Small Molecules targeted

Wintner, F.A., Moallemi, C.C. Quantized surface complementarity diversity (QSCD) a model based on small molecule-target complementarity. J. Med. Chem. 2000, 43, 1993-2006. 

Interestingly, given the discussion of the importance of understanding small molecule-target protein interactions early in drug discovery, there is renewed interest in reexamining many older drugs to more fully understand how they work [10]. 

Meli M, et al. Small-molecule targeting of heat shock protein 90 113. 

Henthorn DC, Jaxa-Chamiec AA, Meldmm E. A GAL4-based yeast three-hybrid system for the identification of small molecule-target protein interactions. Biochem. Pharmacol. 2002 63 1619-1628. 

Butcher RA, Bhullar BS, Perlstein EO, Marsischky G, LaBaer J, Schreiber SL. Microarray-based method for monitoring yeast overexpression strains reveals small-molecule targets in TOR pathway. Nat. Chem. Biol. 2006 2 103-109. 

V. Aberg, F. Almqvist, Pilicides—small molecules targeting bacterial virulence. OrganicBiomol. Chem. 5, 1827-1834 (2007)... 

When the target protein of a small molecule is determined, it goes under validation with a number of biophysical, biochemical, and biological experiments, such as forward-affinity binding assay, reverse-affinity binding assay, small molecule-target protein docking model, surface plasmon resonance (SPR)... 

This book offers you the contemporary knowledge and techniques necessary to understand the entire research field of chemical biology. New technologies to dissect the interactions between small molecules and proteins are introduced with some examples of the identification of binding proteins of small molecules. The final chapter will be useful to get a bird s-eye view of recent progress on small molecules targeting proteins. 

De Luca L, Ferro S, Gitto R et al (2010) Small molecules targeting the interaction between HIV-1 integrase and LEDGF/p75 cofactor. Bioorg Med Chem 18 7515-7521... 

Potential biologies (protein therapeutics), biologic targets (antibody targets), and small molecule targets ... 

The potential of small molecules targeting microtubules as cancer therapeutics was demonstrated by the vinca alkaloids, such as vincristine and vinblastine, which have been used in the clinic for 40 years. At high concentrations (10-100 nM), these compounds depolymerize microtubules, which eliminates the mitotic spindle. At lower concentrations that are used clinically, microtubules remain stable but microtubule dynamics are suppressed. Taxol, which also inhibits microtubule dynamics, is widely used to treat a variety of cancers (reviewed in Ref. [16]. These drugs induce a mitotic arrest, which eventually leads to cell death [17] through mechanisms that are only beginning to be understood [18,19, 20]. 

Gray, P.G. Schultz, F.A. Supek, Genome-wide overexpression screen in yeast for small-molecule target... 

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