scholarly journals Entecavir Therapy Induces de Novo HIV Reverse‐Transcriptase M184V Mutation in an Antiretroviral Therapy–Naive Patient

2008 ◽  
Vol 46 (9) ◽  
pp. e88-e91 ◽  
Author(s):  
Martin R. Jakobsen ◽  
Hanne Arildsen ◽  
Henrik B. Krarup ◽  
Martin Tolstrup ◽  
Lars Østergaard ◽  
...  
Keyword(s):  
Antiretroviral Therapy ◽  
Reverse Transcriptase ◽  
De Novo ◽  
Hiv Reverse Transcriptase ◽  
Naive Patient ◽  
M184v Mutation

scholarly journals An Overview of the Cure of HIV/AIDS Harbal Therapy Containing Natural Antioxidant, Vitamins and Minerals

2021 ◽  
Vol 6 (3) ◽  
pp. p26
Author(s):  
Silas David Emmanuel ◽  
I. M. Bugaje ◽  
S. M. Mohammmad
Keyword(s):  
Human Immunodeficiency Virus ◽  
Antiretroviral Therapy ◽  
Reverse Transcriptase ◽  
Aloe Vera ◽  
Hiv Reverse Transcriptase ◽  
Mortality And Morbidity ◽  
Neem Leaves ◽  
Immunodeficiency Virus ◽  
Anti Hiv ◽  
Hiv Aids

Purposes: The unprecedented and sequence through which an estimate of 25 million lives have gone to their early grave yard through Acquired Immune-deficiency Syndrome HIV/AIDS can never be quantified; since, when it was first describes in 1981. In 2017/2018 by (UNAIDS) it was estimated globally for about 36.9millions people were living with Human, Immunodeficiency Virus (HIV) so to say. Henceforth the progress made in the field of treatment in the form of Antiretroviral Therapy (ART) disease has not been fully ascertain for the cure of HIV/AIDS; except, perpetual clinical suppressions. Thus, the current challenges that man kinds faces with the used of perpetual intake of antiretroviral therapy (clinical suppression)/artificial vaccine is un-justifiable. However, search for HIV therapy have open a new chapter in the search for novel drugs from Kaduna Polytechnic procedure. This review focuses on vitamins, antioxidant, mineral and supplement as sources of in-hibitors or eradications for human immunodeficiency virus type-1 (HIV) reverse transcriptase. Objective: To assess whether vitamins, antioxidant, minerals supplement are effective and safe in eradicating mortality and morbidity among populace with HIV infection. Selection criteria: Randomized control trials were selected that compared the effect of vitamins (A, C, D, E, K,), antioxidant, minerals and supplement with regard to treatment measures in HIV infected persons. Methods: To prevent authors bias, based on a systematic search of literature; anti-HIV reverse transcriptase activity of some plant’s species like those of Eucalyptus leaves, Garlic fresh fruits, Baobab leaves, aloe vera, neem leaves, moringa leaves, bitter leaves etc. respectively. Thus, these medicinal plants contain an appreciable or above values antioxidant compound or photochemical like those of Phenolic, anthraquinone, tannin, falconoid, terpenoid, lignin, coumarins etc. respectively. Contrarywise, these phytochemical compounds have been exploited traditionally for the cure of many diseases as well as inhibition of viral replication/transcription. Further investigations have shared more light through which phytochemicals compounds inhibit virus replication either during the viral entry inside the host cell or during their replication. Originality: in view of the current investigation or to accelerate drug discovery and innovation, this review recommends the urgent need to tap into the enrich locally available endogenous knowledge of putative anti- HIV/AIDS, photochemical and their derivatives, (reverse pharmacology, determine pan assay, interferences compounds, microbial enzyme metabolites relationship and their mechanisms to treat virial diseases.

scholarly journals Lamivudine Can Exert a Modest Antiviral Effect against Human Immunodeficiency Virus Type 1 Containing the M184V Mutation

2003 ◽  
Vol 47 (2) ◽  
pp. 747-754 ◽  
Author(s):  
Yudong Quan ◽  
Bluma G. Brenner ◽  
Maureen Oliveira ◽  
Mark A. Wainberg
Keyword(s):  
Human Immunodeficiency Virus ◽  
Reverse Transcriptase ◽  
Mononuclear Cells ◽  
Antiviral Effect ◽  
Hiv Reverse Transcriptase ◽  
Peripheral Blood Mononuclear ◽  
Functional Changes ◽  
Immunodeficiency Virus ◽  
M184v Mutation ◽  
Level Resistance

ABSTRACT The M184V mutation in human immunodeficiency virus (HIV) reverse transcriptase is associated with high-level resistance to both (−)2′,3′-dideoxy-3′-thiacytidine (3TC) and (−)2′,3′-dideoxy-5-fluoro-3′-thiacytidine as well as low-level resistance to 2′,3′-dideoxyinosine, 2′,3′-dideoxycytidine, and abacavir. This mutation is also associated with diminished HIV replicative fitness as well as several functional changes in enzyme activity, including diminutions in polymerase processivity, pyrophosphorylysis, and nucleotide primer unblocking. Despite the fact that M184V encodes up to 1,000-fold resistance to 3TC, we asked whether this drug might still display some antiviral effect in regard to viruses containing this mutation. Cell-free assays revealed that high concentrations of 3TC triphosphate (i.e., >100 μM) could affect chain termination and/or inhibit purified reverse transcriptase containing the M184V substitution. This effect became more pronounced with elongation of reverse transcriptase products. In newly infected cells (i.e., peripheral blood mononuclear cells), we found that the amount of full-length reverse transcriptase product was diminished in the presence of 2 to 10 μM 3TC, although no decrease in the first product of the reverse transcriptase reaction, i.e., minus strong-stop DNA, was observed. In the presence of two other HIV inhibitors, e.g., nevirapine and indinavir, 3TC exerted additive effects in tissue culture at concentrations only marginally higher than the 50% inhibitory concentration (IC50). Reverse transcriptases cloned from clinical isolates harboring M184V in the context of multidrug resistance had similar IC50 values for 3TC triphosphate compared to reverse transcriptase containing only the M184V mutation. These results suggest that viruses containing M184V can retain a higher degree of sensitivity to 3TC than previously assumed.

An integrated molecular dynamics, principal component analysis and residue interaction network approach reveals the impact of M184V mutation on HIV reverse transcriptase resistance to lamivudine

2014 ◽  
Vol 10 (8) ◽  
pp. 2215-2228 ◽  
Author(s):  
Soumendranath Bhakat ◽  
Alberto J. M. Martin ◽  
Mahmoud E. S. Soliman
Keyword(s):  
Reverse Transcriptase ◽  
Interaction Network ◽  
Principal Component ◽  
Hiv Reverse Transcriptase ◽  
Residue Interaction ◽  
Resistant Strains ◽  
Hiv Rt ◽  
Drug Resistant Strains ◽  
The Impact ◽  
M184v Mutation

The emergence of different drug resistant strains of HIV-1 reverse transcriptase (HIV RT) remains of prime interest in relation to viral pathogenesis as well as drug development.

New Efavirenz Derivatives and 1,2,3-Triazolyl-phosphonates as Inhibitors of Reverse Transcriptase of HIV-1

2018 ◽  
Vol 18 (17) ◽  
pp. 1494-1505 ◽  
Author(s):  
Carolina C.P. Costa ◽  
Nubia Boechat ◽  
Monica M. Bastos ◽  
Fernando de C. da Silva ◽  
Andressa Marttorelli ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Triazole Ring ◽  
Biological Evaluation ◽  
World Health ◽  
Hiv Reverse Transcriptase ◽  
Ic50 Values ◽  
Health Organization ◽  
Hiv Drugs ◽  
Immunodeficiency Syndrome ◽  
New Compounds

Background: According to the World Health Organization (WHO), the fight against Acquired Immunodeficiency Syndrome (AIDS) is still one of the most significant challenges facing humanity. Worldwide, it is estimated that 36.7 million people are infected by the Human Immunodeficiency Virus (HIV). Despite the variety of available drugs, the search for new enzymatic inhibitors of HIV is still important due to the presence of adverse effects and the development of resistant strains. Therefore, the present study aimed to design, synthesize, and biologically evaluate novel inhibitors of HIV Reverse Transcriptase (RT). Materials and Methods: These compounds were obtained in two series, and compounds in both series contain a 1,2,3-triazole ring in their structures. The compounds in the first series are Efavirenz (EFV) analogues with the N-1 position substituted by another important fragment as described in the medicinal chemistry literature on anti-HIV drugs. The second series has a phosphonate chain similar to that in the structure of Tenofovir Disoproxil Fumarate (TDF). Results and Conclusion: The results of the biological evaluation showed that all compounds presented high RT inhibition values and lower or comparable inhibitory concentrations (the concentration needed to reduce the enzymatic activity by 50%, IC50 values, 0.8-1.9 µM). Among the compounds in the first series, the three with the lowest IC50 values had values between 0.8-0.9 µM, and of those in the second series, the most potent had an IC50 value of 1.1 µM; compounds in both series were equipotent to TDF (1.2 µM). Thus, the new compounds could be considered lead compounds for the development of new antiretroviral compounds.

scholarly journals Impact of long-term antiretroviral therapy on gut and oral microbiotas in HIV-1-infected patients

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Mayumi Imahashi ◽  
Hirotaka Ode ◽  
Ayumi Kobayashi ◽  
Michiko Nemoto ◽  
Masakazu Matsuda ◽  
...  
Keyword(s):  
Antiretroviral Therapy ◽  
Reverse Transcriptase ◽  
Transcriptase Inhibitor ◽  
Strand Transfer ◽  
Intestinal Dysbiosis ◽  
Α Diversity ◽  
Reverse Transcriptase Inhibitor ◽  
Hiv 1 ◽  
Over Time

AbstractIn HIV-1-infected patients, antiretroviral therapy (ART) is a key factor that may impact commensal microbiota and cause the emergence of side effects. However, it is not fully understood how long-term ART regimens have diverse impacts on the microbial compositions over time. Here, we performed 16S ribosomal RNA gene sequencing of the fecal and salivary microbiomes in patients under different long-term ART. We found that ART, especially conventional nucleotide/nucleoside reverse transcriptase inhibitor (NRTI)-based ART, has remarkable impacts on fecal microbial diversity: decreased α-diversity and increased ß-diversity over time. In contrast, dynamic diversity changes in the salivary microbiome were not observed. Comparative analysis of bacterial genus compositions showed a propensity for Prevotella-enriched and Bacteroides-poor gut microbiotas in patients with ART over time. In addition, we observed a gradual reduction in Bacteroides but drastic increases in Succinivibrio and/or Megasphaera under conventional ART. These results suggest that ART, especially NRTI-based ART, has more suppressive impacts on microbiota composition and diversity in the gut than in the mouth, which potentially causes intestinal dysbiosis in patients. Therefore, NRTI-sparing ART, especially integrase strand transfer inhibitor (INSTI)- and/or non-nucleotide reverse transcriptase inhibitor (NNRTI)-containing regimens, might alleviate the burden of intestinal dysbiosis in HIV-1-infected patients under long-term ART.

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