Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0019693 (HIV)
170,526 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

5'-N-(alpha-Amino-beta-mercaptoacyl)amino-5'-deoxynucleosides have been synthesized by coupling of N-formylthiazolidines derived from D- and L-penicillamine, and D- and L-cysteine to 5'-amino-5'-deoxynucleosides using the DCC/HOSu method, followed by deprotection in N HCl in MeOH under argon. Although these compounds were designed as potential anti-HIV-1 agents, none of them showed anti-HIV-1 activity in MT-4 cells or antiviral effect against some other viruses, at concentrations below the cytotoxicity threshold.
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PMID:Synthesis of 5'-N-(alpha-amino-beta-mercaptoacyl)amino-5'-deoxynucleosides as potential antiviral compounds. 178 31

CD4 molecule, a surface marker of helper T lymphocytes, interacts with gp120 of human immunodeficiency virus (HIV) with a high affinity and, hence, serves as a virus receptor. Soluble chimeric CD4-immunoglobulin (Ig) possesses anti-HIV activity due to its binding activity to gp120. Furthermore, this recombinant molecule has unique Ig-like properties representing Fc receptor-binding activity and a long half-life in vivo. In this report we have thoroughly evaluated the effect of this compound on HIV infection using different in vitro systems. Treatment with 4 micrograms/ml of recombinant CD4-Ig after infection completely blocked the HIV-specific cytopathic effect, antigen expression, and virus release in MT-4 cells, a human T cell line which is highly susceptible to HIV. Similarly, this molecule blocked the HTLV-III/B and YU-1 strains of HIV infection in peripheral blood mononuclear cells even at 1 microgram/ml. Pretreatment of the Fc receptor-positive cell line U937 with this reagent resulted not in enhancement but again in blocking of HIV infection. About 95% of HIV infection was inhibited in U937 cells when cells were treated with this compound at the time of exposure to HIV. Recombinant-CD4-Ig also completely inhibited HIV-induced syncytia formation between MOLT-4 and MOLT-4/HIV and resulting virus release at 8 and 2 micrograms/ml, respectively. Due to its stability and long half-life, this compound could be a promising therapeutic agent against HIV infection.
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PMID:Evaluation of anti-human immunodeficiency virus effect of recombinant CD4-immunoglobulin in vitro: a good candidate for AIDS treatment. 178 69

To reduce the toxicity of amphotericin B methyl ester (AME), which shows some anti-HIV-1 activity, sulfated amphotericin B (SAB) was prepared from amphotericin B (AB), and its anti-HIV-1 activity was examined in vitro. SAB at concentration of 7.8 micrograms/ml completely suppressed the HIV-1-induced cytopathic effect in MT-4 cells, at 3.9 micrograms/ml inhibited the expression of HIV-1 antigen in peripheral blood mononuclear cells infected with freshly isolated HIV-1 and at 22 micrograms/ml completely suppressed formation of giant cells in cocultures of MOLT-4 with MOLT-4/HIV-1 cells. Reverse transcriptase activity was inhibited by SAB, but only at higher concentrations (0.2-1 mg/ml). Furthermore, the toxicity of SAB was lower than that of AME or AB, and SAB did not affect the proliferation of MT-4 cells at concentrations up to 0.5 mg/ml. The anti-coagulant effect of SAB was 10-fold less than that of dextran sulfate (MW = 8000). The anti-HIV-1 effect of SAB is attributed to inhibition of binding of virions to target cells.
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PMID:Anti-HIV-1 activity of sulfated amphotericin B in vitro. 180 84

A series of human immunodeficiency virus type 1 (HIV-1) mutants in vif, vpr, vpu, and nef were constructed from an infectious plasmid (pNL 432) containing the full-length HIV-1 DNA by frameshift mutations. The capacities for replication and cell killing of these mutant viruses were examined in a clonal cell line (M 10) isolated from HTLV-I-transformed MT-4 cells. In all cases, the mutant viruses replicated, expressed HIV-1 antigens, and induced drastic cytopathic effects. However, some M 10 cells survived infection with vif, vpr, and vpu mutant viruses and became persistently HIV-1-infected, whereas no cells survived infection with the nef mutant as well as the wild-type virus. The HIV-1 particles produced from the surviving cells after infection with the vif, vpr, or vpu mutant viruses were fully replicative in M 10 cells without apparent cytopathic effects.
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PMID:Human immunodeficiency virus type 1 vif, vpr, and vpu mutants can produce persistently infected cells. 183 72

Both variants of HIV-1 reported in the literature: slow/low and rapid/high types, were detected among the strains isolated from the subjects examined in 4 foci of HIV-1 infection in the south of the RSFSR and Byelorussia. All the 17 strains isolated in the southern RSFSR foci belonged to the slow/low type and had a low and unstable replication potential in donor peripheral blood mononuclear cells and in MT-4 cell line. All of them were isolated from subjects with asymptomatic infection and from children with initial clinical manifestations of the disease. Only one strain isolated in Byelorussia belonged to the rapid/high type. Its replicative activity was very similar to that of the classical HIV-1--HTLV-IIIB strain. Long-term (up to 7 months) propagation of slow/low strains did not result in any increase of their replicative activity. The capacity to form syncytia was found not only in the rapid/high type strains but also in the majority of slow/low strains under study.
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PMID:[The strain features of the HIV-1 circulating in the USSR based on data from a study of its properties in cell cultures]. 183 79

Fifteen heteropolyoxotungstates were tested for their effects on the proliferation of human immunodeficiency virus type 1 (HIV-1) using an in vitro system consisting of MT-4 cells and HTLV-IIIb. Eight heteropolyoxotungstates (HPOTs) with the Keggin structure or dimerized deficient Keggin structure proved to be potent inhibitors of HIV-1. In contrast, seven non-Keggin HPOTs including HPA 23 did not have significant effects on HIV-1 proliferation at non-toxic doses. [PTi2W10O40]7- (PM-19) was the most potent inhibitor of HIV-1 among the 15 HPOTs tested. The inhibition of HIV-1 replication by PM-19 presumably results from impaired virus adsorption and/or penetration into target cells. Viral spread of HIV-1 and HIV-2 on cell-to-cell basis was also susceptible to PM-19. In combination, PM-19 and 3'-azido-3'-deoxythymidine were synergistic in inhibiting HIV-1 proliferation.
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PMID:Inhibition of proliferation of human immunodeficiency virus type 1 by novel heteropolyoxotungstates in vitro. 185 2

The addition of 5-10% of fresh normal human serum (NHS) from normal individuals into a culture of primarily HIV-1-infected CD4+ leukemic T-cell lines CEM and MT4 was found to rescue the infected cells from cytopathic death, enabling the cells to achieve growth within 10 days. The HIV-1-infected cells cultured in ordinary medium with fetal calf serum (FCS) all died within 10 days. The effect of NHS was ascribed to human complement component factor B and one or more factor B-dependent heat-labile co-factors. The cells which survived in the presence of NHS rapidly lost surface expression of CD4 and became completely resistant to rechallenge by HIV-1. Viral genomes were dramatically reduced in surviving cells within 30 days, and one cell-line CEM completely expelled them during this period. The results suggest that factor B has protective and potential therapeutic significance in HIV-1 infection.
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PMID:Human complement component factor B rescues HIV-1-infected leukemic T cells from cytopathic death. 187 41

An antimicrobial peptide, tachyplesin I, isolated from hemocytes of the Japanese horseshoe crab (Tachypleus tridentatus) was examined for its inhibitory effects on human immunodeficiency virus (HIV) infection in vitro. At a concentration of 7.5 micrograms/ml, tachyplesin I suppressed the development of cytopathic effects (CPE) by more than 70% in MT-4 cells infected with HIV (lymphadenopathy-associated virus). This inhibitory effect was observed only when the drug was added during the adsorption period of the virus to the cells. In cocultures of MOLT-4 and persistently HIV-infected cells (MOLT-4/HIV), tachyplesin I at the same concentration completely inhibited multinucleated giant cell formation. Infectivity of HIV was reduced by 10(-2.5) in medium free from fetal calf serum containing tachyplesin I at a concentration of 200 micrograms/ml. Tachyplesin I did not show any inhibitory effect on reverse transcriptase activity of HIV at concentrations of 9-80 micrograms/ml at which tachyplesin I inhibited HIV infection. These results suggest that the anti-HIV action of tachyplesin I was due to the inhibition of virus adsorption.
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PMID:Inhibitory effect of tachyplesin I on the proliferation of human immunodeficiency virus in vitro. 188 8

Trichosanthin was purified from fresh Chinese root tubers of Trichosanthes kirilowii and evaluated for anti-HIV activity. Trichosanthin inhibited syncytium formation between infected H9 cells and uninfected Sup-T1 cells from 0.5 to 4 micrograms/ml. Trichosanthin also inhibited HIV replication in H9 and CEM-SS cells at 1 microgram/ml, but was toxic for MT-4 cells (HTLV-I-positive), at doses greater than 0.25 microgram/ml. This new purification procedure confirms the anti-HIV activity of trichosanthin on some cell lines in different biological assays.
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PMID:Toxicity and activity of purified trichosanthin. 189 92

Human immunodeficiency virus type 1 (HIV-1) primarily infects CD4+ lymphocytes and macrophages and causes AIDS in humans. Retroviral vectors allowing neomycin phosphotransferase (npt) gene expression were engineered to express 5' sequences of HIV-1 RNA in the antisense or sense orientation and used to transform the human CD4+ lymphocyte-derived MT4 cell line. Cells expressing antisense or sense RNA to the HIV-1 tat mRNA leader sequence, as part of the 3' untranslated region of the npt mRNA, remained sensitive to HIV-1 infection. In contrast, resistance to HIV-1 infection was observed in cells expressing antisense RNA to the HIV-1 primer-binding site or to the region 5' to the primer-binding site as part of the 3' region of the npt mRNA. Cells expressing the tat mRNA leader sequence in the sense orientation as a precise replacement of the 5' untranslated region of npt mRNA were also resistant to HIV-1. These results indicate that sense and antisense approaches can be used to interfere with HIV-1 multiplication.
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PMID:Inhibition of human immunodeficiency virus type 1 multiplication by antisense and sense RNA expression. 189 1


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