1. Academic Validation
  2. FKBP Ligands-Where We Are and Where to Go?

FKBP Ligands-Where We Are and Where to Go?

  • Front Pharmacol. 2018 Dec 5;9:1425. doi: 10.3389/fphar.2018.01425.
Jürgen M Kolos 1 Andreas M Voll 1 Michael Bauder 1 Felix Hausch 1
Affiliations

Affiliation

  • 1 Department of Chemistry, Institute of Chemistry and Biochemistry, Darmstadt University of Technology, Darmstadt, Germany.
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.

Keywords

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

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