Discovery of VU6015929: A Selective Discoidin Domain Receptor 1/2 (DDR1/2) Inhibitor to Explore the Role of DDR1 in Antifibrotic Therapy.

Jeffries, Daniel E; Borza, Corina M; Blobaum, Anna L; Pozzi, Ambra; Lindsley, Craig W

Jeffries, Daniel E; Borza, Corina M; Blobaum, Anna L; Pozzi, Ambra; Lindsley, Craig W.

Afiliación

Jeffries DE; Department of Chemistry, Vanderbilt University, Nashville, Tennessee 37232, United States.
Borza CM; Department of Medicine, Division of Nephrology, Vanderbilt University, Nashville, Tennessee 37232, United States.
Blobaum AL; Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, United States.
Pozzi A; Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University School of Medicine, Nashville, Tennessee 37232, United States.
Lindsley CW; Department of Medicine, Division of Nephrology, Vanderbilt University, Nashville, Tennessee 37232, United States.

ACS Med Chem Lett ; 11(1): 29-33, 2020 Jan 09.

Article en En | MEDLINE | ID: mdl-31938459

RESUMEN

Herein, we report the discovery of a potent and selective dual DDR1/2 inhibitor, 7e (VU6015929), displaying low cytotoxicity, good kinome selectivity, and possessing an acceptable in vitro DMPK profile with good rodent in vivo pharmacokinetics. VU6015929 potently blocks collagen-induced DDR1 activation and collagen-IV production, suggesting DDR1 inhibition as an exciting target for antifibrotic therapy.

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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2020 Tipo del documento: Article País de afiliación: Estados Unidos

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