ACS Omega · 2024 · 18 citations · 73 references
Life SciencesBiochemistryOncologyDrug DesignDrug DiscoveryEnzymologyAllosteric Drug DesignAllosteric RegulationEnzyme InhibitionEnzyme KineticsAllosteric Drug DiscoveryAllosteric InhibitionAllosteric Inhibition MechanismsAllosteric Kinase InhibitorsAnticancer ActivityKinase InhibitorsProtein Kinase InhibitorsSelectivity
CK2 is a vital enzyme that phosphorylates a large number of substrates and thereby controls many processes in the body. Its upregulation was reported in many cancer types. Inhibitors of CK2 might have anticancer activity, and two compounds are currently under clinical trials. However, both compounds are ATP-competitive inhibitors that may have off-target side effects. The development of allosteric and dual inhibitors can overcome this drawback. These inhibitors showed higher selectivity and specificity for the CK2 enzyme compared to the ATP-competitive inhibitors. The present review summarizes the efforts exerted in the last five years in the design of CK2 inhibitors.
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The Global Phosphorylation Landscape of SARS-CoV-2 Infection
Mehdi Bouhaddou, Danish Memon, Bjoern Meyer et al. · Cell · 2020 · 1.1K citations · Full text
Fabrice Pierre, Peter Chua, Sean O’Brien et al. · Journal of Medicinal Chemistry · 2010 · 299 citations · Full text