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February 23, 2026Journal of Medicinal ChemistryOpen Access

Orally Bioavailable Cyclin A/B RxL Inhibitors: Optimization of a Novel Class of Macrocyclic Peptides That Target E2F-High and G1–S-Checkpoint-Compromised Cancers

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Authors

JSJustin A. ShapiroNDNathan J. DupperBFBreena Fraga-Walton

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Overview

Findings demonstrate tumor regression in cancer models with a new lead compound, suggesting effective oral bioavailability.

Key Points

  • The study aims to optimize macrocyclic peptides targeting Cyclin A/B for treating specific cancers.
  • Optimized macrocyclic peptides for drug-like properties and oral bioavailability.
  • Conducted tumor regression assessments in cell-line-derived xenograft models.
  • Evaluated the lead compound in Phase 1 clinical trial for efficacy.
  • Identified a lead compound demonstrating significant tumor regression in cancer models.
  • Achieved improved oral bioavailability for the optimized macrocyclic peptides.

Cite This Study

Shapiro et al. (2026) studied this question.

synapsesocial.com/papers/699ba07072792ae9fd870218https://doi.org/10.1021/acs.jmedchem.5c02445
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