Coughter J P, Johnston J L, Archer G L
Department of Microbiology/Immunology, Medical College of Virginia, Virginia Commonwealth University, Richmond 23298-0001.
Antimicrob Agents Chemother. 1987 Jul;31(7):1027-32. doi: 10.1128/AAC.31.7.1027.
Resistance to trimethoprim (Tp) is mediated by a plasmid-encoded gene in staphylococci. The gene is responsible for high-level resistance (MIC, greater than 1,000 micrograms/ml) in both its native host and when cloned on high-copy-number vectors in Escherichia coli. Analysis of subclones of the staphylococcal Tp gene on E. coli expression vectors and estimation of the size of full and truncated proteins produced in E. coli minicells generated an approximate size limit of 505 base pairs for the gene and 18,500 daltons for the gene product. Crude extracts of E. coli containing the cloned gene had dihydrofolate reductase (DHFR) specific activity that was more than 100 times greater than that of control cells and more than 1,000 times more resistant to trimethoprim inhibition. The amount of trimethoprim required for a 50% reduction in the specific activity of staphylococcal DHFR differed from those of cells containing DHFR types I, II, or III, enzymes mediating Tp in members of the family Enterobacteriaceae. In addition, the size of the monomeric staphylococcal DHFR protein was larger than that of any of the gram-negative DHFRs both compared with published sequence data and as observed by direct comparison on polyacrylamide gels. Finally, there was no homology between a DNA fragment containing the cloned staphylococcal gene and DNA encoding any of the gram-negative DHFRs. Thus, the staphylococcal Tp gene codes for a single protein with DHFR activity that appears to be unrelated to DHFR genes that mediate Tp in members of the Enterobacteriaceae.
金黄色葡萄球菌对甲氧苄啶(Tp)的耐药性由质粒编码基因介导。该基因在其天然宿主以及克隆到大肠杆菌高拷贝数载体上时,均导致高水平耐药(最低抑菌浓度大于1000微克/毫升)。对大肠杆菌表达载体上金黄色葡萄球菌Tp基因的亚克隆进行分析,并估计在大肠杆菌微小细胞中产生的完整和截短蛋白的大小,得出该基因的近似大小限制为505个碱基对,基因产物大小为18500道尔顿。含有克隆基因的大肠杆菌粗提物具有二氢叶酸还原酶(DHFR)比活性,该比活性比对照细胞高100倍以上,对甲氧苄啶抑制的耐药性比对照细胞高1000倍以上。使金黄色葡萄球菌DHFR比活性降低50%所需的甲氧苄啶量,与含有I型、II型或III型DHFR(介导肠杆菌科成员对Tp耐药的酶)的细胞所需的量不同。此外,与已发表的序列数据相比,以及通过在聚丙烯酰胺凝胶上直接比较观察到,单体金黄色葡萄球菌DHFR蛋白的大小比任何革兰氏阴性DHFR都大。最后,含有克隆金黄色葡萄球菌基因的DNA片段与编码任何革兰氏阴性DHFR的DNA之间没有同源性。因此,金黄色葡萄球菌Tp基因编码一种具有DHFR活性的单一蛋白,该蛋白似乎与介导肠杆菌科成员对Tp耐药的DHFR基因无关。