Preferred Label : BTK Degrader AC0676;
NCIt definition : An orally bioavailable chimeric degrader of Bruton's tyrosine kinase (BTK) comprised
of an E3 ubiquitin ligase ligand conjugated to a BTK-binding ligand, with potential
antineoplastic activity. Upon oral administration, BTK degrader AC0676 specifically
targets and binds to, with its BTK-targeting moiety, wild-type (WT) and various mutant
forms, including, but not limited to, C481S and L528W. Upon binding, the E3 ubiquitin
ligase ligand moiety binds to E3 ubiquitin ligase. This catalyzes ubiquitination and
proteasome-mediated degradation of BTK, and prevents the activation of the B-cell
antigen receptor (BCR) signaling pathway. This prevents both B-cell activation 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 B-lymphocyte development, activation, signaling, proliferation
and survival.;
Molecule name : AC 0676; AC-0676; AC676;
NCI Metathesaurus CUI : CL1907461;
Origin ID : C200461;
concept_is_in_subset
- has_target
