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Updated: Sep 23, 2026

A Semi-Quantitative Drug Affinity Responsive Target Stability (DARTS) assay for studying Rapamycin/mTOR interaction
Published on: August 27, 2019
The evolving landscape of drug targets
Liliana Halip1, Sorin Avram2, John P Overington3
1Department of Computational Chemistry, Romanian Academy, 'Coriolan Drăgulescu' Institute of Chemistry Timișoara, Timișoara, Romania.
Abstract:
Since the turn of the century, drug discovery has been transformed by advances in genetics, genomics and proteomics, as well as automation, data science and the diversification of therapeutic modalities beyond synthetic small molecules and natural product derivatives. This transformation has led to the expansion of the drug target landscape, enabling advances in the treatment of many diseases, including some that previously lacked pharmacotherapies. In this Review, we map and quantify key elements of these changes over the past 25 years, such as trends in the number and type of targets through which drugs mediate their therapeutic effects, which now include 686 biomolecules modulated by 1,702 drugs. We also discuss trends we believe will continue or change, as target druggability continues to evolve with the emergence of new therapeutic modalities.
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