RIPTACs: A groundbreaking approach to drug discovery

Zonghui Ma, Andrew A. Bolinger, Jia Zhou

Research output: Contribution to journalReview articlepeer-review

2 Scopus citations

Abstract

Regulated induced proximity targeting chimeras (RIPTACs), a new class of heterobifunctional molecules, show promise in specifically targeting and eliminating cancer cells while leaving healthy cells unharmed. As a groundbreaking drug discovery approach, RIPTACs work by forming a stable complex with two proteins, one specifically found in cancer cells (target protein, TP) and the other pan-essential for cell survival (effector protein, EP), selectively disrupting the function of the EP in cancer cells and causing cell death. Interestingly, the TPs need not be linked to disease progression, broadening the spectrum of potential drug targets. This review summarizes the discovery and recent advances of the RIPTAC strategy. Additionally, it discusses the associated opportunities and challenges as well as future perspectives in this field.

Original languageEnglish (US)
Article number103774
JournalDrug Discovery Today
Volume28
Issue number11
DOIs
StatePublished - Nov 2023

Keywords

  • RIPTACs
  • bifunctional molecules
  • cancer therapy
  • effector protein (EP)
  • protein–protein interactions (PPIs)
  • target protein (TP)
  • ternary complex

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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