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- NCIT_C187349 IAO_0000115 "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." @default.
- NCIT_C187349 NCIT_A7 NCIT_C104142 @default.
- NCIT_C187349 NCIT_NHC0 "C187349" @default.
- NCIT_C187349 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C187349 NCIT_P107 "Cereblon Modulator BTX-1188" @default.
- NCIT_C187349 NCIT_P108 "Cereblon Modulator BTX-1188" @default.
- NCIT_C187349 NCIT_P208 "CL1792157" @default.
- NCIT_C187349 NCIT_P322 "CTRP" @default.
- NCIT_C187349 NCIT_P322 "GDC" @default.
- NCIT_C187349 NCIT_P399 "810822" @default.
- NCIT_C187349 normalizedInformationContent "100" @default.
- NCIT_C187349 referenceCount "1" @default.
- NCIT_C187349 hasExactSynonym "BTX 188" @default.
- NCIT_C187349 hasExactSynonym "BTX-1188" @default.
- NCIT_C187349 hasExactSynonym "BTX1188" @default.
- NCIT_C187349 hasExactSynonym "Cereblon Modulator BTX-1188" @default.
- NCIT_C187349 hasExactSynonym "PHM BTX-1188" @default.
- NCIT_C187349 hasExactSynonym "Protein Degrader BTX-1188" @default.
- NCIT_C187349 hasExactSynonym "Protein Homeostatic Modulator BTX-1188" @default.
- NCIT_C187349 inSubset NCIT_C116977 @default.
- NCIT_C187349 inSubset NCIT_C116978 @default.
- NCIT_C187349 inSubset NCIT_C128784 @default.
- NCIT_C187349 inSubset NCIT_C157711 @default.
- NCIT_C187349 inSubset NCIT_C157712 @default.
- NCIT_C187349 inSubset NCIT_C176424 @default.
- NCIT_C187349 type Class @default.
- NCIT_C187349 isDefinedBy ncit.owl @default.
- NCIT_C187349 label "Cereblon Modulator BTX-1188" @default.
- NCIT_C187349 subClassOf NCIT_C187349 @default.
- NCIT_C187349 subClassOf NCIT_C1908 @default.
- NCIT_C187349 subClassOf NCIT_C1909 @default.
- NCIT_C187349 subClassOf NCIT_C308 @default.