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Impact of linker strain and flexibility in the design of a fragment-based inhibitor
The linking together of molecular fragments that bind to adjacent sites on an enzyme can lead to high affinity inhibitors. Ideally, this strategy would employ linkers that do not perturb the optimal binding geometries of the fragments and do not have excessive conformational flexibility that would i...
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| Autori principali: | , , , , |
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| Natura: | Artigo |
| Lingua: | Inglês |
| Pubblicazione: |
2009
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| Soggetti: | |
| Accesso online: | https://ncbi.nlm.nih.gov/pmc/articles/PMC3178264/ https://ncbi.nlm.nih.gov/pubmed/19396178 https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/nchembio.163 |
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