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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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Detalhes bibliográficos
Main Authors: Chung, Suhman, Parker, Jared B., Bianchet, Mario, Amzel, L. Mario, Stivers, James T.
Formato: Artigo
Idioma:Inglês
Publicado em: 2009
Assuntos:
Acesso em linha: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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