Entry Database : PDB / ID : 7jov Structure visualization Downloads & linksTitle CRYSTAL STRUCTURE OF RHO-ASSOCIATED PROTEIN KINASE 2 (ROCK2) IN COMPLEX WITH A PHENYLPYRAZOLE AMIDE INHIBITOR ComponentsRho-associated protein kinase 2 Details Keywords TRANSFERASE/TRANSFERASE INHIBITOR / ROCK1 / KINASE / TRANSFERASE / TRANSFERASE-TRANSFERASE INHIBITOR COMPLEXFunction / homology Function and homology informationFunction Domain/homology Component
cellular response to acetylcholine / positive regulation of centrosome duplication / positive regulation of connective tissue growth factor production / positive regulation of amyloid precursor protein catabolic process / regulation of angiotensin-activated signaling pathway / Rho-dependent protein serine/threonine kinase activity / negative regulation of protein localization to lysosome / positive regulation of connective tissue replacement / regulation of keratinocyte differentiation / positive regulation of fibroblast growth factor production ... cellular response to acetylcholine / positive regulation of centrosome duplication / positive regulation of connective tissue growth factor production / positive regulation of amyloid precursor protein catabolic process / regulation of angiotensin-activated signaling pathway / Rho-dependent protein serine/threonine kinase activity / negative regulation of protein localization to lysosome / positive regulation of connective tissue replacement / regulation of keratinocyte differentiation / positive regulation of fibroblast growth factor production / response to transforming growth factor beta / negative regulation of myosin-light-chain-phosphatase activity / regulation of nervous system process / regulation of cell junction assembly / negative regulation of bicellular tight junction assembly / modulation by host of viral process / regulation of cellular response to hypoxia / positive regulation of protein localization to early endosome / embryonic morphogenesis / negative regulation of nitric oxide biosynthetic process / negative regulation of biomineral tissue development / cellular response to testosterone stimulus / regulation of establishment of endothelial barrier / RHO GTPases Activate ROCKs / regulation of stress fiber assembly / regulation of cell motility / actomyosin structure organization / Sema4D induced cell migration and growth-cone collapse / response to angiotensin / aortic valve morphogenesis / regulation of establishment of cell polarity / RHOBTB1 GTPase cycle / cortical actin cytoskeleton organization / regulation of focal adhesion assembly / positive regulation of amyloid-beta formation / RHOB GTPase cycle / tau-protein kinase activity / EPHA-mediated growth cone collapse / mRNA destabilization / positive regulation of cardiac muscle hypertrophy / RHOC GTPase cycle / centrosome duplication / RHOH GTPase cycle / Rho protein signal transduction / mitotic cytokinesis / endopeptidase activator activity / smooth muscle contraction / RHOA GTPase cycle / epithelial to mesenchymal transition / canonical NF-kappaB signal transduction / regulation of cell adhesion / positive regulation of stress fiber assembly / EPHB-mediated forward signaling / positive regulation of endothelial cell migration / blood vessel diameter maintenance / negative regulation of angiogenesis / protein localization to plasma membrane / response to ischemia / regulation of actin cytoskeleton organization / tau protein binding / regulation of circadian rhythm / small GTPase binding / VEGFA-VEGFR2 Pathway / cytoplasmic ribonucleoprotein granule / G alpha (12/13) signalling events / rhythmic process / actin cytoskeleton organization / protease binding / Potential therapeutics for SARS / positive regulation of MAPK cascade / cytoskeleton / non-specific serine/threonine protein kinase / positive regulation of cell migration / positive regulation of protein phosphorylation / protein phosphorylation / negative regulation of gene expression / protein serine kinase activity / protein serine/threonine kinase activity / centrosome / positive regulation of gene expression / structural molecule activity / RNA binding / ATP binding / nucleus / metal ion binding / plasma membrane / cytoplasm / cytosol Similarity search - Function : / Rho-associated protein kinase 2, HR1 domain / ROCK, Rho binding domain / Rho-associated protein kinase 1/2 / Rho Binding / Rho-binding (RhoBD) domain profile. / HR1 rho-binding domain / REM-1 domain profile. / Zinc finger phorbol-ester/DAG-type profile. / Protein kinase C conserved region 1 (C1) domains (Cysteine-rich domains) ... : / Rho-associated protein kinase 2, HR1 domain / ROCK, Rho binding domain / Rho-associated protein kinase 1/2 / Rho Binding / Rho-binding (RhoBD) domain profile. / HR1 rho-binding domain / REM-1 domain profile. / Zinc finger phorbol-ester/DAG-type profile. / Protein kinase C conserved region 1 (C1) domains (Cysteine-rich domains) / Protein kinase C-like, phorbol ester/diacylglycerol-binding domain / C1-like domain superfamily / Extension to Ser/Thr-type protein kinases / AGC-kinase, C-terminal / AGC-kinase C-terminal domain profile. / PH domain profile. / Pleckstrin homology domain. / Pleckstrin homology domain / PH-like domain superfamily / Serine/threonine-protein kinase, active site / Serine/Threonine protein kinases active-site signature. / Protein kinase domain / Serine/Threonine protein kinases, catalytic domain / Protein kinase, ATP binding site / Protein kinases ATP-binding region signature. / Protein kinase domain profile. / Protein kinase domain / Protein kinase-like domain superfamily Similarity search - Domain/homologyBiological species Homo sapiens (human)Method X-RAY DIFFRACTION / SYNCHROTRON / MOLECULAR REPLACEMENT / Resolution : 2.586 Å DetailsAuthors Muckelbauer, J.K. CitationJournal : Bioorg.Med.Chem.Lett. / Year : 2020Title : Discovery of a phenylpyrazole amide ROCK inhibitor as a tool molecule for in vivo studies.Authors: Hu, Z. / Wang, C. / Glunz, P.W. / Li, J. / Cheadle, N.L. / Chen, A.Y. / Chen, X.Q. / Myers, J.E. / Guarino, V.R. / Rose, A. / Sack, J.S. / Sitkoff, D. / Taylor, D.S. / Xu, S. / Yan, C. / ... Authors : Hu, Z. / Wang, C. / Glunz, P.W. / Li, J. / Cheadle, N.L. / Chen, A.Y. / Chen, X.Q. / Myers, J.E. / Guarino, V.R. / Rose, A. / Sack, J.S. / Sitkoff, D. / Taylor, D.S. / Xu, S. / Yan, C. / Zhang, H. / Zhang, L. / Hennan, J. / Adam, L.P. / Wexler, R.R. / Quan, M.L. History Deposition Aug 7, 2020 Deposition site : RCSB / Processing site : RCSBRevision 1.0 Sep 2, 2020 Provider : repository / Type : Initial releaseRevision 1.1 Mar 6, 2024 Group : Data collection / Database references / Category : chem_comp_atom / chem_comp_bond / database_2Item : _database_2.pdbx_DOI / _database_2.pdbx_database_accession
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