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Probing cancer with small-molecule tools-Progress and challenges
Susanne Müller1, Domenico Sanfelice2, Paul Workman2
1Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences, Johann Wolfgang Goethe-University, Max-von-Laue-Straße 15, 60438 Frankfurt am Main, Germany; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, UK; Chemical Probes Portal, www.chemicalprobes.org.
Chemical probes are essential small molecules for cancer research, aiding in understanding protein function and drug discovery. Further advancements are needed to ensure high-quality probes for all human proteins.
Area of Science:
- Chemical biology
- Cancer research
- Drug discovery
Background:
- Chemical probes are versatile small-molecule tools used in fundamental and translational cancer research.
- They complement genetic technologies for protein function annotation and are crucial for target validation and drug discovery.
Purpose of the Study:
- To review progress in chemical probe development over the last decade.
- To identify key challenges and propose solutions for improving chemical probe selection and utilization.
- To outline a strategy for creating high-quality chemical probes for all human proteins.
Main Methods:
- Literature review of advancements in chemical probe development.
- Analysis of current best practices and limitations in chemical probe usage.
- Discussion of strategies for future chemical probe generation.
Main Results:
- Significant progress has been made in chemical probe development over the past ten years.
- Key issues hindering optimal use and selection of chemical probes have been identified.
- A potential pathway for generating a high-quality chemical probe for every human protein has been proposed.
Conclusions:
- Chemical probes remain indispensable tools in cancer research and drug discovery.
- Improvements in selection and application are necessary to maximize their potential.
- A concerted effort is required to develop comprehensive chemical probe resources for the human proteome.
