| Name | dihydrofolate reductase |
|---|---|
| Synonyms | DHFR; DHFRP 1; DHFRP1; Dihydrofolate reductase; Dihydrofolate reductases |
| Name | biphenyl |
|---|---|
| CAS | 1,1′-biphenyl |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 19152636 | Liu J, Bolstad DB, Smith AE, Priestley ND, Wright DL, Anderson AC: Probing the active site of Candida glabrata dihydrofolate reductase with high resolution crystal structures and the synthesis of new inhibitors. Chem Biol Drug Des. 2009 Jan;73(1):62-74. Using a crystal structure of dihydrofolate reductase from C. glabrata bound to an initial lead compound, we designed a class of biphenyl antifolates that potently and selectively inhibit both the enzyme and the growth of the fungal culture. |
83(1,1,1,3) | Details |
| 19249312 | Frey KM, Liu J, Lombardo MN, Bolstad DB, Wright DL, Anderson AC: Crystal structures of wild-type and mutant methicillin-resistant Staphylococcus aureus dihydrofolate reductase reveal an alternate conformation of that may be linked to trimethoprim resistance. J Mol Biol. 2009 Apr 17;387(5):1298-308. Epub 2009 Feb 26. We screened this series against wild-type and mutant (F98Y) S. aureus DHFR and found that several are active against both enzymes and specifically that the meta-biphenyl class of these inhibitors is the most potent. |
34(0,1,1,4) | Details |
| 19560363 | Paulsen JL, Liu J, Bolstad DB, Smith AE, Priestley ND, Wright DL, Anderson AC: In vitro biological activity and structural analysis of 2,4-diamino-5-(2'-arylpropargyl) pyrimidine inhibitors of Candida albicans. Bioorg Med Chem. 2009 Jul 15;17(14):4866-72. Epub 2009 Jun 17. In order to develop new antifungal agents effective against two species of Candida, we have designed a series of dihydrofolate reductase (DHFR) inhibitors. The meta-biphenyl series of this class exhibits the greatest enzyme inhibition, selectivity and antifungal activity. |
2(0,0,0,2) | Details |