eEF2K inhibitor

eEF2K inhibitors are a class of research-stage small molecules designed to target eukaryotic elongation factor 2 kinase (eEF2K), also known as Ca2+/calmodulin-dependent protein kinase III (CAMKIII). eEF2K is an atypical α-kinase that regulates the elongation phase of protein synthesis by phosphorylating eEF2 at the threonine-56 residue, which leads to the inhibition of translation. This kinase is frequently overexpressed in various cancer types, including prostate and breast cancer, where it facilitates adaptation to cellular stressors such as hypoxia, nutrient deprivation, and acidosis. Consequently, eEF2K inhibitors are being investigated as potential oncology therapeutics, often in combination with other agents like anti-androgens or autophagy inhibitors, to overcome drug resistance and impair tumor survival mechanisms. Additionally, research is exploring their utility in neurodegenerative and cardiovascular conditions.

Other names

eukaryotic elongation factor 2 kinase inhibitorCa2+/calmodulin-dependent protein kinase III inhibitorCAMKIII inhibitor