Laboratory of Molecular Modeling Applied to the Chemical and Biological Defense (LMCBD), Military Institute of Engineering, 22290-270, Rio de Janeiro, RJ, Brazil.
J Biomol Struct Dyn. 2011 Oct;29(2):351-67. doi: 10.1080/07391102.2011.10507390.
Considering the risk represented by plague today as a potential biological warfare agent, we propose cytosolic Yersinia pestis dihydrofolate reductase (YpDHFR) as a new target to the design of selective plague chemotherapy. This enzyme has a low homology with the human enzyme and its crystallographic structure has been recently deposited in the Protein Data Bank (PDB). Comparisons of the docking energies and molecular dynamic behaviors of five known DHFR inhibitors inside a 3D model of YpDHFR (adapted from the crystallographic structure) and human DHFR (HssDHFR), revealed new potential interactions and suggested insights into the design of more potent HssDHFR inhibitors as well as selective inhibitors for YpDHFR.
考虑到鼠疫作为一种潜在的生物战剂所带来的风险,我们提出胞质鼠疫耶尔森氏菌二氢叶酸还原酶(YpDHFR)作为设计选择性鼠疫化学疗法的新靶点。该酶与人类酶的同源性较低,其晶体结构最近已存入蛋白质数据库(PDB)。在 YpDHFR(源自晶体结构)和人二氢叶酸还原酶(HssDHFR)的 3D 模型中,对五种已知 DHFR 抑制剂的对接能和分子动力学行为进行比较,揭示了新的潜在相互作用,并为设计更有效的 HssDHFR 抑制剂以及针对 YpDHFR 的选择性抑制剂提供了新的思路。