Cereblon E3 Ubiquitin Ligase Modulating Drug BMS-986449

**Semantic type:** Pharmacologic Substance

**Definition:** A modulator of the E3 ubiquitin ligase complex containing cereblon (CRL4-CRBN E3 ubiquitin ligase), with potential immunomodulating and antineoplastic activities. Upon administration, BMS-986449 specifically targets and 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, some of which are transcriptional repressors in regulatory T-cells (Tregs), such as Ikaros family zinc finger protein 2 (IKZF2; zinc finger protein Helios), and IKZF4 (zinc finger protein Eos). This reprograms Tregs and leads to the modulation of the immune system, including activation of T-lymphocytes, and results in a T-cell-mediated anti-tumor immune response.

**Synonyms:** - BMS 986449 - BMS-986449 - BMS986449 - CelMoD BMS-986449 - Cereblon E3 Ubiquitin Ligase Modulating Agent BMS-986449 - Cereblon Modulating Drug BMS-986449 - Cereblon Modulator BMS-986449 - IKZF2/IKZF4 Degrader BMS-986449