4.7 Review

FKBP Ligands-Where We Are and Where to Go?

Journal

FRONTIERS IN PHARMACOLOGY
Volume 9, Issue -, Pages -

Publisher

FRONTIERS MEDIA SA
DOI: 10.3389/fphar.2018.01425

Keywords

FKBP ligands; FKBP12; FKBP51; AIPL1; MIP; Rapamycin; FK506; SAFit

Funding

  1. M4 Award 2015 from the StMWIVT [BIO-1601-0003]
  2. BMBF/ERA-IB grant TACRODRUGS [031B0269B]
  3. German Research Foundation
  4. Open Access Publishing Fund of Technische Universitat Darmstadt

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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.

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