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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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Detalles Bibliográficos
Autores principales: Chung, Suhman, Parker, Jared B., Bianchet, Mario, Amzel, L. Mario, Stivers, James T.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: 2009
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