Cell type-specific anti-human immunodeficiency virus type 1 activity of the transactivation inhibitor Ro5-3335.

Abstract:

:The drug Ro5-3335 [7-chloro-5-(2-pyrryl)-3H-1,4-benzodiazepin-2(H)-one] inhibits human immunodeficiency virus type 1 (HIV-1) gene expression at the transcriptional level through interference with Tat-mediated transactivation (M.-C. Hsu, A. D. Schutt, M. Holly, L. W. Slice, M. I. Sherman, D. D. Richman, M. J. Potash, and D. J. Volsky, Science 254:1799-1802, 1991). We confirmed this specific inhibitory effect in a quantitative bioassay based on transactivation of a chimeric gene comprising the HIV-1 long terminal repeat promoter fused to the lacZ gene of Escherichia coli and transfected in a HeLa cell line expressing Tat. Ro5-3335 was found to inhibit HIV-1 long terminal repeat-driven lacZ gene expression at a 50% inhibitory concentration of 0.5 microM. The in vitro anti-HIV-1 activity of Ro5-3335 was highly dependent on the nature of the host cells. The highest selectivity index, 50, was found in phytohemagglutinin-stimulated peripheral blood lymphocytes. The selectivity index was between 1 and 10 in the CD4+ T-cell lines CEM, MOLT-4 (clone 8), and HUT-78. In MT-4 and MT-2 cells, Ro5-3335 had no inhibitory effect on HIV-1 replication. The absence of anti-HIV-1 activity of Ro5-3335 in MT-4 cells was confirmed by using different parameters of virus replication and different multiplicities of infection. In persistently HIV-1-infected HUT-78/IIIB/LAI cells, Ro5-3335 failed to demonstrate any activity at subtoxic concentrations. The cytotoxicity of Ro5-3335 was significantly lower in peripheral blood lymphocytes than in the CD4+ T-cell lines.

authors

Witvrouw M,Pauwels R,Vandamme AM,Schols D,Reymen D,Yamamoto N,Desmyter J,De Clercq E

doi

10.1128/aac.36.12.2628

subject

Has Abstract

pub_date

1992-12-01 00:00:00

pages

2628-33

issue

12

eissn

0066-4804

issn

1098-6596

journal_volume

36

pub_type

杂志文章
  • Population Pharmacokinetics of High-Dose Continuous-Infusion Meropenem and Considerations for Use in the Treatment of Infections Due to KPC-Producing Klebsiella pneumoniae.

    abstract::We assessed the population pharmacokinetics of high-dose continuous-infusion (HDCI) meropenem in a cohort of patients with Klebsiella pneumoniae carbapenemase (KPC)-producing Klebsiella pneumoniae (KPC-Kp) infections. Monte Carlo simulations were used to define the permissible HDCI meropenem regimens that could be saf...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00794-17

    authors: Cojutti P,Sartor A,Righi E,Scarparo C,Bassetti M,Pea F

    更新日期:2017-09-22 00:00:00

  • An Integrated HOCl-Producing E-Scaffold Is Active Against Monomicrobial and Polymicrobial Biofilms.

    abstract::Oxidizing agents like hypochlorous acid (HOCl) have antimicrobial activity. We developed an integrated electrochemical scaffold or 'e-scaffold' that delivers a continuous low dose of HOCl aimed at targeting microbial biofilms without exceeding concentrations toxic to humans, as a prototype of a device being developed ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02007-20

    authors: Flurin L,Raval YS,Mohamed A,Greenwood-Quaintance KE,Cano EJ,Beyenal H,Patel R

    更新日期:2021-01-04 00:00:00

  • Penicillin-resistant mechanisms in Pseudomonas aeruginosa: effects of penicillin G and carbenicillin on transpeptidase and C -alanine carboxypeptidase activities.

    abstract::A membrane fraction from Pseudomonas aeruginosa KM 338 was shown to catalyze in vitro peptidoglycan synthesis from uridine 5'-diphosphate-N-acetylmuramyl-l-alanyl-d- glutamyl-meso-diaminopimelyl-d-alanyl-d-alanine and uridine 5'-diphosphate-N-acetylglucosamine. Synthesized peptidoglycan was partially cross-linked by t...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.6.6.672

    authors: Suginaka H,Ichikawa A,Kotani S

    更新日期:1974-12-01 00:00:00

  • Efficacy of high doses of levofloxacin in experimental foreign-body infection by methicillin-susceptible Staphylococcus aureus.

    abstract::Antimicrobial efficacy in orthopedic device infections is diminished because of bacterial biofilms which express tolerance to antibiotics. Recently, the use of high doses of levofloxacin with rifampin has been recommended for staphylococcal infections. In the present study, we evaluated the efficacy of levofloxacin at...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00523-06

    authors: Murillo O,Doménech A,Garcia A,Tubau F,Cabellos C,Gudiol F,Ariza J

    更新日期:2006-12-01 00:00:00

  • Polyethylene glycol-based hydrogels for controlled release of the antimicrobial subtilosin for prophylaxis of bacterial vaginosis.

    abstract::Current treatment options for bacterial vaginosis (BV) have been shown to be inadequate at preventing recurrence and do not provide protection against associated infections, such as that with HIV. This study examines the feasibility of incorporating the antimicrobial peptide subtilosin within covalently cross-linked p...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02446-14

    authors: Sundara Rajan S,Cavera VL,Zhang X,Singh Y,Chikindas ML,Sinko PJ

    更新日期:2014-05-01 00:00:00

  • High incidence of sensitivity to yeast killer toxins among Candida and Torulopsis isolates of human origin.

    abstract::Among yeast strains of human origin belonging to the genera Candida, Cryptococcus, Torulopsis, and Rhodotorula which were examined for killer and sensitive characteristics with killer and sensitive strains of Cryptococcus, Hansenula, Kluyveromyces, Pichia, Saccharomyces, and Torulopsis as screening organisms, a high i...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.17.3.350

    authors: Middelbeek EJ,Hermans JM,Stumm C,Muytjens HL

    更新日期:1980-03-01 00:00:00

  • Isolates with low-level vancomycin resistance associated with persistent methicillin-resistant Staphylococcus aureus bacteremia.

    abstract::Low-level vancomycin-resistant Staphylococcus aureus (vancomycin-intermediate S. aureus [VISA] and heterogenous VISA [hVISA]) is increasingly reported and leads to glycopeptide treatment failure. Various phenotypic features have been reported for these isolates, but the genetic changes leading to hVISA and VISA have y...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00422-06

    authors: Howden BP,Johnson PD,Ward PB,Stinear TP,Davies JK

    更新日期:2006-09-01 00:00:00

  • Target- and resistance-based mechanistic studies with TP-434, a novel fluorocycline antibiotic.

    abstract::TP-434 is a novel, broad-spectrum fluorocycline antibiotic with activity against bacteria expressing major antibiotic resistance mechanisms, including tetracycline-specific efflux and ribosomal protection. The mechanism of action of TP-434 was assessed using both cell-based and in vitro assays. In Escherichia coli cel...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.06187-11

    authors: Grossman TH,Starosta AL,Fyfe C,O'Brien W,Rothstein DM,Mikolajka A,Wilson DN,Sutcliffe JA

    更新日期:2012-05-01 00:00:00

  • Interaction of oxyimino beta-lactams with a class C beta-lactamase and a mutant with a spectrum extended to beta-lactams.

    abstract::The class C beta-lactamase of Citrobacter freundii GN346 is a typical cephalosporinase comprising 361 amino acids, and substitution of the glutamic acid at position 219 in the enzyme by lysine was previously shown to broaden its substrate spectrum to oxyimino beta-lactams (K. Tsukamoto, R. Ohno, and T. Sawai, J. Bacte...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.38.6.1374

    authors: Nukaga M,Tsukamoto K,Yamaguchi H,Sawai T

    更新日期:1994-06-01 00:00:00

  • Effect of tryptophan-N-formylated gramicidin on growth of Plasmodium berghei in mice.

    abstract::The effect of tryptophan-N-formylated gramicidin (NFG) on the growth of Plasmodium berghei in mice was tested in three different experiments. NFG was shown to be capable of inhibiting the growth of the parasite in a dose-dependent way, although its action did not result in elimination of the parasite and was only temp...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.41.8.1778

    authors: Otten-Kuipers MA,Franssen FF,Nieuwenhuijs H,Overdulve JP,Roelofsen B,Op den Kamp JA

    更新日期:1997-08-01 00:00:00

  • Impaired fitness and transmission of macrolide-resistant Campylobacter jejuni in its natural host.

    abstract::Campylobacter jejuni is a major zoonotic pathogen transmitted to humans via the food chain and is prevalent in chickens, a natural reservoir for this pathogenic organism. Due to the importance of macrolide antibiotics in clinical therapy of human campylobacteriosis, development of macrolide resistance in Campylobacter...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.05516-11

    authors: Luangtongkum T,Shen Z,Seng VW,Sahin O,Jeon B,Liu P,Zhang Q

    更新日期:2012-03-01 00:00:00

  • Molecular basis of tetracycline action: identification of analogs whose primary target is not the bacterial ribosome.

    abstract::Tetracycline analogs fell into two classes on the basis of their mode of action. Tetracycline, chlortetracycline, minocycline, doxycycline, and 6-demethyl-6-deoxytetracycline inhibited cell-free translation directed by either Escherichia coli or Bacillus subtilis extracts. A second class of analogs tested, including c...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.35.11.2306

    authors: Rasmussen B,Noller HF,Daubresse G,Oliva B,Misulovin Z,Rothstein DM,Ellestad GA,Gluzman Y,Tally FP,Chopra I

    更新日期:1991-11-01 00:00:00

  • Comparative concentrations of cefoxitin in human lungs and sera.

    abstract::Eleven patients about to undergo pulmonary surgery received a bolus injection of 1 g of cefoxitin. The concentrations of cefoxitin in the serum 1 and 2 h after dosage were 38.5 +/- 1.89 and 23.7 +/- 2.56 mug/ml; the lung concentrations at the respective times were 12.6 +/- 0.7 and 10.06 +/- 0.43 mug/ml. ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.23.2.323

    authors: Perea EJ,Garcia-Iglesias MC,Ayarra J,Loscertales J

    更新日期:1983-02-01 00:00:00

  • Effects of surotomycin on Clostridium difficile viability and toxin production in vitro.

    abstract::The increasing incidence and severity of infection by Clostridium difficile have stimulated attempts to develop new antimicrobial therapies. We report here the relative abilities of two antibiotics (metronidazole and vancomycin) in current use for treating C. difficile infection and of a third antimicrobial, surotomyc...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00275-15

    authors: Bouillaut L,McBride S,Sorg JA,Schmidt DJ,Suarez JM,Tzipori S,Mascio C,Chesnel L,Sonenshein AL

    更新日期:2015-07-01 00:00:00

  • Trifluoromethionine, a prodrug designed against methionine gamma-lyase-containing pathogens, has efficacy in vitro and in vivo against Trichomonas vaginalis.

    abstract::Methionine gamma-lyase, the enzyme which catalyzes the single-step conversion of methionine to alpha-ketobutyrate, ammonia, and methanethiol, is highly active in many anaerobic pathogenic microorganisms but has no counterpart in mammals. This study tested the hypothesis that this pathogen-specific enzyme can be exploi...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.45.6.1743-1745.2001

    authors: Coombs GH,Mottram JC

    更新日期:2001-06-01 00:00:00

  • Systemic absorption of rifamycin SV MMX administered as modified-release tablets in healthy volunteers.

    abstract::The new oral 200-mg rifamycin SV MMX modified-release tablets, designed to deliver rifamycin SV directly into the colonic lumen, offer considerable advantages over the existing immediate-release antidiarrheic formulations. In two pharmacokinetics studies of healthy volunteers, the absorption, urinary excretion, and fe...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章,随机对照试验

    doi:10.1128/AAC.01504-10

    authors: Di Stefano AF,Rusca A,Loprete L,Dröge MJ,Moro L,Assandri A

    更新日期:2011-05-01 00:00:00

  • High-throughput Giardia lamblia viability assay using bioluminescent ATP content measurements.

    abstract::The human pathogen Giardia lamblia is an anaerobic protozoan parasite that causes giardiasis, one of the most common diarrheal diseases worldwide. Although several drugs are available for the treatment of giardiasis, drug resistance has been reported and is likely to increase, and recurrent infections are common. The ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00618-10

    authors: Chen CZ,Kulakova L,Southall N,Marugan JJ,Galkin A,Austin CP,Herzberg O,Zheng W

    更新日期:2011-02-01 00:00:00

  • Drug Development against Smallpox: Present and Future.

    abstract::Forty years after the last endemic smallpox case, variola virus (VARV) is still considered a major threat to humans due to its possible use as a bioterrorism agent. For many years, the risk of disease reemergence was thought to solely be through deliberate misuse of VARV strains kept in clandestine laboratories. Howev...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章,评审

    doi:10.1128/AAC.01683-19

    authors: Delaune D,Iseni F

    更新日期:2020-03-24 00:00:00

  • Regional dissemination of KPC-producing Klebsiella pneumoniae.

    abstract::Production of a Klebsiella pneumoniae carbapenemase (KPC) is the most common mechanism of carbapenem resistance in the United States; however, until now, KPC-producing isolates have not been found in western Michigan. Molecular typing of two KPC-producing K. pneumoniae isolates from Michigan showed their similarity to...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00784-09

    authors: Kitchel B,Sundin DR,Patel JB

    更新日期:2009-10-01 00:00:00

  • Paradoxical Effect of Polymyxin B: High Drug Exposure Amplifies Resistance in Acinetobacter baumannii.

    abstract::Administering polymyxin antibiotics in a traditional fashion may be ineffective against Gram-negative ESKAPE (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter species) pathogens. Here, we explored increasing the dose intensity of poly...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02831-15

    authors: Tsuji BT,Landersdorfer CB,Lenhard JR,Cheah SE,Thamlikitkul V,Rao GG,Holden PN,Forrest A,Bulitta JB,Nation RL,Li J

    更新日期:2016-06-20 00:00:00

  • Tilorone hydrochloride: an oral interferon-inducing agent.

    abstract::Tilorone hydrochloride characteristically induces an unusually delayed and prolonged interferon response not commonly associated with other synthetic inducers. Maximum circulating interferon levels of 8,000 to 10,000 units/ml were detected 12 hr postinoculation and persisted for up to 30 hr after administration of til...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.2.2.73

    authors: Stringfellow DA,Glasgow LA

    更新日期:1972-08-01 00:00:00

  • Optimizing Echinocandin dosing and susceptibility breakpoint determination via in vivo pharmacodynamic evaluation against Candida glabrata with and without fks mutations.

    abstract::Echinocandins are a preferred therapy for invasive candidiasis due to their potency and broad spectrum. Resistance, especially in Candida glabrata, is an emerging threat to their use. Pharmacodynamic (PD) studies examining reduced susceptibility secondary to fks mutations in C. glabrata are lacking. The current study ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01102-12

    authors: Lepak A,Castanheira M,Diekema D,Pfaller M,Andes D

    更新日期:2012-11-01 00:00:00

  • In vitro activities of enoxacin, enrofloxacin, sparfloxacin, and ciprofloxacin against Escherichia coli strains isolated from diarrheic lambs and kids.

    abstract::The in vitro activities of four fluoroquinolone compounds were tested against 92 Escherichia coli strains of ovine and caprine origin under aerobic and anaerobic incubation conditions. The four fluoroquinolones proved to be highly effective against the E. coli isolates tested. When bacteria were cultured anaerobically...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.38.10.2469

    authors: Cid D,Piriz S,Ruiz-Santa-Quiteria JA,Valle J,Garcia S,Vadillo S,de la Fuente R

    更新日期:1994-10-01 00:00:00

  • Classical β-Lactamase Inhibitors Potentiate the Activity of Daptomycin against Methicillin-Resistant Staphylococcus aureus and Colistin against Acinetobacter baumannii.

    abstract::We asked whether beta-lactamase inhibitors (BLIs) increased the activity of daptomycin (DAP) against methicillin-resistant Staphylococcus aureus (MRSA), the peptide antibiotic colistin (COL) against the emerging Gram-negative nosocomial pathogen Acinetobacter baumannii, and the human host defense peptide cathelicidin ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01745-16

    authors: Sakoulas G,Rose W,Berti A,Olson J,Munguia J,Nonejuie P,Sakoulas E,Rybak MJ,Pogliano J,Nizet V

    更新日期:2017-01-24 00:00:00

  • Screening of Neisseria gonorrhoeae for tolerant response to beta-lactam antibiotics.

    abstract::Minimal inhibitory concentrations (MICs) and minimal bactericidal concentrations (MBCs) of penicillin, ampicillin, cefoxitin, and cefuroxime were determined for 103 beta-lactamase-negative Neisseria gonorrhoeae clinical isolates belonging to five different auxotypes. MBC determinations were base on killing 99.9% of th...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.19.4.645

    authors: de Repentigny L,Turgeon PL

    更新日期:1981-04-01 00:00:00

  • BENZNIDAZOLE IN CEREBROSPINAL FLUID. A CASE SERIES OF CHAGAS DISEASE MENINGOENCEPHALITIS IN HIV POSITIVE PATIENTS.

    abstract::BackgroundChagas disease reactivation in HIV positive people is an opportunistic infection with 79-100% mortality. It commonly involves the central nervous system (CNS). Early treatment with trypanocidal drugs such as benznidazole (BNZ) is crucial for this severe manifestation of Trypanosoma cruzi infection. However, ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01922-20

    authors: Fernández ML,Marson ME,Mastrantonio GE,Corti MA,Fleitas U,Lloveras SC,Lista N,Priarone MM,Domínguez C,Garcia-Bournissen F

    更新日期:2020-12-23 00:00:00

  • Novel type of plasmid-borne resistance to trimethoprim.

    abstract::A novel trait for transferable resistance to high concentrations of trimethoprim was found to dominate among enterobacteria collected from different parts of Sri Lanka. Drug resistance was a result of the production of dihydrofolate reductase with a decreased sensitivity to antifolates. By characterization of the part...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.31.1.60

    authors: Sundström L,Vinayagamoorthy T,Sköld O

    更新日期:1987-01-01 00:00:00

  • Cefiderocol Resistance in Acinetobacter baumannii: Roles of β-Lactamases, Siderophore Receptors, and Penicillin Binding Protein 3.

    abstract::Cefiderocol is a siderophore cephalosporin active against many multidrug-resistant (MDR) Gram-negative pathogens. We examined the resistance mechanisms in 12 Acinetobacter baumannii strains with cefiderocol MICs ranging from ≤0.03 to >32 μg/ml. Cefiderocol resistance could not be explained by β-lactamase activity. Cef...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01221-20

    authors: Malik S,Kaminski M,Landman D,Quale J

    更新日期:2020-10-20 00:00:00

  • Increasing ceftriaxone resistance and multiple alterations of penicillin-binding proteins among penicillin-resistant Streptococcus pneumoniae isolates in Taiwan.

    abstract::The rate of nonsusceptibility of penicillin-resistant Streptococcus pneumoniae strains to ceftriaxone increased significantly in Taiwan in 2005. Approximately 90% of the ceftriaxone-nonsusceptible isolates were found to be of four major serotypes (serotypes 6B, 14, 19F, and 23F). Seven amino acid alterations in the pe...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01563-06

    authors: Chiu CH,Su LH,Huang YC,Lai JC,Chen HL,Wu TL,Lin TY

    更新日期:2007-09-01 00:00:00

  • In vitro activity of ceftobiprole against aerobic and anaerobic strains isolated from diabetic foot infections.

    abstract::Against 443 aerobic and anaerobic bacteria isolated from diabetic foot infections, ceftobiprole MICs (microg/ml) at which 90% of the isolates tested were inhibited were as follows: methicillin-resistant Staphylococcus aureus, 1; methicillin-susceptible S. aureus and Staphylococcus lugdunensis, 0.5; Anaerococcus prevot...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00722-06

    authors: Goldstein EJ,Citron DM,Merriam CV,Warren YA,Tyrrell KL,Fernandez HT

    更新日期:2006-11-01 00:00:00