New geldanamycin derivatives with anti Hsp properties by mutasynthesis
Literature Information
Publication Date
2019-05-07
DOI
10.1039/C9OB00892F
Impact Factor
3.876
Authors
Jekaterina Hermane, Simone Eichner, Lena Mancuso, Benjamin Schröder, Florenz Sasse, Carsten Zeilinger, Andreas Kirschning
View Original
Abstract
Mutasynthetic supplementation of the AHBA blocked mutant strain of S. hygroscopicus, the geldanamycin producer, with 21 aromatic and heteroaromatic amino acids provided new nonquinoid geldanamycin derivatives. Large scale (5 L) fermentation provided four new derivatives in sufficient quantity for full structural characterisation. Among these, the first thiophene derivative of reblastatin showed strong antiproliferative activity towards several human cancer cell lines. Additionally, inhibitory effects on human heat shock protein Hsp90α and bacterial heat shock protein from H. pylori HpHtpG were observed, revealing strong displacement properties for labelled ATP and demonstrating that the ATP-binding site of Hsps is the target site for the new geldanamycin derivatives.
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Source Journal
Organic & Biomolecular Chemistry
CiteScore:
3.4
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10.3%
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