Background

Background

Celine Cano is a Reader in Medicinal Chemistry at Newcastle University. She graduated from the University of Poitiers, receiving her Ph.D. in 2004 for her work on the synthesis of biomolecules by 1,3-dipolar cycloadditions with carbohydrates. In 2004, she carried out post-doctoral work in the group of Professor John A. Joule at the University of Manchester working on the synthesis of analogues of cofactors of oxomolybdoenzymes. In 2005 she joined the Northern Institute for Cancer Research at Newcastle University as a research fellow, working on the synthesis of inhibitors of the DNA-dependent protein kinase (DNA-PK). She was appointed to a lectureship in Medicinal Chemistry at Newcastle University in 2008 and has since played a key role in helping to establish Newcastle as an internationally recognised centre for anti-cancer drug discovery. Celine was awarded the Elsevier Reaxys 2016 Prize for Medicinal Chemistry in recognition of her research into anticancer drug discovery. 

She is the academic lead for the Medicinal Chemistry and Chemical Biology Group within the School of Natural and Environmental Sciences.

Qualifications

• 2000-2004 University of Poitiers University (France) – PhD in Organic Chemistry
• 1999-2000  University of Poitiers (France) – MRes in Chemistry
• 1995-1998  University of Poitiers (France) – MChem in Chemistry

Previous Positions

• 2013-2017 Senior Lecturer, School of Chemistry, Northern Institute of Cancer Research, Newcastle University
• 2008-2013 Lecturer, Northern Institute of Cancer Research, Newcastle University
• 2005-2007 Research Fellow, Northern Institute of Cancer Research, Newcastle University
• 2004-2005 Research Associate, Chemistry Department, The University of Manchester

Area of Expertise

Medicinal Chemistry and Chemical Biology

Memberships

• Fellow of the Royal Society of Chemistry.
• Member of the British Association for Cancer Research and the European Association for Cancer Research.

ORCID iD: 0000-0002-2032-2272;    Google Scolar;    Scopus Author iD: 24480527500 

Research

Current Funding and Collaborations: 

• 2018-2020       MRC DPFS Drug discovery award.  Lead PIs, S. Wedge (Pharmacology), C. Cano (Chemistry), M.E.M. Noble and J.A. Endicott (Structural Biology) 
• 2015-2020       CRUK Programme Grant. Lead PIs, S. Wedge, M. Waring, M.E.M. Noble, J.A. Endicott, I. Hardcastle, and C. Cano, “The Cancer Research UK Programme for Drug Discovery at the Northern Institute for Cancer Research, Newcastle University”
• 2012-2017       Astex Strategic Drug Discovery Alliance (Astex Pharmaceuticals, Newcastle University and CRT) Lead PIs (Newcastle): C. Cano, J.A. Endicott, R.J. Griffin, I.R. Hardcastle, R. Maxwell, M. Waring, M.E.M. Noble and S. Wedge

Teaching

Stage 1 

• CHY1101 Organic Chemistry Tutorials

Stage 2

• Module leader of CHY2103 Medicinal Chemistry and Drug Design

Stage 3

• CHY3109/CHY3110 Advanced Medicinal Chemistry (Semester 1) - Chemical Biology
• CHY3109/CHY3110 Advanced Medicinal Chemistry (Semester 2) - Chemotherapy
• CHY3109 Advanced Laboratory Course in Medicinal Chemistry
• CHY3011 Research Literature projects

Stage 4

• CHY8821 Methods in Drug Discovery
• CHY8823 Theory and Practice of Chemotherapy
• CHY8411 MChem lab placement

 Teaching Administration

• Module leader for 3 modules as part of our Chemistry with Medicinal Chemistry BSc and MChem Honours degrees (CHY2103, CHY3109 and CHY3110)
• Module leader for 1 module as part of our MSc in Drug Chemistry (CHY8823)
• Member of the Northern Institute for Cancer Research Teaching and Training Committee (2009-present)
• Member of the School of Chemistry Teaching and Training Committee (2014-2016)

Publications

• Articles

  • Miller DC, Reuillon T, Molyneux L, Blackburn T, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hardcastle I, Harnor SJ, Heptinstall A, Lochhead P, Martin MP, Martin NC, Myers S, Newell DR, Noble RA, Phillips N, Rigoreau L, Thomas H, Tucker JA, Wang L-Z, Waring MJ, Wong A-C, Wedge SR, Noble MEM, Cano C. Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor. Journal of Medicinal Chemistry 2022, 65(9), 6513-6540.
  • Davison G, Martin MP, Turberville S, Dormen S, Heath R, Heptinstall AB, Lawson M, Miller DC, Ng YM, Sanderson JN, Hope I, Wood DJ, Cano C, Endicott JA, Hardcastle IR, Noble MEM, Waring MJ. Mapping ligand interactions of bromodomains BRD4 and ATAD2 with FragLites and PepLites ─ Halogenated probes of druglike and peptide-like molecular interactions. Journal of Medicinal Chemistry 2022, 65(22), 15416-15432.
  • Gai C, Harnor SJ, Zhang S, Cano C, Zhuang C, Zhao Q. Advanced approaches of developing targeted covalent drugs. RSC Medicinal Chemistry 2022, 13(12), 1460-1475.
  • Chessari G, Hardcastle IR, Ahn JS, Anil B, Anscome E, Bawn RH, Bevan LD, Blackburn TJ, Buck I, Cano C, Carbain B, Castro J, Cons B, Cully SJ, St Denis J, Endicott JA, Fazal L, Golding BT, Griffin RJ, Haggerty K, Harnor S, Hearn K, Hobson S, Holvey RS, Howard S, Jennings C, Johnson CN, Lunec J, Miller DC, Newell DR, Noble MEM, Reeks J, Revill CH, Riedinger C, Tamanini E, Thomas H, Thompson NT, Vinkovic M, Wedge SR, Williams PA, Wilsher N, Zhang B, Zhao Y. Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein–Protein Interaction. Journal of Medicinal Chemistry 2021, 64(7), 4071-4088.
  • Picazo EMH, Heptinstall AB, Wilson DM, Cano C, Golding BT, Waring MJ. Cyclisations and fragmentations in the alkylation of 6-chloro-5-hydroxy-4-aminopyrimidines with aminoalkyl chlorides. Journal of Heterocyclic Chemistry 2021, 58(4), 947-951.
  • Al-Khawaldeh I, Aldred GG, Alyassiri M, Basmadjian C, Bordoni C, Harnor SJ, Heptinstall AB, Hobson SJ, Jennings CE, Khalifa S, Lebraud H, Miller DC, Shrives HJ, de Souza JV, Stewart HL, Temple M, Totobenazara J, Tucker JA, Tudhope SJ, Wang LZ, Bronowska AK, Cano C, Endicott JA, Golding BT, Hardcastle IR, Hickson I, Wedge SR, Willmore E, Noble MEM, Waring MJ. An alkynylpyrimidine-based covalent inhibitor that targets a unique cysteine in NF-κB-inducing kinase (NIK). Journal of Medicinal Chemistry 2021, 64(14), 10001-10018.
  • Byrne MJ, Nasir N, Basmadjian C, Bhatia C, Cunnison RF, Carr KH, Mas-Droux C, Yeoh S, Cano C, Bayliss R. Nek7 conformational flexibility and inhibitor binding probed through protein engineering of the R-spine. Biochemical Journal 2020, 477(8), 1525-1539.
  • Ford BE, Chachra SS, Alshawi A, Brennan A, Harnor S, Cano C, Baker DJ, Smith DM, Fairclough RJ, Agius L. Chronic glucokinase activator treatment activates liver Carbohydrate response element binding protein and improves hepatocyte ATP homeostasis during substrate challenge. Diabetes, Obesity and Metabolism 2020, 22(11), 1985-1994.
  • Matheson CJ, Coxon CR, Bayliss R, Boxall K, Carbain B, Fry AM, Hardcastle IR, Harnor SJ, Mas-Droux C, Newell DR, Richards MW, Sivaprakasam M, Turner D, Griffin RJ, Golding BT, Cano C. 2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase. RSC Medicinal Chemistry 2020, 11(6), 707-731.
  • Willoughby CE, Jiang Y, Thomas HD, Willmore E, Kyle S, Wittner A, Phillips N, Zhao Y, Tudhope SJ, Prendergast L, Junge G, Lourenco LM, Finlay MRV, Turner P, Munck JM, Griffin RJ, Rennison T, Pickles J, Cano C, Newell DR, Reeves HL, Ryan AJ, Wedge SR. Selective DNA-PKcs Inhibition Extends the Therapeutic Index of Localized Radiotherapy and Chemotherapy. Journal of Clinical Investigation 2019, 130, 1-14.
  • Myers SM, Miller DC, Molyneux L, Arasta M, Bawn RH, Blackburn TJ, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hammonds T, Hardcastle IR, Harnor SJ, Heptinstall AB, Lochhead PA, Martin MP, Martin NC, Newell DR, Owen PJ, Pang LC, Reuillon T, Rigoreau LJM, Thomas HD, Tucker JA, Wang L-Z, Wong A-C, Noble MEM, Wedge SR, Cano C. Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4. European Journal of Medicinal Chemistry 2019, 178, 530-543.
  • Wood D, Lopez-Fernandez JD, Knight LE, Al-Khawaldeh I, Gai C, Lin S, Martin MP, Miller DC, Cano C, Endicott JA, Hardcastle IR, Noble MEM, Waring MJ. FragLites - minimal, halogenated fragments displaying pharmacophore doublets. An efficient approach to druggability assessment and hit generation. Journal of Medicinal Chemistry 2019, 62(7), 3741-3752.
  • Unterlass JE, Baslé A, Blackburn TJ, Tucker J, Turlais F, Cano C, Noble MME, Curtin NJ. Validating and enabling phosphoglycerate dehydrogenase (PHGDH) as a target for fragment-based drug discovery in PHGDH-amplified breast cancer. Oncotarget 2018, 9, 13139-13153.
  • Miller DC, Martin MP, Adhikari S, Brennan A, Endicott JA, Golding BT, Hardcastle IR, Heptinstall A, Hobson S, Jennings C, Molyneux L, Ng Y, Wedge SR, Noble MEM, Cano C. Identification of a novel ligand for the ATAD2 bromodomain with selectivity over BRD4 through a fragment growing approach. Organic and Biomolecular Chemistry 2018, 16(11), 1843-1850.
  • Hill SL, Dunn M, Cano C, Harnor SJ, Hardcastle IR, Grundlingh J, Dargan PI, Wood DM, Tucker S, Bartram T, Thomas SHL. Human Toxicity Caused by Indole and Indazole Carboxylate Synthetic Cannabinoid Receptor Agonists: From Horizon Scanning to Notification. Clinical Chemistry 2018, 64(2), 346-354.
  • Harnor S, Brennan A, Cano C. Targeting DNA-Dependent Protein Kinase for Cancer Therapy. ChemMedChem 2017, 12(12), 895-900.
  • Coxon RC, Wong C, Bayliss R, Boxall K, Carr KH, Fry AM, Hardcastle IR, Matheson CJ, Newell DR, Sivaprakasam M, Thomas H, Turner D, Yeoh S, Wang LZ, Griffin RJ, Golding BT, Cano C. Structure-guided design of purine-based probes for selective Nek2 inhibition. Oncotarget 2017, 8, 19089-19124.
  • Unterlass JE, Wood RJ, Basle A, Tucker J, Cano C, Noble MM, Curtin NJ. Structural insights into the enzymatic activity and potential substrate promiscuity of human 3-phosphoglycerate dehydrogenase (PHGDH). Oncotarget 2017, 8(61), 104478-104491.
  • Harnor SJ, Brennan A, Cano C. Inhibition of the DNA-Dependent Protein Kinase for Cancer Therapy. Medicinal Chemistry 2017, 7, 172-177.
  • Coxon C, Anscombe E, Harnor S, Martin M, Carbain B, Golding B, Hardcastle I, Harlow L, Korolchuk S, Matheson C, Newell D, Noble M, Sivaprakasam M, Tudhope SJ, Turner D, Wang L, Wedge SR, Wong C, Griffin R, Endicott J, Cano C. Cyclin-Dependent Kinase (CDK) Inhibitors; Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines. Journal of Medicinal Chemistry 2017, 60, 1746-1767.
  • Cortese D, Konstantin C, Guglielmo S, Wang LZ, Golding BT, Cano C, Fruttero R. 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) Inhibitors. ChemMedChem 2016, 11(6), 1705-1708.
  • Myers SM, Bawn RH, Bisset LC, Blackburn TJ, Cottyn B, Molyneux L, Wong AC, Cano C, Clegg W, Harrington RW, Leung H, Rigoreau L, Vidot S, Golding BT, Griffin RJ, Hammonds T, Newell DR, Hardcastle IR. High-throughput screening and hit validation of extracellular-related kinase 5 (ERK5) inhibitors. ACS Combinatorial Science 2016, 18(8), 444-455.
  • Reuillon T, Alhasan SF, Beale GS, Bertoli A, Brennan A, Cano C, Reeves HL, Newell DR, Golding BT, Miller DC, Griffin RJ. Design and synthesis of biphenyl and biphenyl ether inhibitors of sulfatases. Chemical Science 2016, 7(4), 2821-2826.
  • Zaytsev AV, Pickles JE, Harnor SJ, Henderson AP, Alyasiri M, Waddell PG, Cano C, Griffin RJ, Golding BT. Concise syntheses of bridged morpholines. RSC Advances 2016, 6(59), 53955-53957.
  • Beale G, Haagensen E, Thomas H, Wang LZ, Revill C, Payne S, Golding BT, Hardcastle IR, Newell DR, Griffin RJ, Cano C. Combined PI3K and CDK2 inhibition induces cell death and enhances in vivo anti-tumour activity in colorectal cancer. British Journal of Cancer 2016, 115, 682-690.
  • Mitcheson DF, Bottrill AR, Carr K, Coxon CR, Cano C, Golding BT, Griffin RJ, Fry AM, Doerig C, Bayliss R, Tobin AB. A new tool for the chemical genetic investigation of the Plasmodium falciparum Pfnek-2 NIMA-related kinase. Malaria Journal 2016, 15, 535.
  • Anscombe E, Meschini E, Mora-Vidal R, Martin MP, Staunton D, Geitmann M, Danielson UH, Stanley WA, Wang LZ, Reuillon T, Golding BT, Cano C, Newell DR, Noble MEM, Wedge SR, Endicott JA, Griffin RJ. Identification and characterization of an irreversible inhibitor of CDK2. Chemistry & Biology 2015, 22(9), 1159-1164.
  • Carbain B, Coxon CR, Lebraud H, Elliott KJ, Matheson CJ, Meschini E, Roberts AR, Turner DM, Wong C, Cano C, Griffin RJ, Hardcastle IR, Golding BT. Trifluoroacetic Acid in 2,2,2-Trifluoroethanol Facilitates S_NAr Reactions of Heterocycles with Arylamines. Chemistry: A European Journal 2014, 20(8), 2311-2317.
  • Harnor SJ, Rennison T, Galler M, Cano C, Griffin RJ, Newell DR, Golding BT. Synthesis of 3 '-deoxy-3'-fluorothymidine (FLT) 5 '-O-glucuronide: a reference standard for imaging studies with [¹⁸F]FLT. MedChemComm 2014, 5(7), 984-988.
  • Lebraud H, Coxon CR, Archard VS, Bawn CM, Carbain B, Matheson CJ, Turner DM, Cano C, Griffin RJ, Hardcastle IR, Baisch U, Harrington RW, Golding BT. Model system for irreversible inhibition of Nek2: thiol addition to ethynylpurines and related substituted heterocycles. Organic & Biomolecular Chemistry 2014, 12, 141-148.
  • Mould E, Berry P, Jamieson D, Hill C, Cano C, Tan N, Elliott S, Durkacz B, Newell D, Willmore E. Identification of dual DNA-PK MDR1 inhibitors for the potentiation of cytotoxic drug activity. Biochemical Pharmacology 2014, 88(1), 58-65.
  • Carbain B, Paterson DJ, Anscombe E, Campbell AJ, Cano C, Echalier A, Endicott JA, Golding BT, Haggerty K, Hardcastle IR, Jewsbury PJ, Newell DR, Noble MEM, Roche C, Wang LZ, Griffin RJ. 8-Substituted O-6-Cyclohexylmethylguanine CDK2 Inhibitors: Using Structure-Based Inhibitor Design to Optimize an Alternative Binding Mode. Journal of Medicinal Chemistry 2014, 57(1), 56-70.
  • Lebraud H, Cano C, Carbain B, Hardcastle IR, Harrington RW, Griffin RJ, Golding BT. Trifluoroethanol solvent facilitates selective N-7 methylation of purines. Organic & Biomolecular Chemistry 2013, 11(11), 1874-1878.
  • Couty S, Westwood I, Kalusa A, Cano C, Travers J, Boxall K, Chow C, Burns S, Schmitt J, Pickard P, Barillari C, McAndrew C, Clarke P, Linardopoulos S, Griffin R, Aherne W, Raynaud F, Workman P, Jones K, Montfort R. The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design. Oncotarget 2013, 4(10), 1647-1661.
  • Cano C, Saravanan K, Bailey C, Bardos J, Curtin NJ, Frigerio M, Golding BT, Hardcastle IR, Hummersone MG, Menear KA, Newell DR, Richardson CJ, Shea K, Smith GCM, Thommes P, Ting A, Griffin RJ. 1-Substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones Endowed with Dual DNA-PK PI3-K Inhibitory Activity. Journal of Medicinal Chemistry 2013, 56(16), 6386-6401.
  • Clapham KM, Rennison T, Jones G, Craven F, Bardos J, Golding BT, Griffin RJ, Haggerty K, Hardcastle IR, Thommes P, Ting A, Cano C. Potent enantioselective inhibition of DNA-dependent protein kinase (DNA-PK) by atropisomeric chromenone derivatives. Organic & Biomolecular Chemistry 2012, 10(33), 6747-6757.
  • Tavecchio M, Munck JM, Cano C, Newell DR, Curtin NJ. Further characterisation of the cellular activity of the DNA-PK inhibitor, NU7441, reveals potential cross-talk with homologous recombination. Cancer Chemotherapy and Pharmacology 2012, 69(1), 155-164.
  • Munck JM, Batey MA, Zhao Y, Jenkins H, Richardson C, Cano C, Tavecchio M, Barbeau J, Bardos J, Cornell L, Griffin RJ, Menear KA, Slade A, Thommes P, Martin NMB, Newell DR, Smith GCM, Curtin NJ. Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K. Molecular Cancer Therapeutics 2012, 11(8), 1789-1798.
  • Rodriguez SA, Clapham KM, Barrett L, Cano C, Desage ME, Griffin RJ, Hardcastle IR, Payne SL, Rennison T, Richardson C, Golding BT. Versatile Synthesis of Functionalised Dibenzothiophenes via Suzuki Coupling and Microwave-assisted Ring Closure. Organic & Biomolecular Chemistry 2011, 9(17), 6066-6074.
  • Clapham KM, Bardos J, Finlay R, Golding BT, Griffen EJ, Griffin RJ, Hardcastle IR, Menear KA, Ting A, Turner P, Young GL, Cano C. DNA-dependent protein kinase (DNA-PK) inhibitors: Structure–activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain. Bioorganic & Medicinal Chemistry Letters 2011, 21(3), 966-970.
  • Marchetti F, Cano C, Curtin NJ, Golding BT, Griffin RJ, Haggerty K, Newell DR, Parsons RJ, Payne SL, Wang LZ, Hardcastle IR. Synthesis and biological evaluation of 5-substituted O⁴-alkylpyrimidines as CDK2 inhibitors. Organic & Biomolecular Chemistry 2010, 8(10), 2397-2407.
  • Payne SL, Rodriguez-Aristegui S, Bardos J, Cano C, Golding BT, Hardcastle IR, Peacock M, Parveen N, Griffin RJ. Mapping the ATP-binding domain of DNA-dependent protein kinase (DNA-PK) with coumarin- and isocoumarin-derived inhibitors. Bioorganic & Medicinal Chemistry Letters 2010, 20(12), 3649-3653.
  • Cano C, Barbeau OR, Bailey C, Cockcroft XL, Curtin NJ, Duggan H, Frigerio M, Golding BT, Hardcastle IR, Hummersone MG, Knights C, Menear KA, Newell DR, Richardson CJ, Smith GC, Spittle B, Griffin RJ. 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. Journal of Medicinal Chemistry 2010, 53(24), 8498-8507.
  • Cano C, Golding BT, Haggerty K, Hardcastle IR, Peacock M, Griffin RJ. Atropisomeric 8-arylchromen-4-ones exhibit enantioselective inhibition of the DNA-dependent protein kinase (DNA-PK). Organic & Biomolecular Chemistry 2010, 8(8), 1922-1928.
  • Willmore E, Elliott SL, Mainou-Fowler T, Summerfield GP, Jackson GH, O'Neill F, Lowe C, Carter A, Harris R, Pettitt AR, Cano-Soumillac C, Griffin RJ, Cowell IG, Austin CA, Durkacz BW. DNA-dependent protein kinase is a therapeutic target and an indicator of poor prognosis in B-cell chronic lymphocytic leukemia. Clinical Cancer Research 2008, 14(12), 3984-3992.
  • Murr M, Cano C, Golding BT, Hardcastle IR, Hummersome M, Frigerio M, Curtin NJ, Menear K, Richardson C, Smith G, Griffin R. 8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK). Bioorganic and Medicinal Chemistry Letters 2008, 18(17), 4885-4890.
  • Barbeau OR, Cano-Soumillac C, Griffin RJ, Hardcastle IR, Smith GCM, Richardson C, Clegg W, Harrington RW, Golding BT. Quinolinone and pyridopyrimidinone inhibitors of DNA-dependent protein kinase. Organic & Biomolecular Chemistry 2007, 5(16), 2670-2677.
  • Hollick J, Rigoreau L, Cano-Soumillac C, Cockcroft X, Curtin NJ, Frigerio M, Golding BT, Guiard S, Hardcastle IR, Hickson I, Hummersone M, Menear K, Martin N, Matthews I, Newell DR, Ord R, Richardson C, Smith G, Griffin RJ. 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 kinase. Journal of Medicinal Chemistry 2007, 50(8), 1958-1972.
  • Bashiardes G, Cano C, Mauzé B. Stereoselective Cycloaddition on Carbohydrates for the Synthesis of New Bicyclic Oxazolidines Bearing a Quaternary Bridgehead. Synlett 2005, (9), 1425-1428.
  • Bashiardes G, Cano C, Mauzé B. Regio- and Enantioselective Synthesis of Novel Functionalized Pyranopyrrolidines by 1,3-Dipolar Cycloaddition of Carbohydrates. Synlett 2005, (4), 587-590.
  • Alphonse F-A, Karim R, Cano-Soumillac C, Hebray M, Collison D, Garner CD, Joule JA. 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 oxidoreductase. Tetrahedron 2005, 61(46), 11010-11019.

• Book Chapters

  • Cano C, Harnor SJ, Willmore E, Wedge SR. Targeting DNA-PK as a Therapeutic Approach in Oncology. In: Pollard J; Curtin N, ed. Targeting the DNA Damage Response for Anti-Cancer Therapy. New York: Humana Press Inc, 2018, pp.339-357.
  • Harnor S, Pickles J, Cano C. Modulation of the DNA-Damage Response by Inhibitors of the Phosphatidylinositol 3-Kinase Related Kinase (PIKK) Family. In: Waring M, ed. Topics in Medicinal Chemistry. Springer, 2017, pp.1-38.

• Conference Proceedings (inc. Abstracts)

  • Unterlass JE, Aljufri N, Bex S, Cano C, Noble MEM, Curtin NJ. Towards structure-based drug design of 3-phosphoglycerate dehydrogenase inhibitors. In: AACR 106th Annual Meeting 2015. 2015, Philadelphia, PA, USA: American Association for Cancer Research.
  • Bertoli A, Adhikari S, Harnor SJ, Zhao Y, Lunec J, Wedge SR, Tudhope S, Wittner A, Golding BT, Hardcastle IR, Cano C, Newell DR, Griffin RJ. Validation studies with small-molecule modulators of the MDM2/MDMX-p53 binding interaction. In: 247th ACS National Meeting and Exposition. 2014, Dallas, TX, USA: American Chemical Society.
  • Tudhope S, Zhao Y, Wittner A, Wilmore E, Bertoli A, Adhikari S, Harnor SJ, Del Bello F, Piergentili A, Lunec J, Hardcastle IR, Griffin RJ, Golding BR, Cano C, Newell DR, Wedge SR. Profiling inhibitors of MDM2: p53 and MDMX: p53 in relation to MDMX protein levels. In: AACR Annual Meeting 2014. 2014, San Diego, CA: American Association for Cancer Research.
  • Myers S, Martin N, Bawn R, Blackburn T, Barrett L, Reuillon T, Golding B, Griffin R, Hammonds T, Hardcastle I, Leung H, Newell D, Rigoreau L, Wong A, Cano C. Development of extracellular signal-regulated kinase 5 (ERK5) inhibitors for anti-cancer therapy. In: 26th EORTC – NCI – AACR Symposium on Molecular Targets and Cancer Therapeutics. 2014, Barcelona, Spain: Elsevier.
  • Lebraud H, Golding BT, Meschini E, Cano C, Anscombe E, Wang LZ, Endicott JA, Noble MEM, Newell DR, Griffin RJ. Anticancer agents targeted against cyclin-dependent kinase 2 (CDK2): Structure-based design of irreversible and reversible inhibitors. In: 247th ACS National Meeting and Exposition. 2014, Dallas, Texas: American Chemical Society.
  • Cully SJ, Blackburn TJ, Cano C, Golding BT, Griffin RJ, Lunec J, Newell D, Noble M, Zhao Y, Hardcastle IR. Regiospecific synthesis of isoindolinones as MDM2 inhibitors. In: 245th ACS National Meeting and Exposition. 2013, New Orleans, Louisiana: American Chemical Society.
  • Barrett L, Rennison T, Clapham KM, Rodriguez-Aristegui S, Bardos J, Curtin NJ, Dennis M, Finlay R, Golding BT, Hardcastle IR, Newell DR, Young G, Cano C, Griffin RJ. Development of potent inhibitors of DNA-dependent protein kinase (DNA-PK). In: 245th ACS National Meeting and Exposition. 2013, New Orleans, Louisiana: American Chemical Society.
  • Myers SM, Bawn RH, Cottyn B, Golding BT, Griffin RJ, Hammonds T, Leung H, Newell D, Rigoreau L, Wong AC, Hardcastle IR, Cano C. Hit validation of ERK5 inhibitors: Expectations and challenges. In: ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY. 2012, 1155 16TH ST, NW, WASHINGTON, DC 20036 USA: AMER CHEMICAL SOC.
  • Matheson CJ, Aherne W, Bayliss R, Boxall K, Cano C, Golding BT, Hardcastle IR, Mas-Droux C, Newell DR, Wang LZ, Griffin RJ. Design and synthesis of 8-substituted purines as inhibitors of Nek2 kinase. In: ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY. 2012, 1155 16TH ST, NW, WASHINGTON, DC 20036 USA: AMER CHEMICAL SOC.
  • Bawn RH, Golding BT, Griffin RJ, Hammonds T, Leung H, Newell D, Rigoreau L, Wong AC, Cano C, Hardcastle IR. Development of substituted benzothiazoles as ERK5 inhibitors. In: ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY. 2011, 1155 16TH ST, NW, WASHINGTON, DC 20036 USA: AMER CHEMICAL SOC.
  • Carbain B, Roche C, Endicott JA, Golding BT, Hardcastle IR, Cano C, Zhen-Wang L, Newell DR, Noble MEM, Griffin RJ. Structure-based design of C8-substituted O6-alkylguanine CDK1 and 2 inhibitors. In: European Journal of Cancer Supplements: 22nd EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics. 2010, Berlin: Elsevier.
  • Clapham KM, Rennison T, Rodriguez-Aristegui S, Bardos J, Curtin NJ, Golding BT, Hardcastle IR, Newell DR, Cano C, Griffin RJ. Development of potent inhibitors of DNA-dependent protein kinase (DNA-PK). In: EJC Supplements: 22nd EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics. 2010, Berlin, Germany: Pergamon.
  • Saravanan K, Albertella M, Cano C, Curtin NJ, Frigerio M, Golding BT, Haggerty K, Hardcastle IR, Hummersone M, Menear K, Newell DR, Rennison T, Richardson C, Rigoreau L, Rodriguez-Aristegui S, Smith GCM, Griffin RJ. Identification of potent water-soluble DNA-dependent protein kinase (DNA-PK) inhibitors using a small-molecule library approach [abstract]. In: Proceedings of the 99th Annual Meeting of the American Association for Cancer Research. 2008, San Diego, CA: AACR.
  • Cano C, Curtin NJ, Golding BT, Haggerty K, Hardcastle IR, Hummersone M, Menear K, Richardson C, Smith GCM, Griffin RJ. Development of potent water-soluble inhibitors of the DNA-dependent protein kinase (DNA-PK). In: EJC SUPPLEMENTS. 2008, THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND: PERGAMON-ELSEVIER SCIENCE LTD.
  • Cano C, Curtin NJ, Golding BT, Haggerty K, Hardcastle IR, Hummersone M, Menear K, Richardson C, Smith GCM, Griffin RJ. Development of Potent Water-soluble Inhibitors of DNA-Dependent Protein Kinase (DNA-PK). In: 20th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics. 2008, Geneva, Switzerland: European Journal of Cancer Supplements: Pergamon.

• Letter

  • Guglielmo S, Cortese D, Cano C, Fruttero R. Molecular dynamics simulations reveal the determinants of cyclin-dependent kinase 2 inhibition by 5-nitrosopyrimidine derivatives. Journal of Biomolecular Structure and Dynamics 2020, 38(13), 4016-4024.

• Patents

  • Chessari G, Howard S, Buck IM, Cons BD, Johnson CN, Holvey RS, Rees DC, StDenis JD, Tamanini E, Golding BT, Hardcastle IR, Cano CF, Miller DC, Noble MEM, Osborne JD, Peach J, Lewis A, Hirst KL, Whittaker BP, Watson DW, Mitchell DR, Griffin RJ. Preparation of isoindolinones as inhibitors of the MDM2-​p53 interaction having anticancer activity;WO 2017055860. WO2017055860, 2017.
  • Chessari G, Howard S, Buck IM, Cons BD, Johnson CN, Holvey RS, Rees DC, StDenis JD, Tamanini E, Golding BT, Hardcastle IR, Cano CF, Miller DC, Noble MEM, Osborne JD, Peach J, Lewis A, Hirst KL, Whittaker BP, Watson DW, Mitchell DR, Griffin RJ. Preparation of isoindolinones as inhibitors of the MDM2-​p53 interaction having anticancer activity. WO/2017055859, 06/04/2017.
  • Chessari G, Howard S, Buck IM, Cons BD, Johnson CN, Holvey RS, Rees DC, St Denis JD, Tamanini E, Golding BT, Hardcastle IR, Cano CF, Miller DC, Noble MEM, Griffin RJ, Osborne JD, Peach J, Lewis A, Hirst KL, Whittaker BP, Watson DR. ISOINDOLINONE INHIBITORS OF THE MDM2-P53 INTERACTION HAVING ANTICANCER ACTIVITY. PCT/GB2016/053041, 06/04/2017.
  • Reuillon T, Miller D, Myers S, Molyneux L, Cano C, Hardcastle I, Griffin R, Rigoreau L, Golding B, Noble M. Pyrrolcarboxamide Derivatives for the Inhibition of ERK5. WO/2016/042341, 24/03/2016.

• Reviews

  • Miller DC, Harnor SJ, Martin MP, Noble RA, Wedge SR, Cano C. Modulation of ERK5 Activity as a Therapeutic Anti-Cancer Strategy. Journal of Medicinal Chemistry 2023, 66(7), 4491-4502.
  • Potts AJ, Cano C, Thomas SHL, Hill SL. Synthetic cannabinoid receptor agonists: classification and nomenclature. Clinical Toxicology 2020, 58(2), 82-98.
  • Heptinstall AB, Adiyasa IWS, Cano C, Hardcastle IR. Recent advances in CDK inhibitors for cancer therapy. Future Medicinal Chemistry 2018, 10(11), 1369–1388.
  • Cano C. Five-membered rings with two non-adjacent heteroatoms with at least one other element. Comprehensive Heterocyclic Chemistry III: A Review of the Literature 1995-2007 2008, 4/15, 1271-1304.
  • Cano-Soumillac C. Five-membered rings with two adjacent heteroatoms with at least one other element. Comprehensive Heterocyclic Chemistry III, A review of the literature 1995-2007 2008, 4/15, 1243-1270.