Target, targets libraries

A Polmski, RD Eemstem, S Shi, A Kuki. LiBrain Software for automated design of exploratory and targeted combinatorial libraries. In IM Chaiken, KD Janda, eds. Molecular Diversity and Combinatorial Chemistry Libraries and Drug Discovery. ACS Conf Proc Ser. Washington, DC Am Chem Soc, 1996, pp 219-232. 

Centerpieces of combinatorial concepts include the synthesis of compound libraries instead of the preparation of single target compounds. Library synthesis is supplemented by approaches to optimize the diversity of a compound collection (diversity-oriented synthesis) and by efforts to create powerful interfaces between combinatorial synthesis and bioassays. 

Specific structural fragments of biologically active molecules can be used as the core elements for generating targeted libraries. The most straightfor-... 

Andrews KM, Cramer RD. Toward general methods of targeted library design topomer shape similarity searching with diverse structures as queries. / Med Chem 2000 43 1723-40. 

Rosania GR, Lee JW, Ding L, Yoon HS, Chang YT (2003) Combinatorial approach to organelle-targeted fluorescent library based on the styryl scaffold. J Am Chem Soc 125 1130-1131... 

This chapter will cover recent developments in the design of diverse and protein family-targeted libraries, their physicochemical properties, and contemporary methods for screening them. 

Mena, M. A., Treynor, T. P., Mayo, S. L. and Daugherty, P. S. (2006). Blue fluorescent proteins with enhanced brightness and photostability from a structurally targeted library. Nat. Biotechnol. 24, 1569-71. 

Keywords Combinatorial Chemistry m Solid-Phase Synthesis m Solid-Phase Scavenger m Linker m Targeted Library m Small Molecule Libraries... 

Targeted libraries have been most effective when based upon the display of diverse functionality about a minimal mechanism-based pharmacophore targeting an enzyme family. Early successes with this approach were first achieved with proteases.1221 Our own efforts to design libraries which target enzyme families require that the minimal pharmacophore serves as the site for attachment to solid support.1231 The pharmacophore is the only invariant part of the inhibitor structure, which... 

We have also developed targeted library approaches towards cysteine proteases, which are important pharmaceutical targets due to their role in the pathogenesis of many diseases.1251 A common feature of virtually all cysteine protease inhibitors is an electrophilic functionality, such as a carbonyl or a Michael acceptor, which can react with the nucleophilic active site cysteine residue. We specifi-... 

M. Whittaker, Discovery of Protease Inhibitors Using Targeted Libraries , Curr. Opin. Chem. Biol 1998, 2, 386-396. 

Tab. 18.1 Targeted combinatorial libraries and their associated recognition elements...

Targeted libraries are developed from knowledge of natural substrates or known inhibitors, which might venture to introduce some desirable physical properties [35]. 

Homann, M.J., Vail, R.B., Previte, E., Tamarez, M., Morgan, B., Dodds, D.R. and Zaks, A., Rapid identification of enantioselective ketone reductions using targeted microbial libraries. Tetrahedron, 2004, 60,12,9-191. 

Medium-sized/Target-class Libraries and Collections 181... 

---