FK506, also known as tacrolimus, is a clinically important immunosuppressant drug and has promising therapeutic potentials owing to its antifungal, neuroprotective, and neuroregenerative activities. To generate various FK506 derivatives, the structure of FK506 has been modified by chemical methods or biosynthetic pathway engineering. Herein, we describe the mode of the antifungal action of FK506 and the structure-activity relationship of FK506 derivatives in the context of immunosuppressive and antifungal activities. In addition, we discuss the neurotrophic mechanism of FK506 known to date, along with the neurotrophic FK506 derivatives with significantly reduced immunosuppressive activity. This review suggests the possibility to generate novel FK506 derivatives as antifungal as well as neuroregenerative/neuroprotective agents.

中文翻译：

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作为抗真菌剂和神经营养剂的非免疫抑制 FK506 衍生物的开发。

FK506，也称为他克莫司，是一种临床上重要的免疫抑制药物，由于其抗真菌、神经保护和神经再生活性而具有广阔的治疗潜力。为了生成各种 FK506 衍生物，已通过化学方法或生物合成途径工程对 FK506 的结构进行修饰。在此，我们描述了 FK506 的抗真菌作用模式以及 FK506 衍生物在免疫抑制和抗真菌活性背景下的结构-活性关系。此外，我们讨论了迄今为止已知的 FK506 的神经营养机制，以及免疫抑制活性显着降低的神经营养 FK506 衍生物。这篇综述表明有可能产生新的 FK506 衍生物作为抗真菌剂以及神经再生/神经保护剂。