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Recent Progress in FKBP Ligand Development.
Curr Mol Pharmacol. 2015; 9(1):27-36.CM

Abstract

FK506-binding proteins have been implicated in numerous human diseases suggesting novel therapeutic opportunities. In particular, the large FKBP51 has emerged as an important regulator of the stress-coping system and as an established risk factor for stress-related disorders. The principal druggabilty of FKBPs is evidenced by the prototypical high affinity ligands FK506 and rapamycin but the development of more refined and selective chemical probes for FKBPs has been challenging. In this review we summarize recent advances in the development of FKBP ligands, which cumulated in the first highly selective ligands for FKBP51. The best ligand SAFit2 allowed the proof-of-concept in mice for FKBP51 inhibitors as potentially novel antidepressants. Finally, we discuss pending issues that need to be addressed for the further development of FKBP51-directed drugs.

Authors+Show Affiliations

No affiliation info availableNo affiliation info availableMax Planck Institute of Psychiatry, Kraepelinstr. 2-10, 80804 Munich, Germany. hausch@psych.mpg.de.

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

25986570

Citation

Feng, Xixi, et al. "Recent Progress in FKBP Ligand Development." Current Molecular Pharmacology, vol. 9, no. 1, 2015, pp. 27-36.
Feng X, Pomplun S, Hausch F. Recent Progress in FKBP Ligand Development. Curr Mol Pharmacol. 2015;9(1):27-36.
Feng, X., Pomplun, S., & Hausch, F. (2015). Recent Progress in FKBP Ligand Development. Current Molecular Pharmacology, 9(1), 27-36.
Feng X, Pomplun S, Hausch F. Recent Progress in FKBP Ligand Development. Curr Mol Pharmacol. 2015;9(1):27-36. PubMed PMID: 25986570.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Recent Progress in FKBP Ligand Development. AU - Feng,Xixi, AU - Pomplun,Sebastian, AU - Hausch,Felix, PY - 2014/11/11/received PY - 2015/02/26/revised PY - 2015/05/17/accepted PY - 2015/5/20/entrez PY - 2015/5/20/pubmed PY - 2016/10/7/medline SP - 27 EP - 36 JF - Current molecular pharmacology JO - Curr Mol Pharmacol VL - 9 IS - 1 N2 - FK506-binding proteins have been implicated in numerous human diseases suggesting novel therapeutic opportunities. In particular, the large FKBP51 has emerged as an important regulator of the stress-coping system and as an established risk factor for stress-related disorders. The principal druggabilty of FKBPs is evidenced by the prototypical high affinity ligands FK506 and rapamycin but the development of more refined and selective chemical probes for FKBPs has been challenging. In this review we summarize recent advances in the development of FKBP ligands, which cumulated in the first highly selective ligands for FKBP51. The best ligand SAFit2 allowed the proof-of-concept in mice for FKBP51 inhibitors as potentially novel antidepressants. Finally, we discuss pending issues that need to be addressed for the further development of FKBP51-directed drugs. SN - 1874-4702 UR - https://www.unboundmedicine.com/medline/citation/25986570/Recent_Progress_in_FKBP_Ligand_Development_ L2 - http://www.eurekaselect.com/131452/article DB - PRIME DP - Unbound Medicine ER -