K. Hudson

发表

The use of 18F-Fluoro-deoxy-glucose positron emission tomography (18F-FDG PET) as a non-invasive pharmacodynamic biomarker to determine the minimally pharmacologically active dose of AZD8835, a novel PI3Kα inhibitor

H. Barjat, A. Pritchard, F. Blé, 2017, PloS one.

Design and synthesis of novel lactate dehydrogenase A inhibitors by fragment-based lead generation.

Jon Winter, David Whittaker, Gareth Davies, 2012, Journal of medicinal chemistry.

Sensitivity to PI3K and AKT inhibitors is mediated by divergent molecular mechanisms in subtypes of DLBCL.

G. Ott, G. Lenz, S. Barry, 2017, Blood.

Constitutive Cdc25B tyrosine phosphatase activity in adult brain neurons with M phase-type alterations in Alzheimer’s disease

I. Vincent, D. Nochlin, K. Hudson, 2001, Neuroscience.

Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase.

J. Nissink, G. Walker, R. Ducray, 2011, Bioorganic & medicinal chemistry letters.

Enzymatic Characterisation of USP7 Deubiquitinating activity and Inhibition

R. Ward, K. Hudson, Peter B. Simpson, 2011, Cell Biochemistry and Biophysics.

Design of selective PI3Kα inhibitors starting from a promiscuous pan kinase scaffold.

S. Green, B. Barlaam, S. Cosulich, 2015, Bioorganic & medicinal chemistry letters.

A novel DYRK1B inhibitor AZ191 demonstrates that DYRK1B acts independently of GSK3β to phosphorylate cyclin D1 at Thr(286), not Thr(288).

S. Cook, D. Oxley, S. Guichard, 2014, The Biochemical journal.

A Generic Platform for Cellular Screening Against Ubiquitin Ligases

J. Nissink, R. Hay, Husam A J Alwan, 2016, Scientific Reports.

Activation of protein kinase B β and γ isoforms by insulin in vivo and by 3-phosphoinositide-dependent protein kinase-1 in vitro : comparison with protein kinase B α

P. Cohen, D. Alessi, A. Paterson, 1998 .

Activation of protein kinase B beta and gamma isoforms by insulin in vivo and by 3-phosphoinositide-dependent protein kinase-1 in vitro: comparison with protein kinase B alpha.

P. Cohen, D. Alessi, A. Paterson, 1998, The Biochemical journal.

Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.

Peter D Smith, J. Kendrew, Rebecca P A Ellston, 2006, Bioorganic & medicinal chemistry letters.

A new series of neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.

James S. Scott, B. Barlaam, R. Ducray, 2008, Bioorganic & medicinal chemistry letters.

Functional significance of co-occurring mutations in PIK3CA and MAP3K1 in breast cancer

E. Harrington, Á. Avivar-Valderas, Marcello Maresca, 2018, Oncotarget.

Intermittent High-Dose Scheduling of AZD8835, a Novel Selective Inhibitor of PI3Kα and PI3Kδ, Demonstrates Treatment Strategies for PIK3CA-Dependent Breast Cancers

O. Delpuech, S. Green, Á. Avivar-Valderas, 2016, Molecular Cancer Therapeutics.

Targeting KRAS-dependent tumors with AZD4785, a high-affinity therapeutic antisense oligonucleotide inhibitor of KRAS

P. Lyne, B. Monia, D. Blakey, 2017, Science Translational Medicine.

PI3Kδ Forms Distinct Multiprotein Complexes at the TCR Signalosome in Naïve and Differentiated CD4+ T Cells

K. Okkenhaug, S. Barry, P. Hawkins, 2021, Frontiers in Immunology.

Modeling RAS Phenotype in Colorectal Cancer Uncovers Novel Molecular Traits of RAS Dependency and Improves Prediction of Response to Targeted Agents in Patients

Justin Guinney, Claus Bendtsen, Charles Ferté, 2013, Clinical Cancer Research.

Identification of DYRK1B as a substrate of ERK1/2 and characterisation of the kinase activity of DYRK1B mutants from cancer and metabolic syndrome

S. Cook, Mark Cockerill, T. Dunkley, 2015, Cellular and Molecular Life Sciences.

Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers.

S. Green, Rebecca P A Ellston, B. Barlaam, 2015, Bioorganic & medicinal chemistry letters.

Discovery of a novel aminopyrazine series as selective PI3Kα inhibitors.

S. Green, B. Barlaam, S. Cosulich, 2017, Bioorganic & medicinal chemistry letters.

PI3Kα/δ inhibition promotes anti-tumor immunity through direct enhancement of effector CD8+ T-cell activity

S. Barry, B. Sidders, K. Hudson, 2018, Journal of Immunotherapy for Cancer.

Amitai Etzioni Retrospective

Amitai Etzioni, K. Hudson, 2017 .

Identification of DYRK1B as a substrate of ERK1/2 and characterisation of the kinase activity of DYRK1B mutants from cancer and metabolic syndrome

S. Cook, Mark Cockerill, T. Dunkley, 2015, Cellular and Molecular Life Sciences.

Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis.

Mark Cockerill, J. Debreczeni, S. Guichard, 2015, Journal of medicinal chemistry.

Abstract 2830: Discovery of AZD8835, a potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment ofPIK3CA-dependent cancers

S. Green, R. Morgentin, S. Cosulich, 2015 .

Sensitivity to PI3K and AKT inhibitors is mediated by divergent molecular mechanisms in subtypes of DLBCL.

G. Ott, G. Lenz, S. Barry, 2017, Blood.