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Frank Ebetino
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Research Profile (preview)
Chemicals & Drugs
Physiology
Concepts & Ideas
Anatomy
Disorders
Living Beings
Genes & Molecular Sequences
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Network (preview)
16
Rogers, Michael
12
Russell, Graham
9
Coxon, Fraser
8
Dunford, James
5
Cross-Doersen, Doreen
5
Crossdoersen, Doreen
5
Tian, Xinrong
5
Mazur, Adam
5
Wos, John
4
Watts, DJ
4
Phipps, Roger
4
Mishra, Rajesh
4
Sheldon, Russell
4
Solinsky, Mark
4
Pinney, Beth
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Publications
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All Publications
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2009: Hald Andreas; Hansen Rikke R; Thomsen Mette W; Ding Ming; Croucher Peter I; Gallagher Orla; Ebetino Frank H; Kassem Moustapha; Heegaard Anne-Marie
Cancer-induced bone loss and associated pain-related behavior is reduced by risedronate but not its phosphonocarboxylate analog NE-10790.
International journal of cancer. Journal international du cancer 2009;125(5):1177-85.
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2009: Baron Rudi A; Tavaré Richard; Figueiredo Ana C; Blazewska Katarzyna M; Kashemirov Boris A; McKenna Charles E; Ebetino Frank H; Taylor Adam; Rogers Michael J; Coxon Fraser P; Seabra Miguel C
Phosphonocarboxylates inhibit the second geranylgeranyl addition by Rab geranylgeranyl transferase.
The Journal of biological chemistry 2009;284(11):6861-8.
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2008: Lawson Michelle A; Coulton Les; Ebetino Frank H; Vanderkerken Karin; Croucher Peter I
Geranylgeranyl transferase type II inhibition prevents myeloma bone disease.
Biochemical and biophysical research communications 2008;377(2):453-7.
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2008: Fournier Pierrick G J; Daubiné Florence; Lundy Mark W; Rogers Michael J; Ebetino Frank H; Clézardin Philippe
Lowering bone mineral affinity of bisphosphonates as a therapeutic strategy to optimize skeletal tumor growth inhibition in vivo.
Cancer research 2008;68(21):8945-53.
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2008: Tian Xinrong; Switzer Adrian G; Derose Steve A; Mishra Rajesh K; Solinsky Mark G; Mumin Rashid N; Ebetino Frank H; Jayasinghe Lalith R; Webster Mark E; Colson Anny-Odile; Crossdoersen Doreen; Pinney Beth B; Farmer Julie A; Dowty Martin E; Obringer Cindy M; Cruze Charles A; Burklow Melissa L; Suchanek Paula M; Dong Lily; Dirr Mary Kay; Sheldon Russell J; Wos John A
Discovery of orally bioavailable 1,3,4-trisubstituted 2-oxopiperazine-based melanocortin-4 receptor agonists as potential antiobesity agents.
Journal of medicinal chemistry 2008;51(19):6055-66.
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2008: Russell R G G; Watts N B; Ebetino F H; Rogers M J
Mechanisms of action of bisphosphonates: similarities and differences and their potential influence on clinical efficacy.
Osteoporosis international : a journal established as result of cooperation between the European Foundation for Osteoporosis and the National Osteoporosis Foundation of the USA 2008;19(6):733-59.
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2008: Henneman Zachary J; Nancollas George H; Ebetino F Hal; Russell R Graham G; Phipps Roger J
Bisphosphonate binding affinity as assessed by inhibition of carbonated apatite dissolution in vitro.
Journal of biomedical materials research. Part A 2008;85(4):993-1000.
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2008: Deprèle Sylvine; Kashemirov Boris A; Hogan James M; Ebetino Frank H; Barnett Bobby L; Evdokimov Artem; McKenna Charles E
Farnesyl pyrophosphate synthase enantiospecificity with a chiral risedronate analog, [6,7-dihydro-5H-cyclopenta[c]pyridin-7-yl(hydroxy)methylene]bis(phosphonic acid) (NE-10501): Synthetic, structural, and modeling studies.
Bioorganic & medicinal chemistry letters 2008;18(9):2878-82.
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2008: Coxon Fraser P; Thompson Keith; Roelofs Anke J; Ebetino F Hal; Rogers Michael J
Visualizing mineral binding and uptake of bisphosphonate by osteoclasts and non-resorbing cells.
Bone 2008;42(5):848-60.
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2008: Dunford James E; Kwaasi Aaron A; Rogers Michael J; Barnett Bobby L; Ebetino Frank H; Russell R Graham G; Oppermann Udo; Kavanagh Kathryn L
Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase.
Journal of medicinal chemistry 2008;51(7):2187-95.
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2008: Liu Xue-Wei; Ma Jimei; Colson Anny-Odile; Doersen Doreen Cross; Ebetino Frank H
Synthesis and biological activity of novel peptide mimetics as melanocortin receptor agonists.
Bioorganic & medicinal chemistry letters 2008;18(3):1223-8.
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2007: Russell R Graham G; Xia Zhidao; Dunford James E; Oppermann Udo; Kwaasi Aaron; Hulley Philippa A; Kavanagh Kathryn L; Triffitt James T; Lundy Mark W; Phipps Roger J; Barnett Bobby L; Coxon Fraser P; Rogers Michael J; Watts Nelson B; Ebetino Frank H
Bisphosphonates: an update on mechanisms of action and how these relate to clinical efficacy.
Annals of the New York Academy of Sciences 2007;1117():209-57.
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2007: Marma Mong S; Xia Zhidao; Stewart Charlotte; Coxon Fraser; Dunford James E; Baron Rudi; Kashemirov Boris A; Ebetino Frank H; Triffitt James T; Russell R Graham G; McKenna Charles E
Synthesis and biological evaluation of alpha-halogenated bisphosphonate and phosphonocarboxylate analogues of risedronate.
Journal of medicinal chemistry 2007;50(24):5967-75.
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2007: Roelofs Anke J; Edwards Claire M; Russell R Graham G; Ebetino F Hal; Rogers Michael J; Hulley Philippa A
Apomine enhances the antitumor effects of lovastatin on myeloma cells by down-regulating 3-hydroxy-3-methylglutaryl-coenzyme A reductase.
The Journal of pharmacology and experimental therapeutics 2007;322(1):228-35.
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2006: Wu Yao-Wen; Waldmann Herbert; Reents Reinhard; Ebetino Frank H; Goody Roger S; Alexandrov Kirill
A protein fluorescence amplifier: continuous fluorometric assay for rab geranylgeranyltransferase.
Chembiochem : a European journal of chemical biology 2006;7(12):1859-61.
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2006: Tian Xinrong; Mishra Rajesh K; Switzer Adrian G; Hu X Eric; Kim Nick; Mazur Adam W; Ebetino Frank H; Wos John A; Crossdoersen Doreen; Pinney Beth B; Farmer Julie A; Sheldon Russell J
Design and synthesis of potent and selective 1,3,4-trisubstituted-2-oxopiperazine based melanocortin-4 receptor agonists.
Bioorganic & medicinal chemistry letters 2006;16(17):4668-73.
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2006: Roelofs Anke J; Hulley Philippa A; Meijer Annemieke; Ebetino Frank H; Russell R Graham G; Shipman Claire M
Selective inhibition of Rab prenylation by a phosphonocarboxylate analogue of risedronate induces apoptosis, but not S-phase arrest, in human myeloma cells.
International journal of cancer. Journal international du cancer 2006;119(6):1254-61.
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2006: Tian Xinrong; Field Timothy B; Switzer Adrian G; Mazur Adam W; Ebetino Frank H; Wos John A; Berberich Steve M; Jayasinghe Lalith R; Obringer Cindy M; Dowty Martin E; Pinney Beth B; Farmer Julie A; Crossdoersen Doreen; Sheldon Russell J
Design, synthesis, and evaluation of proline and pyrrolidine based melanocortin receptor agonists. A conformationally restricted dipeptide mimic approach.
Journal of medicinal chemistry 2006;49(15):4745-61.
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2006: Dunford James E; Rogers Michael J; Ebetino Frank H; Phipps Roger J; Coxon Fraser P
Inhibition of protein prenylation by bisphosphonates causes sustained activation of Rac, Cdc42, and Rho GTPases.
Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research 2006;21(5):684-94.
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2006: Kavanagh Kathryn L; Guo Kunde; Dunford James E; Wu Xiaoqiu; Knapp Stefan; Ebetino Frank H; Rogers Michael J; Russell R Graham G; Oppermann Udo
The molecular mechanism of nitrogen-containing bisphosphonates as antiosteoporosis drugs.
Proceedings of the National Academy of Sciences of the United States of America 2006;103(20):7829-34.
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2006: Nancollas G H; Tang R; Phipps R J; Henneman Z; Gulde S; Wu W; Mangood A; Russell R G G; Ebetino F H
Novel insights into actions of bisphosphonates on bone: differences in interactions with hydroxyapatite.
Bone 2006;38(5):617-27.
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2006: Tian Xinrong; Chen Xuemei; Gan Lixian; Hayes Jeffery C; Switzer Adrian G; Solinsky Mark G; Ebetino Frank H; Wos John A; Pinney Beth B; Farmer Julie A; Crossdoersen Doreen; Sheldon Russell J
Synthesis of Tic-D-Phe Psi[CH2-CH2] isostere and its use in the development of melanocortin receptor agonists.
Bioorganic & medicinal chemistry letters 2006;16(6):1721-5.
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2005: Coxon Fraser P; Ebetino Frank H; Mules Emilie H; Seabra Miguel C; McKenna Charles E; Rogers Michael J
Phosphonocarboxylate inhibitors of Rab geranylgeranyl transferase disrupt the prenylation and membrane localization of Rab proteins in osteoclasts in vitro and in vivo.
Bone 2005;37(3):349-58.
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2005: Clézardin Philippe; Ebetino Frank H; Fournier Pierrick G J
Bisphosphonates and cancer-induced bone disease: beyond their antiresorptive activity.
Cancer research 2005;65(12):4971-4.
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2005: Tian Xinrong; Field Timothy; Mazur Adam W; Ebetino Frank H; Wos John A; Crossdoersen Doreen; Pinney Beth B; Sheldon Russell J
Design, synthesis, and evaluation of proline based melanocortin receptor ligands.
Bioorganic & medicinal chemistry letters 2005;15(11):2819-23.
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2004: Koikov L N; Ebetino F H; Hayes J C; Cross-Doersen D; Knittel J J
End-capping of the modified melanocortin tetrapeptide (p-Cl)Phe-D-Phe-Arg-Trp-NH2 as a route to hMC4R agonists.
Bioorganic & medicinal chemistry letters 2004;14(19):4839-42.
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2004: Koikov L N; Ebetino F H; Solinsky M G; Cross-Doersen D; Knittel J J
Analogs of sub-nanomolar hMC1R agonist LK-184 [Ph(CH2)3CO-His-D-Phe-Arg-Trp-NH2]. An additional binding site within the human melanocortin receptor 1?
Bioorganic & medicinal chemistry letters 2004;14(15):3997-4000.
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2003: Koikov L N; Ebetino F H; Solinsky M G; Cross-Doersen D; Knittel J J
Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2).
Bioorganic & medicinal chemistry letters 2003;13(16):2647-50.
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2003: Mazur Adam W; Kulesza Anna; Mishra Rajesh K; Cross-Doersen Doreen; Russell Anne F; Ebetino Frank H
Novel tetrahydropyran-based peptidomimetics from a bioisosteric transformation of a tripeptide. Evidence of their activity at melanocortin receptors.
Bioorganic & medicinal chemistry 2003;11(14):3053-63.
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2003: Kulesza Anna; Ebetino Frank H; Mishra Rajesh K; Cross-Doersen Doreen; Mazur Adam W
Synthesis of 2,4,5-trisubstituted tetrahydropyrans as peptidomimetic scaffolds for melanocortin receptor ligands.
Organic letters 2003;5(8):1163-6.
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2002: Thompson Keith; Dunford James E; Ebetino Frank H; Rogers Michael J
Identification of a bisphosphonate that inhibits isopentenyl diphosphate isomerase and farnesyl diphosphate synthase.
Biochemical and biophysical research communications 2002;290(2):869-73.
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2001: Coxon F P; Helfrich M H; Larijani B; Muzylak M; Dunford J E; Marshall D; McKinnon A D; Nesbitt S A; Horton M A; Seabra M C; Ebetino F H; Rogers M J
Identification of a novel phosphonocarboxylate inhibitor of Rab geranylgeranyl transferase that specifically prevents Rab prenylation in osteoclasts and macrophages.
The Journal of biological chemistry 2001;276(51):48213-22.
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2001: Soper D L; Milbank J B; Mieling G E; Dirr M J; Kende A S; Cooper R; Jee W S; Yao W; Chen J L; Bodman M; Lundy M W; De B; Stella M E; Ebetino F H; Wang Y; deLong M A; Wos J A
Synthesis and biological evaluation of prostaglandin-F alkylphosphinic acid derivatives as bone anabolic agents for the treatment of osteoporosis.
Journal of medicinal chemistry 2001;44(24):4157-69.
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2001: Dunford J E; Thompson K; Coxon F P; Luckman S P; Hahn F M; Poulter C D; Ebetino F H; Rogers M J
Structure-activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates.
The Journal of pharmacology and experimental therapeutics 2001;296(2):235-42.
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2000: Boissier S; Ferreras M; Peyruchaud O; Magnetto S; Ebetino F H; Colombel M; Delmas P; Delaissé J M; Clézardin P
Bisphosphonates inhibit breast and prostate carcinoma cell invasion, an early event in the formation of bone metastases.
Cancer research 2000;60(11):2949-54.
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1998: Luckman S P; Coxon F P; Ebetino F H; Russell R G; Rogers M J
Heterocycle-containing bisphosphonates cause apoptosis and inhibit bone resorption by preventing protein prenylation: evidence from structure-activity relationships in J774 macrophages.
Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research 1998;13(11):1668-78.
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1997: Boissier S; Magnetto S; Frappart L; Cuzin B; Ebetino F H; Delmas P D; Clezardin P
Bisphosphonates inhibit prostate and breast carcinoma cell adhesion to unmineralized and mineralized bone extracellular matrices.
Cancer research 1997;57(18):3890-4.
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1997: Rogers M J; Xiong X; Ji X; Mönkkönen J; Russell R G; Williamson M P; Ebetino F H; Watts D J
Inhibition of growth of Dictyostelium discoideum amoebae by bisphosphonate drugs is dependent on cellular uptake.
Pharmaceutical research 1997;14(5):625-30.
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1995: Rogers M J; Xiong X; Brown R J; Watts D J; Russell R G; Bayless A V; Ebetino F H
Structure-activity relationships of new heterocycle-containing bisphosphonates as inhibitors of bone resorption and as inhibitors of growth of Dictyostelium discoideum amoebae.
Molecular pharmacology 1995;47(2):398-402.
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1994: Rogers M J; Ji X; Russell R G; Blackburn G M; Williamson M P; Bayless A V; Ebetino F H; Watts D J
Incorporation of bisphosphonates into adenine nucleotides by amoebae of the cellular slime mould Dictyostelium discoideum.
The Biochemical journal 1994;303 ( Pt 1)():303-11.
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1994: Rogers M J; Watts D J; Russell R G; Ji X; Xiong X; Blackburn G M; Bayless A V; Ebetino F H
Inhibitory effects of bisphosphonates on growth of amoebae of the cellular slime mold Dictyostelium discoideum.
Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research 1994;9(7):1029-39.
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