title: Receptor-assisted combinatorial chemistry: thermodynamics and kinetics in drug discovery.
abstract: Current drug discovery using combinatorial chemistry involves synthesis followed by screening, but emerging methods involve receptor-assistance to combine these steps. Adding stoichiometric amounts of receptor during library synthesis alters the kinetics or thermodynamics of the synthesis in a way that identifies the best-binding library members. Three main methods have emerged thus far in receptor-assisted combinatorial chemistry: dynamic combinatorial libraries, receptor-accelerated synthesis, and a new method, pseudo-dynamic libraries. Pseudo-dynamic libraries apply both thermodynamics and kinetics to amplify library members to easily observable levels, and attain selectivity heretofore unseen in receptor-assisted systems.
authors.affiliation: Department of Chemistry, McGill University, 801 Sherbrooke W., Montréal, QC H3A 2K6, Canada.
authors.forename: Jeremy D
authors.initials: JD
authors.lastname: Cheeseman
authors.forename: Andrew D
authors.initials: AD
authors.lastname: Corbett
authors.forename: James L
authors.initials: JL
authors.lastname: Gleason
authors.forename: Romas J
authors.initials: RJ
authors.lastname: Kazlauskas
mesh_terms: D020650:Combinatorial Chemistry Techniques / Q000379:methods; D015195:Drug Design; D007700:Kinetics; D008968:Molecular Conformation; D019151:Peptide Library; D011955:Receptors, Drug / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013816:Thermodynamics
chemical_list: D019151:Peptide Library; D011955:Receptors, Drug