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.
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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 |
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