Viral RNA annealing activities of human immunodeficiency virus type 1 nucleocapsid protein require only peptide domains outside the zinc fingers.
- H. de Rocquigny, C. Gabus, A. Vincent, M. Fournié-Zaluski, B. Roques, J. Darlix
- Biology, ChemistryProceedings of the National Academy of Sciences…
- 15 July 1992
It is shown here that synthetic NCp7 with or without the two zinc fingers has the RNA annealing activities of NCp15, and could be used as a model for the design of antiviral agents.
Inhibiting the breakdown of endogenous opioids and cannabinoids to alleviate pain
- B. Roques, M. Fournié-Zaluski, M. Wurm
- BiologyNature reviews. Drug discovery
- 1 April 2012
The effects of Dual enkephalinase inhibitors and FAAH inhibitors are compared and the progress in their rational design is described, to consider the challenges in their clinical development and opportunities for combination therapies.
Identification of metabolic pathways of brain angiotensin II and III using specific aminopeptidase inhibitors: predominant role of angiotensin III in the control of vasopressin release.
- S. Zini, M. Fournié-Zaluski, E. Chauvel, B. Roques, P. Corvol, C. Llorens-Cortes
- Biology, ChemistryProceedings of the National Academy of Sciences…
- 15 October 1996
Ang III behaves as one of the main effector peptides of the brain renin-angiotensin system in the control of vasopressin release, demonstrating for the first time that APA and APN are involved in vivo in the metabolism of brain Ang II and Ang III.
The enkephalinase inhibitor thiorphan shows antinociceptive activity in mice
- B. Roques, M. Fournié-Zaluski, J. Schwartz
- BiologyNature
- 20 November 1980
Thiorphan is reported here that this compound, thiorphan [(DL-3-mercapto-2-benzylpropanoyl)-glycine; patent no. 8008601] protects the enkephalins from the action of enkephalinase in vitro in nanomolar concentration and in vivo after either intracerebroventricular or systemic administration.
Brain renin-angiotensin system blockade by systemically active aminopeptidase A inhibitors: a potential treatment of salt-dependent hypertension.
- M. Fournié-Zaluski, C. Fassot, C. Llorens-Cortes
- Biology, MedicineProceedings of the National Academy of Sciences…
- 18 May 2004
It is reported that brain AngIII exerts a tonic stimulatory effect on blood pressure in a model of salt-dependent hypertension, the DOCA-salt rat, characterized by a depressed systemic but a hyperactive brain RAS, and suggested that RB150, a potent systemically active APA inhibitor, could be the prototype of a new class of antihypertensive agents for the treatment of certain forms of hypertension.
Conformational behaviour of the active and inactive forms of the nucleocapsid NCp7 of HIV-1 studied by 1H NMR.
- N. Morellet, H. de Rocquigny, B. Roques
- Biology, ChemistryJournal of Molecular Biology
- 7 January 1994
Angiotensin III: a central regulator of vasopressin release and blood pressure
- A. Réaux, M. Fournié-Zaluski, C. Llorens-Cortes
- BiologyTrends in endocrinology and metabolism
- 1 May 2001
Aminopeptidase A inhibitors as potential central antihypertensive agents.
- A. Réaux, M. Fournié-Zaluski, C. Llorens-Cortes
- Biology, ChemistryProceedings of the National Academy of Sciences…
- 9 November 1999
In rats, ICV injection of the selective APA inhibitor EC33 blocked the pressor response of exogenous AngII, suggesting that the conversion of AngII to Ang III is required to increase blood pressure (BP), and demonstrates that AngIII is a major effector peptide of the brain RAS, exerting tonic stimulatory control over BP.
Structure of the complex between the HIV-1 nucleocapsid protein NCp7 and the single-stranded pentanucleotide d(ACGCC).
- N. Morellet, H. Déméné, B. Roques
- Biology, ChemistryJournal of Molecular Biology
- 23 October 1998
A mechanism of action for NCp7 in virus morphogenesis and replication is proposed from these results, which could facilitate the design of possible antiviral agents acting by a new mechanism.
Structural analysis of neprilysin with various specific and potent inhibitors.
- C. Oefner, B. Roques, M. Fournié-Zaluski, G. Dale
- Biology, ChemistryActa Crystallographica Section D: Biological…
- 1 February 2004
The crystal structures of the soluble extracellular domain of human NEP complexed with various potent and competitive inhibitors are described and unambiguously reveal the binding mode of the different zinc-chelating groups and the subsite specificity of the enzyme.
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