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Structural Basis for the High-Affinity Inhibition of Mammalian Membranous Adenylyl Cyclase by 2`,3`-O-(N-Methylanthraniloyl)-Inosine 5`-Triphosphate

Hübner, Melanie and Dixit, A. and Mou, T.-C. and Lushington, Gerald H. and Pinto, Cibele S. and Gille, A. and Geduhn, Jens and König, Burkhard and Sprang, S. R. and Seifert, Roland (2011) Structural Basis for the High-Affinity Inhibition of Mammalian Membranous Adenylyl Cyclase by 2`,3`-O-(N-Methylanthraniloyl)-Inosine 5`-Triphosphate. Molecular Pharmacology 80 (1), pp. 87-96.

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Abstract

2',3'-O-(N-Methylanthraniloyl)-inosine 5'-triphosphate (MANT-ITP) is the most potent inhibitor of mammalian membranous adenylyl cyclase (mAC) 5 (AC5, Ki, 1 nM) yet discovered and surpasses the potency of 2',3'-O-(N-methylanthraniloyl)-guanosine 5'-triphosphate (MANT-GTP) 55-fold (Göttle et al., J Pharmacol Exp Ther 329:1156-1165 (2009)). AC5 inhibitors may be valuable drugs for treatment of heart ...

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Item Type:Article
Date:July 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:GRK 760, Graduiertenkolleg Medizinische Chemie
Identification Number:
ValueType
10.1124/mol.111.071894DOI
21498658PubMed ID
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 07:56
Last Modified:16 Aug 2011 08:23
Item ID:21741
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