Molecular Recognition of FDA-Approved Small Molecule Protein Kinase Drugs in Protein Kinases.

ABSTRACT: Protein kinases are key enzymes that catalyze the covalent phosphorylation of substrates via the transfer of the γ-phosphate of ATP, playing a crucial role in cellular proliferation, differentiation, and various cell regulatory processes. Due to their pivotal cellular role, the aberrant function of kinases has been associated with cancers and many other diseases. Consequently, competitive inhibition of the ATP binding site of protein kinases has emerged as an effective means of curing these diseases. Decades of intense development of protein kinase inhibitors (PKIs) resulted in 71 FDA-approved PKI drugs that target dozens of protein kinases for the treatment of various diseases. How do FDA-approved protein kinase inhibitor PKI drugs compete with ATP in their own binding pocket? This is the

SUBMITTER: Zhu Y 

PROVIDER: S-EPMC9611543 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature