Martin Philpott

• Structural analysis of human KDM5B guides histone demethylase inhibitor development.

  Johansson C. et al, (2016), Nature chemical biology, 12, 539 - 545

• Frapid: achieving full automation of FRAP for chemical probe validation.

  Yapp C. et al, (2016), Biomedical optics express, 7, 422 - 441

• Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.

  Chen P. et al, (2016), Journal of medicinal chemistry, 59, 1410 - 1424

• Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.

  Picaud S. et al, (2015), Cancer research, 75, 5106 - 5119

• Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.

  Fedorov O. et al, (2015), Science advances, 1

• Structure enabled design of BAZ2-ICR, a chemical probe targeting the bromodomains of BAZ2A and BAZ2B.

  Drouin L. et al, (2015), Journal of medicinal chemistry, 58, 2553 - 2559

• Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains.

  Hay DA. et al, (2014), Journal of the American Chemical Society, 136, 9308 - 9319

• A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-π interaction.

  Rooney TP. et al, (2014), Angewandte Chemie (International ed. in English), 53, 6126 - 6130

• Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1.

  Jung M. et al, (2014), The Journal of biological chemistry, 289, 9304 - 9319

• Assessing cellular efficacy of bromodomain inhibitors using fluorescence recovery after photobleaching.

  Philpott M. et al, (2014), Epigenetics & chromatin, 7

• [1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains.

  Fedorov O. et al, (2014), Journal of medicinal chemistry, 57, 462 - 476

• Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain.

  Ferguson FM. et al, (2013), Journal of medicinal chemistry, 56, 10183 - 10187

• RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.

  Picaud S. et al, (2013), Proceedings of the National Academy of Sciences of the United States of America, 110, 19754 - 19759

• Chemical probes for bromodomains outside the BET family

  Brennan PE. et al, (2013), ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 246

• PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains.

  Picaud S. et al, (2013), Cancer research, 73, 3336 - 3346

• The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains.

  Hay D. et al, (2013), MedChemComm, 4, 140 - 144

• Maintenance of muscle myosin levels in adult C. elegans requires both the double bromodomain protein BET-1 and sumoylation.

  Fisher K. et al, (2013), Biology open, 2, 1354 - 1363

• Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.

  Fish PV. et al, (2012), Journal of medicinal chemistry, 55, 9831 - 9837

• Developing small molecule inhibitors of the CREBBP bromodomain-histone interaction

  Rooney TPC. et al, (2012), ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 244

• Developing chemical probes for the BET bromodomains

  Hewings DS. et al, (2012), ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 243

• 3,5-Dimethylisoxazoles inhibit the bromodomain-histone protein-protein interaction

  Hewings DS. et al, (2012), ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 243

• Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery.

  Philpott M. et al, (2011), Molecular bioSystems, 7, 2899 - 2908

• Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery.

  Philpott M. et al, (2011), Mol Biosyst, 7, 2899 - 2908

• 3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.

  Hewings DS. et al, (2011), Journal of medicinal chemistry, 54, 6761 - 6770

• Selective inhibition of BET bromodomains.

  Filippakopoulos P. et al, (2010), Nature, 468, 1067 - 1073

• Small-molecule bromodomain inhibitors for cancer therapy

  Qi J. et al, (2010), ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 240

• Food-derived bioactives as potential regulators of the IL-12/IL-23 pathway implicated in inflammatory bowel diseases.

  Danesi F. et al, (2010), Mutation research, 690, 139 - 144

• Genetic analysis of MDR1 and inflammatory bowel disease reveals protective effect of heterozygous variants for ulcerative colitis.

  Huebner C. et al, (2009), Inflammatory bowel diseases, 15, 1784 - 1793

• Nutrigenomics Integrating Genomic Approaches into Nutrition Research

  Ferguson LR. et al, (2009), Molecular Diagnostics: Second Edition, 347 - 363

• Anthocyanidin-containing compounds occur in the periderm cell walls of the storage roots of sweet potato (Ipomoea batatas).

  Philpott M. et al, (2009), Journal of plant physiology, 166, 1112 - 1117

• Interactions among genes influencing bacterial recognition increase IBD risk in a population-based New Zealand cohort.

  Petermann I. et al, (2009), Human immunology, 70, 440 - 446

• Dietary protection against free radicals: a case for multiple testing to establish structure-activity relationships for antioxidant potential of anthocyanic plant species.

  Philpott M. et al, (2009), International journal of molecular sciences, 10, 1081 - 1103

• Genetics, epigenetics and genomic technologies: Importance and application to the study of endocrine-disrupting chemicals

  Ferguson LR. and Philpott M., (2009), Endocrine-Disrupting Chemicals in Food, 291 - 305

• Nucleotide-binding oligomerization domain containing 1 (NOD1) haplotypes and single nucleotide polymorphisms modify susceptibility to inflammatory bowel diseases in a New Zealand caucasian population: a case-control study.

  Huebner C. et al, (2009), BMC research notes, 2

• Single Nucleotide Polymorphisms in IL4, OCTN1 and OCTN2 Genes in Association with Inflammatory Bowel Disease Phenotypes in a Caucasian Population in Canterbury, New Zealand

  Ferguson LR. et al, (2008), The Open Gastroenterology Journal, 2, 50 - 56

• Single nucleotide polymorphisms in human Paneth cell defensin A5 may confer susceptibility to inflammatory bowel disease in a New Zealand Caucasian population.

  Ferguson LR. et al, (2008), Digestive and liver disease : official journal of the Italian Society of Gastroenterology and the Italian Association for the Study of the Liver, 40, 723 - 730

• Nutrition and mutagenesis.

  Ferguson LR. and Philpott M., (2008), Annual review of nutrition, 28, 313 - 329

• Genes, Diet and Chronic Inflammation

  Ferguson LR. and Philpott M., (2008), JOURNAL OF NUTRIGENETICS AND NUTRIGENOMICS, 1, 190 - 190

• A Screen to Test the Role of IL-23 Receptor in Inflammatory Bowel Diseases

  Danesi F. et al, (2008), JOURNAL OF NUTRIGENETICS AND NUTRIGENOMICS, 1, 305 - 305

• Nutrigenomics in the whole-genome scanning era: Crohn's disease as example.

  Ferguson LR. et al, (2007), Cellular and molecular life sciences : CMLS, 64, 3105 - 3118

• Uncoupling gene-diet interactions in inflammatory bowel disease (IBD).

  Ferguson LR. et al, (2007), Genes & nutrition, 2, 71 - 73

• Cell culture models in developing nutrigenomics foods for inflammatory bowel disease.

  Philpott M. et al, (2007), Mutation research, 622, 94 - 102

• Nutrigenomics and chronic inflammation

  Ferguson LR. and Philpott M., (2007), Personalized Nutrition Principles and Applications

• Cancer prevention by dietary bioactive components that target the immune response.

  Ferguson LR. and Philpott M., (2007), Current cancer drug targets, 7, 459 - 464

• Role of polymorphisms in genes for selenoproteins on prostate cancer risk

  Risom L. et al, (2007), ANNALS OF NUTRITION AND METABOLISM, 51, 250 - 250

• Oxidative DNA damage and repair: significance and biomarkers.

  Ferguson LR. et al, (2006), The Journal of nutrition, 136, 2687S - 2689S

• Antioxidant activities of extracts from traditional Maori food plants

  Gould KS. et al, (2006), NEW ZEALAND JOURNAL OF BOTANY, 44, 1 - 4

• Susceptibility to cancer and DNA damage to lymphocytes: can it be counteracted by dietary selenium?

  Ferguson LR. et al, (2006), Nutritional Biotechnology in the Feed and Food Industries Proceedings of Alltech's Twenty-Second Annual Symposium

• New Zealand - Fertile ground for functional foods and nutrigenomics

  Ferguson LR. and Philpott M., (2005), Current Topics in Nutraceutical Research, 3, 199 - 204

• Immunonutrition and cancer.

  Philpott M. and Ferguson LR., (2004), Mutation research, 551, 29 - 42

• Dietary cancer and prevention using antimutagens.

  Ferguson LR. et al, (2004), Toxicology, 198, 147 - 159

• In situ and in vitro antioxidant activity of sweetpotato anthocyanins.

  Philpott M. et al, (2004), Journal of agricultural and food chemistry, 52, 1511 - 1513

• Epigenetic events and protection from colon cancer in New Zealand.

  Ferguson LR. et al, (2004), Environmental and molecular mutagenesis, 44, 36 - 43

• Enhanced coloration reveals high antioxidant potential in new sweetpotato cultivars

  Philpott M. et al, (2003), JOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE, 83, 1076 - 1082

• The antitumour agent 5,6-dimethylxanthenone-4-acetic acid acts in vitro on human mononuclear cells as a co-stimulator with other inducers of tumour necrosis factor.

  Philpott M. et al, (2001), European journal of cancer (Oxford, England : 1990), 37, 1930 - 1937

• Effects of the serotonin receptor antagonist cyproheptadine on the activity and pharmacokinetics of 5,6-dimethylxanthenone-4-acetic acid (DMXAA).

  Zhao L. et al, (2001), Cancer chemotherapy and pharmacology, 47, 491 - 497

• Production of tumour necrosis factor-alpha by cultured human peripheral blood leucocytes in response to the anti-tumour agent 5,6-dimethylxanthenone-4-acetic acid (NSC 640488).

  Philpott M. et al, (1997), British journal of cancer, 76, 1586 - 1591

• Induction of tumour necrosis factor-alpha by single and repeated doses of the antitumour agent 5,6-dimethylxanthenone-4-acetic acid.

  Philpott M. et al, (1995), Cancer chemotherapy and pharmacology, 36, 143 - 148

• Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.

  Chen P. et al, (2016), Journal of medicinal chemistry, 59, 1410 - 1424

• Assessing cellular efficacy of bromodomain inhibitors using fluorescence recovery after photobleaching.

  Philpott M. et al, (2014), Epigenetics & chromatin, 7

• Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains.

  Hay DA. et al, (2014), Journal of the American Chemical Society, 136, 9308 - 9319

• Selective inhibition of BET bromodomains.

  Filippakopoulos P. et al, (2010), Nature, 468, 1067 - 1073

• Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery.

  Philpott M. et al, (2011), Mol Biosyst, 7, 2899 - 2908

Recent Publications

• Structural analysis of human KDM5B guides histone demethylase inhibitor development.

  Johansson C. et al, (2016), Nature chemical biology, 12, 539 - 545

• Frapid: achieving full automation of FRAP for chemical probe validation.

  Yapp C. et al, (2016), Biomedical optics express, 7, 422 - 441

• Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.

  Chen P. et al, (2016), Journal of medicinal chemistry, 59, 1410 - 1424

• Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.

  Picaud S. et al, (2015), Cancer research, 75, 5106 - 5119

• Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.

  Fedorov O. et al, (2015), Science advances, 1