关键词: AIPL1 FK506 FKBP ligands FKBP12 FKBP51 MIP Rapamycin SAFit

来  源:   DOI:10.3389/fphar.2018.01425   PDF(Sci-hub)   PDF(Pubmed)

Abstract:
In recent years, many members of the FK506-binding protein (FKBP) family were increasingly linked to various diseases. The binding domain of FKBPs differs only in a few amino acid residues, but their biological roles are versatile. High-affinity ligands with selectivity between close homologs are scarce. This review will give an overview of the most prominent ligands developed for FKBPs and highlight a perspective for future developments. More precisely, human FKBPs and correlated diseases will be discussed as well as microbial FKBPs in the context of anti-bacterial and anti-fungal therapeutics. The last section gives insights into high-affinity ligands as chemical tools and dimerizers.
摘要:
近年来,FK506结合蛋白(FKBP)家族的许多成员越来越多地与各种疾病相关.FKBPs的结合结构域仅在几个氨基酸残基上不同,但是它们的生物学作用是多方面的。在紧密同源物之间具有选择性的高亲和力配体是稀缺的。这篇综述将概述为FKBP开发的最突出的配体,并强调未来发展的观点。更确切地说,人类FKBP和相关疾病以及微生物FKBP将在抗菌和抗真菌治疗的背景下进行讨论。最后一部分提供了对高亲和力配体作为化学工具和二聚化剂的见解。
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