FEBS Letters | |
Specificity of GDP‐Man:dolichyl‐phosphate mannosyltransferase for the guanosine diphosphate esters of mannose analogues containing deoxy and deoxyfluoro substituents | |
McDowell, William2  Schwarz, Ralph T.1  | |
[1] Laboratoire de Chimie Biologique, Université des Sciences et Techniques de Lille Flandres-Artois, F-59655 Villeneuve d'Ascq Cedex, France;Institut für Virologie, Justus-Liebig-Universität, Frankfurter Strasse 107, D-6300 Giessen, FRG | |
关键词: Deoxy-D-glucose; 2-; Deoxy-2-fluoro-D-mannose; 2-; Deoxy-D-mannose; 3-; Deoxy-D-mannose; 4-; Deoxy-D-mannose; 6-; Enzyme inhibition; (Chick embryo cell); | |
DOI : 10.1016/0014-5793(89)80173-5 | |
学科分类:生物化学/生物物理 | |
来源: John Wiley & Sons Ltd. | |
【 摘 要 】
Guanosine diphosphate (GDP) esters of 2-deoxy-D-glucose (2dGlc), 2-deoxy-2-fluoro-D-mannose (2FMan), 3-deoxy-D-mannose (3dMan), 4-deoxy-D-mannose (4dMan) and 6-deoxy-D-mannose (6dMan) have been synthesised and tested for their ability to act as inhibitors of dolichyl phosphate mannose synthesis (enzyme: GDP-mannose:dolichyl-phosphate mannosyltransferase, EC 2.4.1.83) in chick embryo cell microsomal membranes. The following order of efficiency was found with the apparent K i in parentheses: GDP-6dMan (0.40 μM±0.15) > GDP-3dMan (1.0 μM±0.1) = GDP-2dGlc (1.3 μM±0.2) > GDP-4dMan (3.1 μM±0.1) GDP-2FMan (15 μM±0). For comparison the K m for GDP-Man was 0.52 μM±0.02 and the K i for GDP was 56 μM±2. These results indicate that the 6-hydroxyl group of mannose is not crucial for emzyme-substrate recognition, whereas the 2- and 3-hydroxyls may have some involvement. The 4-hydroxyl appears to be an important determinant for enzyme-substrate recognition in this mannosyltransferase.
【 授权许可】
Unknown
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