Using Protein-Confined Proximity To Determine Chemical Reactivity.

ABSTRACT: Chemical reactivity is essential for functional modification of biomolecules with small molecules and the development of covalent drugs. The reactivity between a chemical functional group of a small molecule and that of a large biomolecule cannot be reliably predicted from the reactivity of the corresponding functional groups separately installed on two small molecules, because the proximity effect on reactivity resulting from the binding of the small molecule to the biomolecule is challenging to achieve by mixing two small molecules. Here we present a new strategy to determine the chemical reactivity of two functional groups in the context of close proximity afforded by proteins. The functional groups to be tested were separately installed at the interface of two interacting proteins in t

SUBMITTER: Kobayashi T 

PROVIDER: S-EPMC5310709 | biostudies-literature | 2016 Nov

REPOSITORIES: biostudies-literature