Comprehensive survey of chemical libraries yielding enzyme inhibitors, receptor agonists and antagonists, and other biologically active agents: 1992 through 1997
- 1 January 1998
- journal article
- review article
- Published by Springer Nature in Molecular Diversity
- Vol. 3 (4) , 199-233
- https://doi.org/10.1023/a:1009699413828
Abstract
This review is a historical accounting of chemical libraries from which biologically active agents have been obtained. The comprehensive tabulation includes citations as early as 1992, when the first descriptions of biologically active libraries were disclosed, and continues through 1997. Four tables are provided listing libraries screened against (1) proteolytic enzymes, (2) non-proteolytic enzymes, (3) G-protein coupled receptors (GPCRs), and (4) other targets not classified in the first three tables (e.g., non-GPCRs, integrins, antiinfectives). A name, generic structure, and size is provided for each library citation, accompanied by the molecular screen and the structure and potency of the most active library member. In total, 86 libraries are presented with 60% of the contributions reported from pharmaceutical and biotechnology companies. Approximately 70% of the libraries have used α-amino acid synthons in their construction and 85% of the libraries include one or more amide bonds.Keywords
This publication has 50 references indexed in Scilit:
- Synthetic Peptide Combinatorial Libraries: A Method for the Identification of Bioactive Peptides Against Phytopathogenic FungiMolecular Plant-Microbe Interactions®, 1997
- Discovery of enzyme inhibitors through combinatorial chemistryMolecular Diversity, 1997
- Selection of a histidine-containing inhibitor of gelatinases through deconvolution of combinatorial tetrapeptide librariesMolecular Diversity, 1997
- ‘Targeted’ molecular diversity: design and development of non-peptide antagonists for cholecystokinin and tachykinin receptorsImmunopharmacology, 1996
- Deconvolution of Combinatorial Libraries for Drug Discovery: Experimental Comparison of Pooling StrategiesJournal of Medicinal Chemistry, 1996
- Synthesis of Potent Cyclic Hexapeptide NK-1 Antagonists. Use of a Minilibrary in Transforming a Peptidal Somatostatin Receptor Ligand into an NK-1 Receptor Ligand via a Polyvalent PeptidomimeticJournal of Medicinal Chemistry, 1996
- Multiple simultaneous synthesis of phenolic librariesMolecular Diversity, 1995
- Inhibitors of human heart chymase based on a peptide library.Proceedings of the National Academy of Sciences, 1995
- Discovery of Nanomolar Ligands for 7-Transmembrane G-Protein-Coupled Receptors from a Diverse N-(Substituted)glycine Peptoid LibraryJournal of Medicinal Chemistry, 1994
- The combinatorial synthesis and chemical and biological evaluation of a 1,4-benzodiazepine library.Proceedings of the National Academy of Sciences, 1994