Cozza Giorgio, Bortolato Andrea, Menta Ernesto, Cavalletti Ennio, Spinelli Silvano, Moro Stefano
Dipartimento di Scienze Farmaceutiche, Università di Padova, Padova, Italy.
Anticancer Agents Med Chem. 2009 Sep;9(7):778-86. doi: 10.2174/187152009789056930.
Protein kinases are one of the largest known families of enzyme characterized by having a well conserved ATP binding pocket. Most of the synthetic kinase inhibitors are ATP-competitive, but display some potential problems, like selectivity, discrepancy between the in vitro and in vivo inhibition assays and an high risk of developing mutation inside the ATP-binding pocket. Recently some new inhibitors with a non-competitive mechanism of action were reported, with interesting results both in vitro and in vivo.
蛋白激酶是已知最大的酶家族之一，其特征在于具有高度保守的ATP结合口袋。大多数合成激酶抑制剂是ATP竞争性的，但存在一些潜在问题，如选择性、体外和体内抑制试验之间的差异以及ATP结合口袋内发生突变的高风险。最近报道了一些具有非竞争性作用机制的新型抑制剂，在体外和体内均产生了有趣的结果。
