Synapse
⌘+K
Synapse
PulseExploreJournal ClubResearchersJournals
Instagram
HomeJournal ClubExplore
April 5, 2026Cancer Research

Abstract 1828: Preclinical evaluation of selective and potent EP300 degraders demonstrates robust antitumor activity and favorable tolerability in hematologic malignancies.

View Full Paper
Ask AI
Bookmark
Share

Authors

MLMeiyun LinFoghorn Therapeutics (United States)WAWesley AustinFoghorn Therapeutics (United States)QZQianhe ZhuoFoghorn Therapeutics (United States)

Discussion

Loading...

Member takes

Overview

Preclinical evaluation reveals that selective EP300 degraders inhibit tumor growth in hematologic malignancies, suggesting a promising therapeutic strategy.

Key Points

  • This research aims to develop selective EP300 degraders to improve treatment outcomes in hematologic malignancies.
  • Developed heterobifunctional compounds for selective EP300 degradation.
  • Conducted in vitro assessments on various hematologic malignancies.
  • Performed xenograft studies to evaluate tumor growth inhibition in MM.1S models.
  • Analyzed pharmacokinetics and pharmacodynamics to correlate exposure and efficacy.
  • EP300 degraders showed robust, dose-dependent tumor growth inhibition.
  • Minimal impact on body weight and no adverse hematologic effects were observed.
  • Positive correlation was found between systemic exposure and EP300 degradation.
  • Demonstrated a favorable therapeutic window compared to dual CBP/EP300 inhibitors.

Cite This Study

Lin et al. (2026) studied this question.

synapsesocial.com/papers/69d1fd9ca79560c99a0a3c1dhttps://doi.org/10.1158/1538-7445.am2026-1828
View Full Paper
Ask AI
Bookmark
Share