H
Hayley Angove
Researcher at Astex
Publications - 4
Citations - 388
Hayley Angove is an academic researcher from Astex. The author has contributed to research in topics: Aurora B kinase & Endoreduplication. The author has an hindex of 4, co-authored 4 publications receiving 347 citations.
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Journal ArticleDOI
Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design.
Andrew James Woodhead,Hayley Angove,Maria Grazia Carr,Gianni Chessari,Miles Congreve,Joseph E. Coyle,Jose Cosme,Brent Graham,Philip J. Day,Robert Downham,Lynsey Fazal,Ruth Feltell,Eva Figueroa,Martyn Frederickson,Jonathan Lewis,Rachel McMenamin,Christopher W. Murray,M. Alistair O’Brien,Lina Parra,Sahil Patel,Theresa Rachael Phillips,David C. Rees,Sharna J. Rich,Donna-Michelle Smith,Gary Trewartha,Mladen Vinkovic,Brian John Williams,Alison Jo-Anne Woolford +27 more
TL;DR: The structure guided optimization of the 2,4-dihydroxybenzamide lead molecule 1 is described and some of the drug discovery strategies employed in the identification of AT13387, which has progressed through preclinical development and is currently being tested in man.
Journal ArticleDOI
The heat shock protein 90 inhibitor, AT13387, displays a long duration of action in vitro and in vivo in non‐small cell lung cancer
Brent Graham,Jayne Curry,Tomoko Smyth,Lynsey Fazal,Ruth Feltell,Isobel Harada,Joe Coyle,Brian Williams,Matthias Reule,Hayley Angove,David M. Cross,John Lyons,Nicola G. Wallis,Neil T. Thompson +13 more
TL;DR: Pharmacokinetic analyses indicated that while AT13387 was rapidly cleared from blood, its retention in tumor xenografts was markedly extended, and it was efficacious in a range of Xenograft models, in particular, its efficacious once weekly administration in human lung carcinoma xenografteds.
Journal ArticleDOI
Aurora B kinase inhibition in mitosis: Strategies for optimizing the use of Aurora kinase inhibitors such as AT9283
Jayne Curry,Hayley Angove,Lynsey Fazal,John Lyons,Matthias Reule,Neil Thompson,Nicola G. Wallis +6 more
TL;DR: Combining Aurora B kinase inhibition with paclitaxel, which arrests cells in mitosis, in a xenograft model resulted in promising efficacy without additional toxicity, which has implications for optimizing the efficacy of Aurora kinase inhibitors in clinical practice.
Journal ArticleDOI
Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors.
Young Shin Cho,Hayley Angove,Christopher Thomas Brain,Chen Christine Hiu-Tung,Hong Cheng,Robert Cheng,Rajiv Chopra,Kristy Chung,Miles Congreve,Claudio Dagostin,Deborah J. Davis,Ruth Feltell,John William Giraldes,Steven Douglas Hiscock,Sunkyu Kim,Steven Kovats,Bharat Lagu,Kim Lewry,Alice Loo,Yipin Lu,Luzzio Michael,Wiesia Maniara,Rachel McMenamin,Paul N. Mortenson,Rajdeep Benning,Marc O'Reilly,David C. Rees,Junqing Shen,Troy Smith,Yaping Wang,Glyn Williams,Alison Jo-Anne Woolford,Wrona Wojciech,Mei Xu,Fan Yang,Steven Howard +35 more
TL;DR: The discovery of potent and highly selective inhibitors of both CDK4 and CDK6 via structure-guided optimization of a fragment-based screening hit is described.