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Discovery of TDI-10229 : A Potent and Orally Bioavailable Inhibitor of Soluble Adenylyl Cyclase (sAC, ADCY10)

Title data

Fushimi, Makoto ; Buck, Hannes ; Balbach, Melanie ; Gorovyy, Anna ; Ferreira, Jacob ; Rossetti, Thomas ; Kaur, Navpreet ; Levin, Lonny R. ; Buck, Jochen ; Quast, Jonathan ; van den Heuvel, Joop ; Steegborn, Clemens ; Finkin-Groner, Efrat ; Kargman, Stacia ; Michino, Mayako ; Foley, Michael A. ; Miller, Michael ; Liverton, Nigel J. ; Huggins, David J. ; Meinke, Peter T.:
Discovery of TDI-10229 : A Potent and Orally Bioavailable Inhibitor of Soluble Adenylyl Cyclase (sAC, ADCY10).
In: ACS Medicinal Chemistry Letters. Vol. 12 (2021) Issue 8 . - pp. 1283-1287.
ISSN 1948-5875
DOI: https://doi.org/10.1021/acsmedchemlett.1c00273

Abstract in another language

Soluble adenylyl cyclase (sAC) has gained attention as a potential therapeutic target given the role of this enzyme in intracellular signaling. We describe successful efforts to design improved sAC inhibitors amenable for in vivo interrogation of sAC inhibition to assess its potential therapeutic applications. This work culminated in the identification of TDI-10229 (12), which displays nanomolar inhibition of sAC in both biochemical and cellular assays and exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound.

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 08:46
Last Modified: 10 Nov 2022 08:46
URI: https://eref.uni-bayreuth.de/id/eprint/72735