MARK2 inhibitors belong to a class of compounds designed to selectively target and modulate the activity of the MARK2 enzyme, also known as microtubule affinity-regulating kinase 2. MARK2 is a serine/threonine protein kinase that plays a crucial role in regulating cellular processes such as cell division, polarity, and intracellular transport. As a member of the AMP-activated protein kinase (AMPK) family, MARK2 is involved in the phosphorylation of microtubule-associated proteins, contributing to the dynamic instability and organization of microtubules within the cytoskeleton.
MARK2 inhibitors involve the identification and synthesis of small molecules that can selectively bind to the active site of the enzyme, disrupting its catalytic function. These inhibitors often leverage the structural knowledge of the kinase domain of MARK2 to achieve specificity and potency. The chemical optimization of MARK2 inhibitors involves fine-tuning the molecular structure to enhance their binding affinity and pharmacokinetic properties, with the ultimate goal of providing valuable tools for probing the biological functions of MARK2 and potentially influencing disease-related cellular pathways.