Behr Jean-Bernard
Université de Reims Champagne-Ardenne, Institut de Chimie Moléculaire de Reims, CNRS UMR 6229, UFR des Sciences Exactes et Naturelles, BP 1039-51687 Reims Cedex 2, France.
Chimia (Aarau). 2011;65(1-2):49-53. doi: 10.2533/chimia.2011.49.
During the last 30 past years, more life-threatening fungal infections have appeared due to the increasing frequency of patients with weakened immune systems. Inhibition of fungal enzymes involved in the biosynthesis of sterols is considered to be a safe and effective option for antifungal therapy. However, the intensive use of sterol-biosynthesis inhibitors for years has resulted in resistance development. Consequently, the search for alternative therapeutics must be intensified. In this context, the biosynthesis of chitin, an essential component of the fungal cell wall that is absent in mammalian cells, was envisioned as a safe and selective therapeutic target. We present here recent successes in the inhibition of chitin synthase, the enzyme involved in the last step of the biosynthesis of chitin.
在过去30年里，由于免疫系统减弱的患者数量不断增加，出现了更多危及生命的真菌感染。抑制参与甾醇生物合成的真菌酶被认为是抗真菌治疗的一种安全有效的选择。然而，多年来甾醇生物合成抑制剂的大量使用导致了耐药性的产生。因此，必须加强对替代疗法的研究。在这种背景下，几丁质（一种在哺乳动物细胞中不存在的真菌细胞壁的重要成分）的生物合成被设想为一个安全且有选择性的治疗靶点。我们在此展示了在抑制几丁质合酶（参与几丁质生物合成最后一步的酶）方面取得的最新成果。
