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A structural biology view of target drugability.
Egner, Ursula; Hillig, Roman C.
Afiliación
  • Egner U; Head of Structural Biology Bayer Schering Pharma AG, Lead Discovery Berlin - Structural Biology, 13342 Berlin, Germany +49 30 46811522 ; +49 30 46891522 ; Ursula.Egner@bayerhealthcare.com.
Expert Opin Drug Discov ; 3(4): 391-401, 2008 Apr.
Article en En | MEDLINE | ID: mdl-23489095
BACKGROUND: With long and costly drug development times there is a need in the pharmaceutical industry to prioritize targets early in the drug discovery process. One of the possible criteria is 'protein drugability', a term with multiple understandings in the literature. Among others, it is the likelihood of finding a selective, low-molecular weight molecule that binds with high affinity to the target. OBJECTIVE: Which methods are available for drugability prediction? What can be achieved by such predictions and how can they influence the target prioritization process? METHODS: The main focus is on sequence- and structure-related computational methods for drugability prediction, giving an overview on their background as well as their bias and limitations with an emphasis on the structural biology point of view. RESULTS/CONCLUSION: Structural drugability assessment presents one criterion for prioritization of a target portfolio by enabling classification of targets into low, average, or high drugability.

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Tipo de estudio: Prognostic_studies Idioma: En Revista: Expert Opin Drug Discov Año: 2008 Tipo del documento: Article Pais de publicación: Reino Unido

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Tipo de estudio: Prognostic_studies Idioma: En Revista: Expert Opin Drug Discov Año: 2008 Tipo del documento: Article Pais de publicación: Reino Unido