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.

Advances in parallel screening of drug candidates / B. Paolo, M. Cretich, C. Oldani, O. Giulio, G. di Carlo, D. Laura E., C. Marcella. - In: CURRENT MEDICINAL CHEMISTRY. - ISSN 0929-8673. - 15:17(2008), pp. 1706-1719.

Advances in parallel screening of drug candidates

C. Oldani;G. di Carlo;
2008

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.
detection; drug; drug discovery; high throughput screening; lead; small molecule microarrays; molecular medicine; pharmacology
Settore BIO/11 - Biologia Molecolare
Settore CHIM/03 - Chimica Generale e Inorganica
2008
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/540660
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