RIPTACs: A groundbreaking approach to drug discovery.

Proteins / metabolism Drug Discovery
RIPTACs bifunctional molecules cancer therapy effector protein (EP) protein–protein interactions (PPIs) target protein (TP) ternary complex

Journal

Drug discovery today
ISSN: 1878-5832
Titre abrégé: Drug Discov Today
Pays: England
ID NLM: 9604391

Informations de publication

Date de publication:
Nov 2023
Historique:
received: 25 07 2023
revised: 04 09 2023
accepted: 14 09 2023
medline: 20 11 2023
pubmed: 22 9 2023
entrez: 21 9 2023
Statut: ppublish

Résumé

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.

Identifiants

DOI: 10.1016/j.drudis.2023.103774 PMID: 37734702
pubmed: 37734702
pii: S1359-6446(23)00290-8
doi: 10.1016/j.drudis.2023.103774
pii:
doi:

Substances chimiques

Proteins 0

Types de publication

Journal Article Review

Langues

eng

Sous-ensembles de citation

IM

Pagination

103774

Informations de copyright

Copyright © 2023 Elsevier Ltd. All rights reserved.

Auteurs

Zonghui Ma (Z)

Chemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch (UTMB), Galveston, TX 77555, USA.

Andrew A Bolinger (AA)

Chemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch (UTMB), Galveston, TX 77555, USA.

Jia Zhou (J)

Chemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch (UTMB), Galveston, TX 77555, USA. Electronic address: jizhou@utmb.edu.

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Classifications MeSH

questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › RIPTACs: A groundbreaking approach to drug discovery.
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › RIPTACs: A groundbreaking approach to drug discovery.