M
Melanie Silinski
Researcher at Durham University
Publications - 7
Citations - 714
Melanie Silinski is an academic researcher from Durham University. The author has contributed to research in topics: Prodrug & Heat shock protein. The author has an hindex of 6, co-authored 7 publications receiving 657 citations.
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Journal ArticleDOI
SNX2112, a Synthetic Heat Shock Protein 90 Inhibitor, Has Potent Antitumor Activity against HER Kinase–Dependent Cancers
Sarat Chandarlapaty,Ayana Sawai,Qing Ye,Anisa Scott,Melanie Silinski,Ken Huang,Patrick Fadden,Jeff Partdrige,Steven C. Hall,Paul M. Steed,Larry Norton,Neal Rosen,David B. Solit +12 more
TL;DR: Hsp90 inhibition with SNX-2112 (delivered as a prodrug) may represent a promising therapeutic strategy for tumors whose growth and survival is dependent on Hsp90 clients.
Journal ArticleDOI
Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
Kenneth He Huang,James Marvin Veal,Patrick Fadden,John W. Rice,Jeron Eaves,Jon-Paul Strachan,Amy F. Barabasz,Briana Foley,Barta Thomas E,Wei Ma,Melanie Silinski,Mei Hu,Jeffrey M. Partridge,Anisa Scott,Laura G. Dubois,Tiffany Freed,Paul M. Steed,Andy J. Ommen,Emilie D. Smith,Philip F. Hughes,Angela R. Woodward,Hanson Gunnar J,W. Stephen Mccall,Christopher John Markworth,Lindsay Hinkley,Matthew Jenks,Geng Lifeng,Meredith Lewis,James C. Otto,Bert Pronk,Katleen Verleysen,Steven E. Hall +31 more
TL;DR: A novel class of heat shock protein 90 (Hsp90) inhibitors was developed from an unbiased screen to identify protein targets for a diverse compound library, and optimized analogues exhibited nanomolar antiproliferative activity across multiple cancer cell lines.
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Brain-permeable small-molecule inhibitors of Hsp90 prevent alpha-synuclein oligomer formation and rescue alpha-synuclein-induced toxicity.
Preeti Putcha,Karin M Danzer,Lisa R. Kranich,Anisa Scott,Melanie Silinski,Sarah R. Mabbett,Carol D. Hicks,James Marvin Veal,Paul M. Steed,Bradley T. Hyman,Pamela J. McLean +10 more
TL;DR: It is found that several compounds prevented αsyn oligomerization as measured by decreased luciferase activity, led to a reduction in high-molecular-mass oligomeric αsyn, and protected against αsyn cytotoxicity.
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Small molecule inhibitors of Hsp90 potently affect inflammatory disease pathways and exhibit activity in models of rheumatoid arthritis.
John W. Rice,James Marvin Veal,Patrick Fadden,Amy F. Barabasz,Jeffrey M. Partridge,Barta Thomas E,Laura G. Dubois,Kenneth He Huang,Sarah R. Mabbett,Melanie Silinski,Paul M. Steed,Steven E. Hall +11 more
TL;DR: The present results demonstrate that a small molecule Hsp90 inhibitor can impact inflammatory disease processes and provides preclinical validation for consideration of Hsp 90 inhibitors in the treatment of RA.
Journal ArticleDOI
Application of Chemoproteomics to Drug Discovery: Identification of a Clinical Candidate Targeting Hsp90.
Patrick Fadden,Kenneth He Huang,James Marvin Veal,Paul M. Steed,Amy F. Barabasz,Briana Foley,Mei Hu,Jeffrey M. Partridge,John W. Rice,Anisa Scott,Laura G. Dubois,Tiffany Freed,Melanie Silinski,Barta Thomas E,Philip F. Hughes,Andy J. Ommen,Wei Ma,Emilie D. Smith,Angela Woodward Spangenberg,Jeron Eaves,Hanson Gunnar J,Lindsay Hinkley,Matthew Jenks,Meredith Lewis,James C. Otto,Gijsbertus J. Pronk,Katleen Verleysen,Timothy A.J. Haystead,Steven E. Hall +28 more
TL;DR: The chemoproteomics-based approach, which also provides broad target selectivity information, was used to drive the identification of a potent and orally active Hsp90 inhibitor, SNX-5422, which is currently in phase 1 clinical studies.