Linking Phenotype to Kinase: Identification of a Novel Benzoxaborole Hinge-Binding Motif for Kinase Inhibition and Development of High-Potency Rho Kinase Inhibitors

Benzoxaboroles are a novel class of drug-like compounds that have been rich sources of novel inhibitors for various enzymes and of new drugs. While examining benzoxaborole activity in phenotypic screens, our attention was attracted by the (aminomethylphenoxy)benzoxaborole family, which potently inhi...

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Veröffentlicht in:	The Journal of pharmacology and experimental therapeutics 2013-12, Vol.347 (3), p.615-625
Hauptverfasser:	Akama, Tsutomu, Dong, Chen, Virtucio, Charlotte, Sullivan, David, Zhou, Yasheen, Zhang, Yong-Kang, Rock, Fernando, Freund, Yvonne, Liu, Liang, Bu, Wei, Wu, Anne, Fan, Xiao-Qing, Jarnagin, Kurt
Format:	Artikel
Sprache:	eng
Schlagworte:	(1R,4r)-4-((R)-1-aminoethyl)-N-(pyridin-4-yl)cyclohexanecarboxamide Y-39983, (R)-4-(1-aminoethyl)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzamide 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyl-tetrazolium bromide 5-(1,4-diazepane-1-sulfonyl)isoquinoline 6-[4-(aminomethyl)-2-chlorophenoxyl]benzo[c][1,2]oxaborol-1(3H)-ol 6-[4-(aminomethyl)-2-fluorophenoxyl]benzo[c][1,2]oxaborol-1(3H)-ol AN3484 AN3485 Animals Aorta, Thoracic - drug effects area under the curve AUC blood pressure Blood Pressure - drug effects Boron Compounds - metabolism Cytokines - blood dimethylsulfoxide dithiothreitol DMSO DTT glutathione S-transferase GST HA-1077 heart rate high-pressure liquid chromatography HPLC Humans IFN-γ interferon-γ interleukin Jurkat Cells lipopolysaccharide LPS Models, Molecular MTT Muscle Contraction - drug effects Muscle Relaxation - drug effects Muscle, Smooth - drug effects Muscle, Smooth, Vascular - drug effects Myocytes, Smooth Muscle - drug effects myosin phosphatase-1 MYPT1 PBMC PEG400 peripheral blood mononuclear cell PHA pharmacokinetics Phosphorylation phytohemagglutinin PKA polyethylene glycol-400 propylene glycol protein kinase A Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - metabolism Protein Kinase Inhibitors - pharmacology Protein Phosphatase 1 - metabolism Rats Rats, Inbred SHR Rats, Sprague-Dawley Rho-activated kinase rho-Associated Kinases - antagonists & inhibitors rho-Associated Kinases - genetics rho-Associated Kinases - metabolism ROCK SAR Structure-Activity Relationship TNF-α Trachea - drug effects tumor necrosis factor-α X-ray diffraction XRD Y-27632
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