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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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Datensatz-Permalink: https://hdl.handle.net/11858/00-001M-0000-0029-AE16-4 Versions-Permalink: https://hdl.handle.net/11858/00-001M-0000-0029-AE17-2
Genre: Zeitschriftenartikel

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 Urheber:
Feng, Xixi1, Autor           
Sippel, Claudia1, Autor           
Bracher, Andreas2, Autor
Hausch, Felix1, Autor           
Affiliations:
1Dept. Translational Research in Psychiatry, Max Planck Institute of Psychiatry, Max Planck Society, ou_2035295              
2external, ou_persistent22              

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 Zusammenfassung: 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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Sprache(n): eng - English
 Datum: 2015-10-08
 Publikationsstatus: Erschienen
 Seiten: -
 Ort, Verlag, Ausgabe: -
 Inhaltsverzeichnis: -
 Art der Begutachtung: -
 Identifikatoren: ISI: 000362701600014
DOI: 10.1021/acs.jmedchem.5b00785
 Art des Abschluß: -

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Titel: JOURNAL OF MEDICINAL CHEMISTRY
Genre der Quelle: Zeitschrift
 Urheber:
Affiliations:
Ort, Verlag, Ausgabe: Washington, DC 20036, USA : ACS Publications
Seiten: - Band / Heft: 58 (19) Artikelnummer: - Start- / Endseite: 7796 - 7806 Identifikator: ISSN: 0022-2623