Preferred Label : CRL4-CRBN Modulator KPG-818;
NCIt synonyms : Cereblon E3 Ubiquitin Ligase Modulating Agent KPG-818; CRBN E3 Ubiquitin Ligase Complex CRL4-CRBN Modulator KPG-818;
NCIt definition : An orally bioavailable modulator of the E3 ubiquitin ligase complex containing cereblon
(CRL4-CRBN E3 ubiquitin ligase), with potential immunomodulating and antineoplastic
activities. Upon oral administration, CRL4-CRBN modulator KPG-818 specifically targets
and binds to cereblon (CRBN) of the E3 ubiquitin ligase (CRL4-CRBN) complex, thereby
affecting the ubiquitin E3 ligase activity, and targeting certain substrate proteins
for ubiquitination. This induces proteasome-mediated degradation of certain transcription
factors, some of which are transcriptional repressors in T-cells. This leads to modulation
of the immune system, including activation of T-lymphocytes, and downregulation of
the activity of other proteins, some of which play key roles in the proliferation
of certain cancer cell types. CRBN, the substrate recognition component of the CRL4-CRBN
E3 ubiquitin ligase complex, plays a key role in the ubiquitination of certain proteins.;
Molecule name : KPG-818; KPG 818;
NCI Metathesaurus CUI : CL1413416;
Origin ID : C175979;
UMLS CUI : C5446901;
Semantic type(s)
- concept_is_in_subset
