Bernard Roques

Bernard Roques a publié plus de 650 articles et déposé 30 brevets dont 20 Inserm, tous étendus au plan international. Son laboratoire a accueilli plus de 30 post-doctoraux étrangers.

Sélection des principales publications

• Le Pecq JB, Le Bret M, Barbet J, Roques BP. DNA polyintercalating drugs : DNA binding of diacridine derivatives. Proc Natl Acad Sci USA 72: 2915-9, 1975.
• Roques BP, Garbay-Jaureguiberry C, Oberlin R, Anteunis M, Lala AK. Conformation of the endogenous opiate-like pentapeptide Met-enkephalin determined by high field NMR spectroscopy. Nature 262: 778-9, 1976.
• Waksman G, Changeux JP, Roques BP. Structure requirement for agonist and non competitive blocking action of acylcholine derivatives on electrophorus electricus electroplaque. Mol Pharmacol 18: 20-7, 1980.
• Roques BP, Fournie-Zaluski MC, Soroca E, Lecomte JM, Malfroy B, Llorens C, Schwartz JC. The enkephalinase inhibitor thiorphan shows antinociceptive activity in mice. Nature 288: 286-8, 1980.
• Fournie-Zaluski MC, Gacel G, Maigret B, Premilat S, Roques BP. Structural requirements for specific recognition of mu and delta opiate-receptors. Mol Pharmacol 20: 484-91, 1981.
• Roques BP, Lucas-Soroca E, Chaillet P, Costentin J, Fournie-Zaluski MC. Complete differentiation between "enkephalinase" and angiotensin converting enzyme inhibition by retro-thiorphan. Proc Natl Acad Sci USA 80: 3178-82, 1983.
• Garbay-Jaureguiberry C, Robichon A, Dauge V, Rossignol P, Roques BP. Highly selective photoaffinity labelling of mu and delta opioid recetors. Proc Natl Acad Sci USA 81, 7718-7723, 1984.
• Laugaa P, Markovits J, Delbarre A, Le Pecq JB, Roques BP. DNA tris-intercalation : first acridine trimer with DNA affinity in the range of DNA regulatory proteins. Kinetic studies. Biochemistry 24: 5567-75, 1985.
• Waksman G, Hamel E, Fournie-Zaluski MC, Roques BP. Comparative distribution of the neutral endopeptidase "enkephalinase" and mu and delta opioid receptors in rat brain by autoradiography. Proc Natl Acad Sci USA 83: 1523-7, 1986.
• Delbarre A, Delepierre M, Garbay C, Igolen J, Le Pecq JB, Roques BP. Geometry of the antitumor drug ditercalinium bisintercalated into d[CpGpCpG]2 by 1H NMR. Proc Natl Acad Sci USA 84: 2155-9, 1987.
• Devault A, Lazure C, Nault C, Le Moual H, Seidah NG, Chretien M, Kahn P, Powell J, Mallet J, Beaumont A, Roques BP, Crine P, Boileau G. Amino acid sequence of rabbit kidney neutral endopeptidase 24.11 (enkephalinase) deduced from a complementary DNA. EMBO J 6: 1317-22, 1987.
• Charpentier B, Pelaprat D, Durieux C, Dor A, Reibaud M, Blanchard JC, Roques BP. Cyclic cholecystokinin analogues highly selective towards central receptors. Proc Natl Acad Sci USA 85: 1968-72, 1988.
• Roques BP, Beaumont A. Neutral endopeptidase-24,11 inhibitors : from analgesics to antihypertensives? Trends in Pharmacological Sciences 11: 245-9, 1990.
• Morellet N, Jullian N, De Rocquigny H, Maigret B, Darlix JL, Roques BP. Determination of the structure of the nucleocapsid protein NCp7 from the human immunodeficiency virus type 1 by 1H NMR. EMBO J 11: 3059-65, 1992.
• Fournie-Zaluski MC, Soleilhac JM, Turcaud S, Lai-Kuen R, Crine P, Beaumont A, Roques BP. Development of [125I]RB104, a potent inhibitor of neutral endopeptidase-24,11 and its use in detecting nanogram quantities of the enzyme by “Inhibitor Gel Electrophoresis”. Proc Natl Acad Sci. USA 89: 6388-92, 1992.
• Roques BP, Noble F, Dauge V, Fournie-Zaluski Mc, Beaumont A. Neutral endopeptidase 24.11. Structure, inhibition, and experimental and clinical pharmacology. Pharmacol Rev 45: 87-146, 1993.
• Yang YS, Garbay C, Duchesne M, Cornille F, Jullian N, Fromage N, Tocque B, Roques BP. Solution structure of GAP SH3 domain by 1H NMR and spatial arrangement of essential Ras-signaling involved sequence. EMBO J 13: 1270-9, 1994.
• Fournie-Zaluski MC, Gonzalez W, Turcaud S, Pham I, Roques BP, Michel JB. Dual inhibition of angiotensin converting enzyme and neutral endopeptidase by the orally active inhibitor mixanpril I : a new therapeutic approach in hypertension. Proc Natl Acad Sci USA 91: 4072-6, 1994.
• Goudreau N, Cornille F, Duchesne M, Parker F, Tocque B, Garbay C, Roques BP. NMR structure of the N-terminal SH3 domain of Grb2 and its complex with a proline-rich peptide from Sos. Nat Struct Biol 1: 898-907, 1994.
• Maldonado R, Blendy JA, Tzavara E, Gass P, Roques BP, Hanoune J, Schütz G. A mutation in the CREB gene strongly reduces the withdrawal syndrome in morphine dependent mice. Science 273: 657-9, 1996.
• Matthes HWD, Maldonado R, Simonin F, Valverde O, Slowe S, Kitchen I, Befort K, Dierich A, Le Meur M, Dolle P, Tzavara E, Hanoune J, Roques BP, Kieffer BL. Loss of morphine-induced analgesia, reward effect and withdrawal symptoms in mice lacking the µ-opioid-receptor gene. Nature 383: 819-23, 1996.
• Zin S, Fournie-Zaluski MC, Chauve E, Roques BP, Corvol P, Llorens-Cortes C. Identification of metabolic pathways of brain angiotensin II and III using specific aminopeptidase inhibitors : Predominant role of angitensin III in the control of vasopressin release. Proc Natl Acad Sci USA 93: 11968-73, 1996.
• Maldonado R, Saiardi A, Valverde O, Samad Ta, Roques BP, Borrelli E. Absence of opiate rewarding effects in mice lacking dopamine D2 receptors. Nature 388: 586-9, 1997.
• Morellet N, Demene H, Teilleux V, Huynh-Dinh T, De Rocquigny H, Fournie-Zaluski MC, Roques BP. Structure of the complex between the HIV-1 nucleocapsid protein NCp7 and the single-stranded pentanucleotide d(ACGCC). J Mol Biol 283: 419-34, 1998.
• Chen H, Noble F, Coric P, Fournie-Zaluski Mc, Roques BP. Aminophosphinic inhibitors as transition state analogues of enkephalin-degrading enzymes : A new class of central analgesics. Proc Natl Acad Sci USA 95: 12028-33, 1998.
• Reaux A, Fournie-Zaluski MC, David C, Zini S, Roques BP, Corvol P, Llorens-Cortes C. Aminopeptidase A inhibitors as potential central antihypertensive agents. Proc Natl Acad Sci USA 96: 13415-1342, 1999.
• Cussac D, Vidal M, Leprince C, Liu WQ, Cornille F, Tiraboschi G, Roques BP, Garbay C. A Sos-derived peptidimer blocks the Ras signalling pathway by binding both Grb2 SH3 domains and displays antiproliferative activity. FASEB J 13: 31-8, 1999.
• Druillennec S, Dong Cz, Escaich S, Gresh N, Bousseau A, Roques BP, Fournie-Zaluski MC. A mimic of HIV-1 NC protein impairs reverse transcription and display antiviral activity. Proc Natl Acad Sci USA 96: 4886-91, 1999.
• Ledent C, Valverde O, Cossu G, Petitet F, Aubert JF, Beslot F, Böhme A, Imperato A, Pedrazzini T, Roques BP, Vassart G, Fratta W, Parmentier M. Unresponsiveness to cannabinoids and reduced addictive effects of opiates in CB1 receptor knockout mice. Science 283:401-4, 1999.
• Roques BP. Novel approaches to targeting neuropeptide systems. Trends Pharmacol Sci 21: 475-83, 2000.
• Gajiwala KS, Chen H, Cornille F, Roques BP, Reith W, Mach B, Burley SK. Structure of the winged-helix protein hRFX1 reveals a new mode of DNA binding. Nature 403: 916-21, 2000.
• Boya P, Roques BP, Kroemer G. Bacterial and viral proteins regulating apoptosis at the mitochondrial level. EMBO J 20: 4325-31, 2001.
• Mock M, Roques BP. Progress in rapid screening of Bacillus anthracis lethal factor activity. Proc Natl Acad Sci USA 99: 6527-9, 2002.
• Fournie-Zaluski MC, Fassot C, Valentin B, Djordjijevic D, Reaux Le Goazigo A, Corvol P, Roques BP, Llorens-Cortes C. Brain renin angiotensin system blockade by systemically active aminopeptidase A inhibitors : a potential treatment of salt-dependent hypertension. Proc Natl Acad Sci USA 101: 7775-80, 2004.
• Civelli O, Bouvier M, Devi L, Bartfai T, Strange P, Christopoulos A, George S, Sakmar TP, Pin JP, Roques BP, Bockaert J, Leurs R, Seifert R. Twenty questions: The state of GPCR research in 2004. Nature Reviews Drug Discovery 3: 577-626, 2004.
• Raguin O, Fournie-Zaluski MC, Romieu A, Pelegrin A, Chatelet F, Barbet J, Roques BP, Guyon-Gruaz. A. A labeled neutral endopeptidase inhibitor as a potential tool for tumor diagnosis and prognosis. Angew Chem Int Ed Engl 44: 4058-61, 2005.
• Nieto MM, Le Guen S, Kieffer B, Roques BP, Noble F. Physiological control of emotion by endogenous enkephalins involves essentially the delta opioid receptors. Neuroscience 135: 305-13, 2005.
• Sabbah EN, Druillennec S, Morellet N, Bouaziz S, Kroemer G, Roques BP. Interaction between the HIV-1 protein Vpr and the adenine nucleotide translocator. Chem Biol Drug Des 67(2):145-54, 2006.
• Padia SH, Kemp BA, Howell NL, Siragy HM, Fournie-Zaluski MC, Roques BP, Carey RM. Intrarenal aminopeptidase N inhibition augments natriuretic responses to angiotensin III in angiotensin type 1 receptor-blocked rats. Hypertension. Mar;49(3):625-30, 2007. Epub 2006 Dec 26.
• Purohit V, Roques BP, Kim B, Bambara RA. Mechanisms that prevent template inactivation by HIV-1 reverse transcriptase RNase H cleavages. J Biol Chem 27; 282(17): 12598-609, 2007. Epub 2007 Mar 2.
• Bodineau L, Frugière A, Marc Y, Inguimbert N, Fassot C, Balavoine F, Roques B, Llorens-Cortes C. Orally active aminopeptidase A inhibitors reduce blood pressure: a new strategy for treating hypertension. Hypertension 51(5): 1318-25, 2008.
• Tholander F, Roques BP, Fournié-Zaluski MC, Thunnissen MM, Haeggström JZ. Crystal structure of leukotriene A4 hydrolase in complex with kelatorphan, implications for design of zinc metallopeptidase inhibitors. FEBS Lett 4; 584(15): 3446-51, 2010.
• Roques BP, Fournié-Zaluski MC, Wurm M. Inhibiting the breakdown of endogenous opioids and cannabinoids to alleviate pain. Nat Rev Drug Discov 11(4):292-310, 2012. Review.

Rapport

Roques B.Rapport sur la dangerosité des drogues au secrétariat d’État à la Santé. Préface de Bernard Kouchner, janvier 1999, 192 pages.