Sensitized detection of inhibitory fragments and iterative development of non-peptidic protease inhibitors by dynamic ligation screening
| Autor: | Adeeb El-Dahshan, Albert Isidro-Llobet, Michael Lisurek, Marco F. Schmidt, Jörg Rademann, Jinzhi Tan, Rolf Hilgenfeld |
|---|---|
| Rok vydání: | 2008 |
| Předmět: |
medicine.medical_treatment
High-throughput screening Drug Evaluation Preclinical Ligands dynamic chemistry enzyme catalysis Catalysis high‐throughput screening medicinal chemistry medicine Combinatorial Chemistry Techniques Protease Inhibitors Ligation Iterative and incremental development Protease Chemistry Communication fungi General Chemistry Small molecule Combinatorial chemistry Chemical space Communications Coronavirus Peptide Hydrolases combinatorial chemistry |
| Zdroj: | Angewandte Chemie (International Ed. in English) |
| ISSN: | 1521-3773 |
| Popis: | Dedicated to Professor G"nther Jung on the occasion of his 70th birthdayT h e conventional approach to identify biologically active ,druglike small molecules is based on high-throughput screen-ing (HTS) of chemical libraries .However ,the composition oflarge chemical libraries and their screening are time-consum-ing and expensive endeavors ;the success relies heavily on thequality of the available libraries , and even the largest librarycan span only a minute section of the virtual chemical space .T herefore , over the past decade several strategies have beenproposed to facilitate the development process by using theprotein target as a template for ligand assembly . |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Plný text