A structural biology view of target drugability.

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.