Kinetic target-guided synthesis in drug discovery and chemical biology: a comprehensive facts and figures survey
| Autor: | Benoit Deprez, Jouda Jakhlal, Damien Bosc, Rebecca Deprez-Poulain |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
Pharmacology
Alternative methods Scope (project management) 010405 organic chemistry Drug discovery Chemical biology Proteins Success factors Nanotechnology Biology Ligands 010402 general chemistry 01 natural sciences 0104 chemical sciences Kinetics Pharmaceutical Preparations Surveys and Questionnaires Drug Discovery Humans Molecular Medicine Click Chemistry Biochemical engineering |
| Zdroj: | Future Medicinal Chemistry. 8:381-404 |
| ISSN: | 1756-8927 1756-8919 |
| DOI: | 10.4155/fmc-2015-0007 |
| Popis: | For the last 15 years, kinetic target-guided syntheses, including in situ click chemistry, have been used as alternative methods to find ligands to therapeutically relevant proteins. In this review, a comprehensive survey of biological targets used in kinetic target-guided synthesis covers historical and recent examples. The chemical reactions employed and practical aspects, including controls, library sizes and product detection, are presented. A particular focus is on the reagents and warhead selection and design with a critical overview of the challenges encountered. As protein supply remains a key success factor, it appears that increased efforts should be taken toward miniaturization in order to expand the scope of this strategy and qualify it as a fully fledged drug discovery tool. |
| Databáze: | OpenAIRE |
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