Scientific Publications

Clinical

Randomized, double-blind, double-dummy, vehicle-controlled study of ingenol mebutate gel 0.025% and 0.05% for actinic keratosis.

Anderson L, Schmieder GJ, Werschler WP, Tschen EH, Ling MR, Stough DB, Katsamas J.
J Am Acad Dermatol. 2009 Jun; 60(6):934-43
19467365 [PubMed - indexed for MEDLINE]

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PEP005 (ingenol mebutate) gel, a novel agent for the treatment of actinic keratosis: results of a randomized, double-blind, vehicle-controlled, multicentre, phase IIa study

Siller G, Gebauer K, Welburn P, Katsamas J, Ogbourne SM
Australas J Dermatol. 2009 Feb;50(1):16-22
PMID: 19178487

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Basic Science

Immunostimulatory cancer chemotherapy using local ingenol-3-angelate and synergy with immunotherapies

Le TT, Gardner J, Hoang-Le D, Schmidt CW, MacDonald KP, Lambley E, Schroder WA, Ogbourne SM, Suhrbier A.
Vaccine. 2009 May 18; 27 (23): 3053-62. Epub 2009 Apr 3
PMID: 19428919 [PubMed -in process]

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The anti-tumor agent, ingenol-3-angelate (PEP005), promotes the recruitment of cytotoxic neutrophils by activation of vascular endothelial cells in a PKC-delta dependent manner

Hampson P, Kavanagh D, Smith E, Wang K, Lord JM, Ed Rainger G
Cancer Immunol Immunother., 2008 Feb 12 (Epub ahead of print)
PMID: 18265980 [PubMed - as supplied by publisher]

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Neutrophils are a key component of the antitumor efficacy of topical chemotherapy with ingenol-3-angelate

Challacombe JM, Suhrbier A, Parsons PG, Jones B, Hampson P, Kavanagh D, Rainger GE, Morris M, Lord JM, Le TT, Hoang-Le D, Ogbourne SM
J Immunology, 2006 Dec 1, 177(11): 8123-8132
PMID: 17114407 [PubMed - in process]

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Characterization of the interaction of ingenol 3-angelate with protein kinase C

Kedei N, Lundberg DJ, Toth A, Welburn P, Garfield SH, Blumberg PM
Cancer Res, 2004 May 1; 64: 3243-3255
PMID: 15923197 [Pub Med - indexed for MEDLINE]

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Antitumor activity of 3-ingenyl angelate: plasma membrane and mitochondrial disruption and necrotic cell death

Ogbourne SM, Suhrbier A, Jones B, Cozzi SJ, Boyle GM, Morris M, McAlpine D, Johns J, Scott TM, Sutherland KP, Gardner JM, Le TT, Lenarczyk A, Aylward JH, Parsons PG
Cancer Res., 2004 Apr 15; 64(8): 2833-39
PMID: 15087400 [Pub Med - indexed for MEDLINE]

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Other cancers

Epithelial-to-mesenchymal transition and resistance to ingenol-3-angelate, a novel protein kinase C modulator, in colon cancer cells a novel ingenol angelate that modulates PKC functions, alone and in combination with cytotoxic agents in human colon cancer cells

Ghoul A, Serova M, Astorgues-Xerri L, Bieche I, Bousquet G, Varna M, Vidaud M, Phillips E, Weill S, Benhedji K, Lokiec F, Cvitkovic E, Faivre S, Raymond E
Cancer Res., 2009 May 15; 69(10): 4260-9
PMID: 19417139 [PubMed - indexed for MEDLINE]

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The protein kinase C agonist PEP005 increases NF-kappaB expression, induces differentiation and increases constitutive chemokine release by primary acute myeloid leukaemia cells

Olsnes AM, Ersvaer E, Ryningen A, Paulsen K, Hampson P, Lord JM, Gjertsen BT, Kristoffersen EK, Bruserud O
Br J Haematol. 2009 Jun;145(6):761-74
PMID: 19388934 [PubMed - in process]

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Antiproliferative activity of PEP005, a novel ingenol angelate that modulates PKC functions, alone and in combination with cytotoxic agents in human colon cancer cells

Benhadji KA, Serova M, Ghoul A, Cvitkovic E, Le Tourneau C, Ogbourne SM, Lokiec F, Calvo F, Hammel P, Faivre S, Raymond E
Br J Cancer, 2008 Dec 2; 99(11): 1808-1815
PMID: 19034280 [PubMed - indexed for MEDLINE]

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Circulating T cells in patients with untreated acute myelogenous leukemia are heterogeneous and can be activated through the CD3/TCR complex

Ersvaer E, Hampson P, Wendelbo O, Lord JM,Gjertsen B, Bruserud O
Hematology, 2007 Jun; 12(3),199-207
PMID: 17558695 [PubMed - indexed for MEDLINE]

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Effects of protein kinase C modulation by PEP005, a novel ingenol angelate, on mitogen-activated protein kinase and phosphatidylinositol 3-kinase signaling in cancer cells

Serova M, Ghoul A, Benhadji KA, Faivre S, Le Tourneau C, Cvitkovic E, Lokiec F, Lord J, Ogbourne SM, Calvo F, Raymond E
Mol Cancer Ther. 2008 Apr; 7(4):915-22
PMID: 18413805 [PubMed - indexed for MEDLINE]

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T cells remaining after intensive chemotherapy for acute myelogenous leukemia show a broad cytokine release profile including high levels of interferon-� that can be further increased by a novel protein kinase C agonist PEP005

Ersvaer E, Hampson P, HatWeld K, Ulvestad E, Wendelbo O, Lord JM, Gjertsen B, Bruserud O
Cancer Immunol. Immunother, 2007 June;56(6); 913-25. Epub 2006 Nov 8
PMID: 17115221 [PubMed - indexed for MEDLINE]

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Induction of senescence in diterpene ester-treated melanoma cells via protein kinase C-dependent hyperactivation of the mitogen-activated protein kinase pathway

Cozzi SJ, Parsons PG, Ogbourne SM, Pedley J, Boyle GM
Cancer Res., 2006 Oct 15; 66(20): 10083-10091
PMID: 17047072 (PubMed - in process)

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PEP005, a selective small-molecule activator of protein kinase C, has potent antileukemic activity mediated via the delta isoform of PKC

Hampson P, Chahal H, Khanim F, Hayden R, Mulder A, Assi LK, Bunce CM, Lord JM
Blood, 2005 Aug 15; 106(4): 1362-1358 (Epub 2005 Apr 21)
PMID: 15845901 (PubMed - indexed for MEDLINE]

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Ingenol 3-angelate induces dual modes of cell death and differentially regulates tumor necrosis factor-related apoptosis-inducing ligand-induced apoptosis in melanoma cells

Gillespie SK, Zhang XD, Hersey P
Mol Cancer Ther., 2004 Dec; 3(12): 1651-1658
PMID: 15634659 [Pub Med - indexed for MEDLINE]

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