Abstract
The availability of large collections of small-molecule inhibitors of protein interactions would bear a tremendous impact both on academic and therapeutic research. The past recent years have seen a marked acceleration in the discovery of protein interaction inhibitors, through structure-based drug design but mostly through screening efforts. This article attempts to review the impressive number and variety of in vitro and cellular screening assays that have been developed and, for most of them, used successfully to identify smallmolecule inhibitors of protein interactions. Various strategies aimed at improving hit rates are also reviewed, and future challenges to improve discovery success rates are discussed. The growing list of protein interaction inhibitors and the large arsenal of screening methods, now available to most laboratories or screening facilities, will probably convince an increasing number of academic and industrial scientists that protein interactions are more druggable than once feared, and that their respective research interests would greatly benefit from the discovery of protein interaction inhibitors.
Keywords: High-throughput screening, protein interactions, drug discovery, two-hybrid
Current Drug Discovery Technologies
Title: High-Throughput Screening Assays to Discover Small-Molecule Inhibitors of Protein Interactions
Volume: 5 Issue: 3
Author(s): Pierre Colas
Affiliation:
Keywords: High-throughput screening, protein interactions, drug discovery, two-hybrid
Abstract: The availability of large collections of small-molecule inhibitors of protein interactions would bear a tremendous impact both on academic and therapeutic research. The past recent years have seen a marked acceleration in the discovery of protein interaction inhibitors, through structure-based drug design but mostly through screening efforts. This article attempts to review the impressive number and variety of in vitro and cellular screening assays that have been developed and, for most of them, used successfully to identify smallmolecule inhibitors of protein interactions. Various strategies aimed at improving hit rates are also reviewed, and future challenges to improve discovery success rates are discussed. The growing list of protein interaction inhibitors and the large arsenal of screening methods, now available to most laboratories or screening facilities, will probably convince an increasing number of academic and industrial scientists that protein interactions are more druggable than once feared, and that their respective research interests would greatly benefit from the discovery of protein interaction inhibitors.
Export Options
About this article
Cite this article as:
Colas Pierre, High-Throughput Screening Assays to Discover Small-Molecule Inhibitors of Protein Interactions, Current Drug Discovery Technologies 2008; 5 (3) . https://dx.doi.org/10.2174/157016308785739875
DOI https://dx.doi.org/10.2174/157016308785739875 |
Print ISSN 1570-1638 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6220 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Synthesis and Anticancer Study of Novel 4H-Chromen Derivatives
Anti-Cancer Agents in Medicinal Chemistry Design, Synthesis and Mode of Action of Some New 2-(4'-aminophenyl) benzothiazole Derivatives as Potent Antimicrobial Agents
Letters in Drug Design & Discovery Near-Infrared Quantum Dots as Optical Probes for Tumor Imaging
Current Topics in Medicinal Chemistry Cutoff Values of D-Dimer and FDP in Plasma for the Diagnosis of Thrombosis
Vascular Disease Prevention (Discontinued) Self-immolative Linkers in Prodrugs and Antibody Drug Conjugates in Cancer Treatment
Recent Patents on Anti-Cancer Drug Discovery Rapid Fluorimetric Quantitation of Ibandronate by Coupling Quantum Dots and Multicommutated Flow Injection Analysis
Current Pharmaceutical Analysis Hydrogen Sulfide: A New Tool to Design and Develop Drugs
Clinical Anti-Inflammatory & Anti-Allergy Drugs (Discontinued) Prevention of Renal Complications Induced by Non- Steroidal Anti-Inflammatory Drugs
Current Medicinal Chemistry Rapid Biosynthesis of Gold Nanoparticles Using Aqueous-ethanoic Leaf Extract of Heartleaf Moonseed: Characterization and Effect of pH on its Synthesis
Current Nanomaterials Investigating Mitochondrial Dysfunction to Increase Drug Safety in the Pharmaceutical Industry
Current Drug Targets Renin-Angiotensin System in Central Nervous System Diseases and its Interaction with COVID-19
Current Medicinal Chemistry Eco-friendly Synthesis of Pyrido[2,3-d]pyrimidine Analogs and Their Anticancer and Tyrosine Kinase Inhibition Activities
Anti-Cancer Agents in Medicinal Chemistry Synthesis and Evaluation of Vascular Endothelial Growth Factor Receptor-2 Inhibitory Activity of 6,7-Dimethoxycinnoline Derivatives
Letters in Drug Design & Discovery Biophysical Characterization of Antimicrobial Peptides Activity: From In Vitro to Ex Vivo Techniques
Current Protein & Peptide Science Optimization of CDTE Quantum Dots Synthesis Using Capillary Zone Electrophoresis
Current Nanoscience Preparation, characterization and <i>in vitro</i> release of zein-pectin capsules for target delivery
Current Drug Delivery Protein Homeostasis as a Therapeutic Target for Diseases of Protein Conformation
Current Topics in Medicinal Chemistry Recent Highlights on Molecular Hybrids Potentially Useful in Central Nervous System Disorders
Mini-Reviews in Medicinal Chemistry Potentials of Hydrogels in Cancer Therapy
Current Cancer Therapy Reviews Review on Triggered Liposomal Drug Delivery with a Focus on Ultrasound
Current Cancer Drug Targets