Department of Biomedical Sciences, University of Padova, Padova, Italy.
Department of Biomedical Sciences, University of Padova, Padova, Italy; CNR Neuroscience Institute, Padova, Italy.
Adv Protein Chem Struct Biol. 2021;124:23-46. doi: 10.1016/bs.apcsb.2020.09.003. Epub 2021 Jan 9.
CK2 is a constitutively active Ser/Thr protein kinase which phosphorylates hundreds of substrates. Since they are primarily related to survival and proliferation pathways, the best-known pathological roles of CK2 are in cancer, where its targeting is currently being considered as a possible therapy. However, CK2 activity has been found instrumental in many other human pathologies, and its inhibition will expectably be extended to different purposes in the near future. Here, after a description of CK2 features and implications in diseases, we analyze the different inhibitors and strategies available to target CK2, and update the results so far obtained by their in vivo application.
CK2 是一种组成型激活的丝氨酸/苏氨酸蛋白激酶，可磷酸化数百种底物。由于它们主要与生存和增殖途径有关，因此 CK2 的最著名的病理作用是在癌症中，目前正在考虑将其作为一种可能的治疗方法。然而，CK2 的活性在许多其他人类疾病中也起到了重要作用，预计在不久的将来，其抑制剂将被用于不同的目的。在这里，在描述了 CK2 在疾病中的特征和意义之后，我们分析了针对 CK2 的不同抑制剂和策略，并更新了迄今为止通过其体内应用获得的结果。
