Mack Matthias, Grill Simon
Institute for Technical Microbiology, Mannheim University of Applied Sciences, Germany.
Appl Microbiol Biotechnol. 2006 Jul;71(3):265-75. doi: 10.1007/s00253-006-0421-7. Epub 2006 Apr 11.
Flavins are active components of many enzymes. In most cases, riboflavin (vitamin B(2)) as a coenzyme represents the catalytic part of the holoenzyme. Riboflavin is an amphiphatic molecule and allows a large variety of different interactions with the enzyme itself and also with the substrate. A great number of active riboflavin analogs can readily be synthesized by chemical methods and, thus, a large number of possible inhibitors for many different enzyme targets is conceivable. As mammalian and especially human biochemistry depends on flavins as well, the target of the inhibiting flavin analog has to be carefully selected to avoid unwanted effects. In addition to flavoproteins, enzymes, which are involved in the biosynthesis of flavins, are possible targets for anti-infectives. Only a few flavin analogs or inhibitors of flavin biosynthesis have been subjected to detailed studies to evaluate their biological activity. Nevertheless, flavin analogs certainly have the potential to serve as basic structures for the development of novel anti-infectives and it is possible that, in the future, the urgent need for new molecules to fight multiresistant microorganisms will be met.
黄素是许多酶的活性成分。在大多数情况下,作为辅酶的核黄素(维生素B2)代表全酶的催化部分。核黄素是一种两性分子,能够与酶本身以及底物发生多种不同的相互作用。大量活性核黄素类似物可以通过化学方法轻松合成,因此,可以设想有大量针对许多不同酶靶点的潜在抑制剂。由于哺乳动物尤其是人类生物化学也依赖黄素,因此必须谨慎选择抑制性黄素类似物的靶点,以避免产生不良影响。除了黄素蛋白外,参与黄素生物合成的酶也是抗感染药物的可能靶点。只有少数黄素类似物或黄素生物合成抑制剂经过了详细研究以评估其生物活性。然而,黄素类似物肯定有潜力作为开发新型抗感染药物的基本结构,并且未来有可能满足对抗多重耐药微生物的新分子的迫切需求。