7229-50-7
基本信息
門黴素
鏈菌鹼
链霉溶菌素
Streptolydigin
Antibiotic D-45
2-Pyrrolidineacetamide, 4-(2E,4E,6R)-6-(1R,2R,3R,4S,5R)-1,4-dimethylspiro2,9-dioxabicyclo3.3.1non-6-ene-8,2-oxiran-3-yl-1-hydroxy-4-methyl-2,4-heptadienylidene-N,.alpha.-dimethyl-3,5-dioxo-1-(2S,5S,6S)-tetrahydro-5-hydroxy-6-methyl-2H-pyran-2-yl-, (.alpha
2-Pyrrolidineacetamide, 4-[(2E,4E,6R)-6-[(1R,2'R,3R,4S,5R)-1,4-dimethylspiro[2,9-dioxabicyclo[3.3.1]non-6-ene-8,2'-oxiran]-3-yl]-1-hydroxy-4-methyl-2,4-heptadien-1-ylidene]-N,α-dimethyl-3,5-dioxo-1-[(2S,5S,6S)-tetrahydro-5-hydroxy-6-methyl-2H-pyran-2-yl]-, (αS,2S,4E)-
物理化学性质
| 熔点 | 147-148° |
| 比旋光度 | D25 -93° (c = 1.6 in chloroform) |
| 沸点 | 659.54°C (rough estimate) |
| 密度 | 1.1852 (rough estimate) |
| 折射率 | 1.6260 (estimate) |
| 酸度系数(pKa) | 4.50±1.00(Predicted) |
安全数据
| 毒性 | LD50 i.p. in mice: 533 mg/kg (DeBoer) |
常见问题列表
Ki: 18 μM (Bacterial RNA polymerase)
Kd: 15 μM (Bacterial RNA polymerase)
The antibiotic Streptolydigin (Stl) is a derivative of 3-acetyltetramic acid. Binding of Streptolydigin to RNA polymerase strictly depends on a noncatalytic magnesium ion which is likely chelated by the aspartate of the bridge helix of the active center.
Streptolydigin inhibits
T. thermophilus
RNA polymerase with a K
i
of 1.8 μM.
Streptolydigin (Stl) inhibits initiation, elongation, and pyrophosphorolysis by bacterial RNA polymerase. Streptolydigin interacts with three structural elements within RNAP: the Stl pocket, the bridge helix, and the trigger-loop region. The Streptolydigin streptolol moiety interacts with the Streptolydigin pocket and bridge helix, and the Streptolydigin tetramic-acid moiety interacts with the trigger-loop region.