New, Non‐quinone Fluorogeldanamycin Derivatives Strongly Inhibit Hsp90

J Hermane, I Bułyszko, S Eichner, F Sasse… - …, 2015 - Wiley Online Library
Streptomyces hygroscopicus is a natural producer of geldanamycin. Mutasynthetic
supplementation of an AHBA‐blocked mutant with all possible monofluoro 3‐aminobenzoic …

[图书][B] A practical guide to assay development and high-throughput screening in drug discovery

T Chen - 2009 - taylorfrancis.com
The development of suitable assays, the integration of appropriate technology, and the
effective management of the essential infrastructure are all critical to the success of any high …

Structure‐based and in silico design of Hsp90 inhibitors

M Sgobba, G Rastelli - ChemMedChem: Chemistry Enabling …, 2009 - Wiley Online Library
The molecular chaperone Hsp90 is responsible for activation and stabilization of several
oncoproteins in cancer cells, and has emerged as an important target in cancer treatment …

Profiling Hsp90 differential expression and the molecular effects of the Hsp90 inhibitor IPI-504 in high-grade glioma models

K Di, ST Keir, D Alexandru-Abrams, X Gong… - Journal of neuro …, 2014 - Springer
Abstract Retaspimycin hydrochloride (IPI-504), an Hsp90 (heat shock protein 90) inhibitor,
has shown activity in multiple preclinical cancer models, such as lung, breast and ovarian …

[HTML][HTML] New geldanamycin derivatives with anti Hsp properties by mutasynthesis

J Hermane, S Eichner, L Mancuso… - Organic & …, 2019 - pubs.rsc.org
Mutasynthetic supplementation of the AHBA blocked mutant strain of S. hygroscopicus, the
geldanamycin producer, with 21 aromatic and heteroaromatic amino acids provided new …

Potent Non-Benzoquinone Ansamycin Heat Shock Protein 90 Inhibitors from Genetic Engineering of Streptomyces hygroscopicus

HG Menzella, TT Tran, JR Carney… - Journal of medicinal …, 2009 - ACS Publications
Inhibition of the protein chaperone Hsp90 is a promising new approach to cancer therapy.
We describe the preparation of potent non-benzoquinone ansamycins. One of these …

Heat Shock Proteins Revisited: Using a Mutasynthetically Generated Reblastatin Library to Compare the Inhibition of Human and Leishmania Hsp90s

S Mohammadi‐Ostad‐Kalayeh, F Stahl… - …, 2018 - Wiley Online Library
Thirteen new reblastatin derivatives, with alkynyl, amino and fluoro substituents on the
aromatic ring, were prepared by a chemo‐biosynthetic approach using an AHBA (−) mutant …

[HTML][HTML] Discovery and development of natural heat shock protein 90 inhibitors in cancer treatment

Y Li, D Zhang, J Xu, J Shi, L Jiang, N Yao… - Acta Pharmaceutica Sinica …, 2012 - Elsevier
Abstract Heat shock protein 90 (Hsp90) is a highly conserved molecular chaperone that
plays a vital role in the signal transduction of cancers. Hsp90 inhibitors are able to inhibit …

HSP90: chaperone-me-not

JM Patki, SS Pawar - Pathology & Oncology Research, 2013 - Springer
With increasing understanding of the molecular basis of carcinogenesis, its progression and
metastasis, the cancer therapy has shifted from empirical approaches to targeting specific …

Synthesis and characterization of 64Cu-labeled Geldanamycin derivative for imaging HSP90 expression in breast cancer

F Li, Y Fan, L Zhou, DR Martin, Z Liu, Z Li - Nuclear Medicine and Biology, 2024 - Elsevier
Abstract Heat shock protein 90 (HSP90) plays a crucial role in cancer cell growth and
metastasis by stabilizing overexpressed signaling proteins. Inhibiting HSP90 has emerged …