Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 11, Issue 1, Pages 29-33Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.9b00382
Keywords
Discoidin domain receptor 1 (DDR1); tyrosine receptor kinase; collagen; fibrosis
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Funding
- Veterans Affairs Merit Review [1I01BX002025]
- National Institute of Health [R01-DK119212, P30-DK114809]
- VA Senior Research Career Scientist award
- William K. Warren Foundation
- Chair in Medicine
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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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