Open resources for chemical probes and their implications for future drug discovery

  • Introduction: The rational development of new therapeutics requires a thorough understanding of how aberrant signalling affects cellular homeostasis and causes human disease. Chemical probes are tool compounds with well-defined mechanism-of-action enabling modulation of, for example, domain-specific protein properties in a temporal manner, thereby complementing other target validation methods such as genetic gain- and loss-of-function approaches. Areas covered: In this review, the authors summarize recent advances in chemical probe development for emerging target classes such as solute carriers and ubiquitin-related targets and highlight open resources to inform and facilitate chemical probe discovery as well as tool compound selection for target validation and phenotypic screening. Expert opinion: Chemical probes are powerful tools for drug discovery that have led to fundamental insights into biological processes and have paved the way for the development of first-in-class drugs. Open resources can inform on various aspects of chemical probe development and provide access to data and recommendations on use of chemical probes to catalyse collaborative science and help accelerate drug target identification and validation.

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Author:Esra Balıkçı, Anne-Sophie M. C. Marques, Jesper S. HansenORCiDGND, Kilian HuberORCiDGND
Pubmed Id:
Parent Title (English):Expert opinion on drug discovery
Publisher:Taylor & Francis Group
Place of publication:Abingdon
Document Type:Article
Date of Publication (online):2023/04/16
Date of first Publication:2023/04/16
Publishing Institution:Universitätsbibliothek Johann Christian Senckenberg
Release Date:2023/07/17
Tag:Chemical probes; drug discovery; open science; solute carriers; targeted protein degradation; ubiquitination
Page Number:10
First Page:505
Last Page:513
This project received funding from the Innovative Medicines Initiative 2 Joint Undertaking (JU) under grant agreement No 875510. The JU receives support from the European Union’s Horizon 2020 research and innovation program, the European Federation of Pharmaceutical Industries and Associations (EFPIA), the Ontario Institute for Cancer Research, the Royal Institution for the Advancement of Learning McGill University, the KTH Royal Institute of Technology (Kungliga Tekniska Hoegskolan) and Diamond Light Source Limited.
Dewey Decimal Classification:5 Naturwissenschaften und Mathematik / 57 Biowissenschaften; Biologie / 570 Biowissenschaften; Biologie
Licence (German):License LogoCreative Commons - CC BY-NC-ND - Namensnennung - Nicht kommerziell - Keine Bearbeitungen 4.0 International