المؤلفون: Le Bihan, Y-V, Lanigan, RM, Atrash, B, McLaughlin, MG, Velupillai, S, Malcolm, AG, England, KS, Ruda, GF, Mok, NY, Tumber, A, Tomlin, K, Saville, H, Shehu, E, McAndrew, C, Carmichael, L, Bennett, JM, Jeganathan, F, Eve, P, Donovan, A, Hayes, A, Wood, F, Raynaud, FI, Fedorov, O, Brennan, PE, Burke, R, Van Montfort, RLM, Rossanese, OW, Blagg, J, Bavetsias, V

المصدر: European Journal of Medicinal Chemistry
Le Bihan, Y-V, Lanigan, R M, Atrash, B, McLaughlin, M G, Velupillai, S, Malcolm, A G, England, K S, Ruda, G F, Mok, N Y, Tumber, A, Tomlin, K, Saville, H, Shehu, E, McAndrew, C, Carmichael, L, Bennett, J M, Jeganathan, F, Eve, P, Donovan, A, Hayes, A, Wood, F, Raynaud, F I, Fedorov, O, Brennan, P, Burke, R, van Montfort, R L M, Rossanese, O W, Blagg, J & Bavetsias, V 2019, ' C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays ', European Journal of Medicinal Chemistry, vol. 177, pp. 316-337 . https://doi.org/10.1016/j.ejmech.2019.05.041

مصطلحات موضوعية: KDM4 subfamily, Jumonji Domain-Containing Histone Demethylases, Molecular Structure, Pyridines, Pyrimidinones, Crystallography, X-Ray, Article, Pyridopyrimidinones, Structure-Activity Relationship, Cell Line, Tumor, Humans, KDM inhibitors, Drug Screening Assays, Antitumor, Enzyme Inhibitors, KDM5 subfamily, Hydrophobic and Hydrophilic Interactions, Histone demethylases, Protein Binding

وصف الملف: application/pdf; text

URL الوصول: https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::b23e38e79895cd396b4e21c1fb1c9678
http://europepmc.org/articles/PMC6580095

المؤلفون: Sabatini MT; Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon Street, London, WC1H 0AJ, UK., Karaluka V; Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon Street, London, WC1H 0AJ, UK., Lanigan RM; Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon Street, London, WC1H 0AJ, UK., Boulton LT; GlaxoSmithKline, Medicines Research Centre, GunnelsWood Road, Stevenage, Herts, SG12NY, UK., Badland M; Pfizer Global Pharmaceutical Sciences, Discovery Park, Ramsgate Road, Sandwich, UK., Sheppard TD; Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon Street, London, WC1H 0AJ, UK.

المصدر: Chemistry (Weinheim an der Bergstrasse, Germany) [Chemistry] 2018 May 11; Vol. 24 (27), pp. 7033-7043. Date of Electronic Publication: 2018 Apr 30.

نوع المنشور: Journal Article

بيانات الدورية: Publisher: Wiley-VCH Country of Publication: Germany NLM ID: 9513783 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1521-3765 (Electronic) Linking ISSN: 09476539 NLM ISO Abbreviation: Chemistry Subsets: MEDLINE

مواضيع طبية MeSH: Amino Acids/*chemistry , Lewis Acids/*chemistry, Amines/chemistry ; Borates/chemistry ; Catalysis ; Green Chemistry Technology

المؤلفون: Hayes A; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Mok NY; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Liu M; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Thai C; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Henley AT; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Atrash B; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Lanigan RM; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Sejberg J; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Le Bihan YV; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Bavetsias V; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Blagg J; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK., Raynaud FI; a Cancer Research UK Cancer Therapeutics Unit , The Institute of Cancer Research , London , UK.

المصدر: Xenobiotica; the fate of foreign compounds in biological systems [Xenobiotica] 2017 Sep; Vol. 47 (9), pp. 771-777. Date of Electronic Publication: 2016 Oct 26.

نوع المنشور: Journal Article

بيانات الدورية: Publisher: Informa Healthcare Country of Publication: England NLM ID: 1306665 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1366-5928 (Electronic) Linking ISSN: 00498254 NLM ISO Abbreviation: Xenobiotica Subsets: MEDLINE

مواضيع طبية MeSH: Aldehyde Oxidase/*antagonists & inhibitors , Pyrimidines/*metabolism, Animals ; Humans ; Mice ; Models, Molecular ; Proton Magnetic Resonance Spectroscopy ; Structure-Activity Relationship

المؤلفون: Lanigan RM; Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon St, London, WC1H 0AJ, UK. tom.sheppard@ucl.ac.uk., Karaluka V; Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon St, London, WC1H 0AJ, UK. tom.sheppard@ucl.ac.uk., Sabatini MT; Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon St, London, WC1H 0AJ, UK. tom.sheppard@ucl.ac.uk., Starkov P; Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon St, London, WC1H 0AJ, UK. tom.sheppard@ucl.ac.uk., Badland M; Pfizer Global Pharmaceutical Sciences, Discovery Park, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK., Boulton L; GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Herts SG1 2NY, UK., Sheppard TD; Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon St, London, WC1H 0AJ, UK. tom.sheppard@ucl.ac.uk.

المصدر: Chemical communications (Cambridge, England) [Chem Commun (Camb)] 2016 Jul 07; Vol. 52 (57), pp. 8846-9.

نوع المنشور: Journal Article

بيانات الدورية: Publisher: Royal Society of Chemistry Country of Publication: England NLM ID: 9610838 Publication Model: Print Cited Medium: Internet ISSN: 1364-548X (Electronic) Linking ISSN: 13597345 NLM ISO Abbreviation: Chem Commun (Camb) Subsets: PubMed not MEDLINE

المؤلفون: Bavetsias V; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Lanigan RM; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Ruda GF; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford , NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K., Atrash B; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., McLaughlin MG; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Tumber A; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford , NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K., Mok NY; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Le Bihan YV; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Dempster S; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Boxall KJ; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Jeganathan F; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Hatch SB; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford , NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K., Savitsky P; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K., Velupillai S; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K., Krojer T; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K., England KS; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford , NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K., Sejberg J; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Thai C; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Donovan A; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Pal A; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Scozzafava G; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford , NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K., Bennett JM; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford , NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K., Kawamura A; Chemistry Research Laboratory, University of Oxford , Mansfield Road, Oxford OX1 3TA, U.K., Johansson C; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Botnar Research Centre, NIHR Oxford Biomedical Research Unit , Oxford OX3 7LD, U.K., Szykowska A; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K., Gileadi C; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K., Burgess-Brown NA; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K., von Delft F; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Diamond Light Source (DLS), Harwell Science and Innovation Campus , Didcot OX11 0DE, U.K.; Department of Biochemistry, University of Johannesburg , Auckland Park 2006, South Africa., Oppermann U; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Botnar Research Centre, NIHR Oxford Biomedical Research Unit , Oxford OX3 7LD, U.K., Walters Z; Divisions of Molecular Pathology and Cancer Therapeutics, The Institute of Cancer Research , London SM2 5NG, U.K., Shipley J; Divisions of Molecular Pathology and Cancer Therapeutics, The Institute of Cancer Research , London SM2 5NG, U.K., Raynaud FI; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Westaway SM; Epinova Discovery Performance Unit, Medicines Research Centre, GlaxoSmithKline R&D , Stevenage SG1 2NY, U.K., Prinjha RK; Epinova Discovery Performance Unit, Medicines Research Centre, GlaxoSmithKline R&D , Stevenage SG1 2NY, U.K., Fedorov O; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford , NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K., Burke R; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Schofield CJ; Chemistry Research Laboratory, University of Oxford , Mansfield Road, Oxford OX1 3TA, U.K., Westwood IM; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Bountra C; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K., Müller S; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford , NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K., van Montfort RL; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K., Brennan PE; Structural Genomics Consortium (SGC), University of Oxford , ORCRB Roosevelt Drive, Oxford OX3 7DQ, U.K.; Target Discovery Institute (TDI), Nuffield Department of Medicine, University of Oxford , NDMRB Roosevelt Drive, Oxford OX3 7FZ, U.K., Blagg J; Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research , 15 Cotswold Road, London SM2 5NG, U.K.

المصدر: Journal of medicinal chemistry [J Med Chem] 2016 Feb 25; Vol. 59 (4), pp. 1388-409. Date of Electronic Publication: 2016 Jan 07.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE

مواضيع طبية MeSH: Enzyme Inhibitors/*chemistry , Enzyme Inhibitors/*pharmacology , Jumonji Domain-Containing Histone Demethylases/*antagonists & inhibitors , Nuclear Proteins/*antagonists & inhibitors , Pyrimidinones/*chemistry , Pyrimidinones/*pharmacology , Repressor Proteins/*antagonists & inhibitors, Caco-2 Cells ; Cell Membrane Permeability ; Enzyme Inhibitors/pharmacokinetics ; Humans ; Jumonji Domain-Containing Histone Demethylases/chemistry ; Jumonji Domain-Containing Histone Demethylases/metabolism ; Nuclear Proteins/chemistry ; Nuclear Proteins/metabolism ; Pyrimidinones/pharmacokinetics ; Repressor Proteins/chemistry ; Repressor Proteins/metabolism

المؤلفون: Karaluka V; Department of Chemistry, University College London, 20 Gordon St, London, WC1H 0AJ, UK. tom.sheppard@ucl.ac.uk., Lanigan RM, Murray PM, Badland M, Sheppard TD

المصدر: Organic & biomolecular chemistry [Org Biomol Chem] 2015 Nov 28; Vol. 13 (44), pp. 10888-94. Date of Electronic Publication: 2015 Sep 14.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: Royal Society of Chemistry Country of Publication: England NLM ID: 101154995 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1477-0539 (Electronic) Linking ISSN: 14770520 NLM ISO Abbreviation: Org Biomol Chem Subsets: MEDLINE

مواضيع طبية MeSH: Amides/*chemistry , Amines/*chemistry , Borates/*chemistry , Carboxylic Acids/*chemistry , Cyclopentanes/*chemistry , Methyl Ethers/*chemistry, Aminopyridines/chemistry ; Catalysis ; Esterification ; Phenylacetates/chemistry ; Solvents/chemistry

المؤلفون: Gibson SM; Department of Chemistry, University College London, 20 Gordon St, London, WC1H 0AJ, UK. tom.sheppard@ucl.ac.uk., Lanigan RM, Benhamou L, Aliev AE, Sheppard TD

المصدر: Organic & biomolecular chemistry [Org Biomol Chem] 2015 Sep 14; Vol. 13 (34), pp. 9050-4. Date of Electronic Publication: 2015 Jul 29.

نوع المنشور: Journal Article

بيانات الدورية: Publisher: Royal Society of Chemistry Country of Publication: England NLM ID: 101154995 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1477-0539 (Electronic) Linking ISSN: 14770520 NLM ISO Abbreviation: Org Biomol Chem Subsets: PubMed not MEDLINE

المؤلفون: Aliev AE; Department of Chemistry, University College London, London, WC1H 0AJ, United Kingdom., Kulke M, Khaneja HS, Chudasama V, Sheppard TD, Lanigan RM

المصدر: Proteins [Proteins] 2014 Feb; Vol. 82 (2), pp. 195-215. Date of Electronic Publication: 2013 Sep 17.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: Wiley-Liss Country of Publication: United States NLM ID: 8700181 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1097-0134 (Electronic) Linking ISSN: 08873585 NLM ISO Abbreviation: Proteins Subsets: MEDLINE

مواضيع طبية MeSH: Molecular Dynamics Simulation*, Hydroxyproline/*chemistry, Algorithms ; Amino Acid Motifs ; Amino Acid Sequence ; Humans ; Nuclear Magnetic Resonance, Biomolecular ; Proline/chemistry ; Thermodynamics ; Ubiquitin/chemistry

المؤلفون: Lanigan RM; Department of Chemistry, University College London, Christopher Ingold Laboratories, 20 Gordon St, London, WC1H 0AJ, UK., Starkov P, Sheppard TD

المصدر: The Journal of organic chemistry [J Org Chem] 2013 May 03; Vol. 78 (9), pp. 4512-23. Date of Electronic Publication: 2013 Apr 16.

نوع المنشور: Journal Article

بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 2985193R Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-6904 (Electronic) Linking ISSN: 00223263 NLM ISO Abbreviation: J Org Chem Subsets: PubMed not MEDLINE