Entry Database : PDB / ID : 8bi2 Structure visualization Downloads & linksTitle Syk kinase domain in complex with macrocyclic inhibitor 20a ComponentsTyrosine-protein kinase SYK Details Keywords TRANSFERASE / SYK Kinase TRANSFERASE INHIBITORFunction / homology Function and homology informationFunction Domain/homology Component
interleukin-15 receptor binding / regulation of superoxide anion generation / regulation of neutrophil degranulation / regulation of arachidonate secretion / cellular response to lectin / gamma-delta T cell differentiation / positive regulation of interleukin-3 production / positive regulation of gamma-delta T cell differentiation / B cell receptor complex / positive regulation of mast cell cytokine production ... interleukin-15 receptor binding / regulation of superoxide anion generation / regulation of neutrophil degranulation / regulation of arachidonate secretion / cellular response to lectin / gamma-delta T cell differentiation / positive regulation of interleukin-3 production / positive regulation of gamma-delta T cell differentiation / B cell receptor complex / positive regulation of mast cell cytokine production / serotonin secretion by platelet / Toll-like receptor binding / regulation of platelet aggregation / positive regulation of alpha-beta T cell proliferation / leukocyte activation involved in immune response / neutrophil activation involved in immune response / positive regulation of mast cell degranulation / lymph vessel development / regulation of platelet activation / collagen-activated tyrosine kinase receptor signaling pathway / cell activation / positive regulation of killing of cells of another organism / macrophage activation involved in immune response / beta selection / regulation of phagocytosis / cellular response to molecule of fungal origin / early phagosome / FLT3 signaling through SRC family kinases / regulation of tumor necrosis factor-mediated signaling pathway / leukotriene biosynthetic process / positive regulation of monocyte chemotactic protein-1 production / interleukin-3-mediated signaling pathway / cellular response to lipid / regulation of DNA-binding transcription factor activity / positive regulation of cell adhesion mediated by integrin / positive regulation of granulocyte macrophage colony-stimulating factor production / Interleukin-2 signaling / positive regulation of alpha-beta T cell differentiation / blood vessel morphogenesis / Fc epsilon receptor (FCERI) signaling / T cell receptor complex / mast cell degranulation / positive regulation of B cell differentiation / leukocyte cell-cell adhesion / Fc-gamma receptor signaling pathway involved in phagocytosis / positive regulation of interleukin-4 production / Dectin-2 family / stimulatory C-type lectin receptor signaling pathway / positive regulation of cysteine-type endopeptidase activity involved in apoptotic process / Fc-epsilon receptor signaling pathway / positive regulation of receptor internalization / phospholipase binding / amyloid-beta clearance / positive regulation of interleukin-10 production / cellular response to low-density lipoprotein particle stimulus / FCGR activation / positive regulation of type I interferon production / positive regulation of bone resorption / phosphatase binding / Role of phospholipids in phagocytosis / Role of LAT2/NTAL/LAB on calcium mobilization / Signaling by CSF3 (G-CSF) / negative regulation of inflammatory response to antigenic stimulus / cell surface receptor protein tyrosine kinase signaling pathway / GPVI-mediated activation cascade / positive regulation of interleukin-12 production / positive regulation of TORC1 signaling / neutrophil chemotaxis / positive regulation of calcium-mediated signaling / phosphotyrosine residue binding / SH2 domain binding / Integrin signaling / B cell differentiation / FCERI mediated Ca+2 mobilization / regulation of ERK1 and ERK2 cascade / FCGR3A-mediated IL10 synthesis / positive regulation of superoxide anion generation / Antigen activates B Cell Receptor (BCR) leading to generation of second messengers / positive regulation of interleukin-8 production / integrin-mediated signaling pathway / Regulation of signaling by CBL / FCERI mediated MAPK activation / animal organ morphogenesis / FCGR3A-mediated phagocytosis / B cell receptor signaling pathway / non-specific protein-tyrosine kinase / calcium-mediated signaling / non-membrane spanning protein tyrosine kinase activity / positive regulation of protein-containing complex assembly / Inactivation of CSF3 (G-CSF) signaling / receptor internalization / platelet activation / CLEC7A (Dectin-1) signaling / Regulation of actin dynamics for phagocytic cup formation / positive regulation of interleukin-6 production / peptidyl-tyrosine phosphorylation / protein import into nucleus / positive regulation of peptidyl-tyrosine phosphorylation / cellular response to amyloid-beta / positive regulation of tumor necrosis factor production Similarity search - Function Tyrosine-protein kinase, non-receptor SYK/ZAP-70 / Tyrosine-protein kinase SYK/ZAP-70, inter-SH2 domain superfamily / SYK/ZAP-70, N-terminal SH2 domain / : / SH2 domain / Src homology 2 (SH2) domain profile. / Src homology 2 domains / SH2 domain / SH2 domain superfamily / Tyrosine-protein kinase, catalytic domain ... Tyrosine-protein kinase, non-receptor SYK/ZAP-70 / Tyrosine-protein kinase SYK/ZAP-70, inter-SH2 domain superfamily / SYK/ZAP-70, N-terminal SH2 domain / : / SH2 domain / Src homology 2 (SH2) domain profile. / Src homology 2 domains / SH2 domain / SH2 domain superfamily / Tyrosine-protein kinase, catalytic domain / Tyrosine kinase, catalytic domain / Tyrosine protein kinases specific active-site signature. / Tyrosine-protein kinase, active site / Serine-threonine/tyrosine-protein kinase, catalytic domain / Protein tyrosine and serine/threonine kinase / 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 : 1.508 Å DetailsAuthors Read, J.A. / Patel, J. Funding support 1items Details Hide detailsOrganization Grant number Country Not funded
CitationJournal : Bioorg.Med.Chem.Lett. / Year : 2023Title : Optimization of a series of novel, potent and selective Macrocyclic SYK inhibitors.Authors: Grimster, N.P. / Gingipalli, L. / Balazs, A. / Barlaam, B. / Boiko, S. / Boyd, S. / Dry, H. / Goldberg, F.W. / Ikeda, T. / Johnson, T. / Kawatkar, S. / Kemmitt, P. / Lamont, S. / Lorthioir, ... Authors : Grimster, N.P. / Gingipalli, L. / Balazs, A. / Barlaam, B. / Boiko, S. / Boyd, S. / Dry, H. / Goldberg, F.W. / Ikeda, T. / Johnson, T. / Kawatkar, S. / Kemmitt, P. / Lamont, S. / Lorthioir, O. / Mfuh, A. / Patel, J. / Pike, A. / Read, J. / Romero, R. / Sarkar, U. / Sha, L. / Simpson, I. / Song, K. / Su, Q. / Wang, H. / Watson, D. / Wu, A. / Zehnder, T.E. / Zheng, X. / Li, S. / Dong, Z. / Yang, D. / Song, Y. / Wang, P. / Liu, X. / Dowling, J.E. / Edmondson, S.D. History Deposition Nov 1, 2022 Deposition site : PDBE / Processing site : PDBERevision 1.0 Jun 14, 2023 Provider : repository / Type : Initial releaseRevision 1.1 Jun 21, 2023 Group : Database references / Category : citation / Item : _citation.journal_volume / _citation.titleRevision 1.2 May 1, 2024 Group : Data collection / Refinement descriptionCategory : chem_comp_atom / chem_comp_bond / pdbx_initial_refinement_model
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