at Google ScholarTitle 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.
(2022)
.
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: | 10 Nov 2022 10:14 |
| URI: | https://eref.uni-bayreuth.de/id/eprint/72728 |