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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...
Autores principales: | Chung, Suhman, Parker, Jared B., Bianchet, Mario, Amzel, L. Mario, Stivers, James T. |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
2009
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3178264/ https://www.ncbi.nlm.nih.gov/pubmed/19396178 http://dx.doi.org/10.1038/nchembio.163 |
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