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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. and Lushington, Gerald H. and Richter, M. and Gille, A. and Geduhn, Jens and König, Burkhard and Mou, T.-C. and 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
21620805 PubMed ID
Keywords:Adenylyl Cyclase; MANT-nucleotides; Fluorescence spectroscopy; Molecular modelling; Conformational landscape
Subjects:500 Science > 540 Chemistry & allied sciences
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Owner: Regina Hoheisel
Deposited On:12 Aug 2011 07:52
Last Modified:16 Aug 2011 11:40
Item ID:21740
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