ReviewBioorganic & medicinal chemistry2012
Identification and validation of protein targets of bioactive small molecules.
Review in Bioorganic & medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
16 citing papers in PubMed.
- Recent advances in proteomic strategies for target identification of traditional Chinese medicine.Journal of pharmaceutical analysis · 2026Review
- Emerging Target Discovery Strategies Drive the Decoding of Therapeutic Power of Natural Products and Further Drug Development: A Case Study of Celastrol.Exploration (Beijing, China) · 2025Review
- Recent Advances in Pharmaceutical Design: Unleashing the Potential of Novel Therapeutics.Current pharmaceutical biotechnology · 2024Review
- An update of label-free protein target identification methods for natural active products.Theranostics · 2022Review
- Utilizing graph machine learning within drug discovery and development.Briefings in bioinformatics · 2021Article
- Systematically Studying the Effect of Small Molecules Interacting with RNA in Cellular and Preclinical Models.ACS chemical biology · 2021Review
- From genomes to molecular dynamics - A bottom up approach in extrication of SARS CoV-2 main protease inhibitors.Computational toxicology (Amsterdam, Netherlands) · 2021Article
- Novel fluorescent probes of 10-hydroxyevodiamine: autophagy and apoptosis-inducing anticancer mechanisms.Acta pharmaceutica Sinica. B · 2019Article
- Inhibition of Eukaryotic Translation by the Antitumor Natural Product Agelastatin A.Cell chemical biology · 2017Article
- Identification of Small Molecule-binding Proteins in a Native Cellular Environment by Live-cell Photoaffinity Labeling.Journal of visualized experiments : JoVE · 2016Article
- Design, synthesis and biological evaluation of photoaffinity probes of antiangiogenic homoisoflavonoids.Bioorganic & medicinal chemistry letters · 2016Article
- Sensitivity and engineered resistance of myeloid leukemia cells to BRD9 inhibition.Nature chemical biology · 2016Article
- Validation of the Target Protein of Insecticidal Dihydroagarofuran Sesquiterpene Polyesters.Toxins · 2016Article
- Antifungal drug itraconazole targets VDAC1 to modulate the AMPK/mTOR signaling axis in endothelial cells.Proceedings of the National Academy of Sciences of the United States of America · 2015Article
- DrugTargetSeqR: a genomics- and CRISPR-Cas9-based method to analyze drug targets.Nature chemical biology · 2014Article
- Identification of small molecule inhibitors of cytokinesis and single cell wound repair.Cytoskeleton (Hoboken, N.J.) · 2012Article
Corrections and comments
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Authors and funding
2 authors.
Funding
Abstract
Identification and validation of protein targets of bioactive small molecules is an important problem in chemical biology and drug discovery. Currently, no single method is satisfactory for this task. Here, we provide an overview of common methods for target identification and validation that historically were most successful. We have classified for the first time the existing methods into two distinct and complementary types, the 'top-down' and 'bottom-up' approaches. In a typical top-down approach, the cellular phenotype is used as a starting point and the molecular target is approached through systematic narrowing down of possibilities by taking advantage of the detailed existing knowledge of cellular pathways and processes. In contrast, the bottom-up approach entails the direct detection and identification of the molecular targets using affinity-based or genetic methods. A special emphasis is placed on target validation, including correlation analysis and genetic methods, as this area is often ignored despite its importance.
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Registered trials
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