
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmacology and Toxicology (Prof. Schlossmann, formerly Prof. Seifert)
Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König
Projects:DFG
Identification Number:
ValueType
10.1016/j.bcp.2011.05.010DOI
21620805PubMed ID
Keywords:Adenylyl Cyclase; MANT-nucleotides; Fluorescence spectroscopy; Molecular modelling; Conformational landscape
Dewey Decimal Classification:500 Science > 540 Chemistry & allied sciences
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Item ID:21740
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