Ultra high resolution Xray crystallographic study for antibiotic mechanisms of action and resistance

碳青霉烯类抗生素是最重要的抗生素之一，在世界范围内被用作“最后的避难所”。基于X射线结晶学，我们研究了碳青霉烯类抗生素对β-内酰胺酶的抑制机制。(1)碳青霉烯类抗生素对C类β-内酰胺酶的抑制机制。(2)洋葱伯克霍尔德氏菌(Peni)和假鼻疽伯克霍尔德氏菌(Pena)产β-内酰胺酶的晶体结构。(3)Pena碳青霉烯酶-阿维巴坦复合体的晶体结构。(4)B类β-内酰胺酶抑制剂的筛选。

Carbapenems are one of the most important antibiotics and are used worldwide as "Last Resort". We studied four subjects, which are the inhibition mechanisms of carbapenems to beta-lactamases on the basis of Xray crystallography, as listed below. (1) Carbapenems inhibition mechanism for class C beta-lactamases. (2) Crystal structures of the PenA beta-lactamases from Burkholderia cepacia(PenI) and Burkholderia pseudomallei(PenA). (3) Crystal structure of PenA carbapenemase-avibactam complex. (4) Inhibitor screening of class B beta-lactamases.We are showing the overview of the research with crystal structures.