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Design, Synthesis, and Pharmacological Evaluation of Second-Generation Soluble Adenylyl Cyclase (sAC, ADCY10) Inhibitors with Slow Dissociation Rates

Title data

Miller, Michael ; Rossetti, Thomas ; Ferreira, Jacob ; Ghanem, Lubna ; Balbach, Melanie ; Kaur, Navpreet ; Levin, Lonny R. ; Buck, Jochen ; Kehr, Maria ; Coquille, Sandrine ; van den Heuvel, Joop ; Steegborn, Clemens ; Fushimi, Makoto ; Finkin-Groner, Efrat ; Myers, Robert W. ; Kargman, Stacia ; Liverton, Nigel J. ; Huggins, David J. ; Meinke, Peter T.:
Design, Synthesis, and Pharmacological Evaluation of Second-Generation Soluble Adenylyl Cyclase (sAC, ADCY10) Inhibitors with Slow Dissociation Rates.
In: Journal of Medicinal Chemistry. Vol. 65 (2022) Issue 22 . - pp. 15208-15226.
ISSN 1520-4804
DOI: https://doi.org/10.1021/acs.jmedchem.2c01133

Abstract in another language

Soluble adenylyl cyclase (sAC: ADCY10) is an enzyme involved in intracellular signaling. Inhibition of sAC has potential therapeutic utility in a number of areas. For example, sAC is integral to successful male fertility: sAC activation is required for sperm motility and ability to undergo the acrosome reaction, two processes central to oocyte fertilization. Pharmacologic evaluation of existing sAC inhibitors for utility as on-demand, nonhormonal male contraceptives suggested that both high intrinsic potency, fast on and slow dissociation rates are essential design elements for successful male contraceptive applications. During the course of the medicinal chemistry campaign described here, we identified sAC inhibitors that fulfill these criteria and are suitable for in vivo evaluation of diverse sAC pharmacology.

Further data

Item Type: Article in a journal
Refereed: Yes
Institutions of the University: Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry > Chair Biochemistry > Chair Biochemistry - Univ.-Prof. Dr. Clemens Steegborn
Faculties
Faculties > Faculty of Biology, Chemistry and Earth Sciences
Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry
Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry > Chair Biochemistry
Result of work at the UBT: Yes
DDC Subjects: 500 Science > 540 Chemistry
500 Science > 570 Life sciences, biology
Date Deposited: 10 Nov 2022 08:27
Last Modified: 09 Aug 2023 12:37
URI: https://eref.uni-bayreuth.de/id/eprint/72728