一种抗革兰氏阳性致病菌新型靶酶——分选酶

许多革兰氏阳性菌的表面蛋白是经过一种被称为分选酶的半胱氨酸转肽酶的作用而锚定到细胞壁上,由于表面蛋白在病原菌的致病性方面起关键作用,分选酶有可能成为降低革兰氏阳性菌致病性的药物靶点.目前,通过对金黄色葡萄球菌中分选酶A(SrtA)的研究,已初步阐明分选酶的作用机制及其活性位点,与此同时,一些SrtA抑制剂的初步鉴定为今后抑制剂更深层次的筛选提供了基础.

Sortase: New Target Enzyme in Gram-positive Pathogens

Many surface proteins of Gram-positive bacteria are anchored to the cell wall by the action of sortase enzymes, a recently discovered family of cysteine transpeptidases. As the surface proteins of pathogens are frequently required for virulence, the sortase might be a suitable target for the development of anti-Gram-positive drugs. Recently, the mechanism and active sites of sortase was elucidated by the research of sortaseA(SrtA) in Staphylococcus aureus and a series of SrtA inhibitors have been identified for providing the basis for further development of potent inhibitors.