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  Structure-Affinity Relationship Analysis of Selective FKBP51 Ligands

Feng, X., Sippel, C., Bracher, A., & Hausch, F. (2015). Structure-Affinity Relationship Analysis of Selective FKBP51 Ligands. JOURNAL OF MEDICINAL CHEMISTRY, 58(19), 7796-7806. doi:10.1021/acs.jmedchem.5b00785.

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Item Permalink: http://hdl.handle.net/11858/00-001M-0000-0028-FAC6-8 Version Permalink: http://hdl.handle.net/11858/00-001M-0000-0028-FAC9-2
Genre: Journal Article

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 Creators:
Feng, Xixi1, Author
Sippel, Claudia1, Author
Bracher, Andreas2, Author              
Hausch, Felix1, Author
Affiliations:
1external, ou_persistent22              
2Hartl, Franz-Ulrich / Cellular Biochemistry, Max Planck Institute of Biochemistry, Max Planck Society, ou_1565152              

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Free keywords: FK506-BINDING PROTEINS 51; COCHAPERONE; STRESS; CONSTRUCTION; PHYSIOLOGY; DESIGN; CANCER; DOMAIN; MICE
 Abstract: The FK506-binding protein 51 (FICBP51) is a promising drug target for the treatment of stress-related psychiatric or metabolic disorders. Just recently, the first selective ligands for FKBP51 were reported based on an induced fit mechanism, but they are too large for a further drug development process. We therefore designed and synthesized a novel series of selective ligands to explore the requirements necessary for binding to the induced-fit conformation. All ligands of this series show no binding toward the structurally very similar antitarget FKBP52. With the cocrystal structure of the best ligand in this novel series we confirmed the induced fit mechanism. Furthermore, the structure affinity relationship provides information about beneficial structural features, which is valuable for the development of improved FKBP51-directed drugs.

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Language(s): eng - English
 Dates: 2015
 Publication Status: Published in print
 Pages: 11
 Publishing info: -
 Table of Contents: -
 Rev. Method: Peer
 Degree: -

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Title: JOURNAL OF MEDICINAL CHEMISTRY
Source Genre: Journal
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Publ. Info: 1155 16TH ST, NW, WASHINGTON, DC 20036 USA : AMER CHEMICAL SOC
Pages: - Volume / Issue: 58 (19) Sequence Number: - Start / End Page: 7796 - 7806 Identifier: ISSN: 0022-2623