Binding is not enough: flexibility is needed for photocrosslinking of Lck kinase by benzophenone photoligands.

ABSTRACT: Benzophenone photophores are employed widely for photoaffinity-labeling studies. Photolabeling with benzophenone, however, is hardly a routine experiment. Even when a photoprobe binds to its target, photocrosslinking does not necessarily occur. This is because photolabeling by benzophenone is affected by many factors other than target-binding, such as conformational flexibility of photoligand. Despite the widespread recognition of such complications, there has been no systematic study to assess the relative importance of individual factors that can affect photolabeling efficiency. In order to gain an insight into this problem, we conducted a structure-activity relationship (SAR) study of benzophenone photoligands for Lck kinase, in which photoligands with varying target-binding affinity an

SUBMITTER: Kawamura A 

PROVIDER: S-EPMC2581794 | biostudies-literature | 2008 Oct

REPOSITORIES: biostudies-literature