Pharmaleads
Immeuble Paris BioPark
11 Rue Watt
75013 PARIS
Tel: +33 (0)1 44 06 70 00
fax: +33 (0)1 44 06 60 99
CONTACTEZ-NOUS

Pharmaleads’ publications

1.  Padia S.H., Howell N.L., Kemp B.A., Fournié-Zaluski M.C., Roques B.P., Carey R.M., Intrarenal Aminopeptidase N Inhibition Restores Defective Angiotensin II Type 2-Mediated Natriuresis in Spontaneously Hypertensive Rats, Hypertension 2010, 55 part 2, 474-480.

2.  Roques B.P., Potentiation of the control of pain by endogeneous enkephalins through inhibition of their enzymatic inactivation, a new approach towards physiological analgesics, (in French), Douleur Analg., 2009, 22 : 1-93.  

3.  Gonzalez-Rodríguez S., Pevida M., Roques B.P., Fournié-Zaluski M.C., Hidalgo A., Menéndez L., Baamonde A., Involvement of enkephalins in the inhibition of osteosarcoma-induced thermal hyperalgesia evoked by the blockade of peripheral P2X3 receptors, Neurosci Lett. 2009 Nov 20; 465(3):285-9.

4.  Fournié-Zaluski M.C., Poras H., Roques B.P., Nakajima Y., Ito K., Yoshimoto T., Structure of aminopeptidase N from Escherichia coli complexed with the transition-state analogue aminophosphinic inhibitor PL250”, Acta Crystallographica, Section D: Biological Crystallography,  2009,  D65(8),  814-822.

5.  Poras H., Ouimet T., Orng S-V., Fournié-Zaluski M.C., Popoff M., Roques B.P.,  Detection and quantification of botulinum neurotoxin type A by a novel rapid in vitro fluorimetric assay, Applied and Environmental Microbiology,  2009,  75(13),  4382-4390.

6.  Cabanero D., Celerier E., García-Nogales P., Mata M., Roques B.P., Maldonado R., Puig M.M., Thepro-nociceptive effects of remifentanil or surgical injury in mice are associated with a decrease in delta-opioid receptor mRNA levels: Prevention of the nociceptive response by on-site delivery of enkephalins, Pain 2009, 141, 88-96.

7.  Sevalle J., Amoyel A., Robert P., Fournié-Zaluski M.C., Roques B.P., Checler F., Aminopeptidase A contributes to the N-terminal truncation of amyloid β-peptide, J Neurochem, 2009, 109, 248-256.

8.  Roques B.P., Neuropeptide inactivation or metabolism in Squire L.R., Encyclopedia of Neuroscience, 2009, 6, 789-799, Oxford Academic Press.

9.  Menendez L., Meana A., Poras H., Fournié-Zaluski M.C., Roques B.P.,  Baamonde A. Inhibition of osteosarcoma-induced thermal hyperalgesia in mice by the orally active dual enkephalinase inhibitor PL37, potentialisation by gabapentin,  Eur J Pharmacol,  2008,  596(1-3),  50-55.

10.  Ouimet T., Poras H., Orng S-V., Duquesnoy S., Fournié-Zaluski M.C., Roques B.P., Design of fluorogenic substrates for botulinum toxin A quantification and identification of a novel cooperative exosite for substrate binding, Toxicon, 2008, 51, 17

11.  Lancelot E., Amirbekian V., Brigger I., Raynaud J.S., Ballet S., David C., Rousseaux O., Le Greneur S., Port M., Lijnen H.R., Bruneval P., Michel J.B., Ouimet T., Roques B.P., Amirbekian S., Hyafil F., Vucic E., Aguinaldo J.G., Corot C., Fayad Z.A., Evaluation of matrix metalloproteinases in atherosclerosis using a novel non-invasive imaging approach, Arterioscler Thromb Vasc Biol, 2008 Mar; 28(3):425-32.

12.  Noble F., Benturquia N., Bilkei-Gorzo A., Zimmer A., Roques B.P., Use of preproenkephalin knockout mice and selective inhibitors of enkephalinases to investigate the role of enkephalins in various behaviours, Psychopharmacology, 2008, 196:327-335.

13.  Karine T., Bonnard E., Dubacq S., Fournié-Zaluski M.C., Roques B.P., Calvino B., Antinociceptive and anti-allodynic effects of oral PL37, a complete inhibitor of enkephalin-catabolizing enzymes, in a rat model of peripheral neuropathic pain induced by vincristine, Eur J Pharmacol,  2008, 600:71-77.

14.  Tholander F., Muroya A., Roques B.P., Fournié-Zaluski M.C., Thunnissen M., Haeggström J.Z.,  Structure-Based Dissection of the Active Site Chemistry of Leukotriene A4 Hydrolase: Implications for M1 Aminopeptidases and Inhibitor Design, Chem Biol 2008, 15, 9020-929.

15.  Padia S.H., Kemp, B.A., Howell N.L., Fournié-Zaluski M.C., Roques B. P., Carey R.M., Conversion of Renal Angiotensin II to Angiotensin III is critical for AT2 receptor-mediated natriuresis in rats, Hypertension, 2008, 51(2):460-465

16.  Noble F., Roques B.P., Protection of endogenous enkephalin catabolism as natural approach to novel analgesic and antidepressant drugs », Expert Opinion, Therapeutics Targets (2007);11(2):145-159.

17.  Cordonnier L, Sanchez M, Roques B.P., Noble F., Blockade of morphine-induced behavioral sensitization by a combination of amisulpride and RB101, comparison with classical opioid maintenance treatments”, Br J Pharmacol. 2007 May; 151(1):94-102.

18.  Padia S.H., Kemp B.A., Howell N.L., Siragy H.M., Fournié-Zaluski M.C., Roques B.P., Carey R.M., Intrarenal aminopeptidase N inhibition augments natriuretic responses to angiotensin III in angiotensin type 1 receptor-blocked rats, Hypertension. 2007 Mar; 49(3):625-30.

19.  Jardinaud F., Roques B.P., Noble F., Tolerance to the reinforcing effects of morphine in delta9-tetrahydrocannabinol treated mice, Behavioural Brain Res., 2006, 173, 255-26.

20.  Sihn G., Savary K., Michaud A., Fournié-Zaluski M.C., Roques B.P., Corvol P., Gasc J.M., Aminopeptidase N during the ontogeny of the chick, Differentiation 2006 Mar; 74(2-3):119-28.

21.  Jardinaud F., Crété D., Canestrelli C., Ledent C., Roques B.P., Noble F., CB1 receptors knock-out mice show similar behavioral modifications to wild type mice when enkephalin catabolism is inhibited, Brain Res., 2005, 1063, 77-83.

22.  Cordonnier L., Sanchez M., Roques B.P., Noble F., Facilitation of enkephalin-induced delta-opioid behavioral responses by chronic amisulpride treatment, Neuroscience, 2005, 135(1), 1-10.

23.  Mas Nieto M., Guen S.L., Kieffer B.L., Roques B.P., Noble F., Physiological control of emotion-related behaviors by endogenous enkephalins involves essentially the delta opioid receptors”, Neuroscience. 2005; 135(2):305-13.

24.  Anne C., Turcaud S., Blommaert A.G., Darchen F., Johnson E.A., Roques B.P., Partial protection against Botulinum B neurotoxin-induced blocking of exocytosis by a potent inhibitor of its metallopeptidase activity, Chembiochem. 2005 Aug. 6(8):1375-80.

25.  Raguin O., Fournié-Zaluski M.C., Romieu A., Pelegrin A., Chatelet F., Pelaprat D., Barbet J., Roques B.P., Gruaz-Guyon A., A labeled neutral endopeptidase inhibitor as a potential tool for tumor diagnosis and prognosis, Angew. Chem. Int. Ed Engl. 2005 Jun 27; 44(26):4058-61.

26.  Oefner C., Roques B.P., Fournié-Zaluski M.C., Dale G.E., Structural analysis of neprilysin with various specific and potent inhibitors”, Acta Crystallogr. D Biol. Crystallogr. 2004 Feb; 60 (Pt 2):392-396.27.  

27.  Jardinaud F., Banisadr G., Noble F., Mélik-Parsadaniantz S., Chen H., Dugave C., Laplace H., Rostène W., Fournié-Zaluski M.C., Roques B.P., Popovici T. Ontogenic and adult whole body distribution of aminopeptidase N in rat investigated by autoradiography, Biochimie 2004, 86, 105-113.28.  

28.  Roques B.P., Noble F., Inhibitors of enkephalin-Inactivating Enzymes and delta opioid responses. in The Delta Receptor, chapter 17 (2004) pp. 277-296, Eds K.J. Chang, F. Porreca and J.H. Woods.29.  

29.  Le Guen S., Mas Nieto M., Canestrelli C., Chen H., Fournié-Zaluski M.C., Cupo A., Maldonado R., Roques B.P., Noble F. , Pain management by a new series of dual inhibitors of enkephalin degrading enzymes: long lasting antinociceptive properties and potentiation by CCK2 antagonist or methadone, Pain. 2003 Jul; 104(1-2):139-48.

30.  Selkti M., Tomas A., Gaucher J.H., Prangé T., Fournié-Zaluski M.C., Chen H., Roques B.P., Interactions of a new αaminophosphinic derivative with the active site of TLN (thermolysin): a model for zinc metalloendopeptidase inhibition, Acta Crystallogr. D Biol. Crystallogr. 2003, 59(Pt. 7), 1200-1205.

31.  Anne C., Turcaud S., Quancard J., Teffo F., Meudal H., Fournie-Zaluski M.C., Roques B.P., Development of potent inhibitors of botulinum neurotoxin type B, J Med Chem. 2003 Oct 23; 46(22):4648-56.32.  

32.  Anne C., Blommaert A., Turcaud S., Martin A.S., Meudal H., Roques B.P., Thio-derived disulfides as potent inhibitors of botulinum neurotoxin type B: implications for zinc interaction. Bioorg. Med. Chem. 2003 Oct 15; 11(21):4655-60.33.  

33.  Fournié-Zaluski M.C., Roques B.P., New Selective Aminopeptidases N Inhibitors as Potential Therapeutics”, Ectopeptidases, Langner and Ansorge Kluwer Academic/Plenum Publishers, Chapter 3, New York, 2002.

34.  Mock M., Roques B.P., Progress in rapid screening of Bacillus anthracis lethal factor activity, Proc. Natl. Acad. Sci. U S A. 2002 May 14; 99(10):6527-9.

35.  Benoist J.M., Keime F., Montagne J., Noble F., Fournié-Zaluski M.C., Roques B.P., Willer J.C., Le Bars D., Depressant effect on a C-fiber reflex in the rat, of RB 101, a dual inhibitor of enkephalin-degrading enzymes. Eur. J. Pharmacol., 2002, 445(3), 201-210.

36.  Le Guen S., Noble F., Fournié-Zaluski M.C., Roques B.P., Besson J.M., Buritova J., RB 101(s), a dual inhibitor of enkephalinases does not induce antinociceptive tolerance, or cross-tolerance with morphine: a c-Fos study at the spinal level. Eur. J. Pharmacol., 2002, 441(3), 141-150.

37.  Anne C., Cornille F., Lenoir C., Roques B.P., High-throughput fluorogenic assay for determination of botulinum type B neurotoxin protease activity, Anal. Biochem. 2001 Apr 15; 291(2):253-61.

38.  Roques B.P., Anne C., Turcaud S., Fournié-Zaluski M.C., Mechanism of action of clostridial neurotoxins and rational inhibitor design, Biol. Cell. 2000 Sep; 92(6):445-7. Review.

Pharmaleads’ latest oral presentations

a.   Ouimet T., Poras H., Orng S-V., Fournié-Zaluski M.C., Popoff M., Roques B.P., Detection and quantification of Botulinum Neurotoxin type A by a novel rapid in vitro fluorigenic assay, Interagency Botulism Research Coordinating Committee, 46th annual meeting, Alexandria VA, 2009.

b.   Courtois S., Poras H., Pinon A., Vialette M., Ouimet T., Fournié-Zaluski M.C., RALF Project: Rapid Analysis of Legionella by Fluorescence”, Kick-off meeting ANR Preccood 2008, Montpellier, 2009.

c.   Schreiter A., Gore C., Roques B.P., Fournié-Zaluski M.C., Stein C., Machelska H., Protection of opioid peptide catabolism for pain control in peripheral inflamed tissue, , International Research Narcotics Conference, Portland OR, 2009.

d.   Ouimet T., Poras H., Orng S-V., Duquesnoy S., Fournié-Zaluski M.C., Roques B.P., Design of fluorigenic peptide substrates for Botulinum Toxin A. Quantification and identification of novel cooperative sites for substrates binding, Toxins 2008, Bavenno (Italy), 2008.

e.   Padia S.H., Keller S.R., Gildea J.J., Kemp, B.A., Howell N.L., Roques B. P., Fournié-Zaluski M.C., Carey R.M., Intrarenal APN inhibition enables natriuretic responses and AT2R recruitment in SH‎R, Hypertensions Council Meeting, AHA, 2008.

f.    Poras H., Dangé E., Bonnard E., Wurm M., Fournié-Zaluski M.C., Roques B.P., Protection of endogenous enkephalins by PL37, a dual NEP/APN inhibitor induces potent analgesic responses p.o. in neuropathic pain, 29th International Symposium of Medicinal Chemistry, Vienna, 2008.

g.   Chen S., Kuan S., Walker K., Murphy P., Richardson S., Ouimet T., Roques B.P., Evaluation of a Fluorogenic-based Assay to Detect Botulinum Toxin Type B Activity, 45th Annual Meeting of the Interagency Botulism Research Coordinating Committee, Philadelphia PE, 2008.

h.   Curto-Reyes V., Juarez L., Meana A., Menendez L., Baamonde A., Fournié-Zaluski M.C., Poras H., Roques B.P., Peripheral enkephalins, protected from their peptidase-related catabolism by the dual inhibitor PL37, inhibit thermal hyperalgesia in a model of murine osteosarcoma, International Narcotics Research Conference, Berlin, 2007.

i.    Poras H., Orng S-V., Popoff M., Fournié-Zaluski M.C., Roques B.P., Développement d’un substrat à fluorescence reprimée spécifique de BoNTA, 15ème Groupement Français Peptides et Protéines, Dinard, 2007.

j.    Gore C., Mousa S. A., Roques B.P., Stein C., Machelska H., Peripheral analgesia by preventing opioid peptide degradation in inflamed tissue”, International Research Narcotics Conference, Berlin 2007.