RIPTACs: A groundbreaking approach to drug discovery

  • Drug Discov Today. 2023 Nov;28(11):103774. doi: 10.1016/j.drudis.2023.103774.
Zonghui Ma  1 ,  Andrew A Bolinger  1 ,  Jia Zhou  2
Affiliations
  • 1. Chemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch (UTMB), Galveston, TX 77555, USA.
  • 2. Chemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch (UTMB), Galveston, TX 77555, USA. Electronic address: [email protected].
PMID: 37734702 DOI: 10.1016/j.drudis.2023.103774
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.

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