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Discovery and development of nucleoside and nucleotide reverse-transcriptase inhibitors

Involvement of Novel Human Immunodeficiency Virus Type 1 Reverse Transcriptase Mutations in the Regulation of Resistance to Nucleoside Inhibitors

Involvement of Novel Human Immunodeficiency Virus Type 1 Reverse Transcriptase Mutations in the Regulation of Resistance to Nucleoside Inhibitors

... side analogue mutations” (NAMs; M41L, D67N, K70R, L210W, T215Y, and K219E/Q) can confer resistance by promoting a phosphorolysis reaction that selectively removes the nucleoside analogue from the terminated DNA ...

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AZOLES AS NON NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NNRTIs): MINI REVIEW

AZOLES AS NON NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NNRTIs): MINI REVIEW

... Non-nucleoside reverse transcriptase inhibitors (NNRTIs) in addition with Nucleoside reverse transcriptase inhibitors (NRTIs) and protease inhibitors (PIs) ...

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Inhibitory activity of 9 phenylcyclohepta[d]pyrimidinedione derivatives against different strains of HIV 1 as non nucleoside reverse transcriptase inhibitors

Inhibitory activity of 9 phenylcyclohepta[d]pyrimidinedione derivatives against different strains of HIV 1 as non nucleoside reverse transcriptase inhibitors

... non-nucleoside reverse transcriptase inhibitor (NNRTI) binding site have been rationally designed based on the structure of the NNRTI binding ...the development of such compounds is the right ...

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PROGRESS AND PROSPECTS IN THERAPEUTICS AGAINST HIV INFECTION

PROGRESS AND PROSPECTS IN THERAPEUTICS AGAINST HIV INFECTION

... the development of safe and effective medications for the treatment of viral ...two nucleoside reverse transcriptase inhibitors (NsRTIs) plus a third antiretroviral drug for ...

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Impact of Y181C and/or H221Y mutation patterns of HIV 1 reverse transcriptase on phenotypic resistance to available non nucleoside and nucleoside inhibitors in China

Impact of Y181C and/or H221Y mutation patterns of HIV 1 reverse transcriptase on phenotypic resistance to available non nucleoside and nucleoside inhibitors in China

... hardly reverse to wild types in absence of drug pressure ...the development of NNRTI resistance may be more complex (≥3 NNRTI resistance mutations) than the first-generation NNRTIs resistance ...

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Frequency of Mutations Conferring Resistance to Nucleoside Reverse Transcriptase Inhibitors in Human Immunodeficiency Virus Type 1 Infected Patients in Korea

Frequency of Mutations Conferring Resistance to Nucleoside Reverse Transcriptase Inhibitors in Human Immunodeficiency Virus Type 1 Infected Patients in Korea

... KRG has been used singly or together with ZDV for HIV- 1-infected patients since late 1991 as an alternative medicine (1, 3, 6; Cho et al., Abstr. 97th Gen. Meet. Am. Soc. Micro- biol.). Many beneficial effects have been ...

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HIV-1 and HIV-2 Reverse Transcriptases: Different Mechanisms of Resistance to Nucleoside Reverse Transcriptase Inhibitors

HIV-1 and HIV-2 Reverse Transcriptases: Different Mechanisms of Resistance to Nucleoside Reverse Transcriptase Inhibitors

... template/DNA primer and RNA template/DNA primer were used in these assays, and both of the substrates have the same sequence. Because the Q151M mutation is known to selectively interfere with the incorporation of AZTTP ...

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Comparative Study of Various Non-Nucleoside Reverse Transcriptase Inhibitors on Different Reverse Transcriptase Enzyme

Comparative Study of Various Non-Nucleoside Reverse Transcriptase Inhibitors on Different Reverse Transcriptase Enzyme

... of nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs/ NTRIs) and non-nucleoside reverse tran- scriptase inhibitors (NNRTIs), protease inhibitors ...

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A Novel Molecular Mechanism of Dual Resistance to Nucleoside and Nonnucleoside Reverse Transcriptase Inhibitors

A Novel Molecular Mechanism of Dual Resistance to Nucleoside and Nonnucleoside Reverse Transcriptase Inhibitors

... Reverse transcriptase (RT) of HIV-1 was the first target for development of drugs against HIV-1 infection and remains a major target for the exploration of new therapeutic ...comprise ...

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Benzophenone Derivatives: a Novel Scaffold as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors

Benzophenone Derivatives: a Novel Scaffold as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors

... the development of NNRTI, especially to improve their antiviral ...HIV inhibitors, the SARs of BPs were provided in this manuscript, which were overviewed as below: (1) the carbonyl between the A- and ...

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Two Coselected Distal Mutations in HIV-1 Reverse Transcriptase (RT) Alter Susceptibility to Nonnucleoside RT Inhibitors and Nucleoside Analogs

Two Coselected Distal Mutations in HIV-1 Reverse Transcriptase (RT) Alter Susceptibility to Nonnucleoside RT Inhibitors and Nucleoside Analogs

... . M230I has the smallest effect on excision, which agrees with the data obtained in the virology assays. Some mutations in the RT active site, including M184I/V, cause AZT hypersensitivity by reducing the ability of RT ...

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Identification of cellular deoxyhypusine synthase as a novel target for antiretroviral therapy

Identification of cellular deoxyhypusine synthase as a novel target for antiretroviral therapy

... (e.g., reverse transcriptase and protease ...inhibitor–resistant, nucleoside reverse transcriptase inhibitor–resistant, and non-nucleoside reverse transcriptase ...

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Selection of Resistance in Protease Inhibitor-Experienced, Human Immunodeficiency Virus Type 1-Infected Subjects Failing Lopinavir- and Ritonavir-Based Therapy: Mutation Patterns and Baseline Correlates

Selection of Resistance in Protease Inhibitor-Experienced, Human Immunodeficiency Virus Type 1-Infected Subjects Failing Lopinavir- and Ritonavir-Based Therapy: Mutation Patterns and Baseline Correlates

... and nucleoside reverse transcriptase inhibitor (NRTI)-experienced, nonnucleoside reverse tran- scriptase inhibitor (NNRTI)-naive patients, maximal virologic response to treatment with LPV-RTV ...

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The urgent need for more potent antiretroviral therapy in low-income countries to achieve UNAIDS 90-90-90 and complete eradication of AIDS by 2030

The urgent need for more potent antiretroviral therapy in low-income countries to achieve UNAIDS 90-90-90 and complete eradication of AIDS by 2030

... non-nucleoside reverse transcriptase inhibitors (NNRTIs), efavirenz and nevirapine, has been increasing with roll-out of combined antiretroviral therapy (cART) with 29% annual increase in some ...

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Non-Hepatic Adverse Effects of Antiretroviral Therapy for HIV Treatment and Care

Non-Hepatic Adverse Effects of Antiretroviral Therapy for HIV Treatment and Care

... Non-nucleoside reverse transcriptase inhibitors, Protease Inhibitors, Nucleoside reverse transcriptase inhibitors, Entry and Fusion Inhibitors and ...

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Theoretical Studies of The Contraction and Extension Effect in The B-Ring of TIBO Derivatives

Theoretical Studies of The Contraction and Extension Effect in The B-Ring of TIBO Derivatives

... non-nucleoside reverse transcriptase inhibitors are designed by contraction and extension of the seven-membered ring of TIBO to six- and eight-membered rings respectively using PM3, HF and DFT ...

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Differential Sensitivities of Retroviruses to Integrase Strand Transfer Inhibitors

Differential Sensitivities of Retroviruses to Integrase Strand Transfer Inhibitors

... Integrase inhibitors are emerging anti-human immunodeficiency virus (HIV) drugs, and multiple retrovi- ruses and transposable elements were evaluated here for susceptibilities to raltegravir (RAL) and elvitegravir ...

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Susceptibility of the Porcine Endogenous Retrovirus to Reverse Transcriptase and Protease Inhibitors

Susceptibility of the Porcine Endogenous Retrovirus to Reverse Transcriptase and Protease Inhibitors

... triphosphorylated nucleoside analogs of zidovudine (AZT-TP), lamivudine (2⬘,3⬘-deoxy-3⬘-thiacytidine; 3TC-TP), zalcitabine (dideoxycy- tosine [ddC]-TP), stavudine (2⬘,3⬘-didehydro-3⬘-deoxythymi- dine; d4T-TP), and ...

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Once-Daily Highly Active Antiretroviral Therapy for HIV-Infected Children: Safety and Efficacy of an Efavirenz-Containing Regimen

Once-Daily Highly Active Antiretroviral Therapy for HIV-Infected Children: Safety and Efficacy of an Efavirenz-Containing Regimen

... bility and effectiveness of a once-daily regimen of efavirenz with 3 nucleoside reverse transcriptase inhibitors as first-line or second-line highly active antiretro- viral therapy in a [r] ...

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Analysis of resistant mutations in reverse transcriptase domain of hepatitis B virus from patients from Islamabad, Pakistan

Analysis of resistant mutations in reverse transcriptase domain of hepatitis B virus from patients from Islamabad, Pakistan

... nucleos(t)ide nucleoside/ nucleotide analogues while secondary mutations, often called compensatory mutations, are those which cause amino acid substitutions to restore the replication capability of viral ...

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