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Doriano Fabbro

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Stefan Knapp; Bernhard Kuster; Karen E Lackey; Paulo Mazzafera; Nicholas C O Tomkinson; Timothy M Willson; Paul Workman; Paulo Arruda; Julian Blagg; Stephen Burley; David H Drewry; Aled Edwards; Doriano Fabbro; Paul Gillespie; Nathanael S Gray; William J Zuercher
A public-private partnership to unlock the untargeted kinome.
Julien Chapelat; Peter Drueckes; Doriano Fabbro; Andreas L Marzinzik; Henrik Moebitz; Frédéric Berst; Joerg Trappe; Dieter Seebach
The Substrate-Activity-Screening methodology applied to receptor tyrosine kinases: a proof-of-concept study.
Doriano Fabbro
BCR-ABL signaling: A new STATus in CML.

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2013: Stefan Knapp; Bernhard Kuster; Karen E Lackey; Paulo Mazzafera; Nicholas C O Tomkinson; Timothy M Willson; Paul Workman; Paulo Arruda; Julian Blagg; Stephen Burley; David H Drewry; Aled Edwards; Doriano Fabbro; Paul Gillespie; Nathanael S Gray; William J Zuercher
A public-private partnership to unlock the untargeted kinome.
Nature chemical biology 2013;9(1):3-6.
2012: Julien Chapelat; Peter Drueckes; Doriano Fabbro; Andreas L Marzinzik; Henrik Moebitz; Frédéric Berst; Joerg Trappe; Dieter Seebach
The Substrate-Activity-Screening methodology applied to receptor tyrosine kinases: a proof-of-concept study.
European journal of medicinal chemistry 2012;57():1-9.
2012: Doriano Fabbro
BCR-ABL signaling: A new STATus in CML.
Nature chemical biology 2012;8(3):228-9.
2012: Sauveur-Michel Maira; Georg Martiny-Baron; Daniel Menezes; Tobi Nagel; Sabina Pecchi; Robert Schlegel; Christian Schnell; William R Sellers; Kevin Shoemaker; Dario Sterker; Saskia Brachmann; Matthew Burger; Patrick Chène; Alain De Pover; Marion Dorsch; Doriano Fabbro; Christine Fritsch; Carlos García-Echeverría; Daniel Guthy; Francesco Hofmann; Alan Huang; Mark Knapp; Marion Wiesmann; Christopher J Wilson; Charles F Voliva
Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor.
Molecular cancer therapeutics 2012;11(2):317-28.
2012: Nataliya Kotelevets; Doriano Fabbro; Andrea Huwiler; Uwe Zangemeister-Wittke
Targeting sphingosine kinase 1 in carcinoma cells decreases proliferation and survival by compromising PKC activity and cytokinesis.
PloS one 2012;7(6):e39209.
2012: Doriano Fabbro; Sandra W Cowan-Jacob; Henrik Möbitz; Georg Martiny-Baron
Targeting cancer with small-molecular-weight kinase inhibitors.
Methods in molecular biology (Clifton, N.J.) 2012;795():1-34.
2011: Julien Chapelat; Peter Drueckes; Doriano Fabbro; Andreas L Marzinzik; Henrik Moebitz; Frédéric Berst; Joerg Trappe; Dieter Seebach
Substrate profiling of IGF-1R and InsR: identification of a potent pentamer substrate.
Bioorganic & medicinal chemistry letters 2011;21(23):7030-3.
2011: Emmanouil Kyriakakis; Juergen Mestan; Dennis Pfaff; Maria Philippova; Marco Cavallari; Gennaro De Libero; Paul Erne; Doriano Fabbro; Therese J Resink
IL-8-mediated angiogenic responses of endothelial cells to lipid antigen activation of iNKT cells depend on EGFR transactivation.
Journal of leukocyte biology 2011;90(5):929-39.
2011: Oleg Fedorov; Kilian Huber; Andreas Eisenreich; Panagis Filippakopoulos; Oliver King; Alex N Bullock; Damian Szklarczyk; Lars J Jensen; Doriano Fabbro; Jörg Trappe; Ursula Rauch; Franz Bracher; Stefan Knapp
Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing.
Chemistry & biology 2011;18(1):67-76.
2011: Georg Martiny-Baron; Johannes Voshol; Daniel D'Dorazio; Dorothea Haasen; Doriano Fabbro
Characterization of kinase inhibitors using reverse phase protein arrays.
Methods in molecular biology (Clifton, N.J.) 2011;785():79-107.
2010: Wolfgang Jahnke; Robert M Grotzfeld; Xavier Pellé; André Strauss; Gabriele Fendrich; Sandra W Cowan-Jacob; Simona Cotesta; Doriano Fabbro; Pascal Furet; Jürgen Mestan; Andreas L Marzinzik
Binding or bending: distinction of allosteric Abl kinase agonists from antagonists by an NMR-based conformational assay.
Journal of the American Chemical Society 2010;132(20):7043-8.
2010: Doriano Fabbro; Paul W Manley; Wolfgang Jahnke; Janis Liebetanz; Alexandra Szyttenholm; Gabriele Fendrich; Andre Strauss; Jianming Zhang; Nathanael S Gray; Francisco Adrian; Markus Warmuth; Xavier Pelle; Robert Grotzfeld; Frederic Berst; Andreas Marzinzik; Sandra W Cowan-Jacob; Pascal Furet; Jürgen Mestan
Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site.
Biochimica et biophysica acta 2010;1804(3):454-62.
2010: Paul W Manley; Peter Drueckes; Gabriele Fendrich; Pascal Furet; Janis Liebetanz; Georg Martiny-Baron; Jürgen Mestan; Jörg Trappe; Markus Wartmann; Doriano Fabbro
Extended kinase profile and properties of the protein kinase inhibitor nilotinib.
Biochimica et biophysica acta 2010;1804(3):445-53.
2009: Jan Van Oostrum; Claudio Calonder; Daniel Rechsteiner; Markus Ehrat; Jürgen Mestan; Doriano Fabbro; Hans Voshol
Tracing pathway activities with kinase inhibitors and reverse phase protein arrays.
Proteomics. Clinical applications 2009;3(4):412-22.
2009: Sandra W Cowan-Jacob; Henrik Möbitz; Doriano Fabbro
Structural biology contributions to tyrosine kinase drug discovery.
Current opinion in cell biology 2009;21(2):280-7.
2008: Fadoua Bouchikhi; Emilie Rossignol; Martine Sancelme; Bettina Aboab; Fabrice Anizon; Doriano Fabbro; Michelle Prudhomme; Pascale Moreau
Synthesis and biological evaluation of diversely substituted indolin-2-ones.
European journal of medicinal chemistry 2008;43(11):2316-22.
2008: Emilie Rossignol; Eric Debiton; Doriano Fabbro; Pascale Moreau; Michelle Prudhomme; Fabrice Anizon
In-vitro antiproliferative activities and kinase inhibitory potencies of meridianin derivatives.
Anti-cancer drugs 2008;19(8):789-92.
2008: Sauveur-Michel Maira; Frédéric Stauffer; Josef Brueggen; Pascal Furet; Christian Schnell; Christine Fritsch; Saskia Brachmann; Patrick Chène; Alain De Pover; Kevin Schoemaker; Doriano Fabbro; Daniela Gabriel; Marjo Simonen; Leon O Murphy; Peter Finan; William R Sellers; Carlos García-Echeverría
Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity.
Molecular cancer therapeutics 2008;7(7):1851-63.
2008: Mickey Croyle; Nagako Akeno; Jeffrey A Knauf; Doriano Fabbro; Xu Chen; Jacqueline E Baumgartner; Heidi A Lane; James A Fagin
RET/PTC-induced cell growth is mediated in part by epidermal growth factor receptor (EGFR) activation: evidence for molecular and functional interactions between RET and EGFR.
Cancer research 2008;68(11):4183-91.
2008: Ralf Amstutz; Marco Wachtel; Heinz Troxler; Peter Kleinert; Margret Ebauer; Torsten Haneke; Christoph Oehler-Jänne; Doriano Fabbro; Felix K Niggli; Beat W Schäfer
Phosphorylation regulates transcriptional activity of PAX3/FKHR and reveals novel therapeutic possibilities.
Cancer research 2008;68(10):3767-76.
2007: Karoline V Gleixner; Matthias Mayerhofer; Karoline Sonneck; Alexander Gruze; Puchit Samorapoompichit; Christian Baumgartner; Francis Y Lee; Karl J Aichberger; Paul W Manley; Doriano Fabbro; Winfried F Pickl; Christian Sillaber; Peter Valent
Synergistic growth-inhibitory effects of two tyrosine kinase inhibitors, dasatinib and PKC412, on neoplastic mast cells expressing the D816V-mutated oncogenic variant of KIT.
Haematologica 2007;92(11):1451-9.
2007: Mathieu Sassatelli; Fadoua Bouchikhi; Bettina Aboab; Fabrice Anizon; Doriano Fabbro; Michelle Prudhomme; Pascale Moreau
In-vitro antiproliferative activities and kinase inhibitory potencies of glycosyl-isoindigo derivatives.
Anti-cancer drugs 2007;18(9):1069-74.
2007: Sumin Kang; Shaozhong Dong; Ting-Lei Gu; Ailan Guo; Michael S Cohen; Sagar Lonial; Hanna Jean Khoury; Doriano Fabbro; D Gary Gilliland; P Leif Bergsagel; Jack Taunton; Roberto D Polakiewicz; Jing Chen
FGFR3 activates RSK2 to mediate hematopoietic transformation through tyrosine phosphorylation of RSK2 and activation of the MEK/ERK pathway.
Cancer cell 2007;12(3):201-14.
2007: Nagako Akeno-Stuart; Mickey Croyle; Jeffrey A Knauf; Roberta Malaguarnera; Donata Vitagliano; Massimo Santoro; Christine Stephan; Konstantina Grosios; Markus Wartmann; Robert Cozens; Giorgio Caravatti; Doriano Fabbro; Heidi A Lane; James A Fagin
The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells.
Cancer research 2007;67(14):6956-64.
2007: Georg Martiny-Baron; Doriano Fabbro
Classical PKC isoforms in cancer.
Pharmacological research : the official journal of the Italian Pharmacological Society 2007;55(6):477-86.
2007: Ellen Weisberg; Laurence Catley; Renee D Wright; Daisy Moreno; Lolita Banerji; Arghya Ray; Paul W Manley; Jürgen Mestan; Doriano Fabbro; Jingrui Jiang; Elizabeth Hall-Meyers; Linda Callahan; Jamie L DellaGatta; Andrew L Kung; James D Griffin
Beneficial effects of combining nilotinib and imatinib in preclinical models of BCR-ABL+ leukemias.
Blood 2007;109(5):2112-20.
2007: Sandra W Cowan-Jacob; Gabriele Fendrich; Andreas Floersheimer; Pascal Furet; Janis Liebetanz; Gabriele Rummel; Paul Rheinberger; Mario Centeleghe; Doriano Fabbro; Paul W Manley
Structural biology contributions to the discovery of drugs to treat chronic myelogenous leukaemia.
Acta crystallographica. Section D, Biological crystallography 2007;63(Pt 1):80-93.
2006: Ellen Weisberg; Renee D Wright; Jingrui Jiang; Arghya Ray; Daisy Moreno; Paul W Manley; Doriano Fabbro; Elizabeth Hall-Meyers; Laurence Catley; klaus podar; Andrew L Kung; James D Griffin
Effects of PKC412, nilotinib, and imatinib against GIST-associated PDGFRA mutants with differential imatinib sensitivity.
Gastroenterology 2006;131(6):1734-42.
2006: Nadia Rucci; Irene Recchia; Adriano Angelucci; Marina Alamanou; Andrea Del Fattore; Dario Fortunati; Mira Susa; Doriano Fabbro; Mauro Bologna; Anna Teti
Inhibition of protein kinase c-Src reduces the incidence of breast cancer metastases and increases survival in mice: implications for therapy.
The Journal of pharmacology and experimental therapeutics 2006;318(1):161-72.
2006: Francisco J Adrián; Qiang Ding; Taebo Sim; Anastasia Velentza; Christine Sloan; Yi Liu; Guobao Zhang; Wooyoung Hur; Sheng Ding; Paul Manley; Jürgen Mestan; Doriano Fabbro; Nathanael S Gray
Allosteric inhibitors of Bcr-abl-dependent cell proliferation.
Nature chemical biology 2006;2(2):95-102.
2006: Karoline V Gleixner; Matthias Mayerhofer; Karl J Aichberger; Sophia Derdak; Karoline Sonneck; Alexandra Böhm; Alexander Gruze; Puchit Samorapoompichit; Paul W Manley; Doriano Fabbro; Winfried F Pickl; Christian Sillaber; Peter Valent
PKC412 inhibits in vitro growth of neoplastic human mast cells expressing the D816V-mutated variant of KIT: comparison with AMN107, imatinib, and cladribine (2CdA) and evaluation of cooperative drug effects.
Blood 2006;107(2):752-9.
2005: Jing Chen; Benjamin H Lee; Ifor Williams; Jeffery L Kutok; Constantine S Mitsiades; Nicole Duclos; Sarah Cohen; Jennifer Adelsperger; Rachel Okabe; Allison Coburn; Sandra Moore; Brian J P Huntly; Doriano Fabbro; Kenneth C Anderson; James D Griffin; D Gary Gilliland
FGFR3 as a therapeutic target of the small molecule inhibitor PKC412 in hematopoietic malignancies.
Oncogene 2005;24(56):8259-67.
2005: Benjamin H Lee; Ifor Williams; Ema Anastasiadou; Christina L Boulton; Sarah W Joseph; Sonia M Amaral; David P Curley; Nicole Duclos; Brian J P Huntly; Doriano Fabbro; James D Griffin; D Gary Gilliland
FLT3 internal tandem duplication mutations induce myeloproliferative or lymphoid disease in a transgenic mouse model.
Oncogene 2005;24(53):7882-92.
2005: Elizabeth H Stover; Jing Chen; Benjamin H Lee; Jan Cools; Elizabeth P McDowell; Jennifer Adelsperger; Dana Cullen; Allison Coburn; Sandra A Moore; Rachel Okabe; Doriano Fabbro; Paul W Manley; James D Griffin; D Gary Gilliland
The small molecule tyrosine kinase inhibitor AMN107 inhibits TEL-PDGFRbeta and FIP1L1-PDGFRalpha in vitro and in vivo.
Blood 2005;106(9):3206-13.
2005: Joseph D Growney; Jennifer J Clark; Jennifer Adelsperger; Richard Stone; Doriano Fabbro; James D Griffin; D Gary Gilliland
Activation mutations of human c-KIT resistant to imatinib mesylate are sensitive to the tyrosine kinase inhibitor PKC412.
Blood 2005;106(2):721-4.
2005: Sandra W Cowan-Jacob; Gabriele Fendrich; Paul W Manley; Wolfgang Jahnke; Doriano Fabbro; Janis Liebetanz; Thomas Meyer
The crystal structure of a c-Src complex in an active conformation suggests possible steps in c-Src activation.
Structure (London, England : 1993) 2005;13(6):861-71.
2005: Barbara Hofstetter; Van Vuong; Angela Broggini-Tenzer; Stephan Bodis; I Frank Ciernik; Doriano Fabbro; Markus Wartmann; Gerd Folkers; Martin Pruschy
Patupilone acts as radiosensitizing agent in multidrug-resistant cancer cells in vitro and in vivo.
Clinical cancer research : an official journal of the American Association for Cancer Research 2005;11(4):1588-96.
2005: Ellen Weisberg; Paul W Manley; Werner Breitenstein; Josef Brüggen; Sandra W Cowan-Jacob; Arghya Ray; Brian J P Huntly; Doriano Fabbro; Gabriele Fendrich; Elizabeth Hall-Meyers; Andrew L Kung; Jürgen Mestan; George Q Daley; Linda Callahan; Laurence Catley; Cara Cavazza; Mohammad Azam; Azam Mohammed; Donna Neuberg; Renee D Wright; D Gary Gilliland; James D Griffin
Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl.
Cancer cell 2005;7(2):129-41.
2004: Mark A Pearson; Doriano Fabbro
Targeting protein kinases in cancer therapy: a success?
Expert review of anticancer therapy 2004;4(6):1113-24.
2004: Jing Chen; Daniel J DeAngelo; Jeffery L Kutok; Ifor Williams; Benjamin H Lee; Martha Wadleigh; Nicole Duclos; Sarah Cohen; Jennifer Adelsperger; Rachel Okabe; Allison Coburn; Ilene Galinsky; Brian J P Huntly; Pamela S Cohen; Thomas Meyer; Doriano Fabbro; Johannes Roesel; Lolita Banerji; James D Griffin; Sheng Xiao; Jonathan A Fletcher; Richard M Stone; D Gary Gilliland
PKC412 inhibits the zinc finger 198-fibroblast growth factor receptor 1 fusion tyrosine kinase and is active in treatment of stem cell myeloproliferative disorder.
Proceedings of the National Academy of Sciences of the United States of America 2004;101(40):14479-84.
2004: Jan Cools; Nicole Mentens; Pascal Furet; Doriano Fabbro; Jennifer J Clark; James D Griffin; Peter Marynen; D Gary Gilliland
Prediction of resistance to small molecule FLT3 inhibitors: implications for molecularly targeted therapy of acute leukemia.
Cancer research 2004;64(18):6385-9.
2004: Clifford D Mol; Doriano Fabbro; David J Hosfield
Structural insights into the conformational selectivity of STI-571 and related kinase inhibitors.
Current opinion in drug discovery & development 2004;7(5):639-48.
2004: Daniel Zingg; Oliver Riesterer; Doriano Fabbro; Christoph Glanzmann; Stephan Bodis; Martin Pruschy
Differential activation of the phosphatidylinositol 3'-kinase/Akt survival pathway by ionizing radiation in tumor and primary endothelial cells.
Cancer research 2004;64(15):5398-406.
2004: Peter Traxler; Peter R Allegrini; Ralf Brandt; Josef Brueggen; Robert Cozens; Doriano Fabbro; Konstantina Grosios; Heidi A Lane; Paul M J McSheehy; Jürgen Mestan; Thomas Meyer; Careen Tang; Markus Wartmann; Jeanette Wood; Giorgio Caravatti
AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity.
Cancer research 2004;64(14):4931-41.
2004: Jing Chen; Nathan Wall; Kerry Kocher; Nicole Duclos; Doriano Fabbro; Donna Neuberg; James D Griffin; Yang Shi; D Gary Gilliland
Stable expression of small interfering RNA sensitizes TEL-PDGFbetaR to inhibition with imatinib or rapamycin.
The Journal of clinical investigation 2004;113(12):1784-91.
2004: Yiguo Hu; Yuhua Liu; Shawn Pelletier; Elisabeth Buchdunger; Markus Warmuth; Doriano Fabbro; Michael Hallek; Richard A Van Etten; Shaoguang Li
Requirement of Src kinases Lyn, Hck and Fgr for BCR-ABL1-induced B-lymphoblastic leukemia but not chronic myeloid leukemia.
Nature genetics 2004;36(5):453-61.
2004: Doriano Fabbro
An interview with Doriano Fabbro, Ph.D., Novartis Biomedical Research Institute. Interviewed by Vicki Glaser.
Assay and drug development technologies 2004;2(2):109-14.
2004: Carlos García-Echeverría; Mark A Pearson; Andreas Marti; Thomas Meyer; Jürgen Mestan; Johann Zimmermann; Jiaping Gao; Josef Brueggen; Hans-Georg Capraro; Robert Cozens; Dean B Evans; Doriano Fabbro; Pascal Furet; Diana Graus Porta; Janis Liebetanz; Georg Martiny-Baron; Stephan Ruetz; Francesco Hofmann
In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase.
Cancer cell 2004;5(3):231-9.
2004: Sandra W Cowan-Jacob; Valerie Guez; Gabriele Fendrich; James D Griffin; Doriano Fabbro; Pascal Furet; Janis Liebetanz; Jürgen Mestan; Paul W Manley
Imatinib (STI571) resistance in chronic myelogenous leukemia: molecular basis of the underlying mechanisms and potential strategies for treatment.
Mini reviews in medicinal chemistry 2004;4(3):285-99.
2004: Carlos García-Echeverría; Doriano Fabbro
Therapeutically targeted anticancer agents: inhibitors of receptor tyrosine kinases.
Mini reviews in medicinal chemistry 2004;4(3):273-83.
2004: Yongqin Wan; Wooyoung Hur; Charles Y Cho; Yi Liu; Francisco J Adrian; Olivier Lozach; Stéphane Bach; Thomas Mayer; Doriano Fabbro; Laurent Meijer; Nathanael S Gray
Synthesis and target identification of hymenialdisine analogs.
Chemistry & biology 2004;11(2):247-59.
2004: Irene Recchia; Nadia Rucci; Alessia Funari; Silvia Migliaccio; Anna Taranta; Maurizio Longo; Michaela Kneissel; Mira Susa; Doriano Fabbro; Anna Teti
Reduction of c-Src activity by substituted 5,7-diphenyl-pyrrolo[2,3-d]-pyrimidines induces osteoclast apoptosis in vivo and in vitro. Involvement of ERK1/2 pathway.
Bone 2004;34(1):65-79.
2003: S. Armaz Aschrafi; Rochus Franzen; Soheyla Shabahang; Doriano Fabbro; Josef Pfeilschifter; Andrea Huwiler
Ceramide induces translocation of protein kinase C-alpha to the Golgi compartment of human embryonic kidney cells by interacting with the C2 domain.
Biochimica et biophysica acta 2003;1634(1-2):30-9.
2003: Stefania Sarno; Erika De Moliner; Maria Ruzzene; Mario Angelo Pagano; Roberto Battistutta; Jenny Bain; Doriano Fabbro; Joseph Schoepfer; Matthew Elliott; Pascal Furet; Flavio Meggio; Giuseppe Zanotti; Lorenzo A Pinna
Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA).
The Biochemical journal 2003;374(Pt 3):639-46.
2003: Irene Recchia; Nadia Rucci; Claudio Festuccia; Mauro Bologna; Andrew R Mackay; Silvia Migliaccio; Maurizio Longo; Mira Susa; Doriano Fabbro; Anna Teti
Pyrrolopyrimidine c-Src inhibitors reduce growth, adhesion, motility and invasion of prostate cancer cells in vitro.
European journal of cancer (Oxford, England : 1990) 2003;39(13):1927-35.
2003: Eric Vangrevelinghe; Kaspar Zimmermann; Joseph Schoepfer; Robert Portmann; Doriano Fabbro; Pascal Furet
Discovery of a potent and selective protein kinase CK2 inhibitor by high-throughput docking.
Journal of medicinal chemistry 2003;46(13):2656-62.
2003: Jan Cools; Elizabeth H Stover; Christina L Boulton; Jason Gotlib; Robert D Legare; Sonia M Amaral; David P Curley; Nicole Duclos; Rebecca Rowan; Jeffery L Kutok; Benjamin H Lee; Ifor Williams; Steven E Coutre; Richard M Stone; Daniel J DeAngelo; Peter Marynen; Paul W Manley; Thomas Meyer; Doriano Fabbro; Donna Neuberg; Ellen Weisberg; James D Griffin; D Gary Gilliland
PKC412 overcomes resistance to imatinib in a murine model of FIP1L1-PDGFRα-induced myeloproliferative disease.
Cancer cell 2003;3(5):459-69.
2003: Venugopal J R V Mukku; RuAngelie Edrada-Ebel; Francis J Schmitz; Michelle Kelly Shanks; Babathosh Chaudhuri; Doriano Fabbro
New sesquiterpene quinols from a Micronesian sponge, Aka sp.
Journal of natural products 2003;66(5):686-9.
2003: Markus Warmuth; Nicola Simon; Olga Mitina; Ruth Mathes; Doriano Fabbro; Paul W Manley; Elisabeth Buchdunger; Karin Forster; Ismail Moarefi; Michael Hallek
Dual-specific Src and Abl kinase inhibitors, PP1 and CGP76030, inhibit growth and survival of cells expressing imatinib mesylate-resistant Bcr-Abl kinases.
Blood 2003;101(2):664-72.
2003: Markus Warmuth; Robert Damoiseaux; Yi Liu; Doriano Fabbro; Nathanael S Gray
SRC family kinases: potential targets for the treatment of human cancer and leukemia.
Current pharmaceutical design 2003;9(25):2043-59.
2003: Stephan Ruetz; Doriano Fabbro; Johann Zimmermann; Thomas Meyer; Nathanael S Gray
Chemical and biological profile of dual Cdk1 and Cdk2 inhibitors.
Current medicinal chemistry. Anti-cancer agents 2003;3(1):1-14.
2002: Rochus Franzen; Doriano Fabbro; S. Armaz Aschrafi; Josef Pfeilschifter; Andrea Huwiler
Nitric oxide induces degradation of the neutral ceramidase in rat renal mesangial cells and is counterregulated by protein kinase C.
The Journal of biological chemistry 2002;277(48):46184-90.
2002: Doriano Fabbro; Carlos García-Echeverría
Targeting protein kinases in cancer therapy.
Current opinion in drug discovery & development 2002;5(5):701-12.
2002: Paul W Manley; Sandra W Cowan-Jacob; Elisabeth Buchdunger; Doriano Fabbro; Gabriele Fendrich; Pascal Furet; Thomas Meyer; Jürg Zimmermann
Imatinib: a selective tyrosine kinase inhibitor.
European journal of cancer (Oxford, England : 1990) 2002;38 Suppl 5():S19-27.
2002: Doriano Fabbro; David Parkinson; Alex Matter
Protein tyrosine kinase inhibitors: new treatment modalities?
Current opinion in pharmacology 2002;2(4):374-81.
2002: Ellen Weisberg; Christina L Boulton; Louise M Kelly; Paul Manley; Doriano Fabbro; Thomas Meyer; D Gary Gilliland; James D Griffin
Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412.
Cancer cell 2002;1(5):433-43.
2002: Doriano Fabbro; Stephan Ruetz; Elisabeth Buchdunger; Sandra W Cowan-Jacob; Gabriele Fendrich; Janis Liebetanz; Jürgen Mestan; Terence O'Reilly; Peter Traxler; Bhabatosh Chaudhuri; Heinz Fretz; Jürg Zimmermann; Thomas Meyer; Giorgio Caravatti; Pascal Furet; Paul W Manley
Protein kinases as targets for anticancer agents: from inhibitors to useful drugs.
Pharmacology & therapeutics 2002;93(2-3):79-98.
2002: Andres Virchis; Kanagasabai Ganeshaguru; Steve Hart; Dylan Jones; Linda Fletcher; Faith Wright; R Gitendra Wickremasinghe; Anthony Man; Katalin Csermak; Thomas Meyer; Doriano Fabbro; Kate Champain; Alan Yap; H Grant Prentice; Atul Mehta
A novel treatment approach for low grade lymphoproliferative disorders using PKC412 (CGP41251), an inhibitor of protein kinase C.
The hematology journal : the official journal of the European Haematology Association / EHA 2002;3(3):131-6.
2001: C Hess; Van Vuong; Ivan Hegyi; Oliver Riesterer; J Wood; Doriano Fabbro; Christoph Glanzmann; Stephan Bodis; Martin Pruschy
Effect of VEGF receptor inhibitor PTK787/ZK222584 [correction of ZK222548] combined with ionizing radiation on endothelial cells and tumour growth.
British journal of cancer 2001;85(12):2010-6.
2001: Angela Tenzer; Daniel Zingg; S Rocha; B Hemmings; Doriano Fabbro; Christoph Glanzmann; P August Schubiger; Stephan Bodis; Martin Pruschy
The phosphatidylinositide 3'-kinase/Akt survival pathway is a target for the anticancer and radiosensitizing agent PKC412, an inhibitor of protein kinase C.
Cancer research 2001;61(22):8203-10.
2001: Rajeev Soni; Terence O'Reilly; Pascal Furet; Lionel Muller; Christine Stephan; Sabine Zumstein-Mecker; Heinz Fretz; Doriano Fabbro; Bhabatosh Chaudhuri
Selective in vivo and in vitro effects of a small molecule inhibitor of cyclin-dependent kinase 4.
Journal of the National Cancer Institute 2001;93(6):436-46.
2001: Stefanie Homann; B Schacher; Sabine Zumstein-Mecker; Doriano Fabbro; G Bold; S Ferrari
Expression and purification of human recombinant GST-FGF receptor-1.
Journal of biotechnology 2001;86(1):51-8.
2001: K Zaugg; S Rocha; H Resch; Ivan Hegyi; Christoph Oehler; Christoph Glanzmann; Doriano Fabbro; Stephan Bodis; Martin Pruschy
Differential p53-dependent mechanism of radiosensitization in vitro and in vivo by the protein kinase C-specific inhibitor PKC412.
Cancer research 2001;61(2):732-8.
2000: S Rocha; Maria Soengas; Scott W Lowe; Christoph Glanzmann; Doriano Fabbro; K Winterhalter; Stephan Bodis; Martin Pruschy
Protein kinase C inhibitor and irradiation-induced apoptosis: relevance of the cytochrome c-mediated caspase-9 death pathway.
Cell growth & differentiation : the molecular biology journal of the American Association for Cancer Research 2000;11(9):491-9.
2000: A Paula Simões-Wüst; Robert A Olie; Oliver Gautschi; Siân H Leech; Robert Häner; Jonathan Hall; Doriano Fabbro; Rolf A Stahel; Uwe Zangemeister-Wittke
Bcl-xl antisense treatment induces apoptosis in breast carcinoma cells.
International journal of cancer. Journal international du cancer 2000;87(4):582-90.
2000: Robert A Olie; A Paula Simões-Wüst; B Baumann; Siân H Leech; Doriano Fabbro; Rolf A Stahel; Uwe Zangemeister-Wittke
A novel antisense oligonucleotide targeting survivin expression induces apoptosis and sensitizes lung cancer cells to chemotherapy.
Cancer research 2000;60(11):2805-9.
2000: Doriano Fabbro; Stephan Ruetz; Stephan Bodis; Martin Pruschy; Katalin Csermak; Anthony Man; Peter A Campochiaro; J Wood; Terence O'Reilly; Thomas Meyer
PKC412--a protein kinase inhibitor with a broad therapeutic potential.
Anti-cancer drug design 2000;15(1):17-28.
1999: B Gay; S Suarez; C Weber; J Rahuel; Doriano Fabbro; Pascal Furet; Giorgio Caravatti; Joseph Schoepfer
Effect of potent and selective inhibitors of the Grb2 SH2 domain on cell motility.
The Journal of biological chemistry 1999;274(33):23311-5.
1999: Pascale Moreau; Fabrice Anizon; Martine Sancelme; Michelle Prudhomme; D Sevère; Jean-François Riou; Jean-François Goossens; Jean-Pierre Hénichart; Christian Bailly; E Labourier; J Tazzi; Doriano Fabbro; T Meyer; AM Aubertin
Synthesis, mode of action, and biological activities of rebeccamycin bromo derivatives.
Journal of medicinal chemistry 1999;42(10):1816-22.
1999: T Meyer; U Regenass; Doriano Fabbro; E Alteri; J Rösel; M Müller; Giorgio Caravatti; A Matter
Author errata.
International journal of cancer. Journal international du cancer 1999;81(4):669.
1999: Doriano Fabbro; Elisabeth Buchdunger; J Wood; Jürgen Mestan; Francesco Hofmann; S Ferrari; Helmut Mett; Terence O'Reilly; Thomas Meyer
Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent.
Pharmacology & therapeutics 1999;82(2-3):293-301.
1999: Pascale Moreau; Fabrice Anizon; Martine Sancelme; Michelle Prudhomme; Christian Bailly; D Sevère; Jean-François Riou; Doriano Fabbro; T Meyer; AM Aubertin
Syntheses and biological activities of rebeccamycin analogues. Introduction of a halogenoacetyl substituent.
Journal of medicinal chemistry 1999;42(4):584-92.
1998: Andrea Huwiler; Doriano Fabbro; Josef Pfeilschifter
Selective ceramide binding to protein kinase C-alpha and -delta isoenzymes in renal mesangial cells.
Biochemistry 1998;37(41):14556-62.
1998: Fabrice Anizon; Pascale Moreau; Martine Sancelme; Aline Voldoire; Michelle Prudhomme; M Ollier; D Sevère; Jean-François Riou; Christian Bailly; Doriano Fabbro; T Meyer; AM Aubertin
Syntheses, biochemical and biological evaluation of staurosporine analogues from the microbial metabolite rebeccamycin.
Bioorganic & medicinal chemistry 1998;6(9):1597-604.
1998: Pascale Moreau; Fabrice Anizon; Martine Sancelme; Michelle Prudhomme; Christian Bailly; C Carrasco; M Ollier; D Sevère; Jean-François Riou; Doriano Fabbro; T Meyer; AM Aubertin
Syntheses and biological evaluation of indolocarbazoles, analogues of rebeccamycin, modified at the imide heterocycle.
Journal of medicinal chemistry 1998;41(10):1631-40.
1998: T Geiger; M Müller; Nicholas Dean; Doriano Fabbro
Antitumor activity of a PKC-alpha antisense oligonucleotide in combination with standard chemotherapeutic agents against various human tumors transplanted into nude mice.
Anti-cancer drug design 1998;13(1):35-45.
1997: Fabrice Anizon; L Belin; Pascale Moreau; Martine Sancelme; Aline Voldoire; Michelle Prudhomme; M Ollier; D Sevère; Jean-François Riou; Christian Bailly; Doriano Fabbro; T Meyer
Syntheses and biological activities (topoisomerase inhibition and antitumor and antimicrobial properties) of rebeccamycin analogues bearing modified sugar moieties and substituted on the imide nitrogen with a methyl group.
Journal of medicinal chemistry 1997;40(21):3456-65.
1997: A Ziegler; GH Luedke; Doriano Fabbro; K H Altmann; Rolf A Stahel; Uwe Zangemeister-Wittke
Induction of apoptosis in small-cell lung cancer cells by an antisense oligodeoxynucleotide targeting the Bcl-2 coding sequence.
Journal of the National Cancer Institute 1997;89(14):1027-36.
1997: E R Pereira; Michelle Prudhomme; Martine Sancelme; M Ollier; D Severe; Jean-François Riou; Huguette Crevel; Jean-Pierre Savineau; Doriano Fabbro; T Meyer
Synthesis and biological evaluation of monoindolyl and indolocarbazolyl oxazolones and imidazolones.
Chemical & pharmaceutical bulletin 1997;45(4):733-6.
1996: E R Pereira; L Belin; Martine Sancelme; M Prudhomme; M Ollier; Maryse Rapp; D Sevère; Jean-François Riou; Doriano Fabbro; T Meyer
Structure-activity relationships in a series of substituted indolocarbazoles: topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties.
Journal of medicinal chemistry 1996;39(22):4471-7.
1996: J Zimmermann; Giorgio Caravatti; Helmut Mett; Thomas Meyer; M Müller; NB Lydon; Doriano Fabbro
Phenylamino-pyrimidine (PAP) derivatives: a new class of potent and selective inhibitors of protein kinase C (PKC).
Archiv der Pharmazie 1996;329(7):371-6.
1989: Thomas Meyer; U Regenass; Doriano Fabbro; E Alteri; J Rösel; M Müller; Giorgio Caravatti; A Matter
A derivative of staurosporine (CGP 41 251) shows selectivity for protein kinase C inhibition and in vitro anti-proliferative as well as in vivo anti-tumor activity.
International journal of cancer. Journal international du cancer 1989;43(5):851-6.