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A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction
Published on: August 27, 2019
How many drug targets are there?
John P Overington1, Bissan Al-Lazikani, Andrew L Hopkins
1Inpharmatica Ltd., 1 New Oxford Street, London, WC1A 1NU, UK. j.overington@inpharmatica.co.uk
This study reconciles debates on drug targets, proposing a consensus number for approved therapeutics. It highlights a steady rate of new target innovation but a slower pace for new target families, emphasizing polypharmacology and gene-family approaches.
Area of Science:
- Pharmacology and Drug Discovery
- Genomics and Bioinformatics
Background:
- The number of molecular targets for approved drugs has been a subject of ongoing debate.
- Previous reports on drug target numbers appear contradictory, necessitating a comprehensive survey.
Purpose of the Study:
- To reconcile conflicting data and establish a consensus number of current drug targets for all approved therapeutic drug classes.
- To analyze historical trends in drug target innovation and the development of drugs against new target families.
Main Methods:
- Comprehensive survey and reconciliation of previously published reports on drug targets.
- Analysis of historical rates of target innovation and development of drugs against new target families.
Main Results:
- A consensus number of current drug targets for approved therapeutic drugs is proposed.
- A relatively constant historical rate of target innovation (new drug targets launched) was observed.
- The rate of developing drugs against new target families is significantly lower than new target innovation.
- Recent approvals of protein kinase-targeting drugs highlight the importance of polypharmacology and gene-family-led approaches.
Conclusions:
- The study provides a unified perspective on the number of drug targets.
- Drug development shows consistent innovation in new targets but lags in exploring new target families.
- Polypharmacology and a gene-family-led strategy are powerful approaches for developing novel therapies.
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