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


Journal

ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073

Informations de publication

Date de publication:
12 Aug 2021
Historique:
received: 12 05 2021
accepted: 08 07 2021
entrez: 20 8 2021
pubmed: 21 8 2021
medline: 21 8 2021
Statut: epublish

Résumé

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

Identifiants

pubmed: 34413957
doi: 10.1021/acsmedchemlett.1c00273
pmc: PMC8366019
doi:

Types de publication

Journal Article

Langues

eng

Pagination

1283-1287

Subventions

Organisme : NIA NIH HHS
ID : F31 AG069501
Pays : United States
Organisme : NICHD NIH HHS
ID : R01 HD088571
Pays : United States
Organisme : NICHD NIH HHS
ID : F31 HD105363
Pays : United States
Organisme : NICHD NIH HHS
ID : P50 HD100549
Pays : United States
Organisme : NIA NIH HHS
ID : R01 AG061290
Pays : United States

Informations de copyright

© 2021 American Chemical Society.

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

Références

Dev Cell. 2005 Aug;9(2):249-59
pubmed: 16054031
Pharmacol Ther. 2018 Oct;190:173-186
pubmed: 29807057
ChemMedChem. 2014 Apr;9(4):823-32
pubmed: 24616449
SLAS Discov. 2017 Oct;22(9):1168-1174
pubmed: 28426937
Biol Reprod. 2020 Aug 4;103(2):176-182
pubmed: 32307523
Proc Natl Acad Sci U S A. 2004 Mar 2;101(9):2993-8
pubmed: 14976244
Mol Inform. 2010 Jan 12;29(1-2):97-110
pubmed: 27463852
Nat Chem Biol. 2016 Oct;12(10):838-44
pubmed: 27547922
J Am Chem Soc. 2015 Feb 25;137(7):2695-703
pubmed: 25625324
Interface Focus. 2021 Apr 6;11(2):20200034
pubmed: 33633833
Dev Biol. 2006 Aug 15;296(2):353-62
pubmed: 16842770
Hum Reprod. 2019 Jun 4;34(6):1155-1164
pubmed: 31119281
Biochim Biophys Acta. 2014 Dec;1842(12 Pt B):2535-47
pubmed: 25193033

Auteurs

Makoto Fushimi (M)

Tri-Institutional Therapeutics Discovery Institute, New York, New York 10021, United States.

Hannes Buck (H)

Department of Pharmacology, Weill Cornell Medicine, New York, New York 10021, United States.

Melanie Balbach (M)

Department of Pharmacology, Weill Cornell Medicine, New York, New York 10021, United States.

Anna Gorovyy (A)

Department of Pharmacology, Weill Cornell Medicine, New York, New York 10021, United States.

Jacob Ferreira (J)

Department of Pharmacology, Weill Cornell Medicine, New York, New York 10021, United States.

Thomas Rossetti (T)

Department of Pharmacology, Weill Cornell Medicine, New York, New York 10021, United States.

Navpreet Kaur (N)

Department of Pharmacology, Weill Cornell Medicine, New York, New York 10021, United States.

Lonny R Levin (LR)

Department of Pharmacology, Weill Cornell Medicine, New York, New York 10021, United States.

Jochen Buck (J)

Department of Pharmacology, Weill Cornell Medicine, New York, New York 10021, United States.

Jonathan Quast (J)

Department of Biochemistry, University of Bayreuth, 95440 Bayreuth, Germany.

Joop van den Heuvel (J)

Helmholtz-Zentrum für Infektionsforschung, 38124 Braunschweig, Germany.

Clemens Steegborn (C)

Department of Biochemistry, University of Bayreuth, 95440 Bayreuth, Germany.

Efrat Finkin-Groner (E)

Tri-Institutional Therapeutics Discovery Institute, New York, New York 10021, United States.

Stacia Kargman (S)

Tri-Institutional Therapeutics Discovery Institute, New York, New York 10021, United States.

Mayako Michino (M)

Tri-Institutional Therapeutics Discovery Institute, New York, New York 10021, United States.

Michael A Foley (MA)

Tri-Institutional Therapeutics Discovery Institute, New York, New York 10021, United States.

Michael Miller (M)

Tri-Institutional Therapeutics Discovery Institute, New York, New York 10021, United States.

Nigel J Liverton (NJ)

Tri-Institutional Therapeutics Discovery Institute, New York, New York 10021, United States.

David J Huggins (DJ)

Tri-Institutional Therapeutics Discovery Institute, New York, New York 10021, United States.
Department of Physiology and Biophysics, Weill Cornell Medicine, New York, New York 10021, United States.

Peter T Meinke (PT)

Tri-Institutional Therapeutics Discovery Institute, New York, New York 10021, United States.
Department of Pharmacology, Weill Cornell Medicine, New York, New York 10021, United States.

Classifications MeSH