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Front Cover: Toward Second‐Generation Cardiomyogenic and Anti‐cardiofibrotic 1,4‐Dihydropyridine‐Class TGFβ Inhibitors (ChemMedChem 8/2019)
Author(s) -
Längle Daniel,
Werner Tessa R.,
Wesseler Fabian,
Reckzeh Elena,
Schaumann Niklas,
Drowley Lauren,
Polla Magnus,
Plowright Alleyn T.,
Hirt Marc N.,
Eschenhagen Thomas,
Schade Dennis
Publication year - 2019
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201900212
Subject(s) - cardiac fibrosis , front cover , chemistry , pharmacology , transforming growth factor , fibrosis , medicine , cover (algebra) , engineering , mechanical engineering
The Front Cover shows b ‐annelated 1,4‐dihydropyridines as unique degraders of type II TGFβ receptors that might serve as novel therapeutic modalities after ischemic injury of the heart. TGFβ inhibition by these compounds showed efficacy both in human iPSC‐derived cardiac progenitor cells and in a cardiac fibrosis model using 3D‐engineered heart tissue constructs. An early hit‐to‐lead study addressed intrinsic shortcomings of these dihydropyridines, including physicochemical and metabolic liabilities. Herein reported compound data underlines their utility as new tools for experimental pharmacology of cardiac diseases. More information can be found in the Full Paper by Dennis Schade et al. on page 810 in Issue 8, 2019 (DOI: 10.1002/cmdc.201900036).