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Browsing publications by Dr Celine Cano.

Newcastle AuthorsTitleYearFull text
Dr Celine Cano
Professor Jane Endicott
Dr Ian Hardcastle
Dr Claire Jennings
Suzanne Kyle
et al.
Discovery of ASTX295, a potent, next-generation small molecule antagonist of MDM2 with differentiated pharmacokinetic profile2024
Dr Elaine Willmore
Suzanne Kyle
Dr Yan Zhao
Huw Thomas
Dr Kenneth Rankin
et al.
Targeting the MDM2-p53 interaction: Time- and concentration-dependent studies in tumor and normal human bone marrow cells reveal strategies for an enhanced therapeutic index2024
Nikol Zografou Barredo
Dr Alex Hallatt
Dr Jennyfer Goujon-Ricci
Dr Celine Cano
A beginner’s guide to current synthetic linker strategies towards VHL-recruiting PROTACs2023
Duncan Miller
Dr Suzannah Harnor
Dr Mathew Martin
Dr Richard Noble
Professor Steve Wedge
et al.
Modulation of ERK5 Activity as a Therapeutic Anti-Cancer Strategy2023
Dr Suzannah Harnor
Dr Celine Cano
Advanced approaches of developing targeted covalent drugs2022
Gemma Davison
Dr Mathew Martin
Dr Shannon Turberville
Selma Dormen
Dr Richard Heath
et al.
Mapping ligand interactions of bromodomains BRD4 and ATAD2 with FragLites and PepLites ─ Halogenated probes of druglike and peptide-like molecular interactions2022
Duncan Miller
Tristan Reuillon
Dr Lauren Molyneux
Dr Tim Blackburn
Dr Noel Edwards
et al.
Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor2022
Islam Al-Khawaldeh
Dr Christine Basmadjian
Dr Cinzia Bordoni
Dr Suzannah Harnor
Amy Heptinstall
et al.
An alkynylpyrimidine-based covalent inhibitor that targets a unique cysteine in NF-κB-inducing kinase (NIK)2021
Edwige Picazo
Amy Heptinstall
Dr Celine Cano
Emeritus Professor Bernard Golding
Professor Mike Waring
et al.
Cyclisations and fragmentations in the alkylation of 6-chloro-5-hydroxy-4-aminopyrimidines with aminoalkyl chlorides2021
Dr Ian Hardcastle
Dr Ruth Bawn
Dr Tim Blackburn
Dr Celine Cano
Dr Sarah Cully
et al.
Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein–Protein Interaction2021
Christopher Matheson
Christopher Coxon
Dr Benoit Carbain
Dr Ian Hardcastle
Dr Suzannah Harnor
et al.
2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase2020
Dr Brian Ford
Dr Shruti Chachra
Ahmed Alshawi
Alfie Brennan
Dr Suzannah Harnor
et al.
Chronic glucokinase activator treatment activates liver Carbohydrate response element binding protein and improves hepatocyte ATP homeostasis during substrate challenge2020
Dr Celine Cano
Molecular dynamics simulations reveal the determinants of cyclin-dependent kinase 2 inhibition by 5-nitrosopyrimidine derivatives2020
Dr Christine Basmadjian
Dr Celine Cano
Nek7 conformational flexibility and inhibitor binding probed through protein engineering of the R-spine2020
Dr Adam Potts
Dr Celine Cano
Professor Simon Thomas
Dr Simon Hill
Synthetic cannabinoid receptor agonists: classification and nomenclature2020
Daniel Wood
Daniel Lopez Fernandez
Leanne Knight
Islam Al-Khawaldeh
Dr Conghao Gai
et al.
FragLites - minimal, halogenated fragments displaying pharmacophore doublets. An efficient approach to druggability assessment and hit generation2019
Stephanie Myers
Duncan Miller
Dr Lauren Molyneux
Dr Mercedeh Arasta
Dr Ruth Bawn
et al.
Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD42019
Dr Catherine Willoughby
Huw Thomas
Dr Elaine Willmore
Suzanne Kyle
Dr Anita Wittner
et al.
Selective DNA-PKcs Inhibition Extends the Therapeutic Index of Localized Radiotherapy and Chemotherapy2019
Dr Simon Hill
Dr Michael Dunn
Dr Celine Cano
Dr Suzannah Harnor
Dr Ian Hardcastle
et al.
Human Toxicity Caused by Indole and Indazole Carboxylate Synthetic Cannabinoid Receptor Agonists: From Horizon Scanning to Notification2018
Duncan Miller
Dr Mathew Martin
Santosh Adhikari
Alfie Brennan
Professor Jane Endicott
et al.
Identification of a novel ligand for the ATAD2 bromodomain with selectivity over BRD4 through a fragment growing approach2018
Amy Heptinstall
Dr Celine Cano
Dr Ian Hardcastle
Recent advances in CDK inhibitors for cancer therapy2018
Dr Celine Cano
Dr Suzannah Harnor
Dr Elaine Willmore
Professor Steve Wedge
Targeting DNA-PK as a Therapeutic Approach in Oncology2018
Judith Unterlass
Dr Arnaud Basle
Dr Julie Tucker
Dr Celine Cano
Professor Martin Noble
et al.
Validating and enabling phosphoglycerate dehydrogenase (PHGDH) as a target for fragment-based drug discovery in PHGDH-amplified breast cancer2018
Christopher Coxon
Dr Suzannah Harnor
Dr Mathew Martin
Dr Benoit Carbain
Emeritus Professor Bernard Golding
et al.
Cyclin-Dependent Kinase (CDK) Inhibitors; Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines2017
Dr Suzannah Harnor
Alfie Brennan
Dr Celine Cano
Inhibition of the DNA-Dependent Protein Kinase for Cancer Therapy2017
Professor David Rees
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
Dr Celine Cano
Duncan Miller
et al.
ISOINDOLINONE INHIBITORS OF THE MDM2-P53 INTERACTION HAVING ANTICANCER ACTIVITY2017
Dr Suzannah Harnor
James Pickles
Dr Celine Cano
Modulation of the DNA-Damage Response by Inhibitors of the Phosphatidylinositol 3-Kinase Related Kinase (PIKK) Family2017
Professor David Rees
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
Dr Celine Cano
Duncan Miller
et al.
Preparation of isoindolinones as inhibitors of the MDM2-​p53 interaction having anticancer activity2017
Professor David Rees
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
Dr Celine Cano
Duncan Miller
et al.
Preparation of isoindolinones as inhibitors of the MDM2-​p53 interaction having anticancer activity;WO 20170558602017
Judith Unterlass
Dr Arnaud Basle
Dr Julie Tucker
Dr Celine Cano
Professor Martin Noble
et al.
Structural insights into the enzymatic activity and potential substrate promiscuity of human 3-phosphoglycerate dehydrogenase (PHGDH)2017
Dr Christopher Wong
Dr Ian Hardcastle
Christopher Matheson
Professor Herbie Newell
Dr Mangaleswaran Sivaprakasam
et al.
Structure-guided design of purine-based probes for selective Nek2 inhibition2017
Dr Suzannah Harnor
Alfie Brennan
Dr Celine Cano
Targeting DNA-Dependent Protein Kinase for Cancer Therapy2017
Christopher Coxon
Dr Celine Cano
Emeritus Professor Bernard Golding
Professor Roger Griffin
A new tool for the chemical genetic investigation of the Plasmodium falciparum Pfnek-2 NIMA-related kinase2016
Dr Gary Beale
Dr Emma Haagensen
Huw Thomas
Lan Wang
Charlotte Revill
et al.
Combined PI3K and CDK2 inhibition induces cell death and enhances in vivo anti-tumour activity in colorectal cancer2016
Dr Victorovich Zaytsev
James Pickles
Dr Suzannah Harnor
Dr Alistair Henderson
Mohammed Al Yasiri
et al.
Concise syntheses of bridged morpholines2016
Tristan Reuillon
Dr Sari Alhasan
Dr Gary Beale
Annalisa Bertoli
Alfie Brennan
et al.
Design and synthesis of biphenyl and biphenyl ether inhibitors of sulfatases2016
Stephanie Myers
Dr Ruth Bawn
Betty Cottyn
Dr Lauren Molyneux
Dr Celine Cano
et al.
High-throughput screening and hit validation of extracellular-related kinase 5 (ERK5) inhibitors2016
Tristan Reuillon
Duncan Miller
Stephanie Myers
Dr Lauren Molyneux
Dr Celine Cano
et al.
Pyrrolcarboxamide Derivatives for the Inhibition of ERK52016
Emeritus Professor Bernard Golding
Dr Celine Cano
Synthesis and Biological Evaluation of N2-Substituted 2,4-Diamino-6-cyclohexylmethoxy-5-nitrosopyrimidines and Related 5-Cyano-NNO-azoxy Derivatives as Cyclin-Dependent Kinase 2 (CDK2) Inhibitors2016
Elisa Meschini
Dr Regina Mora Vidal
Dr Mathew Martin
Dr Will Stanley
Tristan Reuillon
et al.
Identification and characterization of an irreversible inhibitor of CDK22015
Judith Unterlass
Nabila Aljufri
Sophie Bex
Dr Celine Cano
Professor Martin Noble
et al.
Towards structure-based drug design of 3-phosphoglycerate dehydrogenase inhibitors2015
Dr Benoit Carbain
Dr Allyson Campbell
Dr Celine Cano
Professor Jane Endicott
Emeritus Professor Bernard Golding
et al.
8-Substituted O-6-Cyclohexylmethylguanine CDK2 Inhibitors: Using Structure-Based Inhibitor Design to Optimize an Alternative Binding Mode2014
Honorine Lebraud
Emeritus Professor Bernard Golding
Elisa Meschini
Dr Celine Cano
Lan Wang
et al.
Anticancer agents targeted against cyclin-dependent kinase 2 (CDK2): Structure-based design of irreversible and reversible inhibitors2014
Dr Ruth Bawn
Tristan Reuillon
Emeritus Professor Bernard Golding
Professor Roger Griffin
Dr Ian Hardcastle
et al.
Development of extracellular signal-regulated kinase 5 (ERK5) inhibitors for anti-cancer therapy2014
Emily Mould
Philip Berry
Dr David Jamieson
Dr Chris Hill
Dr Celine Cano
et al.
Identification of dual DNA-PK MDR1 inhibitors for the potentiation of cytotoxic drug activity2014
Honorine Lebraud
Christopher Coxon
Vicky Archard
Carlo Bawn
Dr Benoit Carbain
et al.
Model system for irreversible inhibition of Nek2: thiol addition to ethynylpurines and related substituted heterocycles2014
Dr Susan Tudhope
Dr Yan Zhao
Dr Anita Wittner
Annalisa Bertoli
Santosh Adhikari
et al.
Profiling inhibitors of MDM2: p53 and MDMX: p53 in relation to MDMX protein levels2014
Dr Suzannah Harnor
Dr Tommy Rennison
Dr Martin Galler
Dr Celine Cano
Professor Roger Griffin
et al.
Synthesis of 3 '-deoxy-3'-fluorothymidine (FLT) 5 '-O-glucuronide: a reference standard for imaging studies with [18F]FLT2014
Dr Benoit Carbain
Christopher Coxon
Honorine Lebraud
Dr Kris Elliott
Christopher Matheson
et al.
Trifluoroacetic Acid in 2,2,2-Trifluoroethanol Facilitates SNAr Reactions of Heterocycles with Arylamines2014
Annalisa Bertoli
Santosh Adhikari
Dr Suzannah Harnor
Dr Yan Zhao
Professor John Lunec
et al.
Validation studies with small-molecule modulators of the MDM2/MDMX-p53 binding interaction2014
Dr Celine Cano
Dr Kappusamy Saravanan
Professor Nicola Curtin
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
et al.
1-Substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones Endowed with Dual DNA-PK PI3-K Inhibitory Activity2013
Dr Tommy Rennison
Sonsoles Rodriguez-Aristegui
Professor Nicola Curtin
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
et al.
Development of potent inhibitors of DNA-dependent protein kinase (DNA-PK)2013
Sarah Cully
Dr Celine Cano
Emeritus Professor Bernard Golding
Professor Roger Griffin
Professor John Lunec
et al.
Regiospecific synthesis of isoindolinones as MDM2 inhibitors2013
Dr Celine Cano
Professor Roger Griffin
The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design2013
Honorine Lebraud
Dr Celine Cano
Dr Benoit Carbain
Dr Ian Hardcastle
Dr Ross Harrington
et al.
Trifluoroethanol solvent facilitates selective N-7 methylation of purines2013
Dr Joanne Martin
Michael Batey
Dr Yan Zhao
Dr Celine Cano
Dr Michele Tavecchio
et al.
Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K2012
Dr Michele Tavecchio
Dr Joanne Martin
Dr Celine Cano
Professor Herbie Newell
Professor Nicola Curtin
et al.
Further characterisation of the cellular activity of the DNA-PK inhibitor, NU7441, reveals potential cross-talk with homologous recombination2012
Dr Tommy Rennison
Faye Craven
Emeritus Professor Bernard Golding
Professor Roger Griffin
Dr Karen Haggerty
et al.
Potent enantioselective inhibition of DNA-dependent protein kinase (DNA-PK) by atropisomeric chromenone derivatives2012
Dr Kate Smith
Emeritus Professor Bernard Golding
Elizabeth Griffin
Professor Roger Griffin
Dr Ian Hardcastle
et al.
DNA-dependent protein kinase (DNA-PK) inhibitors: Structure–activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain2011
Sonsoles Rodriguez-Aristegui
Dr Lauren Molyneux
Dr Celine Cano
Dr Marine Desage-El-Murr
Professor Roger Griffin
et al.
Versatile Synthesis of Functionalised Dibenzothiophenes via Suzuki Coupling and Microwave-assisted Ring Closure2011
Dr Celine Cano
Emeritus Professor Bernard Golding
Dr Karen Haggerty
Dr Ian Hardcastle
Professor Roger Griffin
et al.
Atropisomeric 8-arylchromen-4-ones exhibit enantioselective inhibition of the DNA-dependent protein kinase (DNA-PK)2010
Dr Kate Smith
Dr Tommy Rennison
Sonsoles Rodriguez-Aristegui
Professor Nicola Curtin
Emeritus Professor Bernard Golding
et al.
Development of potent inhibitors of DNA-dependent protein kinase (DNA-PK)2010
Dr Celine Cano
Dr Olivier Barbeau
Professor Nicola Curtin
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
et al.
DNA-Dependent Protein Kinase (DNA-PK) Inhibitors. Synthesis and Biological Activity of Quinolin-4-one and Pyridopyrimidin-4-one Surrogates for the Chromen-4-one Chemotype2010
Sara Payne
Sonsoles Rodriguez-Aristegui
Dr Celine Cano
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
et al.
Mapping the ATP-binding domain of DNA-dependent protein kinase (DNA-PK) with coumarin- and isocoumarin-derived inhibitors2010
Dr Benoit Carbain
Dr Celine Roche
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
Dr Celine Cano
et al.
Structure-based design of C8-substituted O6-alkylguanine CDK1 and 2 inhibitors2010
Dr Francesco Marchetti
Dr Celine Cano
Professor Nicola Curtin
Emeritus Professor Bernard Golding
Professor Roger Griffin
et al.
Synthesis and biological evaluation of 5-substituted O4-alkylpyrimidines as CDK2 inhibitors2010
Dr Celine Cano
Emeritus Professor Bernard Golding
Dr Ian Hardcastle
Professor Nicola Curtin
Professor Roger Griffin
et al.
8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK)2008
Dr Celine Cano
Professor Nicola Curtin
Emeritus Professor Bernard Golding
Dr Karen Haggerty
Dr Ian Hardcastle
et al.
Development of Potent Water-soluble Inhibitors of DNA-Dependent Protein Kinase (DNA-PK)2008
Dr Elaine Willmore
Dr sarah Johnson
Dr Tryfonia Mainou-Fowler
Professor Graham Jackson
Dr Celine Cano
et al.
DNA-dependent protein kinase is a therapeutic target and an indicator of poor prognosis in B-cell chronic lymphocytic leukemia2008
Dr Celine Cano
Five-membered rings with two adjacent heteroatoms with at least one other element2008
Dr Celine Cano
Five-membered rings with two non-adjacent heteroatoms with at least one other element2008
Dr Kappusamy Saravanan
Dr Celine Cano
Professor Nicola Curtin
Emeritus Professor Bernard Golding
Dr Karen Haggerty
et al.
Identification of potent water-soluble DNA-dependent protein kinase (DNA-PK) inhibitors using a small-molecule library approach [abstract]2008
Jonathan Hollick
Dr Laurent Rigoreau
Dr Celine Cano
Professor Nicola Curtin
Emeritus Professor Bernard Golding
et al.
Pyranone, thiopyranone, and pyridone inhibitors of phosphatidylinositol 3-kinase related kinases. Structure-activity relationships for DNA-dependent protein kinase inhibition, and identification of the first potent and selective inhibitor of the ataxia telangiectasia mutated kinase2007
Dr Olivier Barbeau
Dr Celine Cano
Professor Roger Griffin
Dr Ian Hardcastle
Professor William Clegg
et al.
Quinolinone and pyridopyrimidinone inhibitors of DNA-dependent protein kinase2007
Dr Celine Cano
A bis(η5-cyclopentadienyl)cobalt complex of a bis-dithiolene: a chemical analogue of the metal centres of the DMSO reductase family of molybdenum and tungsten enzymes, in particular ferredoxin aldehyde oxidoreductase2005
Dr Celine Cano
Regio- and Enantioselective Synthesis of Novel Functionalized Pyranopyrrolidines by 1,3-Dipolar Cycloaddition of Carbohydrates2005
Dr Celine Cano
Stereoselective Cycloaddition on Carbohydrates for the Synthesis of New Bicyclic Oxazolidines Bearing a Quaternary Bridgehead2005