Maga, G, Amacker, M, Hübscher, U, Gosselin, G, Imbach, J L, Mathé, C, ...
We have compared the HIV-1 RT mutants containing the single substitutions L100I, K103N, V106A, V179D, Y181I and Y188L, known to confer NNI-resistance in treated patients, to HIV-1 RT wt for their...
A. Rochdi, M. Taourirte, H. B. Lazrek, J. L. Barascut, J. L. Imbach
The E- and Z- phosphonoalkenyl acyclonucleosides of uracil and thymine were synthesized under Michael addition conditions. Introduction of an alkyl, alkenyl or alkynyl group at the N-3 position of...
Maga, G, Amacker, M, Hübscher, U, Gosselin, G, Imbach, J L, Mathé, C, ...
In order to identify the basis for the relaxed enantio-selectivity of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) and to evaluate possible cross-resistance patterns between...
Wyatt, J R, Vickers, T A, Roberson, J L, Buckheit, R W, Klimkait, T, DeBaets, E, ...
The phosphorothioate oligonucleotide T2G4T2 was identified as an inhibitor of HIV infection in vitro by combinatorial screening of a library of phosphorothioate oligonucleotides that contained all...
Hernandez-Santiago, B., Placidi, L., Cretton-Scott, E., Faraj, A., Bridges, E. G., Bryant, M. L., ...
β-l-Thymidine (l-dT) and β-l-2′-deoxycytidine (l-dC) are potent and highly specific inhibitors of hepatitis B virus (HBV) replication both in vivo and in vitro (50% effective concentrations, 0.19...
Peyrottes, S, Vasseur, J J, Imbach, J L, Rayner, B
Syntheses of non ionic oligodeoxynucleoside phosphoramidates (P-NH2) and mixed phosphoramidate- phosphodiester oligomers were accomplished on automated solid supported DNA synthesizer using both...
Tosquellas, G, Alvarez, K, Dell'Aquila, C, Morvan, F, Vasseur, J J, Imbach, J L, ...
A modified phosphoramidite method has been designed for the solid-phase synthesis of two dodecathymidine phosphotriesters and two dodecathymidine thionophosphotriesters. In these analogs, each...
Maga, G, Amacker, M, Hübscher, U, Gosselin, G, Imbach, J L, Mathé, C, ...
In order to identify the basis for the relaxed enantio-selectivity of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) and to evaluate possible cross-resistance patterns between...
Lipophilic pro-oligonucleotides are rapidly and efficiently internalized in HeLa cells.
Vivès, E, Dell'Aquila, C, Bologna, J C, Morvan, F, Rayner, B, Imbach, J L
Model t-Bu-SATE pro-dodecathymidines labeled with fluorescein and exhibiting various lipophilicities were evaluated for their uptake by cells in culture. Pro-oligonucleotides with appropriate...
Shirasaka, T, Chokekijchai, S, Yamada, A, Gosselin, G, Imbach, J L, Mitsuya, H
We determined the anti-human immunodeficiency virus type 1 (anti-HIV-1) activities of various dideoxy-nucleoside analogs by using phytohemagglutinin-activated peripheral blood mononuclear cells...
Vidalin, O, Major, M E, Rayner, B, Imbach, J L, Trépo, C, Inchauspé, G
We have explored different domains within the hepatitis C virus (HCV) 5' noncoding region as potential targets for inhibition of HCV translation by antisense oligodeoxynucleotides (ODNs). Inhibition...
Gosselin, G, Schinazi, R F, Sommadossi, J P, Mathé, C, Bergogne, M C, Aubertin, A M, ...
The L enantiomer of 2',3'-dideoxycytidine (DDC) was recently shown to inhibit selectively human immunodeficiency virus type 1 (HIV-1) in vitro. In the current study, the potent anti-HIV activity of...
Schinazi, R F, Gosselin, G, Faraj, A, Korba, B E, Liotta, D C, Chu, C K, ...
(-)-beta-L-2',3'-Dideoxycytidine (beta-L-DDC), (+)-beta-D-2',3'-dideoxycytidine (beta-D-DDC), (-)-beta-L-2',3'-dideoxy-5-fluorocytidine (beta-L-FDDC),...
Faraj, A, Agrofoglio, L A, Wakefield, J K, McPherson, S, Morrow, C D, Gosselin, G, ...
(-)-beta-L-2',3'-Dideoxycytidine (L-ddC) and (-)-beta-L-2',3'-dideoxy-5-fluorocytidine (L-FddC) have been reported to be potent and selective inhibitors of human immunodeficiency virus type 1 (HIV-1)...
Gautier, C, Morvan, F, Rayner, B, Huynh-Dinh, T, Igolen, J, Imbach, J L, ...
A new set of molecules made of an intercalating agent (oxazolopyridocarbazole, OPC) covalently linked through a polymethylene chain of various length to the 3' end of alpha-anomeric or beta-anomeric...
Morvan, F, Rayner, B, Imbach, J L, Lee, M, Hartley, J A, Chang, D K, ...
The beta-complementary hexamer, beta-d[GTACGC], to the alpha-sequence, alpha-d[CATGCG], was synthesized by the phosphotriester method. The non-exchangeable proton assignments were obtained using 1D-...
Bellon, L, Barascut, J L, Maury, G, Divita, G, Goody, R, Imbach, J L
We present the synthesis and the study of properties of a new series of modified oligonucleotides, namely 4'-thio-oligo-beta-D-ribonucleotides (4'-S-RNA). Homo-oligonucleotides of this class (4'-SU6...
Tanaka, H, Vickart, P, Bertrand, J R, Rayner, B, Morvan, F, Imbach, J L, ...
The potential use of alpha-beta-anomeric duplex oligonucleotides to inhibit transcription factor activity by the decoy approach is investigated in this report. Indeed, several alpha-beta-anomeric...
Morvan, F, Rayner, B, Imbach, J L, Chang, D K, Lown, J W
The novel deoxyribonucleotide alpha-[d(CpCpTpTpCpC)] and its complement beta-[d(GpGpApApGpG)] were synthesized by the phosphotriester method. 1H-NMR-NOE examination of the alpha-hexamer revealed that...
Debart, F, Rayner, B, Degols, G, Imbach, J L
The non natural oligoribonucleotide alpha-[r(UCUUAACCCACA)] consisting exclusively of alpha-anomeric ribonucleoside units was synthesized according to the phosphoramidite methodology and the solid...
Paoletti, J, Bazile, D, Morvan, F, Imbach, J L, Paoletti, C
The temperature dependence of the formation of a complex between an alpha-d(CCTTCC) hexanucleotide and its complementary beta-d(GGAAGG) sequence was studied and compared to the formation of the...
Gagnor, C, Rayner, B, Leonetti, J P, Imbach, J L, Lebleu, B
ps- and aps-alpha anomeric oligodeoxyribonucleotides were designed to recognize in parallel (ps) or antiparallel (aps) orientation two different sites of a 1000 base-long mRNA. Northern blots...
Lown, J W, Hanstock, C C, Bleackley, R C, Imbach, J L, Rayner, B, Vasseur, J J
The two deoxyribonucleotides [d(CpGpApTpCpG)]2 and [d(CpGpCpG)]2 were synthesized by the phosphotriester method. Their duplex form under the conditions of the 1H-nmr experiments was proven by end 32P...
Doornbos, J, Gosselin, G, Imbach, J L, Altona, C
In this paper the conformational analysis of the 2'-5' linked xylotrinucleotide xA2'-5'xA2'-5'xA is reported. The title compound is an analogue of A2'-5'A2'-5'A, which compound was shown to display...
Conformational analysis of oligoarabinonucleotides. An NMR and CD study.
Doornbos, J, Barascut, J L, Lazrek, H, Imbach, J L, Van Westrenen, J, Visser, G M, ...
A 500 and 300 MHz proton NMR study of the series of oligoarabinonucleotides 5'aAMP, 3'aAMP, aA-aA, (aA-)2aA and (aA-)3aA is presented. In addition, circular dichroism is used to study the stacking...
Zelphati, O, Imbach, J L, Signoret, N, Zon, G, Rayner, B, Leserman, L
Phosphodiester and phosphorothioate oligonucleotides in alpha and beta configurations directed against the initiation codon region of the HIV-1 rev gene were evaluated for their ability to inhibit...
alpha-DNA. VII. Solid phase synthesis of alpha-anomeric oligodeoxyribonucleotides.
Morvan, F, Rayner, B, Leonetti, J P, Imbach, J L
An efficient procedure for the synthesis of unnatural alpha-anomeric oligodeoxyribonucleotides is described. This solid-phase procedure is based on the use of alpha-nucleoside phosphoramidites and...
Bazile, D, Gautier, C, Rayner, B, Imbach, J L, Paoletti, C, Paoletti, J
The influence of the intercalating oxazolopyridocarbazolium (HOPC) on the stabilization of modified oligonucleotides: alpha-T4c5OPC or beta-T4c5OPC associated to beta-oligo (dA) was studied. It...
Bertrand, J R, Vasseur, J J, Rayner, B, Imbach, J L, Paoletti, J, Paoletti, C, ...
A 13 mers abasic oligonucleotide was synthetized. It was therefore possible to compare thermal stability and reactivity of duplex oligonucleotides either with an apurinic/apyrimidinic site or without...
Gagnor, C, Bertrand, J R, Thenet, S, Lemaître, M, Morvan, F, Rayner, B, ...
alpha and beta-anomeric d(G2T12G2) oligodeoxyribonucleotides were compared for their hybridization to rA12: the observed melting temperatures are 27 degrees C for beta-oligodeoxyribonucleotide/RNA...
Morvan, F, Rayner, B, Imbach, J L, Thenet, S, Bertrand, J R, Paoletti, J, ...
This paper describes for the first time the synthesis of alpha-oligonucleotides containing the four usual bases. Two unnatural hexadeoxyribonucleotides: alpha-[d(CpApTpGpCpG)] and...
Morvan, F, Rayner, B, Imbach, J L, Chang, D K, Lown, J W
High field 2-D-1H-NMR techniques permitted the assignment of all non-exchangeable protons of the unnatural deoxyribonucleotides alpha-[d(CpApTpGpCpG)] and alpha-[d(CpGpCpApTpG)]. 1-D and 2-D NOESY...
Verri, A, Montecucco, A, Gosselin, G, Boudou, V, Imbach, J L, Spadari, S, ...
We demonstrate that l-ATP is recognized by some enzymes that are involved in the synthesis of nucleotides and nucleic acids. l-ATP, as well as its natural d-enantiomer, acts as a phosphate donor in...
Wyatt, J R, Vickers, T A, Roberson, J L, Buckheit, R W, Klimkait, T, DeBaets, E, ...
The phosphorothioate oligonucleotide T2G4T2 was identified as an inhibitor of HIV infection in vitro by combinatorial screening of a library of phosphorothioate oligonucleotides that contained all...
Hernandez-Santiago, B., Placidi, L., Cretton-Scott, E., Faraj, A., Bridges, E. G., Bryant, M. L., ...
β-l-Thymidine (l-dT) and β-l-2′-deoxycytidine (l-dC) are potent and highly specific inhibitors of hepatitis B virus (HBV) replication both in vivo and in vitro (50% effective concentrations, 0.19...
Peyrottes, S, Vasseur, J J, Imbach, J L, Rayner, B
Syntheses of non ionic oligodeoxynucleoside phosphoramidates (P-NH2) and mixed phosphoramidate- phosphodiester oligomers were accomplished on automated solid supported DNA synthesizer using both...
Tosquellas, G, Alvarez, K, Dell'Aquila, C, Morvan, F, Vasseur, J J, Imbach, J L, ...
A modified phosphoramidite method has been designed for the solid-phase synthesis of two dodecathymidine phosphotriesters and two dodecathymidine thionophosphotriesters. In these analogs, each...
Maga, G, Amacker, M, Hübscher, U, Gosselin, G, Imbach, J L, Mathé, C, ...
In order to identify the basis for the relaxed enantio-selectivity of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) and to evaluate possible cross-resistance patterns between...
Lipophilic pro-oligonucleotides are rapidly and efficiently internalized in HeLa cells.
Vivès, E, Dell'Aquila, C, Bologna, J C, Morvan, F, Rayner, B, Imbach, J L
Model t-Bu-SATE pro-dodecathymidines labeled with fluorescein and exhibiting various lipophilicities were evaluated for their uptake by cells in culture. Pro-oligonucleotides with appropriate...
Shirasaka, T, Chokekijchai, S, Yamada, A, Gosselin, G, Imbach, J L, Mitsuya, H
We determined the anti-human immunodeficiency virus type 1 (anti-HIV-1) activities of various dideoxy-nucleoside analogs by using phytohemagglutinin-activated peripheral blood mononuclear cells...
Vidalin, O, Major, M E, Rayner, B, Imbach, J L, Trépo, C, Inchauspé, G
We have explored different domains within the hepatitis C virus (HCV) 5' noncoding region as potential targets for inhibition of HCV translation by antisense oligodeoxynucleotides (ODNs). Inhibition...
Gosselin, G, Schinazi, R F, Sommadossi, J P, Mathé, C, Bergogne, M C, Aubertin, A M, ...
The L enantiomer of 2',3'-dideoxycytidine (DDC) was recently shown to inhibit selectively human immunodeficiency virus type 1 (HIV-1) in vitro. In the current study, the potent anti-HIV activity of...
Schinazi, R F, Gosselin, G, Faraj, A, Korba, B E, Liotta, D C, Chu, C K, ...
(-)-beta-L-2',3'-Dideoxycytidine (beta-L-DDC), (+)-beta-D-2',3'-dideoxycytidine (beta-D-DDC), (-)-beta-L-2',3'-dideoxy-5-fluorocytidine (beta-L-FDDC),...
Faraj, A, Agrofoglio, L A, Wakefield, J K, McPherson, S, Morrow, C D, Gosselin, G, ...
(-)-beta-L-2',3'-Dideoxycytidine (L-ddC) and (-)-beta-L-2',3'-dideoxy-5-fluorocytidine (L-FddC) have been reported to be potent and selective inhibitors of human immunodeficiency virus type 1 (HIV-1)...
Gautier, C, Morvan, F, Rayner, B, Huynh-Dinh, T, Igolen, J, Imbach, J L, ...
A new set of molecules made of an intercalating agent (oxazolopyridocarbazole, OPC) covalently linked through a polymethylene chain of various length to the 3' end of alpha-anomeric or beta-anomeric...
Morvan, F, Rayner, B, Imbach, J L, Lee, M, Hartley, J A, Chang, D K, ...
The beta-complementary hexamer, beta-d[GTACGC], to the alpha-sequence, alpha-d[CATGCG], was synthesized by the phosphotriester method. The non-exchangeable proton assignments were obtained using 1D-...
Bellon, L, Barascut, J L, Maury, G, Divita, G, Goody, R, Imbach, J L
We present the synthesis and the study of properties of a new series of modified oligonucleotides, namely 4'-thio-oligo-beta-D-ribonucleotides (4'-S-RNA). Homo-oligonucleotides of this class (4'-SU6...
Tanaka, H, Vickart, P, Bertrand, J R, Rayner, B, Morvan, F, Imbach, J L, ...
The potential use of alpha-beta-anomeric duplex oligonucleotides to inhibit transcription factor activity by the decoy approach is investigated in this report. Indeed, several alpha-beta-anomeric...
Morvan, F, Rayner, B, Imbach, J L, Chang, D K, Lown, J W
The novel deoxyribonucleotide alpha-[d(CpCpTpTpCpC)] and its complement beta-[d(GpGpApApGpG)] were synthesized by the phosphotriester method. 1H-NMR-NOE examination of the alpha-hexamer revealed that...
Debart, F, Rayner, B, Degols, G, Imbach, J L
The non natural oligoribonucleotide alpha-[r(UCUUAACCCACA)] consisting exclusively of alpha-anomeric ribonucleoside units was synthesized according to the phosphoramidite methodology and the solid...
Paoletti, J, Bazile, D, Morvan, F, Imbach, J L, Paoletti, C
The temperature dependence of the formation of a complex between an alpha-d(CCTTCC) hexanucleotide and its complementary beta-d(GGAAGG) sequence was studied and compared to the formation of the...
Gagnor, C, Rayner, B, Leonetti, J P, Imbach, J L, Lebleu, B
ps- and aps-alpha anomeric oligodeoxyribonucleotides were designed to recognize in parallel (ps) or antiparallel (aps) orientation two different sites of a 1000 base-long mRNA. Northern blots...
Lown, J W, Hanstock, C C, Bleackley, R C, Imbach, J L, Rayner, B, Vasseur, J J
The two deoxyribonucleotides [d(CpGpApTpCpG)]2 and [d(CpGpCpG)]2 were synthesized by the phosphotriester method. Their duplex form under the conditions of the 1H-nmr experiments was proven by end 32P...
Doornbos, J, Gosselin, G, Imbach, J L, Altona, C
In this paper the conformational analysis of the 2'-5' linked xylotrinucleotide xA2'-5'xA2'-5'xA is reported. The title compound is an analogue of A2'-5'A2'-5'A, which compound was shown to display...
Conformational analysis of oligoarabinonucleotides. An NMR and CD study.
Doornbos, J, Barascut, J L, Lazrek, H, Imbach, J L, Van Westrenen, J, Visser, G M, ...
A 500 and 300 MHz proton NMR study of the series of oligoarabinonucleotides 5'aAMP, 3'aAMP, aA-aA, (aA-)2aA and (aA-)3aA is presented. In addition, circular dichroism is used to study the stacking...
Zelphati, O, Imbach, J L, Signoret, N, Zon, G, Rayner, B, Leserman, L
Phosphodiester and phosphorothioate oligonucleotides in alpha and beta configurations directed against the initiation codon region of the HIV-1 rev gene were evaluated for their ability to inhibit...
alpha-DNA. VII. Solid phase synthesis of alpha-anomeric oligodeoxyribonucleotides.
Morvan, F, Rayner, B, Leonetti, J P, Imbach, J L
An efficient procedure for the synthesis of unnatural alpha-anomeric oligodeoxyribonucleotides is described. This solid-phase procedure is based on the use of alpha-nucleoside phosphoramidites and...
Bazile, D, Gautier, C, Rayner, B, Imbach, J L, Paoletti, C, Paoletti, J
The influence of the intercalating oxazolopyridocarbazolium (HOPC) on the stabilization of modified oligonucleotides: alpha-T4c5OPC or beta-T4c5OPC associated to beta-oligo (dA) was studied. It...