公开(公告)号：US07566550B2

公开(公告)日：2009-07-28

申请号：US10687402

申请日：2003-10-16

Applicant: Jaya Sivaswami Tyagi ,  Deepak Kumar Saini

Inventor： Jaya Sivaswami Tyagi ,  Deepak Kumar Saini

IPC: C12Q1/48

CPC classification number: C12Q1/18 ,  A61K45/06 ,  C12Q1/485 ,  G01N33/6893 ,  G01N2500/00

Abstract: The present invention relates to a package of screening methods for developing drugs against pathogenic microbes having two-component system of DevR-DevS and/or DevR-Rv2027c and its homologues, said method comprising steps of over-expressing DevR, DevS, and Rv2027c and their single domain derivatives including mutant variant proteins, autophosphorylating DevS, and Rv2027c proteins and thereafter, phosphotransfering to DevR and its derivatives in SDS-PAGE or High-throughput format in the presence of a test compound, and determining the drug-potential of the test compound, wherein the potential of the drug is inversely proportional to (i) the degree of autophosphorylation of DevS and Rv2027c, (ii). the degree of phosphotransfer-based dephosphorylation of DevR and/its single domain derivative, and (iii). the degree of dephosphorylation of phosphorylated species of DevS and Rv2027c and/their single domain derivatives, and a method of treatment, and a composition thereof.

Abstract translation: 本发明涉及一种用于开发具有DevR-DevS和/或DevR-Rv2027c及其同源物的双组分系统的致病微生物药物的筛选方法的包装，所述方法包括过表达DevR，DevS和Rv2027c的步骤，以及 其单结构域衍生物包括突变体变体蛋白，自磷酸化DevS和Rv2027c蛋白，此后，在测试化合物存在下以SDS-PAGE或高通量形式磷酸转移至DevR及其衍生物，并测定试验的药物 - 电位 化合物，其中药物的潜力与（i）DevS和Rv2027c的自磷酸化程度成反比（ii）。 DevR和/或其单结构域衍生物的磷酸转移脱磷酸化程度，和（iii）。 DevS和Rv2027c及其单结构域衍生物的磷酸化物质的脱磷酸化程度及其处理方法及其组合物。