Preferred Label : Cereblon Modulator SP-3164;
NCIt synonyms : CRBN Modulator SP-3164; CRBN-binding Molecular Glue SP-3164; Protein Degrader SP-3164;
NCIt definition : An orally bioavailable avadomide derivative, which contains the stable, active (S)-enantiomer
form of avadomide, and modulator of cereblon (CRBN), which is 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 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. 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 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. SP3164 uses deuterium to stabilize the (S)-enantiomer of avadomide
and prevent interconversion to the undesired (R)-enantiomer, which increases the binding
affinity to CRBN.;
Molecule name : SP-3164; SP 3164;
Origin ID : C201074;
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