Details
| Original language | English |
|---|---|
| Pages (from-to) | 302-311 |
| Number of pages | 10 |
| Journal | CHEMBIOCHEM |
| Volume | 16 |
| Issue number | 2 |
| Publication status | Published - 8 Jan 2015 |
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.
Keywords
- Fluorinated compounds, Geldanamycin, Hsp90, Inhibitors, Mutasynthesis, Single molecule force spectroscopy
ASJC Scopus subject areas
- Biochemistry, Genetics and Molecular Biology(all)
- Biochemistry
- Biochemistry, Genetics and Molecular Biology(all)
- Molecular Medicine
- Biochemistry, Genetics and Molecular Biology(all)
- Molecular Biology
- Chemistry(all)
- Organic Chemistry
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In: CHEMBIOCHEM, Vol. 16, No. 2, 08.01.2015, p. 302-311.
Research output: Contribution to journal › Article › Research › peer review
}
TY - JOUR
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 - http://www.scopus.com/inward/record.url?scp=84920867067&partnerID=8YFLogxK
U2 - 10.1002/cbic.201402375
DO - 10.1002/cbic.201402375
M3 - Article
C2 - 25572106
AN - SCOPUS:84920867067
VL - 16
SP - 302
EP - 311
JO - CHEMBIOCHEM
JF - CHEMBIOCHEM
SN - 1439-4227
IS - 2
ER -