Synthetic small molecule

Kuner, R, Bohrmann, B., Tjemberg, L.O., Naslund, ]., Huber, G., Celenk, S., Gruninger-Leitch, F., Richards, J.G., Jakob-Roetne, R., Kemp, J.A., and Nordstedt, C., Controlling polymerization of beta-amyloid and prion-derived peptides with synthetic small molecule ligands, /. Biol. Chem., 275,1673,2000. 

These catalysts, their structures, modes of action, and uses, are discussed in the rest of the book. Both synthetic small-molecule catalysts as well as some of Nature s finest enzymes are discussed and the role of hydrogen bonding in catalysis is described in detail. 

Modern anti-infective chemotherapy is founded on the deployment of an arsenal of potent and safe small-molecule inhihitors of microbial growth. As a result, it is not an understatement to say that antibiotics and antibacterial agents have revolutionized health care during the last century. These compounds are, respectively, natural product and synthetic small molecules that inhibit bacterial growth. For simplicity, in this review, the term antibiotic will be used to refer to both natural products and synthetic molecules. 

Ding S, Wu TYH, Brinker A, Peters EC, Hur W, Gray NS, Schnltz PG. Synthetic small molecules that control stem cell fate. Proc. Natl. Acad. Sci. 2003 100 7632-7637. 

Transition-state inhibitors stably mimic the transition state of the enzymatic reaction, and thereby interact with the substrate-bin-ding and catalytic machinery of the enzyme in a low-energy conformation. Transition-state analogs are competitive, reversible inhibitors, although some have extremely low Kj s and very slow off-rates. All proteases activate a nucleophile to attack a carbonyl, which leads to the formation of a tetrahedral intermediate that then collapses to form the enzyme products—two peptides. Thus, synthetic small molecules that mimic the tetrahedral intermediate of the protease reaction are attractive transition-state analogs. A classic class of protease transition-state inhibitors uses a boronic acid scaffold (4, 10). Boronic acid adopts a stable tetrahedral conformation in the protease active site that is resistant to nucleophilic attack. Boronic acid inhibitors, which are derivatized with different specificity elements, have been developed against every class of protease... 

Warashina M, et al. A synthetic small molecule that induces... 

Banaszynski LA, Chen LC, Maynard-Smith LA, Ooi AG, Wandless TJ. A rapid, reversible, and tunable method to regulate protein function in living cells using synthetic small molecules. Cell 2006 126 995-1004. 

TABLE 2 Information Contained in a Typical Specification for a Synthetic Small Molecule... 

Lundgren K et al (2009) BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90. Mol Cancer Ther 8(4) 921-929... 

SYNTHETIC SMALL MOLECULES OF DIFFERENT STRUCTURE TARGETING BINDING SITES DISTINCT FROM THAT OF COLCHICINOIDS... 

Fig. 8 Synthetic Small Molecules of Different Structures Targeting Various Binding Sites...

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