Kinase Targeted Anticancer Agents: A Perspective

Shannelle Diana Habániková, Rubina Dad, Chandra S Azad
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Abstract

The phosphate group present in the ATP (adenosine triphosphate) is transferred to the hydroxy group-containing tyrosine, serine, or threonine residue by the protein kinases encoded in the human genome. Till now, a large number of these kinases have been reported to be associated with the initiation and progression of human cancers. In clinical trials, it has been demonstrated that small-molecule kinase inhibitors can effectively cure a wide range of cancers. The FDA approved more than 40 kinase inhibitors for cancer treatment since the early 1980s when the first protein kinase inhibitor was developed. In this review, the authors explained the relevancies of the kinase with cancer. In addition, several FDA-approved drug candidates have been classified according to their binding with kinases.
激酶靶向抗癌药物的研究进展
存在于ATP(三磷酸腺苷)中的磷酸基团通过人类基因组编码的蛋白激酶转移到含有酪氨酸、丝氨酸或苏氨酸残基的羟基上。到目前为止,大量这些激酶已被报道与人类癌症的发生和发展有关。在临床试验中,已经证明小分子激酶抑制剂可以有效地治愈多种癌症。自20世纪80年代初第一个蛋白激酶抑制剂被开发出来以来,FDA批准了40多种用于癌症治疗的激酶抑制剂。在这篇综述中,作者解释了激酶与癌症的相关性。此外,一些fda批准的候选药物已根据其与激酶的结合进行分类。
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