Loading...
Please wait, while we are loading the content...
Similar Documents
DNA display of fragment pairs as a tool for the discovery of novel biologically active small molecules† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c4sc01654h
| Content Provider | Semantic Scholar |
|---|---|
| Author | Daguer, J.-P. Zambaldo, Claudio Ciobanu, Madalina G. Morieux, P. Barluenga, Sofia Winssinger, Nicolas |
| Copyright Year | 2015 |
| Abstract | Fragment-based lead discovery has proven to be a powerful method in the drug discovery process. The combinatorial output that is accessible by combining fragments is very attractive; however, identifying fragment pairs that bind synergistically and linking them productively can be challenging. Several technologies have now been established to prepare and screen nucleic acid-encoded libraries (ssDNA, dsDNA, PNA), and it has been shown that pairs of molecules combined by hybridization can bind synergistically to a target. Herein we apply this concept to combinatorially pair two libraries of small molecule fragments, use the fittest fragments supplemented with closely related analogs to build a focused library covalently linking the fragments with different spacers, and apply this strategy to the discovery of a potent ligand for Hsp70. |
| Starting Page | 739 |
| Ending Page | 744 |
| Page Count | 6 |
| File Format | PDF HTM / HTML |
| DOI | 10.1039/c4sc01654h |
| PubMed reference number | 30154995 |
| Journal | Medline |
| Volume Number | 6 |
| Alternate Webpage(s) | https://pubs.rsc.org/en/content/articlepdf/2015/sc/c4sc01654h |
| Alternate Webpage(s) | https://doi.org/10.1039/c4sc01654h |
| Journal | Chemical science |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |
