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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Advances in Parallel Screening of Drug Candidates

Author(s): Paolo Bergese, Marina Cretich, Claudio Oldani, Giulio Oliviero, Gabriele Di Carlo, Laura E. Depero and Marcella Chiari

Volume 15, Issue 17, 2008

Page: [1706 - 1719] Pages: 14

DOI: 10.2174/092986708784872366

Price: $65


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

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