Bruton's tyrosine kinase
BTK plays a crucial role in B cell development as it is required for transmitting signals from the pre-B cell receptor that forms after successful immunoglobulin heavy chain rearrangement.PIP3 binding induces BTK to phosphorylate phospholipase C (PLC), which in turn hydrolyzes PIP2, a phosphatidylinositol, into two second messengers, inositol triphosphate (IP3) and diacylglycerol (DAG), which then go on to modulate the activity of downstream proteins during B-cell signalling.[12] As BTK is also linked to autoimmune disorders,[13][14] recent efforts have sought to evaluate BTK inhibition as a therapeutic strategy for treatment of diseases such as multiple sclerosis (MS) and rheumatoid arthritis (RA).[15] Approved drugs that inhibit BTK: Various drugs that inhibit BTK are in clinical trials:[24] Bruton's tyrosine kinase is named for Ogden Bruton, who first described XLA in 1952.[10][40] Later studies in 1993 and 1994 reported the discovery of BTK (initially termed B cell progenitor kinase or BPK) and found that BTK levels are reduced in B cells from XLA patients.
AliasesHomoloGeneGeneCardsX chromosome (human)RNA expressionGene ontologyOrthologsEntrezEnsemblUniProtPubMedWikidatatyrosine kinaseB cellpleckstrin homologyprotein kinase domainimmunoglobulin heavy chainmast cellreceptorphosphatidylinositol (3,4,5)-trisphosphatephospholipase Cphosphatidylinositolinositol triphosphatediacylglycerolprimary immunodeficiencyX-linked agammaglobulinemiabone marrowX chromosomemutationsmantle cell lymphoma (MCL)chronic lymphocytic leukemia (CLL)multiple sclerosis (MS)rheumatoid arthritis (RA)IbrutinibAcalabrutinibmantle cell lymphomaChronic lymphocytic leukemiaZanubrutinibby mouthTirabrutinibPirtobrutinibOrelabrutinibsmall lymphocytic lymphomaEvobrutinibmultiple sclerosisTolebrutinibRemibrutinibchronic spontaneous urticarianon-Hodgkin lymphomaHM71224autoimmune diseasesHanmi Pharmaceuticalacute myeloid leukaemiamyelodysplastic syndromesNemtabrutinibOgden BrutoninteractARID3ABLNK (SLP-65)SH3BP5BibcodeFood and Drug AdministrationClinicalTrials.govMedical Subject HeadingsUCSC Genome BrowserPDBe-KBProtein kinasestyrosine kinasesReceptor tyrosine kinasesGrowth factor receptorsEGF receptor familyInsulin receptorPDGF receptor familyPDGFRAPDGFRBFGF receptorVEGF receptorsVEGFR1VEGFR2VEGFR3HGF receptorTrk receptorEPH receptorLTK receptorTIE receptorROR receptorDDR receptorPTK7 receptorRYK receptorMuSK receptorAATYK receptorAATYK2AXL receptorRET receptorNon-receptor tyrosine kinasesEnzymesActive siteBinding siteCatalytic triadOxyanion holeEnzyme promiscuityDiffusion-limited enzymeCofactorEnzyme catalysisAllosteric regulationCooperativityEnzyme inhibitorEnzyme activatorEC numberEnzyme superfamilyEnzyme familyList of enzymesEnzyme kineticsEadie–Hofstee diagramHanes–Woolf plotLineweaver–Burk plotMichaelis–Menten kineticsOxidoreductasesTransferasesHydrolasesLyasesIsomerasesLigasesTranslocases