Department of Pharmaceutical Chemistry, Khalsa College of Pharmacy, Amritsar, Punjab 143002, India.
School of Pharmacy, College of Pharmacy, Taipei Medical University, 250 Wuxing Street, Taipei 11031, Taiwan.
Anticancer Agents Med Chem. 2022 Aug 4;22(15):2662-2670. doi: 10.2174/1871520622666220404081302.
Protein kinases are amongst the most focused enzymes in the current century to design, synthesize and formulate drugs that ought to be effective in the treatment of various disordered and diseased states involving either overexpression or deficiency situations. The ATP pocket on the kinases is the active binding site for most of the kinase inhibitors. However, the kinase mutations prevent the binding of kinase inhibitors to the ATP pocket. The enzyme becomes inactive even in the mutated state when the switch pocket site on the enzyme is occupied by switch pocket inhibitors. This review comprises detailed information regarding various classical protein kinases and switch pocket kinase inhibitors with their mechanism of action so that new molecules can be designed to encounter mutations in the kinase enzyme.
蛋白激酶是本世纪重点研究的酶之一，旨在设计、合成和制定药物，以有效治疗涉及过表达或缺乏情况的各种紊乱和疾病状态。激酶的 ATP 口袋是大多数激酶抑制剂的有效结合部位。然而，激酶突变会阻止激酶抑制剂与 ATP 口袋结合。当酶的开关口袋位点被开关口袋抑制剂占据时，即使在突变状态下，酶也会变得失活。本综述包含了各种经典蛋白激酶和开关口袋激酶抑制剂的详细信息及其作用机制，以便设计新的分子来应对激酶酶的突变。
