Preferred Label : BTK Inhibitor TT-01488;
NCIt definition : An orally bioavailable reversible inhibitor of Bruton's tyrosine kinase (BTK; Bruton
agammaglobulinemia tyrosine kinase), with potential antineoplastic activity. Upon
oral administration, BTK inhibitor TT-01488 non-covalently binds to and inhibits the
activity of BTK, including the C481S mutated form, 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. 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. BTK C481S mutation plays an important role in resistance
to certain BTK inhibitors.;
Molecule name : TT 01488; TT-01488;
NCI Metathesaurus CUI : CL1791987;
Origin ID : C187100;
UMLS CUI : C5706344;
Semantic type(s)
- concept_is_in_subset
- has_target
