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Rapid experimental SAD phasing and hot-spot identification with halogenated fragments

Through X-ray crystallographic fragment screening, 4-bromopyrazole was discovered to be a ‘magic bullet’ that is capable of binding at many of the ligand ‘hot spots’ found in HIV-1 reverse transcriptase (RT). The binding locations can be in pockets that are ‘hidden’ in the unliganded crystal form, a...

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Detalles Bibliográficos
Autores principales: Bauman, Joseph D., Harrison, Jerry Joe E. K., Arnold, Eddy
Formato: Online Artículo Texto
Lenguaje:English
Publicado: International Union of Crystallography 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4704079/
https://www.ncbi.nlm.nih.gov/pubmed/26870381
http://dx.doi.org/10.1107/S2052252515021259