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Small molecule-mediated TGF-β type II receptor degradation promotes cardiomyogenesis in embryonic stem cells.
ITD-1 is a highly selective TGF-β inhibitor and reveals an unexpected role for T GF-β signaling in controlling cardiomyocyte differentiation from multipotent cardiovascular precursors. Expand
Reduction of N(ω)-hydroxy-L-arginine by the mitochondrial amidoxime reducing component (mARC).
It is shown for the first time that both human isoforms of the newly identified mARC (mitochondrial amidoxime reducing component) enhance the rate of reduction of NOHA, in the presence of NADH cytochrome b₅ reductase and cy tochrome b ₅, by more than 500-fold, providing the first hints that mARC might be involved in mitochondrial NOHA reduction and could be of physiological significance in affecting endogenous nitric oxide levels. Expand
Modulating the NO generating system from a medicinal chemistry perspective: current trends and therapeutic options in cardiovascular disease.
Novel developments essentially imply a paradigm shift from purely symptomatic to more causative therapeutics which opens up opportunities to not only treat ischemic heart disease but many more cardiovascular diseases. Expand
Structure-activity relationship of novel and known inhibitors of human dimethylarginine dimethylaminohydrolase-1: alkenyl-amidines as new leads.
The binding pocket of the guanidine-moiety was investigated by screening differently substituted guanidines, amidines and isothioureas in order to collect information on possible binding modes in the active site. Expand
Differentiation of cardiomyocytes and generation of human engineered heart tissue
This protocol describes the differentiation of cardiomyocytes from hiPSCs; standardized generation of defined embryoid bodies, growth factor and small-molecule-based cardiac differentiation; and standardizedgeneration of EHTs. Expand
Synthesis and SAR of b-annulated 1,4-dihydropyridines define cardiomyogenic compounds as novel inhibitors of TGFβ signaling.
A medium-throughput murine embryonic stem cell (mESC)-based high-content screening of 17000 small molecules for cardiogenesis led to the identification of a b-annulated 1,4-dihydropyridine (1,4-DHP)Expand
Small molecules targeting in vivo tissue regeneration.
Current progress using small molecules targeting in vivo aspects of regeneration, including adult stem cells, stem cell niches, and mechanisms of homing, mobilization, and engraftment as well as somatic cell proliferation are discussed. Expand
New Prodrugs of the Antiprotozoal Drug Pentamidine
The objective of this investigation was the systematic characterisation and evaluation of eight pentamidine prodrugs in order to identify the most appropriate strategy to improve the properties of the parent drug. Expand
Synthesis and biological evaluation of L-valine-amidoximeesters as double prodrugs of amidines.
Bioactivation of N-valoxybenzamidine and N,N'-bis(valoxy)pentamidine via hydrolysis and reduction has been demonstrated in vitro with porcine and human subcellular enzyme preparations and the mitochondrial Amidoxime Reducing Component (mARC). Expand