New, Non‐quinone Fluorogeldanamycin Derivatives Strongly Inhibit Hsp90

Jekaterina Hermane; Ilona Bułyszko; Simone Eichner; Florenz Sasse; Wera Collisi; Antti Poso; Emilia Schax; Johanna Gabriela Walter; Thomas Scheper; Klaus Kock; Christian Herrmann; Pooyan Aliuos; Günter Reuter; Carsten Zeilinger; Andreas Kirschning

doi:10.1002/cbic.201402375

New, Non‐quinone Fluorogeldanamycin Derivatives Strongly Inhibit Hsp90

Jekaterina Hermane
, Ilona Bułyszko
, Simone Eichner
, Florenz Sasse
, Wera Collisi
, Antti Poso
, Emilia Schax
, Johanna Gabriela Walter
, Thomas Scheper
, Klaus Kock
, Christian Herrmann
, Pooyan Aliuos
, Günter Reuter
, Carsten Zeilinger^*
, Andreas Kirschning

^*Corresponding author for this work

Research output: Contribution to journal › Article › Research › peer review

Abstract

Streptomyces hygroscopicus is a natural producer of geldanamycin. Mutasynthetic supplementation of an AHBA-blocked mutant with all possible monofluoro 3-aminobenzoic acids provided new fluorogeldanamycins. These showed strong antiproliferative activity and inhibitory effects on human heat shock protein Hsp90. Binding to Hsp90 in the low nanomolar range was determined from molecular modelling, AFM analysis and by calorimetric studies.

Original language	English
Pages (from-to)	302-311
Number of pages	10
Journal	CHEMBIOCHEM
Volume	16
Issue number	2
DOIs	https://doi.org/10.1002/cbic.201402375
Publication status	Published - 8 Jan 2015

Keywords

Fluorinated compounds
Geldanamycin
Hsp90
Inhibitors
Mutasynthesis
Single molecule force spectroscopy

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Organic Chemistry

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10.1002/cbic.201402375

Cite this

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abstract = "Streptomyces hygroscopicus is a natural producer of geldanamycin. Mutasynthetic supplementation of an AHBA-blocked mutant with all possible monofluoro 3-aminobenzoic acids provided new fluorogeldanamycins. These showed strong antiproliferative activity and inhibitory effects on human heat shock protein Hsp90. Binding to Hsp90 in the low nanomolar range was determined from molecular modelling, AFM analysis and by calorimetric studies.",

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year = "2015",

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doi = "10.1002/cbic.201402375",

language = "English",

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T1 - New, Non‐quinone Fluorogeldanamycin Derivatives Strongly Inhibit Hsp90

AU - Hermane, Jekaterina

AU - Bułyszko, Ilona

AU - Eichner, Simone

AU - Sasse, Florenz

AU - Collisi, Wera

AU - Poso, Antti

AU - Schax, Emilia

AU - Walter, Johanna Gabriela

AU - Scheper, Thomas

AU - Kock, Klaus

AU - Herrmann, Christian

AU - Aliuos, Pooyan

AU - Reuter, Günter

AU - Zeilinger, Carsten

AU - Kirschning, Andreas

PY - 2015/1/8

Y1 - 2015/1/8

N2 - Streptomyces hygroscopicus is a natural producer of geldanamycin. Mutasynthetic supplementation of an AHBA-blocked mutant with all possible monofluoro 3-aminobenzoic acids provided new fluorogeldanamycins. These showed strong antiproliferative activity and inhibitory effects on human heat shock protein Hsp90. Binding to Hsp90 in the low nanomolar range was determined from molecular modelling, AFM analysis and by calorimetric studies.

AB - Streptomyces hygroscopicus is a natural producer of geldanamycin. Mutasynthetic supplementation of an AHBA-blocked mutant with all possible monofluoro 3-aminobenzoic acids provided new fluorogeldanamycins. These showed strong antiproliferative activity and inhibitory effects on human heat shock protein Hsp90. Binding to Hsp90 in the low nanomolar range was determined from molecular modelling, AFM analysis and by calorimetric studies.

KW - Fluorinated compounds

KW - Geldanamycin

KW - Hsp90

KW - Inhibitors

KW - Mutasynthesis

KW - Single molecule force spectroscopy

UR - https://www.scopus.com/pages/publications/84920867067

U2 - 10.1002/cbic.201402375

DO - 10.1002/cbic.201402375

M3 - Article

C2 - 25572106

AN - SCOPUS:84920867067

SN - 1439-4227

VL - 16

SP - 302

EP - 311

JO - CHEMBIOCHEM

JF - CHEMBIOCHEM

IS - 2

ER -

New, Non‐quinone Fluorogeldanamycin Derivatives Strongly Inhibit Hsp90

Abstract

Keywords

ASJC Scopus subject areas

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