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December 8, 2025BloodOpen Access

Novel multifunctional degraders of EP300/CBP and IKZF1/3 with potent anti-myeloma activity

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Authors

DADalya AtacaBMBernice MatusowGBGideon Bollag

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Overview

Novel degraders demonstrate significant anti-myeloma effects, highlighting anti-cancer potential through degradation of key proteins.

Key Points

  • Degradation of key proteins leads to reduced myeloma cell proliferation and improved tumor response.
  • At 30mg/kg, OPN-5667 achieved 117% tumor growth inhibition in murine models of multiple myeloma.
  • Assessment using high throughput profiling confirmed targeted protein degradation and downregulation of IRF4 and MYC.
  • This polypharmacology approach suggests novel therapies could inhibit multiple oncogenic pathways in cancer cells.

Cite This Study

Ataca et al. (2025) studied this question.

synapsesocial.com/papers/69362f514fa91c937236d955https://doi.org/10.1182/blood-2025-573
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1P300/CBP acetyltransferase inhibition and degradation disrupt oncogenic transcriptional programs and reveal epigenetic vulnerabilities in multiple myeloma2025
  2. 2Discovery of Novel Potent Triple IKZF1/2/3 Degraders for the Treatment of Hematological Cancers2025 · 1 citations
  3. 3Deciphering the role of EP300 in maintaining the enhancer landscape and lineage-specific epigenetic vulnerability in multiple myeloma2025
  4. 4EP31670, a dual-BET + p300 inhibitor, demonstrates pre-clinical efficacy, including in combination with JAK inhibition, in the hMPLW515L adoptive transfer model of myelofibrosis (MF)2025 · 2 citations
  5. 5Preclinical activity of investigational menin inhibitor DSP-5336 (Enzomenib)-based combinations against MLL1-rearranged (MLL-r) or mutant-NPM1 AML models2025 · 1 citations