Al-Qadhi Mustafa A, Yahya Tawfeek A A, El-Nassan Hala B
Department of Medicinal Chemistry, Faculty of Pharmacy, Sana'a University, 18084 Sana'a, Yemen.
Department of Medicinal Chemistry, Faculty of Pharmacy, Sana'a University, 18084 Sana'a,Yemen.
ACS Omega. 2024 May 3;9(19):20702-20719. doi: 10.1021/acsomega.3c10478. eCollection 2024 May 14.
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.
CK2是一种重要的酶,它能使大量底物磷酸化,从而控制身体中的许多过程。在许多癌症类型中都报道了其上调情况。CK2抑制剂可能具有抗癌活性,目前有两种化合物正在进行临床试验。然而,这两种化合物都是ATP竞争性抑制剂,可能会有脱靶副作用。变构抑制剂和双重抑制剂的开发可以克服这一缺点。与ATP竞争性抑制剂相比,这些抑制剂对CK2酶表现出更高的选择性和特异性。本综述总结了过去五年在CK2抑制剂设计方面所做的努力。