Linker residues regulate the activity and stability of hexokinase 2, a promising anticancer target.

ABSTRACT: Hexokinase (HK) catalyzes the first step in glucose metabolism, making it an exciting target for the inhibition of tumor initiation and progression due to their elevated glucose metabolism. The upregulation of hexokinase-2 (HK2) in many cancers and its limited expression in normal tissues make it a particularly attractive target for the selective inhibition of cancer growth and the eradication of tumors with limited side effects. The design of such safe and effective anticancer therapeutics requires the development of HK2-specific inhibitors that will not interfere with other HK isozymes. As HK2 is unique among HKs in having a catalytically active N-terminal domain (NTD), we have focused our attention on this region. We previously found that NTD activity is affected by the size of the link

SUBMITTER: Ferreira JC 

PROVIDER: S-EPMC7949118 | biostudies-literature | 2021 Jan-Jun

REPOSITORIES: biostudies-literature