The protein kinase CK1: Inhibition, activation, and possible allosteric modulation

被引:9
作者
Sunkari, Yashoda Krishna [1 ]
Meijer, Laurent [2 ]
Flajolet, Marc [1 ]
机构
[1] Rockefeller Univ, Lab Mol & Cellular Neurosci, New York, NY 10065 USA
[2] Perha Pharmaceut, Hotel Rech, Roscoff, France
关键词
casein kinase 1 (CK1); kinase inhibitor; allosteric; Alzheimer's disease (AD); Neurodegeneration; DNA-encoded library (DEL); STRUCTURAL BASIS; IN-VIVO; DELTA; PHOSPHORYLATION; DISCOVERY; FAMILY; POTENT; CASEIN-KINASE-1; TRAFFICKING; DERIVATIVES;
D O I
10.3389/fmolb.2022.916232
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Protein kinases play a vital role in biology and deregulation of kinases is implicated in numerous diseases ranging from cancer to neurodegenerative diseases, making them a major target class for the pharmaceutical industry. However, the high degree of conservation that exists between ATP-binding sites among kinases makes it difficult for current inhibitors to be highly specific. In the context of neurodegeneration, several groups including ours, have linked different kinases such as CK1 and Alzheimer's disease for example. Strictly CK1-isoform specific regulators do not exist and known CK1 inhibitors are inhibiting the enzymatic activity, targeting the ATP-binding site. Here we review compounds known to target CK1, as well as other inhibitory types that could benefit CK1. We introduce the DNA-encoded library (DEL) technology that might represent an interesting approach to uncover allosteric modulators instead of ATP competitors. Such a strategy, taking into account known allosteric inhibitors and mechanisms, might help designing modulators that are more specific towards a specific kinase, and in the case of CK1, toward specific isoforms.
引用
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页数:10
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