Triiodothyronine Acts as a Smart Influencer on Hsp90 via a Triiodothyronine Binding Site

Lu Fan; Athanasia Warnecke; Julia Weder; Matthias Preller; Carsten Zeilinger

doi:10.3390/ijms23137150

Triiodothyronine Acts as a Smart Influencer on Hsp90 via a Triiodothyronine Binding Site

Lu Fan
, Athanasia Warnecke
, Julia Weder
, Matthias Preller
, Carsten Zeilinger^*

^*Korrespondierende*r Autor*in für diese Arbeit

Zentrum für Biomolekulare Wirkstoffe (BMWZ)

Publikation: Beitrag in Fachzeitschrift › Kurzmitteilung › Forschung › Peer-Review

Abstract

Microarray-based experiments revealed that thyroid hormone triiodothyronine (T3) enhanced the binding of Cy5-labeled ATP on heat shock protein 90 (Hsp90). By molecular docking experiments with T3 on Hsp90, we identified a T3 binding site (TBS) near the ATP binding site on Hsp90. A synthetic peptide encoding HHHHHHRIKEIVKKHSQFIGYPITLFVEKE derived from the TBS on Hsp90 showed, in MST experiments, the binding of T3 at an EC₅₀ of 50 µM. The binding motif can influence the activity of Hsp90 by hindering ATP accessibility or the release of ADP.

Originalsprache	Englisch
Aufsatznummer	7150
Seitenumfang	6
Fachzeitschrift	International Journal of Molecular Sciences
Jahrgang	23
Ausgabenummer	13
Elektronisch veröffentlicht (E-Pub)	28 Juni 2022
DOIs	https://doi.org/10.3390/ijms23137150
Publikationsstatus	Veröffentlicht - Juli 2022

ASJC Scopus Sachgebiete

Katalyse
Molekularbiologie
Spektroskopie
Angewandte Informatik
Physikalische und Theoretische Chemie
Organische Chemie
Anorganische Chemie

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10.3390/ijms23137150Lizenz: CC BY 4.0

Andere Dateien und Links

Verknüpfung zur Publikation in Scopus

Forschungsgruppe 5170, Teilprojekt TP 6: Target-orientiertes Screening einer Cytochalasan-Verbindungsbibliothek
Zeilinger, C. (Projektleiter*in (Principal Investigator))
1 Feb. 2021 → 31 Jan. 2025
Projekt: Forschung
Exzellenzcluster 2177: Hearing4all
Blume, H. C. (Projektleiter*in (Principal Investigator)), Behrens, P. (Projektleiter*in (Principal Investigator)), Heisterkamp, A. (Projektleiter*in (Principal Investigator)) & Blume, C. (Projektleiter*in (Principal Investigator))
1 Jan. 2019 → 31 Dez. 2025
Projekt: Forschung

Dieses zitieren

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title = "Triiodothyronine Acts as a Smart Influencer on Hsp90 via a Triiodothyronine Binding Site",

abstract = "Microarray-based experiments revealed that thyroid hormone triiodothyronine (T3) enhanced the binding of Cy5-labeled ATP on heat shock protein 90 (Hsp90). By molecular docking experiments with T3 on Hsp90, we identified a T3 binding site (TBS) near the ATP binding site on Hsp90. A synthetic peptide encoding HHHHHHRIKEIVKKHSQFIGYPITLFVEKE derived from the TBS on Hsp90 showed, in MST experiments, the binding of T3 at an EC50 of 50 µM. The binding motif can influence the activity of Hsp90 by hindering ATP accessibility or the release of ADP.",

keywords = "Hsp90, molecular docking, protein microarray, thermophoresis, triiodothyronine",

author = "Lu Fan and Athanasia Warnecke and Julia Weder and Matthias Preller and Carsten Zeilinger",

note = "Funding Information: Funding: Parts of the project were funded by FOR 5170: CytoLabs—Systematic Investigation and Exploitation of Cytochalasans, ZE 338/16-1. This work was supported by the DFG Cluster of Excellence EXC 2177/1 “Hearing4all”. ",

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AU - Fan, Lu

AU - Warnecke, Athanasia

AU - Weder, Julia

AU - Preller, Matthias

AU - Zeilinger, Carsten

N1 - Funding Information: Funding: Parts of the project were funded by FOR 5170: CytoLabs—Systematic Investigation and Exploitation of Cytochalasans, ZE 338/16-1. This work was supported by the DFG Cluster of Excellence EXC 2177/1 “Hearing4all”.

PY - 2022/7

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N2 - Microarray-based experiments revealed that thyroid hormone triiodothyronine (T3) enhanced the binding of Cy5-labeled ATP on heat shock protein 90 (Hsp90). By molecular docking experiments with T3 on Hsp90, we identified a T3 binding site (TBS) near the ATP binding site on Hsp90. A synthetic peptide encoding HHHHHHRIKEIVKKHSQFIGYPITLFVEKE derived from the TBS on Hsp90 showed, in MST experiments, the binding of T3 at an EC50 of 50 µM. The binding motif can influence the activity of Hsp90 by hindering ATP accessibility or the release of ADP.

AB - Microarray-based experiments revealed that thyroid hormone triiodothyronine (T3) enhanced the binding of Cy5-labeled ATP on heat shock protein 90 (Hsp90). By molecular docking experiments with T3 on Hsp90, we identified a T3 binding site (TBS) near the ATP binding site on Hsp90. A synthetic peptide encoding HHHHHHRIKEIVKKHSQFIGYPITLFVEKE derived from the TBS on Hsp90 showed, in MST experiments, the binding of T3 at an EC50 of 50 µM. The binding motif can influence the activity of Hsp90 by hindering ATP accessibility or the release of ADP.

KW - Hsp90

KW - molecular docking

KW - protein microarray

KW - thermophoresis

KW - triiodothyronine

UR - https://www.scopus.com/pages/publications/85132836920

U2 - 10.3390/ijms23137150

DO - 10.3390/ijms23137150

M3 - Short/Brief/Rapid Communication

C2 - 35806154

AN - SCOPUS:85132836920

SN - 1661-6596

VL - 23

JO - International Journal of Molecular Sciences

JF - International Journal of Molecular Sciences

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ER -

Triiodothyronine Acts as a Smart Influencer on Hsp90 via a Triiodothyronine Binding Site

Abstract

ASJC Scopus Sachgebiete

Zugriff auf Dokument

Andere Dateien und Links

Projekte

Forschungsgruppe 5170, Teilprojekt TP 6: Target-orientiertes Screening einer Cytochalasan-Verbindungsbibliothek

Exzellenzcluster 2177: Hearing4all

Dieses zitieren