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Literature DB >> 21273068

Identification and initial SAR of silybin: an Hsp90 inhibitor.

Huiping Zhao¹, Gary E Brandt, Lakshmi Galam, Robert L Matts, Brian S J Blagg.

Abstract

Through Hsp90-dependent firefly luciferase refolding and Hsp90-dependent heme-regulated eIF2α kinase (HRI) activation assays, silybin was identified as a novel Hsp90 inhibitor. Subsequently, a library of silybin analogues was designed, synthesized and evaluated. Initial SAR studies identified the essential, non-essential and detrimental functionalities on silybin that contribute to Hsp90 inhibition.

Entities: Chemical Gene

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Year: 2010 PMID： 21273068 DOI： 10.1016/j.bmcl.2010.12.088

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

22 in total

1. Alternative approaches to Hsp90 modulation for the treatment of cancer.

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2. A C-terminal HSP90 inhibitor restores glucocorticoid sensitivity and relieves a mouse allograft model of Cushing disease.

Authors: Mathias Riebold; Christian Kozany; Lee Freiburger; Michael Sattler; Michael Buchfelder; Felix Hausch; Günter K Stalla; Marcelo Paez-Pereda
Journal: Nat Med Date: 2015-02-09 Impact factor: 53.440

Review 3. Anticancer Inhibitors of Hsp90 Function: Beyond the Usual Suspects.

Authors: Gaurav Garg; Anuj Khandelwal; Brian S J Blagg
Journal: Adv Cancer Res Date: 2016-02-10 Impact factor: 6.242

4. Development of a high-throughput screening cancer cell-based luciferase refolding assay for identifying Hsp90 inhibitors.

Authors: Takrima Sadikot; Megan Swink; Jeffery D Eskew; Douglas Brown; Huiping Zhao; Bhaskar R Kusuma; Roger A Rajewski; Brian S J Blagg; Robert L Matts; Jeffrey M Holzbeierlein; George A Vielhauer
Journal: Assay Drug Dev Technol Date: 2013-10-15 Impact factor: 1.738

Review 5. The Chemical Biology of Molecular Chaperones--Implications for Modulation of Proteostasis.

Authors: Kristoffer R Brandvold; Richard I Morimoto
Journal: J Mol Biol Date: 2015-05-21 Impact factor: 5.469

6. Novologues containing a benzamide side chain manifest anti-proliferative activity against two breast cancer cell lines.

Authors: Huiping Zhao; Mercy Anyika; Antwan Girgis; Brian S J Blagg
Journal: Bioorg Med Chem Lett Date: 2014-05-16 Impact factor: 2.823

Identification and initial SAR of silybin: an Hsp90 inhibitor.

1. Alternative approaches to Hsp90 modulation for the treatment of cancer.

2. A C-terminal HSP90 inhibitor restores glucocorticoid sensitivity and relieves a mouse allograft model of Cushing disease.

Review 3. Anticancer Inhibitors of Hsp90 Function: Beyond the Usual Suspects.

4. Development of a high-throughput screening cancer cell-based luciferase refolding assay for identifying Hsp90 inhibitors.

Review 5. The Chemical Biology of Molecular Chaperones--Implications for Modulation of Proteostasis.

6. Novologues containing a benzamide side chain manifest anti-proliferative activity against two breast cancer cell lines.

7. A Scaffold Merging Approach to Hsp90 C-terminal Inhibition: Synthesis and Evaluation of a Chimeric Library.

8. 3-Arylcoumarin derivatives manifest anti-proliferative activity through Hsp90 inhibition.

9. Mechanistic study of the biomimetic synthesis of flavonolignan diastereoisomers in milk thistle.

10. 3D-QSAR Assisted Design, Synthesis and Evaluation of Novobiocin Analogues.