Human immunodeficiency virus type 1 reverse transcriptase expressing the K70E mutation exhibits a decrease in specific activity and processivity. |
Miller MD, Lamy PD, Fuller MD, Mulato AS, Margot NA, Cihlar T, Cherrington JM |
1998 |
Highly favorable antiviral activity and resistance profile of the novel thiocarboxanilide pentenyloxy ether derivatives UC-781 and UC-82 as inhibitors of human immunodeficiency virus type 1 replication. |
Balzarini J, Pelemans H, Aquaro S, Perno CF, Witvrouw M, Schols D, De Clercq E, Karlsson A |
1996 |
Human immunodeficiency virus type 1-specific [2',5'-bis-O-(tert- butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"- oxathiole-2",2"-dioxide)-purine analogues show a resistance spectrum that is different from that of the human immunodeficiency virus type 1-specific non-nucleoside analogues. |
Balzarini J, Velazquez S, San-Felix A, Karlsson A, Perez-Perez MJ, Camarasa MJ, De Clercq E |
1993 |
Marked inhibitory activity of non-nucleoside reverse transcriptase inhibitors against human immunodeficiency virus type 1 when combined with (-)2',3'-dideoxy-3'-thiacytidine. |
Balzarini J, Pelemans H, Pérez-Pérez MJ, San-Félix A, Camarasa MJ, De Clercq E, Karlsson A |
1996 |
Human immunodeficiency virus type 1 drug-resistance patterns with different 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives. |
Balzarini J, Karlsson A, De Clercq E |
1993 |
A single conservative amino acid substitution in the reverse transcriptase of human immunodeficiency virus-1 confers resistance to (+)-(5S)-4,5,6,7-tetrahydro-5-methyl-6-(3-methyl-2-butenyl)imidazo[4,5, 1- jk][1,4]benzodiazepin-2(1H)-thione (TIBO R82150). |
Mellors JW, Im GJ, Tramontano E, Winkler SR, Medina DJ, Dutschman GE, Bazmi HZ, Piras G, Gonzalez CJ, Cheng YC |
1993 |
Balancing Antiviral Potency and Host Toxicity: Identifying a Nucleotide Inhibitor with an Optimal Kinetic Phenotype for HIV-1 Reverse Transcriptase. |
Sohl CD, Kasiviswanathan R, Kim J, Pradere U, Schinazi RF, Copeland WC, Mitsuya H, Baba M, Anderson KS |
2012 |
Diketo hexenoic acid derivatives are novel selective non-nucleoside inhibitors of mammalian terminal deoxynucleotidyl transferases, with potent cytotoxic effect against leukemic cells. |
Locatelli GA, Di Santo R, Crespan E, Costi R, Roux A, Hübscher U, Shevelev IV, Blanca G, Villani G, Spadari S, Maga G |
2005 |
DNA polymerase ζ is a major determinant of resistance to platinum-based chemotherapeutic agents. |
Sharma S, Shah NA, Joiner AM, Roberts KH, Canman CE |
2012 |
Destabilization of the HIV-1 reverse transcriptase dimer upon interaction with N-acyl hydrazone inhibitors. |
Sluis-Cremer N, Arion D, Parniak MA |
2002 |
The role of Thr139 in the human immunodeficiency virus type 1 reverse transcriptase sensitivity to (+)-calanolide A. |
Auwerx J, Rodríguez-Barrios F, Ceccherini-Silberstein F, San-Félix A, Velázquez S, De Clercq E, Camarasa MJ, Perno CF, Gago F, Balzarini J |
2005 |
Mechanism of anti-human immunodeficiency virus action of polyoxometalates, a class of broad-spectrum antiviral agents. |
Yamamoto N, Schols D, De Clercq E, Debyser Z, Pauwels R, Balzarini J, Nakashima H, Baba M, Hosoya M, Snoeck R |
1992 |
Chimeric human immunodeficiency virus type 1 and feline immunodeficiency virus reverse transcriptases: role of the subunits in resistance/sensitivity to non-nucleoside reverse transcriptase inhibitors. |
Auwerx J, North TW, Preston BD, Klarmann GJ, De Clercq E, Balzarini J |
2002 |
Potent DNA chain termination activity and selective inhibition of human immunodeficiency virus reverse transcriptase by 2',3'-dideoxyuridine-5'-triphosphate. |
Hao Z, Cooney DA, Farquhar D, Perno CF, Zhang K, Masood R, Wilson Y, Hartman NR, Balzarini J, Johns DG |
1990 |
Allosteric inhibition of human immunodeficiency virus type 1 reverse transcriptase by tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione compounds. |
Debyser Z, Pauwels R, Andries K, Desmyter J, Engelborghs Y, Janssen PA, De Clercq E |
1992 |
Highly potent and selective inhibition of human immunodeficiency virus type 1 by a novel series of 6-substituted acyclouridine derivatives. |
Baba M, De Clercq E, Tanaka H, Ubasawa M, Takashima H, Sekiya K, Nitta I, Umezu K, Walker RT, Mori S |
1991 |
Mutational analysis of trp-229 of human immunodeficiency virus type 1 reverse transcriptase (RT) identifies this amino acid residue as a prime target for the rational design of new non-nucleoside RT inhibitors. |
Pelemans H, Esnouf R, De Clercq E, Balzarini J |
2000 |
Differences in the inhibition of human immunodeficiency virus type 1 reverse transcriptase DNA polymerase activity by analogs of nevirapine and [2',5'-bis-O-(tert-butyldimethylsilyl)-3'-spiro-5"-(4"-amino-1", 2"-oxathiole-2",2"-dioxide] (TSAO). |
Arion D, Fletcher RS, Borkow G, Camarasa MJ, Balzarini J, Dmitrienko GI, Parniak MA |
1996 |
The amino acid Asn136 in HIV-1 reverse transcriptase (RT) maintains efficient association of both RT subunits and enables the rational design of novel RT inhibitors. |
Balzarini J, Auwerx J, Rodríguez-Barrios F, Chedad A, Farkas V, Ceccherini-Silberstein F, García-Aparicio C, Velázquez S, De Clercq E, Perno CF, Camarasa MJ, Gago F |
2005 |
Marked depletion of glycosylation sites in HIV-1 gp120 under selection pressure by the mannose-specific plant lectins of Hippeastrum hybrid and Galanthus nivalis. |
Balzarini J, Van Laethem K, Hatse S, Froeyen M, Van Damme E, Bolmstedt A, Peumans W, De Clercq E, Schols D |
2005 |
Susceptibility of feline immunodeficiency virus/human immunodeficiency virus type 1 reverse transcriptase chimeras to non-nucleoside RT inhibitors. |
Auwerx J, Esnouf R, De Clercq E, Balzarini J |
2004 |
Potent inhibition of human immunodeficiency virus and herpes simplex virus type 1 by 9-(2-phosphonylmethoxyethyl)adenine in primary macrophages is determined by drug metabolism, nucleotide pools, and cytokines. |
Perno CF, Balestra E, Aquaro S, Panti S, Cenci A, Lazzarino G, Tavazzi B, Di Pierro D, Balzarini J, Calio R |
1996 |
Comparative cytostatic activity of different antiherpetic drugs against herpes simplex virus thymidine kinase gene-transfected tumor cells. |
Balzarini J, Bohman C, Walker RT, De Clercq E |
1994 |
Differential inhibitory effects of several pyrimidine 2',3'-dideoxynucleoside 5'-triphosphates on the activities of reverse transcriptase and various cellular DNA polymerases. |
Ono K, Nakane H, Herdewijn P, Balzarini J, De Clercq E |
1989 |
Polyanionic (i.e., polysulfonate) dendrimers can inhibit the replication of human immunodeficiency virus by interfering with both virus adsorption and later steps (reverse transcriptase/integrase) in the virus replicative cycle. |
Witvrouw M, Fikkert V, Pluymers W, Matthews B, Mardel K, Schols D, Raff J, Debyser Z, De Clercq E, Holan G, Pannecouque C |
2000 |
Common features in the interaction of tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione and 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives with the human immunodeficiency virus type 1 reverse transcriptase. |
Debyser Z, Pauwels R, Baba M, Desmyter J, De Clercq E |
1992 |
Kinetics of different human immunodeficiency virus type 1 reverse transcriptases resistant to human immunodeficiency virus type 1-specific reverse transcriptase inhibitors. |
Debyser Z, De Vreese K, Knops-Gerrits PP, Baekelandt V, Bhikhabhai R, Strandberg B, Pauwels R, Anné J, Desmyter J, De Clercq E |
1993 |
Mechanism of action of 5-(2-chloroethyl)-2'-deoxyuridine, a selective inhibitor of herpes simplex virus replication. |
De Clercq E, Bernaerts R, Merta A, Rosenwirth B |
1990 |
Comparative inhibition of DNA polymerases from varicella zoster virus (TK+ and TK-) strains by (E)-5-(2-bromovinyl)-2'-deoxyuridine 5'-triphosphate. |
Yokota T, Konno K, Shigeta S, De Clercq E |
1984 |