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Assessing potency and binding kinetics of soluble adenylyl cyclase (sAC) inhibitors to maximize therapeutic potential

Title data

Rossetti, Thomas ; Ferreira, Jacob ; Ghanem, Lubna ; Buck, Hannes ; Steegborn, Clemens ; Myers, Robert W. ; Meinke, Peter T. ; Levin, Lonny R. ; Buck, Jochen:
Assessing potency and binding kinetics of soluble adenylyl cyclase (sAC) inhibitors to maximize therapeutic potential.
In: Frontiers in Physiology. Vol. 13 (2022) .
ISSN 1664-042X
DOI: https://doi.org/10.3389/fphys.2022.1013845

Abstract in another language

In mammalian cells, 10 different adenylyl cyclases produce the ubiquitous second messenger, cyclic adenosine monophosphate (cAMP). Amongst these cAMP-generating enzymes, bicarbonate (HCO3 -)-regulated soluble adenylyl cyclase (sAC; ADCY10) is uniquely essential in sperm for reproduction. For this reason, sAC has been proposed as a potential therapeutic target for non-hormonal contraceptives for men. Here, we describe key sAC-focused in vitro assays to identify and characterize sAC inhibitors for therapeutic use. The affinity and binding kinetics of an inhibitor can greatly influence in vivo efficacy, therefore, we developed improved assays for assessing these efficacy defining features.

Further data

Item Type: Article in a journal
Refereed: Yes
Keywords: SPR; binding kinetics; drug development; lead optimization; male contraceptive; picomolar potency; residence time; soluble adenylyl cyclase
Institutions of the University: Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry > Chair Biochemistry > Chair Biochemistry - Univ.-Prof. Dr. Clemens Steegborn
Result of work at the UBT: Yes
DDC Subjects: 500 Science > 540 Chemistry
500 Science > 570 Life sciences, biology
Date Deposited: 10 Nov 2022 08:35
Last Modified: 10 Nov 2022 08:35
URI: https://eref.uni-bayreuth.de/id/eprint/72731