Preferred Label : Cereblon Modulator BTX-1188;
NCIt synonyms : Protein Degrader BTX-1188; PHM BTX-1188; Protein Homeostatic Modulator BTX-1188;
NCIt definition : An orally bioavailable small molecule 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 BTX-1188 specifically targets and 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, and the
degradation of the protein neosubstrate G1 to S phase transition 1 (GSPT1), a translation
termination factor. 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 the proteins IKZF1/3 and GSPT1 may lead to the downregulation
of other proteins that 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 : BTX-1188; BTX 188;
NCI Metathesaurus CUI : CL1792157;
Origin ID : C187349;
UMLS CUI : C5706413;
Semantic type(s)
- concept_is_in_subset
- has_target
