A mimic of HIV-1 nucleocapsid protein impairs reverse transcription and displays antiviral activity
Druillennec, S., Dong, C. Z., Escaich, S., Gresh, N., Bousseau, A., Roques, B. P., ...
Combined inhibition of HIV-1 reverse transcriptase and protease has significantly improved the treatment of AIDS. Nevertheless, resistance to these drugs occurs rapidly because of viral mutations,...
Zini, S, Fournie-Zaluski, M C, Chauvel, E, Roques, B P, Corvol, P, Llorens-Cortes, C
Angiotensin (Ang) II and Ang III are two peptide effectors of the brain renin-angiotensin system that participate in the control of blood pressure and increase water consumption and vasopressin...
Fournié-Zaluski, M C, Gonzalez, W, Turcaud, S, Pham, I, Roques, B P, Michel, J B
In the treatment of cardiovascular disease, it could be of therapeutic interest to associate the hypotensive effects due to the inhibition of angiotensin II formation with the diuretic and...
Fournié-Zaluski, M C, Soleilhac, J M, Turcaud, S, Laï-Kuen, R, Crine, P, Beaumont, A, ...
Neutral endopeptidase 24.11, also known as the common acute lymphoblastic leukemia antigen, is a zinc metallopeptidase involved in the inactivation of biologically active peptides, such as the...
DNA binding properties of a chemically synthesized DNA binding domain of hRFX1.
Cornille, F, Emery, P, Schüler, W, Lenoir, C, Mach, B, Roques, B P, ...
The RFX DNA binding domain (DBD) is a novel highly conserved motif belonging to a large number of dimeric DNA binding proteins which have diverse regulatory functions in eukaryotic organisms, ranging...
Li, X, Quan, Y, Arts, E J, Li, Z, Preston, B D, De Rocquigny, H, ...
Retroviral reverse transcription starts near the 5' end of unspliced viral RNA at a sequence called the primer binding site (PBS), where the tRNA primer anneals to the RNA template for initiation of...
Carteau, S, Batson, S C, Poljak, L, Mouscadet, J F, De Rocquigny, H, Darlix, J L, ...
The integrase (IN) protein of the human immunodeficiency virus mediates integration of the viral DNA into the cellular genome. In vitro, this reaction can be mimicked by using purified recombinant IN...
Housset, V, De Rocquigny, H, Roques, B P, Darlix, J L
Nucleocapsid (NC) protein NCp10 of Moloney murine leukemia virus is encoded by the 3' domain of gag and contains a zinc finger surrounded by basic amino acids. During virion assembly, NC protein is...
Cyclic cholecystokinin analogues with high selectivity for central receptors.
Charpentier, B, Pelaprat, D, Durieux, C, Dor, A, Reibaud, M, Blanchard, J C, ...
Taking as a model the N-terminal folding of the cholecystokinin tyrosine-sulfated octapeptide [CCK-8; Asp-Tyr(SO3H)-Met-Gly-Trp-Met-Asp-Phe-NH2] deduced from conformational studies, two cyclic...
Lambert, B, Jones, B K, Roques, B P, Le Pecq, J B, Yeung, A T
We have demonstrated that the noncovalent complex formed between DNA and an antitumor bifunctional intercalator, ditercalinium, is recognized in vitro as bulky covalent DNA lesions by the purified...
Geometry of the antitumor drug ditercalinium bisintercalated into d(CpGpCpG)2 by 1H NMR.
Delbarre, A, Delepierre, M, Garbay, C, Igolen, J, Le Pecq, J B, Roques, B P
Rigid 7H-pyrido[4,3-c]carbazole dimers, such as Ditercalinium, are DNA bisintercalators that display high DNA affinity and strong antitumor properties. This activity appears crucially dependent on...
De Rocquigny, H, Ficheux, D, Gabus, C, Allain, B, Fournie-Zaluski, M C, Darlix, J L, ...
The 56 amino acid nucleocapsid protein (NCp10) of Moloney Murine Leukemia Virus, contains a CysX2CysX4HisX4Cys zinc finger flanked by basic residues. In vitro NCp10 promotes genomic RNA dimerization,...
Two rotameric forms of open ring 7-methylguanine are present in alkylated polynucleotides.
Boiteux, S, Belleney, J, Roques, B P, Laval, J
High performance liquid chromatography analysis of imidazole open ring 7-methylguanine, 2-6 diamino-4-hydroxy-5N-methyl-formamidopyrimidine (rom7G), showed two well-separated peaks (fI and fII) of...
Waksman, G, Hamel, E, Fournié-Zaluski, M C, Roques, B P
The neutral endopeptidase EC 3.4.24.11, also designated enkephalinase, has been visualized by in vitro autoradiography using the tritiated inhibitor...
Delbarre, A, Gourevitch, M I, Gaugain, B, Le Pecq, J B, Roques, B P
Comparative 1H NMR and optical studies of the interaction between poly(dA-dT), ethidium bromide (Et) and ethidium dimer (Et2) in 0.7 M NaCl are reported as a function of the temperature. Denaturation...
Lambert, B, Roques, B P, Le Pecq, J B
Ditercalinium, an antitumor bifunctional intercalator which forms a high affinity reversible complex with DNA, was found to be specifically cytotoxic for polA and lig7 E. coli strains. In the polA...
Markovits, J, Ramstein, J, Roques, B P, Le Pecq, J B
Ethidium dimer is shown to bind by intercalation, almost equally well, to the B and Z form of poly[(dG-m5dC)].poly[(dG-m5dC)], whereas the ethidium monomer shows a strong preference for the B form....
Le Bret, M, Le Pecq, J B, Barbet, J, Roques, B P
The rate of energy transfer between DNA intercalated ethidium cations calculated by Paoletti and Le Pecq1 using the Forster theory differs from the measured one by a factor of twenty two, if the...
Highly selective photoaffinity labeling of mu and delta opioid receptors.
Garbay-Jaureguiberry, C, Robichon, A, Daugé, V, Rossignol, P, Roques, B P
We report the synthesis and photolabeling properties of two highly selective ligands for mu and delta opioid-binding sites: Tyr-D-Ala-Gly-MePhe (pN3)-Gly-ol (AZ-DAMGE) and Tyr-D-Thr-Gly-Phe...
Roques, B P, Lucas-Soroca, E, Chaillet, P, Costentin, J, Fournié-Zaluski, M C
Thiorphan, N-[(R,S)-3-mercapto-2-benzylpropanoyl]glycine is a highly potent inhibitor (Ki = 3.5 nM) of "enkephalinase," a metalloendopeptidase cleaving the Gly-Phe bond (positions 3 and 4) of...
Yang, Y S, Garbay, C, Duchesne, M, Cornille, F, Jullian, N, Fromage, N, ...
Src homology 3 (SH3) domains are found in numerous cytoplasmic proteins involved in intracellular signal transduction. We used 2-D 1H NMR to determine the structure of the SH3 domain of the guanosine...
Ramboarina, S., Druillennec, S., Morellet, N., Bouaziz, S., Roques, B. P.
The modification of zinc-binding residues inside the conserved CCHC motif of human immunodeficiency virus type 1 NCp7, in particular into CCHH, induces a complete loss of infectivity. Since the...
Morellet, N, Jullian, N, De Rocquigny, H, Maigret, B, Darlix, J L, Roques, B P
The retroviral gag nucleocapsid protein NCp7 (72 amino acids) of HIV-1 (LAV strain), which contains two successive zinc fingers of the Cys-X2-Cys-X4-His-X4-Cys form linked by a stretch of basic...
Lemay, G, Zollinger, M, Waksman, G, Roques, B P, Crine, P, Boileau, G
Neutral endopeptidase-24.11 (EC 3.4.24.11) (NEP) is a transmembrane metallo-endopeptidase that has been shown to be involved in the degradation of several mammalian neuropeptides, including...
Characterization of neutral endopeptidase 24.11 in dog glomeruli.
Landry, C, Santagata, P, Bawab, W, Fournié-Zaluski, M C, Roques, B P, Vinay, P, ...
Neutral endopeptidase (NEP; also known as neprilysin and enkephalinase; EC 3.4.24.11) is a cell-surface metallopeptidase that is present in many mammalian tissues. It is particularly abundant on the...
Dion, N, Le Moual, H, Fournié-Zaluski, M C, Roques, B P, Crine, P, Boileau, G
Neprilysin (EC 3.4.24.11) is a Zn2+ metallopeptidase involved in the degradation of biologically active peptides, e.g. enkephalins and atrial natriuretic peptide. The substrate specificity and...
Identification and characterization of a neutral endopeptidase activity in Aplysia californica.
Bawab, W, Aloyz, R S, Crine, P, Roques, B P, DesGroseillers, L
Kidney plasma membranes of Aplysia californica were shown to contain an endopeptidase activity which cleaved [Leu]enkephalin (Tyr-Gly-Gly-Phe-Leu) and [Leu]enkephalinamide (Tyr-Gly-Gly-Phe-Leu-NH2)...
O'Donohue, M J, Roques, B P, Beaumont, A
We report the isolation, cloning and expression, in Bacillus subtilis, of the gene coding for thermolysin, a thermostable metalloprotease which is produced by Bacillus thermoproteolyticus Rokko. The...
Waksman, G, Hamel, E, Delay-Goyet, P, Roques, B P
The cellular localization of rat brain enkephalinase was studied after induction of selective unilateral lesions using in vitro quantitative autoradiography of the specific binding of the enzyme...
Simonin, F, Valverde, O, Smadja, C, Slowe, S, Kitchen, I, Dierich, A, ...
***micro***-, delta- and kappa-opioid receptors are widely expressed in the central nervous system where they mediate the strong analgesic and mood-altering actions of opioids, and modulate numerous...
Luciani, N, De Rocquigny, H, Turcaud, S, Romieu, A, Roques, B P
The highly potent vasoconstrictor peptide endothelin (ET) is generated from an inactive precursor, big endothelin (bET), by endothelin-converting enzyme (ECE). ECE is a phosphoramidon-sensitive zinc...
Mély, Y, Piémont, E, Sorinas-Jimeno, M, De Rocquigny, H, Jullian, N, Morellet, N, ...
The steady-state and time-resolved fluorescence properties of two zinc-saturated 18-residue synthetic peptides with the amino acid sequence of the NH2-terminal (NCp7 13-30 F16W, where the naturally...
Bombarda, E, Ababou, A, Vuilleumier, C, Gérard, D, Roques, B P, Piémont, E, ...
Depending on the HIV-1 isolate, MN or BH10, the nucleocapsid protein, NCp7, corresponds to a 55- or 71-amino acid length product, respectively. The MN NCp7 contains a single Trp residue at position...
A mimic of HIV-1 nucleocapsid protein impairs reverse transcription and displays antiviral activity
Druillennec, S., Dong, C. Z., Escaich, S., Gresh, N., Bousseau, A., Roques, B. P., ...
Combined inhibition of HIV-1 reverse transcriptase and protease has significantly improved the treatment of AIDS. Nevertheless, resistance to these drugs occurs rapidly because of viral mutations,...
Zini, S, Fournie-Zaluski, M C, Chauvel, E, Roques, B P, Corvol, P, Llorens-Cortes, C
Angiotensin (Ang) II and Ang III are two peptide effectors of the brain renin-angiotensin system that participate in the control of blood pressure and increase water consumption and vasopressin...
Fournié-Zaluski, M C, Gonzalez, W, Turcaud, S, Pham, I, Roques, B P, Michel, J B
In the treatment of cardiovascular disease, it could be of therapeutic interest to associate the hypotensive effects due to the inhibition of angiotensin II formation with the diuretic and...
Fournié-Zaluski, M C, Soleilhac, J M, Turcaud, S, Laï-Kuen, R, Crine, P, Beaumont, A, ...
Neutral endopeptidase 24.11, also known as the common acute lymphoblastic leukemia antigen, is a zinc metallopeptidase involved in the inactivation of biologically active peptides, such as the...
DNA binding properties of a chemically synthesized DNA binding domain of hRFX1.
Cornille, F, Emery, P, Schüler, W, Lenoir, C, Mach, B, Roques, B P, ...
The RFX DNA binding domain (DBD) is a novel highly conserved motif belonging to a large number of dimeric DNA binding proteins which have diverse regulatory functions in eukaryotic organisms, ranging...
Li, X, Quan, Y, Arts, E J, Li, Z, Preston, B D, De Rocquigny, H, ...
Retroviral reverse transcription starts near the 5' end of unspliced viral RNA at a sequence called the primer binding site (PBS), where the tRNA primer anneals to the RNA template for initiation of...
Carteau, S, Batson, S C, Poljak, L, Mouscadet, J F, De Rocquigny, H, Darlix, J L, ...
The integrase (IN) protein of the human immunodeficiency virus mediates integration of the viral DNA into the cellular genome. In vitro, this reaction can be mimicked by using purified recombinant IN...
Housset, V, De Rocquigny, H, Roques, B P, Darlix, J L
Nucleocapsid (NC) protein NCp10 of Moloney murine leukemia virus is encoded by the 3' domain of gag and contains a zinc finger surrounded by basic amino acids. During virion assembly, NC protein is...
Cyclic cholecystokinin analogues with high selectivity for central receptors.
Charpentier, B, Pelaprat, D, Durieux, C, Dor, A, Reibaud, M, Blanchard, J C, ...
Taking as a model the N-terminal folding of the cholecystokinin tyrosine-sulfated octapeptide [CCK-8; Asp-Tyr(SO3H)-Met-Gly-Trp-Met-Asp-Phe-NH2] deduced from conformational studies, two cyclic...
Lambert, B, Jones, B K, Roques, B P, Le Pecq, J B, Yeung, A T
We have demonstrated that the noncovalent complex formed between DNA and an antitumor bifunctional intercalator, ditercalinium, is recognized in vitro as bulky covalent DNA lesions by the purified...
Geometry of the antitumor drug ditercalinium bisintercalated into d(CpGpCpG)2 by 1H NMR.
Delbarre, A, Delepierre, M, Garbay, C, Igolen, J, Le Pecq, J B, Roques, B P
Rigid 7H-pyrido[4,3-c]carbazole dimers, such as Ditercalinium, are DNA bisintercalators that display high DNA affinity and strong antitumor properties. This activity appears crucially dependent on...
De Rocquigny, H, Ficheux, D, Gabus, C, Allain, B, Fournie-Zaluski, M C, Darlix, J L, ...
The 56 amino acid nucleocapsid protein (NCp10) of Moloney Murine Leukemia Virus, contains a CysX2CysX4HisX4Cys zinc finger flanked by basic residues. In vitro NCp10 promotes genomic RNA dimerization,...
Two rotameric forms of open ring 7-methylguanine are present in alkylated polynucleotides.
Boiteux, S, Belleney, J, Roques, B P, Laval, J
High performance liquid chromatography analysis of imidazole open ring 7-methylguanine, 2-6 diamino-4-hydroxy-5N-methyl-formamidopyrimidine (rom7G), showed two well-separated peaks (fI and fII) of...
Waksman, G, Hamel, E, Fournié-Zaluski, M C, Roques, B P
The neutral endopeptidase EC 3.4.24.11, also designated enkephalinase, has been visualized by in vitro autoradiography using the tritiated inhibitor...
Delbarre, A, Gourevitch, M I, Gaugain, B, Le Pecq, J B, Roques, B P
Comparative 1H NMR and optical studies of the interaction between poly(dA-dT), ethidium bromide (Et) and ethidium dimer (Et2) in 0.7 M NaCl are reported as a function of the temperature. Denaturation...
Lambert, B, Roques, B P, Le Pecq, J B
Ditercalinium, an antitumor bifunctional intercalator which forms a high affinity reversible complex with DNA, was found to be specifically cytotoxic for polA and lig7 E. coli strains. In the polA...
Markovits, J, Ramstein, J, Roques, B P, Le Pecq, J B
Ethidium dimer is shown to bind by intercalation, almost equally well, to the B and Z form of poly[(dG-m5dC)].poly[(dG-m5dC)], whereas the ethidium monomer shows a strong preference for the B form....
Le Bret, M, Le Pecq, J B, Barbet, J, Roques, B P
The rate of energy transfer between DNA intercalated ethidium cations calculated by Paoletti and Le Pecq1 using the Forster theory differs from the measured one by a factor of twenty two, if the...
Highly selective photoaffinity labeling of mu and delta opioid receptors.
Garbay-Jaureguiberry, C, Robichon, A, Daugé, V, Rossignol, P, Roques, B P
We report the synthesis and photolabeling properties of two highly selective ligands for mu and delta opioid-binding sites: Tyr-D-Ala-Gly-MePhe (pN3)-Gly-ol (AZ-DAMGE) and Tyr-D-Thr-Gly-Phe...
Roques, B P, Lucas-Soroca, E, Chaillet, P, Costentin, J, Fournié-Zaluski, M C
Thiorphan, N-[(R,S)-3-mercapto-2-benzylpropanoyl]glycine is a highly potent inhibitor (Ki = 3.5 nM) of "enkephalinase," a metalloendopeptidase cleaving the Gly-Phe bond (positions 3 and 4) of...
Yang, Y S, Garbay, C, Duchesne, M, Cornille, F, Jullian, N, Fromage, N, ...
Src homology 3 (SH3) domains are found in numerous cytoplasmic proteins involved in intracellular signal transduction. We used 2-D 1H NMR to determine the structure of the SH3 domain of the guanosine...
Ramboarina, S., Druillennec, S., Morellet, N., Bouaziz, S., Roques, B. P.
The modification of zinc-binding residues inside the conserved CCHC motif of human immunodeficiency virus type 1 NCp7, in particular into CCHH, induces a complete loss of infectivity. Since the...
Morellet, N, Jullian, N, De Rocquigny, H, Maigret, B, Darlix, J L, Roques, B P
The retroviral gag nucleocapsid protein NCp7 (72 amino acids) of HIV-1 (LAV strain), which contains two successive zinc fingers of the Cys-X2-Cys-X4-His-X4-Cys form linked by a stretch of basic...
Lemay, G, Zollinger, M, Waksman, G, Roques, B P, Crine, P, Boileau, G
Neutral endopeptidase-24.11 (EC 3.4.24.11) (NEP) is a transmembrane metallo-endopeptidase that has been shown to be involved in the degradation of several mammalian neuropeptides, including...
Characterization of neutral endopeptidase 24.11 in dog glomeruli.
Landry, C, Santagata, P, Bawab, W, Fournié-Zaluski, M C, Roques, B P, Vinay, P, ...
Neutral endopeptidase (NEP; also known as neprilysin and enkephalinase; EC 3.4.24.11) is a cell-surface metallopeptidase that is present in many mammalian tissues. It is particularly abundant on the...
Dion, N, Le Moual, H, Fournié-Zaluski, M C, Roques, B P, Crine, P, Boileau, G
Neprilysin (EC 3.4.24.11) is a Zn2+ metallopeptidase involved in the degradation of biologically active peptides, e.g. enkephalins and atrial natriuretic peptide. The substrate specificity and...
Identification and characterization of a neutral endopeptidase activity in Aplysia californica.
Bawab, W, Aloyz, R S, Crine, P, Roques, B P, DesGroseillers, L
Kidney plasma membranes of Aplysia californica were shown to contain an endopeptidase activity which cleaved [Leu]enkephalin (Tyr-Gly-Gly-Phe-Leu) and [Leu]enkephalinamide (Tyr-Gly-Gly-Phe-Leu-NH2)...
O'Donohue, M J, Roques, B P, Beaumont, A
We report the isolation, cloning and expression, in Bacillus subtilis, of the gene coding for thermolysin, a thermostable metalloprotease which is produced by Bacillus thermoproteolyticus Rokko. The...