Abstract
In the hit to lead process, a drug candidate is selected from a set of potential leads by screening its binding with potential targets. This review focuses on the lead identification assays that employ a bio-chemical or bio-physical test to detect molecular recognition events between proteins and small molecules in a parallel format.These tests require either the lead or the target immobilization followed by incubation with the set of potential interaction partners and detection of a signal related to the target-ligand binding. In the first part of the review the different detection strategies amenable for drug screening are discussed. In the second part, a review of immobilization approaches for leads or targets, allowing the parallel screening of arrays of molecules, is presented.
Keywords: Lead, drug, detection, drug discovery, high throughput screening, small molecule microarrays
Current Medicinal Chemistry
Title: Advances in Parallel Screening of Drug Candidates
Volume: 15 Issue: 17
Author(s): Paolo Bergese, Marina Cretich, Claudio Oldani, Giulio Oliviero, Gabriele Di Carlo, Laura E. Depero and Marcella Chiari
Affiliation:
Keywords: Lead, drug, detection, drug discovery, high throughput screening, small molecule microarrays
Abstract: In the hit to lead process, a drug candidate is selected from a set of potential leads by screening its binding with potential targets. This review focuses on the lead identification assays that employ a bio-chemical or bio-physical test to detect molecular recognition events between proteins and small molecules in a parallel format.These tests require either the lead or the target immobilization followed by incubation with the set of potential interaction partners and detection of a signal related to the target-ligand binding. In the first part of the review the different detection strategies amenable for drug screening are discussed. In the second part, a review of immobilization approaches for leads or targets, allowing the parallel screening of arrays of molecules, is presented.
Export Options
About this article
Cite this article as:
Bergese Paolo, Cretich Marina, Oldani Claudio, Oliviero Giulio, Di Carlo Gabriele, Depero E. Laura and Chiari Marcella, Advances in Parallel Screening of Drug Candidates, Current Medicinal Chemistry 2008; 15 (17) . https://dx.doi.org/10.2174/092986708784872366
DOI https://dx.doi.org/10.2174/092986708784872366 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
Current advances in inherited cardiomyopathy
Describe in detail all novel advances in multimodality imaging related to inherited cardiomyopathy diagnosis and prognosis. Shed light to deeper phenotypic characterization. Acknowledge recent advances in genetics, genomics and precision medicineread more
- 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
-
New Developments in Peroxidation of Polyunsaturated Fatty Acids
Letters in Organic Chemistry Peptoids: Bio-Inspired Polymers as Potential Pharmaceuticals
Current Pharmaceutical Design Unleashing the Potential of Microbial Natural Products in Drug Discovery: Focusing on <i>Streptomyces</i> as Antimicrobials Goldmine
Current Topics in Medicinal Chemistry Sao Paulo Research Conference on Molecular Medicine and Pharmacogenetics, A Joint Meeting with the IUPHAR Sub-Committee on Pharmacogenetics and the Brazilian Pharmacogenetics Network, Sao Paulo, Brazil, September 18-20, 2008
Current Pharmacogenomics and Personalized Medicine Rapid Biosynthesis of Gold Nanoparticles Using Aqueous-ethanoic Leaf Extract of Heartleaf Moonseed: Characterization and Effect of pH on its Synthesis
Current Nanomaterials Damaged Proteins Bearing L-Isoaspartyl Residues and Aging: A Dynamic Equilibrium Between Generation of Isomerized Forms and Repair by PIMT
Current Aging Science Application of Poloxamers for the Development of Drug Delivery System to Treat Leishmaniasis: A Review
Current Drug Targets Neuroinflammation and its Modulation by Flavonoids
Endocrine, Metabolic & Immune Disorders - Drug Targets The Use of Major Analgesics in Patients with Renal Dysfunction
Current Drug Targets Interactions Between Proteins and Platinum-Containing Anti-Cancer Drugs
Mini-Reviews in Medicinal Chemistry Microwave Assisted Functionalization of Materials: from the Mesoscale to the Nanoscale
Current Organic Chemistry The Role of Thiols and Disulfides on Protein Stability
Current Protein & Peptide Science Growing Burden of Diabetes in Sub- Saharan Africa: Contribution of Pesticides ?
Current Diabetes Reviews Role of Antioxidants for the Treatment of Cardiovascular Diseases: Challenges and Opportunities
Current Pharmaceutical Design Synthesis, Cytotoxic Evaluation, Docking and QSAR Study of N-(4-Oxo- 2-(4-((5-Aryl-1,3,4-Thiadiazol-2-yl)Amino)Phenyl)Thiazolidin-3-yl) Benzamides as Antitubulin Agents
Current Topics in Medicinal Chemistry Towards Characteristics of Photodynamic Drugs Specifically Aimed at Microvascular Diseases
Mini-Reviews in Medicinal Chemistry Mechanisms and Treatment of Neuropathic Pain
Central Nervous System Agents in Medicinal Chemistry Application of Sugar-Base Anhydro Bridge for Modification of Nucleosides in the 2’- and/or 3’-Positions - Revisited
Current Organic Chemistry Antibody-Targeted Immunoliposomes for Cancer Treatment
Mini-Reviews in Medicinal Chemistry Polyethylene Glycol Acts as a Mechanistic Stabilizer of L-asparaginase: A Computational Probing
Medicinal Chemistry