Preferred Label : Cereblon Modulator TQB3820;
NCIt synonyms : Cereblon-modulating Agent TQB3820;
NCIt definition : An orally bioavailable modulator of cereblon (CRBN), part of the cullin 4-RING E3
ubiquitin ligase complex (CRL4-CRBN E3 ubiquitin ligase; CUL4-CRBN E3 ubiquitin ligase),
with potential immunomodulating and antineoplastic activities. Upon oral administration,
CRBN modulator TQB3820 specifically binds to CRBN, thereby affecting the ubiquitin
E3 ligase activity. This leads to ubiquitination and induces proteasome-mediated degradation
of the hematopoietic transcription factors Ikaros (IKZF1) and Aiolos (IKZF3), which
are transcriptional repressors in T-cells. This reduces the levels of these transcription
factors, and modulates the activity of the immune system, which may include the activation
of T-lymphocytes. In addition, the degradation of IKZF1 and IKZF3 may lead to the
downregulation of other proteins, including interferon regulatory factor 4 (IRF4)
and c-Myc, which play key roles in the proliferation of certain cancer cell types.
CRBN, the substrate recognition component of the E3 ubiquitin ligase complex, plays
an important role in the ubiquitination of certain proteins.;
Molecule name : TQB 3820; TQB-3820;
NCI Metathesaurus CUI : CL1771922;
Origin ID : C183558;
UMLS CUI : C5666917;
Semantic type(s)
- concept_is_in_subset
- has_target
