Preferred Label : BTK Inhibitor HMPL-760;
NCIt synonyms : Bruton's Tyrosine Kinase Inhibitor HMPL760;
NCIt definition : A third-generation, reversible inhibitor of Bruton's tyrosine kinase (BTK; Bruton
agammaglobulinemia tyrosine kinase), with potential antineoplastic activity. Upon
administration, BTK inhibitor HMPL-760 non-covalently binds to and inhibits the activity
of both wild-type and the C481S mutated form of BTK, a resistance mutation in the
BTK active site in which cysteine is substituted for serine at residue 481. This prevents
the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated
activation of downstream survival pathways. This leads to an inhibition of the growth
of malignant B-cells that overexpress BTK or the C481S mutated form. BTK C481S mutation
plays an important role in resistance to certain BTK inhibitors; HMPL-760 may be able
to overome this resistance. BTK, a member of the Src-related BTK/Tec family of cytoplasmic
tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role
in the development, activation, signaling, proliferation and survival of B-lymphocytes.;
Molecule name : HMPL-760; HMPL 760;
NCI Metathesaurus CUI : CL1773932;
Origin ID : C185593;
UMLS CUI : C5667006;
Semantic type(s)
- concept_is_in_subset
- has_target
