Céline Cano

发表

Structural insights into the enzymatic activity and potential substrate promiscuity of human 3-phosphoglycerate dehydrogenase (PHGDH)

M. Noble, N. Curtin, J. Tucker, 2017, Oncotarget.

Validating and enabling phosphoglycerate dehydrogenase (PHGDH) as a target for fragment-based drug discovery in PHGDH-amplified breast cancer.

M. Noble, N. Curtin, J. Tucker, 2016, Oncotarget.

Cyclin-Dependent Kinase (CDK) Inhibitors: Structure–Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines

M. Noble, J. Endicott, I. Hardcastle, 2016, Journal of medicinal chemistry.

Identification of dual DNA-PK MDR1 inhibitors for the potentiation of cytotoxic drug activity.

D. Jamieson, C. Hill, B. Durkacz, 2014, Biochemical pharmacology.

A beginner's guide to current synthetic linker strategies towards VHL-recruiting PROTACs.

Céline Cano, Nikol A. Zografou-Barredo, Alex J. Hallatt, 2023, Bioorganic & medicinal chemistry.

Structure-guided design of purine-based probes for selective Nek2 inhibition

I. Hardcastle, R. Griffin, B. Golding, 2016, Oncotarget.

Synthetic cannabinoid receptor agonists: classification and nomenclature

S. H. Thomas, C. Cano, S. Thomas, 2020, Clinical toxicology.

Recent advances in CDK inhibitors for cancer therapy.

I. Hardcastle, C. Cano, Amy B Heptinstall, 2018, Future medicinal chemistry.

Advanced approaches of developing targeted covalent drugs.

Qingjie Zhao, Conghao Gai, C. Cano, 2022, RSC medicinal chemistry.

Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4.

M. Noble, J. Endicott, S. Cook, 2019, European journal of medicinal chemistry.

Nek7 conformational flexibility and inhibitor binding probed through protein engineering of the R-spine

M. Byrne, K. Carr, R. Bayliss, 2020, The Biochemical journal.

Selective DNA-PKcs inhibition extends the therapeutic index of localized radiotherapy and chemotherapy

A. Ryan, H. Reeves, S. Wedge, 2019, The Journal of clinical investigation.

Inhibition of the DNA-Dependent Protein Kinase for Cancer Therapy

C. Cano, S. Harnor, Alfie Brennan, 2017 .

1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity.

N. Curtin, I. Hardcastle, R. Griffin, 2013, Journal of medicinal chemistry.

Chemosensitization of Cancer Cells by KU-0060648, a Dual Inhibitor of DNA-PK and PI-3K

N. Curtin, R. Griffin, Yan Zhao, 2011, Molecular Cancer Therapeutics.

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 chemotype.

N. Curtin, I. Hardcastle, R. Griffin, 2010, Journal of medicinal chemistry.

Further characterisation of the cellular activity of the DNA-PK inhibitor, NU7441, reveals potential cross-talk with homologous recombination

N. Curtin, D. Newell, C. Cano, 2011, Cancer Chemotherapy and Pharmacology.

Identification and Characterization of an Irreversible Inhibitor of CDK2

M. Noble, J. Endicott, D. Staunton, 2015, Chemistry & biology.

Cyclin-Dependent Kinase (CDK) Inhibitors: Structure–Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines

M. Noble, J. Endicott, I. Hardcastle, 2016, Journal of medicinal chemistry.

Combined PI3K and CDK2 inhibition induces cell death and enhances in vivo antitumour activity in colorectal cancer

I. Hardcastle, R. Griffin, B. Golding, 2016, British Journal of Cancer.

8-Substituted O(6)-cyclohexylmethylguanine CDK2 inhibitors: using structure-based inhibitor design to optimize an alternative binding mode.

D. Paterson, M. Noble, J. Endicott, 2014, Journal of medicinal chemistry.

Identification and characterization of an irreversible inhibitor of CDK 2

M. Noble, J. Endicott, D. Staunton, 2017 .

2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase

I. Hardcastle, R. Griffin, B. Golding, 2020, RSC medicinal chemistry.

Targeting DNA-PK as a Therapeutic Approach in Oncology

S. Wedge, C. Cano, E. Willmore, 2018 .

Chronic glucokinase activator treatment activates liver Carbohydrate response element binding protein and improves hepatocyte ATP homeostasis during substrate challenge

David M. Smith, L. Agius, C. Cano, 2020, Diabetes, obesity & metabolism.

A new tool for the chemical genetic investigation of the Plasmodium falciparum Pfnek-2 NIMA-related kinase

A. Tobin, R. Griffin, B. Golding, 2016, Malaria Journal.

Trifluoroethanol solvent facilitates selective N-7 methylation of purines.

I. Hardcastle, R. Griffin, B. Golding, 2013, Organic & biomolecular chemistry.

FragLites-Minimal, Halogenated Fragments Displaying Pharmacophore Doublets. An Efficient Approach to Druggability Assessment and Hit Generation.

M. Noble, J. Endicott, M. Waring, 2019, Journal of medicinal chemistry.

Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor

M. Noble, J. Endicott, S. Cook, 2022, Journal of medicinal chemistry.

Mapping Ligand Interactions of Bromodomains BRD4 and ATAD2 with FragLites and PepLites—Halogenated Probes of Druglike and Peptide-like Molecular Interactions

M. Noble, J. Endicott, I. Hardcastle, 2022, Journal of medicinal chemistry.

Chemosensitization of Cancer Cells by KU-0060648, a Dual Inhibitor of DNA-PK and PI-3K

N. Curtin, R. Griffin, Yan Zhao, 2012, Molecular Cancer Therapeutics.

Modulation of ERK5 Activity as a Therapeutic Anti-Cancer Strategy.

S. Wedge, Duncan C Miller, S. Harnor, 2023, Journal of medicinal chemistry.

High-Throughput Screening and Hit Validation of Extracellular-Related Kinase 5 (ERK5) Inhibitors.

I. Hardcastle, R. Griffin, B. Golding, 2016, ACS combinatorial science.

Targeting DNA‐Dependent Protein Kinase for Cancer Therapy

S. Harnor, Alfie Brennan, Céline Cano, 2017, ChemMedChem.

The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design

R. V. van Montfort, P. Workman, R. Griffin, 2013, Oncotarget.

Modulation of the DNA-Damage Response by Inhibitors of the Phosphatidylinositol 3-Kinase Related Kinase (PIKK) Family

C. Cano, S. Harnor, James E. Pickles, 2017 .

An Alkynylpyrimidine-Based Covalent Inhibitor That Targets a Unique Cysteine in NF-κB-Inducing Kinase.

M. Noble, J. Endicott, M. Waring, 2021, Journal of medicinal chemistry.

Potent enantioselective inhibition of DNA-dependent protein kinase (DNA-PK) by atropisomeric chromenone derivatives.

I. Hardcastle, R. Griffin, B. Golding, 2012, Organic & biomolecular chemistry.

DNA-dependent protein kinase (DNA-PK) inhibitors: structure-activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain.

I. Hardcastle, R. Griffin, B. Golding, 2011, Bioorganic & medicinal chemistry letters.

Atropisomeric 8-arylchromen-4-ones exhibit enantioselective inhibition of the DNA-dependent protein kinase (DNA-PK).

I. Hardcastle, R. Griffin, B. Golding, 2010, Organic & biomolecular chemistry.

8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK).

N. Curtin, I. Hardcastle, R. Griffin, 2008, Bioorganic & medicinal chemistry letters.

Trifluoroacetic acid in 2,2,2-trifluoroethanol facilitates S(N)Ar reactions of heterocycles with arylamines.

I. Hardcastle, R. Griffin, B. Golding, 2014, Chemistry.

Versatile synthesis of functionalised dibenzothiophenes via Suzuki coupling and microwave-assisted ring closure.

I. Hardcastle, R. Griffin, B. Golding, 2011, Organic & biomolecular chemistry.

Mapping the ATP-binding domain of DNA-dependent protein kinase (DNA-PK) with coumarin- and isocoumarin-derived inhibitors.

I. Hardcastle, R. Griffin, B. Golding, 2010, Bioorganic & medicinal chemistry letters.

Identiﬁcation and Characterization of an Irreversible Inhibitor of CDK2

M. Noble, J. Endicott, M. Geitmann, 2022 .