登録情報 | データベース: PDB / ID: 5to8 |
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タイトル | Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency |
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要素 | Protein-tyrosine kinase 2-beta |
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キーワード | Transferase/Transferase Inhibitor / kinase / Transferase-Transferase Inhibitor complex |
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機能・相同性 | 機能・相同性情報
regulation of macrophage chemotaxis / neurotransmitter receptor regulator activity / response to cation stress / positive regulation of B cell chemotaxis / marginal zone B cell differentiation / 3-phosphoinositide-dependent protein kinase binding / regulation of ubiquitin-dependent protein catabolic process / endothelin receptor signaling pathway / negative regulation of myeloid cell differentiation / regulation of postsynaptic density assembly ...regulation of macrophage chemotaxis / neurotransmitter receptor regulator activity / response to cation stress / positive regulation of B cell chemotaxis / marginal zone B cell differentiation / 3-phosphoinositide-dependent protein kinase binding / regulation of ubiquitin-dependent protein catabolic process / endothelin receptor signaling pathway / negative regulation of myeloid cell differentiation / regulation of postsynaptic density assembly / blood vessel endothelial cell migration / negative regulation of muscle cell apoptotic process / negative regulation of bone mineralization / cortical cytoskeleton organization / apical dendrite / positive regulation of ubiquitin-dependent protein catabolic process / activation of Janus kinase activity / regulation of release of sequestered calcium ion into cytosol / cellular response to fluid shear stress / focal adhesion assembly / signal complex assembly / chemokine-mediated signaling pathway / NMDA selective glutamate receptor complex / Interleukin-2 signaling / sprouting angiogenesis / long-term synaptic depression / oocyte maturation / Signal regulatory protein family interactions / positive regulation of cell-matrix adhesion / calmodulin-dependent protein kinase activity / positive regulation of DNA biosynthetic process / postsynaptic modulation of chemical synaptic transmission / positive regulation of actin filament polymerization / stress fiber assembly / negative regulation of potassium ion transport / positive regulation of excitatory postsynaptic potential / RHOU GTPase cycle / response to immobilization stress / positive regulation of protein kinase activity / postsynaptic density, intracellular component / glial cell proliferation / glutamate receptor binding / cellular defense response / regulation of cell adhesion / vascular endothelial growth factor receptor signaling pathway / response to glucose / response to mechanical stimulus / cellular response to retinoic acid / peptidyl-tyrosine autophosphorylation / bone resorption / response to cAMP / tumor necrosis factor-mediated signaling pathway / ionotropic glutamate receptor signaling pathway / positive regulation of endothelial cell migration / positive regulation of synaptic transmission, glutamatergic / response to hormone / response to cocaine / positive regulation of translation / response to ischemia / integrin-mediated signaling pathway / long-term synaptic potentiation / regulation of actin cytoskeleton organization / positive regulation of JNK cascade / non-specific protein-tyrosine kinase / non-membrane spanning protein tyrosine kinase activity / Schaffer collateral - CA1 synapse / regulation of synaptic plasticity / response to hydrogen peroxide / epidermal growth factor receptor signaling pathway / VEGFA-VEGFR2 Pathway / positive regulation of neuron projection development / response to calcium ion / peptidyl-tyrosine phosphorylation / positive regulation of angiogenesis / : / positive regulation of reactive oxygen species metabolic process / neuron projection development / MAPK cascade / positive regulation of nitric oxide biosynthetic process / presynapse / lamellipodium / cell cortex / regulation of cell shape / positive regulation of cytosolic calcium ion concentration / cell body / growth cone / positive regulation of cell growth / protein-containing complex assembly / protein tyrosine kinase activity / response to ethanol / adaptive immune response / negative regulation of neuron apoptotic process / protein autophosphorylation / dendritic spine / positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction / postsynaptic density / cell surface receptor signaling pathway / positive regulation of ERK1 and ERK2 cascade / cytoskeleton / response to hypoxia類似検索 - 分子機能 Focal adhesion kinase, targeting (FAT) domain / Focal adhesion kinase, targeting (FAT) domain superfamily / Focal adhesion kinase, N-terminal / FAK1/PYK2, FERM domain C-lobe / Focal adhesion targeting region / FERM N-terminal domain / : / FAK1/PYK2, FERM domain C-lobe / FERM central domain / FERM/acyl-CoA-binding protein superfamily ...Focal adhesion kinase, targeting (FAT) domain / Focal adhesion kinase, targeting (FAT) domain superfamily / Focal adhesion kinase, N-terminal / FAK1/PYK2, FERM domain C-lobe / Focal adhesion targeting region / FERM N-terminal domain / : / FAK1/PYK2, FERM domain C-lobe / FERM central domain / FERM/acyl-CoA-binding protein superfamily / FERM central domain / FERM superfamily, second domain / FERM domain / FERM domain profile. / Band 4.1 domain / Band 4.1 homologues / Tyrosine-protein kinase, catalytic domain / Tyrosine kinase, catalytic domain / Tyrosine protein kinases specific active-site signature. / PH-like domain superfamily / Tyrosine-protein kinase, active site / Protein tyrosine and serine/threonine kinase / Serine-threonine/tyrosine-protein kinase, catalytic domain / Ubiquitin-like domain superfamily / Transferase(Phosphotransferase) domain 1 / Transferase(Phosphotransferase); domain 1 / Phosphorylase Kinase; domain 1 / Phosphorylase Kinase; domain 1 / Protein kinase, ATP binding site / Protein kinases ATP-binding region signature. / Protein kinase domain profile. / Protein kinase domain / Protein kinase-like domain superfamily / 2-Layer Sandwich / Orthogonal Bundle / Mainly Alpha / Alpha Beta類似検索 - ドメイン・相同性 |
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生物種 | Homo sapiens (ヒト) |
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手法 | X線回折 / シンクロトロン / 解像度: 1.9849 Å |
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データ登録者 | Newby, Z.E. |
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引用 | ジャーナル: Bioorg. Med. Chem. Lett. / 年: 2016 タイトル: Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency. 著者: Farand, J. / Mai, N. / Chandrasekhar, J. / Newby, Z.E. / Van Veldhuizen, J. / Loyer-Drew, J. / Venkataramani, C. / Guerrero, J. / Kwok, A. / Li, N. / Zherebina, Y. / Wilbert, S. / Zablocki, J. ...著者: Farand, J. / Mai, N. / Chandrasekhar, J. / Newby, Z.E. / Van Veldhuizen, J. / Loyer-Drew, J. / Venkataramani, C. / Guerrero, J. / Kwok, A. / Li, N. / Zherebina, Y. / Wilbert, S. / Zablocki, J. / Phillips, G. / Watkins, W.J. / Mourey, R. / Notte, G.T. |
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履歴 | 登録 | 2016年10月17日 | 登録サイト: RCSB / 処理サイト: RCSB |
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改定 1.0 | 2016年12月21日 | Provider: repository / タイプ: Initial release |
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改定 1.1 | 2024年3月6日 | Group: Data collection / Database references / カテゴリ: chem_comp_atom / chem_comp_bond / database_2 Item: _database_2.pdbx_DOI / _database_2.pdbx_database_accession |
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