| Literature DB >> 25572106 |
Jekaterina Hermane1, 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.
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.Entities:
Keywords: Hsp90; fluorinated compounds; geldanamycin; inhibitors; mutasynthesis; single molecule force spectroscopy
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Year: 2015 PMID： 25572106 DOI： 10.1002/cbic.201402375
Source DB: PubMed Journal: Chembiochem ISSN： 1439-4227 Impact factor: 3.164