Advances in parallel screening of drug candidates.
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.
Bergese
Paolo
P
Chemistry for Technologies Laboratory and INSTM, University of Brescia, Brescia, Italy.
Cretich
Marina
M
Oldani
Claudio
C
Oliviero
Giulio
G
Di Carlo
Gabriele
G
Depero
Laura E
LE
Chiari
Marcella
M
D004353:Drug Evaluation, Preclinical / Q000379:methods*; D046228:Microarray Analysis; D010777:Photochemistry; D013499:Surface Properties