Preferred Label : Cemsidomide;
NCIt synonyms : MonoDAC CFT7455; Monofunctional Degradation Activating Compound CFT7455; Cereblon E3 Ubiquitin Ligase Modulating Agent CFT7455;
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, cemsidomide specifically binds to cereblon (CRBN),
thereby affecting the ubiquitin E3 ligase activity, and targeting certain substrate
proteins for ubiquitination. This induces proteasome-mediated degradation of certain
transcription factors, including 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.
This also leads to 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.;
UNII : D86MF5H9WJ;
Molecule name : CFT 7455; CFT-7455;
NCI Metathesaurus CUI : CL1662251;
Origin ID : C179502;
UMLS CUI : C5555729;
Semantic type(s)
- concept_is_in_subset
- has_target
