Mechanistic insight into impact of phosphorylation on the enzymatic steps of farnesyltransferase.

ABSTRACT: Farnesyltransferase (FTase) is a heterodimeric enzyme, which catalyzes covalent attachment of the farnesyl group to target proteins, thus coordinating their trafficking in the cell. FTase has been demonstrated to be highly expressed in cancer and neurological diseases; hence considered as a hot target for therapeutic purposes. However, due to the nonspecific inhibition, there has been only one inhibitor that could be translated into the clinic. Importantly, it has been shown that phosphorylation of the α-subunit of FTase increases the activity of the enzyme in certain diseases. As such, understanding the impact of phosphorylation on dynamics of FTase provides a basis for targeting a specific state of the enzyme that emerges under pathological conditions. To this end, we performed 18 μs mol

SUBMITTER: Pekel H 

PROVIDER: S-EPMC9601885 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature