Fragment-based drug discovery using cryo-EM.
Drug Discov Today
; 25(3): 485-490, 2020 03.
Article
en En
| MEDLINE
| ID: mdl-31877353
ABSTRACT
Recent advances in electron cryo-microscopy (cryo-EM) structure determination have pushed the resolutions obtainable by the method into the range widely considered to be of utility for drug discovery. Here, we review the use of cryo-EM in fragment-based drug discovery (FBDD) based on in-house method development. We demonstrate not only that cryo-EM can reveal details of the molecular interactions between fragments and a protein, but also that the current reproducibility, quality, and throughput are compatible with FBDD. We exemplify this using the test system ß-galactosidase (Bgal) and the oncology target pyruvate kinase 2 (PKM2).
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Microscopía por Crioelectrón
/
Descubrimiento de Drogas
Límite:
Humans
Idioma:
En
Revista:
Drug Discov Today
Asunto de la revista:
FARMACOLOGIA
/
TERAPIA POR MEDICAMENTOS
Año:
2020
Tipo del documento:
Article
País de afiliación:
Reino Unido