登録情報 | データベース: PDB / ID: 4pp7 |
---|
タイトル | Highly Potent and Selective 3-N-methylquinazoline-4(3H)-one Based Inhibitors of B-RafV600E Kinase |
---|
要素 | Serine/threonine-protein kinase B-raf |
---|
キーワード | TRANSFERASE/TRANSFERASE INHIBITOR / serine/threonine-protein kinase B-Raf / TRANSFERASE-TRANSFERASE INHIBITOR complex |
---|
機能・相同性 | 機能・相同性情報
CD4-positive, alpha-beta T cell differentiation / CD4-positive or CD8-positive, alpha-beta T cell lineage commitment / negative regulation of synaptic vesicle exocytosis / Signalling to p38 via RIT and RIN / head morphogenesis / myeloid progenitor cell differentiation / ARMS-mediated activation / SHOC2 M1731 mutant abolishes MRAS complex function / Gain-of-function MRAS complexes activate RAF signaling / endothelial cell apoptotic process ...CD4-positive, alpha-beta T cell differentiation / CD4-positive or CD8-positive, alpha-beta T cell lineage commitment / negative regulation of synaptic vesicle exocytosis / Signalling to p38 via RIT and RIN / head morphogenesis / myeloid progenitor cell differentiation / ARMS-mediated activation / SHOC2 M1731 mutant abolishes MRAS complex function / Gain-of-function MRAS complexes activate RAF signaling / endothelial cell apoptotic process / negative regulation of fibroblast migration / positive regulation of D-glucose transmembrane transport / establishment of protein localization to membrane / mitogen-activated protein kinase kinase binding / regulation of T cell differentiation / Negative feedback regulation of MAPK pathway / positive regulation of axonogenesis / Frs2-mediated activation / stress fiber assembly / positive regulation of axon regeneration / face development / MAP kinase kinase activity / synaptic vesicle exocytosis / somatic stem cell population maintenance / thyroid gland development / MAP kinase kinase kinase activity / negative regulation of endothelial cell apoptotic process / positive regulation of substrate adhesion-dependent cell spreading / positive regulation of stress fiber assembly / response to cAMP / ERK1 and ERK2 cascade / cellular response to calcium ion / substrate adhesion-dependent cell spreading / thymus development / cellular response to nerve growth factor stimulus / long-term synaptic potentiation / animal organ morphogenesis / RAF activation / Spry regulation of FGF signaling / Signaling by high-kinase activity BRAF mutants / MAP2K and MAPK activation / epidermal growth factor receptor signaling pathway / visual learning / response to peptide hormone / Negative regulation of MAPK pathway / Signaling by RAF1 mutants / Signaling by moderate kinase activity BRAF mutants / Paradoxical activation of RAF signaling by kinase inactive BRAF / Signaling downstream of RAS mutants / Signaling by BRAF and RAF1 fusions / MAPK cascade / cellular response to xenobiotic stimulus / positive regulation of peptidyl-serine phosphorylation / presynapse / T cell receptor signaling pathway / regulation of cell population proliferation / T cell differentiation in thymus / cell body / scaffold protein binding / negative regulation of neuron apoptotic process / positive regulation of ERK1 and ERK2 cascade / non-specific serine/threonine protein kinase / protein kinase activity / neuron projection / protein phosphorylation / intracellular membrane-bounded organelle / protein serine kinase activity / protein serine/threonine kinase activity / calcium ion binding / protein-containing complex binding / positive regulation of gene expression / negative regulation of apoptotic process / mitochondrion / ATP binding / identical protein binding / nucleus / plasma membrane / cytosol類似検索 - 分子機能 Raf-like Ras-binding domain / Raf-like Ras-binding / Ras-binding domain (RBD) profile. / Raf-like Ras-binding domain / Diacylglycerol/phorbol-ester binding / : / Phorbol esters/diacylglycerol binding domain (C1 domain) / Zinc finger phorbol-ester/DAG-type signature. / Zinc finger phorbol-ester/DAG-type profile. / Protein kinase C conserved region 1 (C1) domains (Cysteine-rich domains) ...Raf-like Ras-binding domain / Raf-like Ras-binding / Ras-binding domain (RBD) profile. / Raf-like Ras-binding domain / Diacylglycerol/phorbol-ester binding / : / Phorbol esters/diacylglycerol binding domain (C1 domain) / Zinc finger phorbol-ester/DAG-type signature. / 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 / Serine-threonine/tyrosine-protein kinase, catalytic domain / Protein tyrosine and serine/threonine kinase / Ubiquitin-like domain superfamily / Transferase(Phosphotransferase) domain 1 / Transferase(Phosphotransferase); domain 1 / Phosphorylase Kinase; domain 1 / Phosphorylase Kinase; domain 1 / Serine/threonine-protein kinase, active site / Serine/Threonine protein kinases active-site signature. / 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 / 2-Layer Sandwich / Orthogonal Bundle / Mainly Alpha / Alpha Beta類似検索 - ドメイン・相同性 Chem-2VX / Serine/threonine-protein kinase B-raf類似検索 - 構成要素 |
---|
生物種 | Homo sapiens (ヒト) |
---|
手法 | X線回折 / 分子置換 / 解像度: 3.4 Å |
---|
データ登録者 | Wenglowsky, S. / Ren, L. / Grina, J. / Hansen, J.D. / Laird, E.R. / Moreno, D. / Dinkel, V. / Gloor, S.L. / Hastings, G. / Rana, S. ...Wenglowsky, S. / Ren, L. / Grina, J. / Hansen, J.D. / Laird, E.R. / Moreno, D. / Dinkel, V. / Gloor, S.L. / Hastings, G. / Rana, S. / Rasor, K. / Sturgis, H.L. / Voegtli, W.C. / Vigers, G.P.A. / Willis, B. / Mathieu, S. / Rudolph, J. |
---|
引用 | ジャーナル: Bioorg.Med.Chem.Lett. / 年: 2014 タイトル: Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase. 著者: Wenglowsky, S. / Ren, L. / Grina, J. / Hansen, J.D. / Laird, E.R. / Moreno, D. / Dinkel, V. / Gloor, S.L. / Hastings, G. / Rana, S. / Rasor, K. / Sturgis, H.L. / Voegtli, W.C. / Vigers, G. / ...著者: Wenglowsky, S. / Ren, L. / Grina, J. / Hansen, J.D. / Laird, E.R. / Moreno, D. / Dinkel, V. / Gloor, S.L. / Hastings, G. / Rana, S. / Rasor, K. / Sturgis, H.L. / Voegtli, W.C. / Vigers, G. / Willis, B. / Mathieu, S. / Rudolph, J. |
---|
履歴 | 登録 | 2014年2月26日 | 登録サイト: RCSB / 処理サイト: RCSB |
---|
改定 1.0 | 2014年4月9日 | Provider: repository / タイプ: Initial release |
---|
改定 1.1 | 2014年5月7日 | Group: Database references |
---|
改定 1.2 | 2024年2月28日 | Group: Data collection / Database references / Derived calculations カテゴリ: chem_comp_atom / chem_comp_bond ...chem_comp_atom / chem_comp_bond / database_2 / struct_ref_seq_dif / struct_site Item: _database_2.pdbx_DOI / _database_2.pdbx_database_accession ..._database_2.pdbx_DOI / _database_2.pdbx_database_accession / _struct_ref_seq_dif.details / _struct_site.pdbx_auth_asym_id / _struct_site.pdbx_auth_comp_id / _struct_site.pdbx_auth_seq_id |
---|
|
---|