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NS3.4A protease as a target for interfering with hepatitis C virus replication.

Drug news & perspectives

Perni RB.
PMID: 12937632
Drug News Perspect. 2000 Mar;13(2):69-77. doi: 10.1358/dnp.2000.13.2.656262.

The hepatitis C virus (HCV) epidemic represents a significant unmet medical need. Current treatment is arduous and less than 50% effective. Indeed, interferon-alpha treatment is so unpleasant that asymptomatic patients will often stop treatment. Heartened by the success of...

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Perni RB. NS3.4A protease as a target for interfering with hepatitis C virus replication. Drug News Perspect. 2000;13(2):69-77doi: 10.1358/dnp.2000.13.2.656262.
Perni, R. B. (2000). NS3.4A protease as a target for interfering with hepatitis C virus replication. Drug news & perspectives, 13(2), 69-77. https://doi.org/10.1358/dnp.2000.13.2.656262
Perni, R B. "NS3.4A protease as a target for interfering with hepatitis C virus replication." Drug news & perspectives vol. 13,2 (2000): 69-77. doi: https://doi.org/10.1358/dnp.2000.13.2.656262
Perni RB. NS3.4A protease as a target for interfering with hepatitis C virus replication. Drug News Perspect. 2000 Mar;13(2):69-77. doi: 10.1358/dnp.2000.13.2.656262. PMID: 12937632.
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Inhibition of MMP-9 expression by ritonavir or saquinavir is associated with inactivation of the AKT/Fra-1 pathway in cervical intraepithelial neoplasia cells.

Oncology letters

Bacigalupo I, Palladino C, Leone P, Toschi E, Sgadari C, Ensoli B, Barillari G.
PMID: 28521396
Oncol Lett. 2017 May;13(5):2903-2908. doi: 10.3892/ol.2017.5835. Epub 2017 Mar 09.

A reduced incidence and decreased clinical progression of uterine cervical intraepithelial neoplasia (CIN) has been observed in women infected with human immunodeficiency virus (HIV) treated with HIV-protease inhibitors (PIs). The HIV-PIs saquinavir (SQV) and ritonavir (RTV) have been demonstrated...

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Bacigalupo I, Palladino C, Leone P, et al. Inhibition of MMP-9 expression by ritonavir or saquinavir is associated with inactivation of the AKT/Fra-1 pathway in cervical intraepithelial neoplasia cells. Oncol Lett. 2017;13(5):2903-2908doi: 10.3892/ol.2017.5835.
Bacigalupo, I., Palladino, C., Leone, P., Toschi, E., Sgadari, C., Ensoli, B., & Barillari, G. (2017). Inhibition of MMP-9 expression by ritonavir or saquinavir is associated with inactivation of the AKT/Fra-1 pathway in cervical intraepithelial neoplasia cells. Oncology letters, 13(5), 2903-2908. https://doi.org/10.3892/ol.2017.5835
Bacigalupo, Ilaria, et al. "Inhibition of MMP-9 expression by ritonavir or saquinavir is associated with inactivation of the AKT/Fra-1 pathway in cervical intraepithelial neoplasia cells." Oncology letters vol. 13,5 (2017): 2903-2908. doi: https://doi.org/10.3892/ol.2017.5835
Bacigalupo I, Palladino C, Leone P, Toschi E, Sgadari C, Ensoli B, Barillari G. Inhibition of MMP-9 expression by ritonavir or saquinavir is associated with inactivation of the AKT/Fra-1 pathway in cervical intraepithelial neoplasia cells. Oncol Lett. 2017 May;13(5):2903-2908. doi: 10.3892/ol.2017.5835. Epub 2017 Mar 09. PMID: 28521396; PMCID: PMC5431249.
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Comparative Effectiveness of Darunavir 1,200 mg Daily and Approved Dosing Strategies for Protease Inhibitor-Experienced Patients.

AIDS research and treatment

Mikula JM, Hsiao CB, Sawyer JR, Ma Q, Morse GD.
PMID: 23956848
AIDS Res Treat. 2013;2013:687176. doi: 10.1155/2013/687176. Epub 2013 Jul 17.

Background. HIV protease inhibitors exhibit concentration-dependent viral inhibition. Higher once daily doses of darunavir boosted with ritonavir (DRV/r) may achieve viral suppression in place of twice daily dosing. International antiretroviral adherence guidelines recommend once daily regimens whenever possible. We...

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Mikula JM, Hsiao CB, Sawyer JR, et al. Comparative Effectiveness of Darunavir 1,200 mg Daily and Approved Dosing Strategies for Protease Inhibitor-Experienced Patients. AIDS Res Treat. 2013;2013:687176doi: 10.1155/2013/687176.
Mikula, J. M., Hsiao, C. B., Sawyer, J. R., Ma, Q., & Morse, G. D. (2013). Comparative Effectiveness of Darunavir 1,200 mg Daily and Approved Dosing Strategies for Protease Inhibitor-Experienced Patients. AIDS research and treatment, 2013687176. https://doi.org/10.1155/2013/687176
Mikula, James M, et al. "Comparative Effectiveness of Darunavir 1,200 mg Daily and Approved Dosing Strategies for Protease Inhibitor-Experienced Patients." AIDS research and treatment vol. 2013 (2013): 687176. doi: https://doi.org/10.1155/2013/687176
Mikula JM, Hsiao CB, Sawyer JR, Ma Q, Morse GD. Comparative Effectiveness of Darunavir 1,200 mg Daily and Approved Dosing Strategies for Protease Inhibitor-Experienced Patients. AIDS Res Treat. 2013;2013:687176. doi: 10.1155/2013/687176. Epub 2013 Jul 17. PMID: 23956848; PMCID: PMC3730211.
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Valspodar: current status and perspectives.

Expert opinion on investigational drugs

Loor F.
PMID: 15992133
Expert Opin Investig Drugs. 1999 Jun;8(6):807-35. doi: 10.1517/13543784.8.6.807.

Valspodar (Amdray, SDZ PSC 833) is derived from cyclosporin, but lacks the immunosuppressive and most of the collateral activities of cyclosporin A (CsA, Sandimmune, Neoral); it exhibits an enhanced capacity to chemosensitise tumour cells showing the classical type multiple...

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Loor F. Valspodar: current status and perspectives. Expert Opin Investig Drugs. 1999;8(6):807-35doi: 10.1517/13543784.8.6.807.
Loor, F. (1999). Valspodar: current status and perspectives. Expert opinion on investigational drugs, 8(6), 807-35. https://doi.org/10.1517/13543784.8.6.807
Loor, F. "Valspodar: current status and perspectives." Expert opinion on investigational drugs vol. 8,6 (1999): 807-35. doi: https://doi.org/10.1517/13543784.8.6.807
Loor F. Valspodar: current status and perspectives. Expert Opin Investig Drugs. 1999 Jun;8(6):807-35. doi: 10.1517/13543784.8.6.807. PMID: 15992133.
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Role of Gag in HIV Resistance to Protease Inhibitors.

Viruses

Clavel F, Mammano F.
PMID: 21994687
Viruses. 2010 Jul;2(7):1411-26. doi: 10.3390/v2071411. Epub 2010 Jul 05.

Cleavage of Gag and Gag-Pol precursors by the viral protease is an essential step in the replication cycle of HIV. Protease inhibitors, which compete with natural cleavage sites, strongly impair viral infectivity and have proven to be highly valuable...

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Clavel F, Mammano F. Role of Gag in HIV Resistance to Protease Inhibitors. Viruses. 2010;2(7):1411-26doi: 10.3390/v2071411.
Clavel, F., & Mammano, F. (2010). Role of Gag in HIV Resistance to Protease Inhibitors. Viruses, 2(7), 1411-26. https://doi.org/10.3390/v2071411
Clavel, François, and Mammano, Fabrizio. "Role of Gag in HIV Resistance to Protease Inhibitors." Viruses vol. 2,7 (2010): 1411-26. doi: https://doi.org/10.3390/v2071411
Clavel F, Mammano F. Role of Gag in HIV Resistance to Protease Inhibitors. Viruses. 2010 Jul;2(7):1411-26. doi: 10.3390/v2071411. Epub 2010 Jul 05. PMID: 21994687; PMCID: PMC3185719.
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Inhibition of human immunodeficiency virus type-1 by cdk inhibitors.

AIDS research and therapy

Guendel I, Agbottah ET, Kehn-Hall K, Kashanchi F.
PMID: 20334651
AIDS Res Ther. 2010 Mar 24;7(1):7. doi: 10.1186/1742-6405-7-7.

Current therapy for human immunodeficiency virus (HIV-1) infection relies primarily on the administration of anti-retroviral nucleoside analogues, either alone or in combination with HIV-protease inhibitors. Although these drugs have a clinical benefit, continuous therapy with the drugs leads to...

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Guendel I, Agbottah ET, Kehn-Hall K, et al. Inhibition of human immunodeficiency virus type-1 by cdk inhibitors. AIDS Res Ther. 2010;7(1):7doi: 10.1186/1742-6405-7-7.
Guendel, I., Agbottah, E. T., Kehn-Hall, K., & Kashanchi, F. (2010). Inhibition of human immunodeficiency virus type-1 by cdk inhibitors. AIDS research and therapy, 7(1), 7. https://doi.org/10.1186/1742-6405-7-7
Guendel, Irene, et al. "Inhibition of human immunodeficiency virus type-1 by cdk inhibitors." AIDS research and therapy vol. 7,1 (2010): 7. doi: https://doi.org/10.1186/1742-6405-7-7
Guendel I, Agbottah ET, Kehn-Hall K, Kashanchi F. Inhibition of human immunodeficiency virus type-1 by cdk inhibitors. AIDS Res Ther. 2010 Mar 24;7(1):7. doi: 10.1186/1742-6405-7-7. PMID: 20334651; PMCID: PMC2852372.
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A combined 3D-QSAR and docking studies for the In-silico prediction of HIV-protease inhibitors.

Chemistry Central journal

Ul-Haq Z, Usmani S, Shamshad H, Mahmood U, Halim SA.
PMID: 23683267
Chem Cent J. 2013 May 17;7(1):88. doi: 10.1186/1752-153X-7-88.

BACKGROUND: Tremendous research from last twenty years has been pursued to cure human life against HIV virus. A large number of HIV protease inhibitors are in clinical trials but still it is an interesting target for researchers due to...

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Ul-Haq Z, Usmani S, Shamshad H, et al. A combined 3D-QSAR and docking studies for the In-silico prediction of HIV-protease inhibitors. Chem Cent J. 2013;7(1):88doi: 10.1186/1752-153X-7-88.
Ul-Haq, Z., Usmani, S., Shamshad, H., Mahmood, U., & Halim, S. A. (2013). A combined 3D-QSAR and docking studies for the In-silico prediction of HIV-protease inhibitors. Chemistry Central journal, 7(1), 88. https://doi.org/10.1186/1752-153X-7-88
Ul-Haq, Zaheer, et al. "A combined 3D-QSAR and docking studies for the In-silico prediction of HIV-protease inhibitors." Chemistry Central journal vol. 7,1 (2013): 88. doi: https://doi.org/10.1186/1752-153X-7-88
Ul-Haq Z, Usmani S, Shamshad H, Mahmood U, Halim SA. A combined 3D-QSAR and docking studies for the In-silico prediction of HIV-protease inhibitors. Chem Cent J. 2013 May 17;7(1):88. doi: 10.1186/1752-153X-7-88. PMID: 23683267; PMCID: PMC3660290.
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The HIV Protease Inhibitor Saquinavir Inhibits HMGB1-Driven Inflammation by Targeting the Interaction of Cathepsin V with TLR4/MyD88.

Molecular medicine (Cambridge, Mass.)

Pribis JP, Al-Abed Y, Yang H, Gero D, Xu H, Montenegro MF, Bauer EM, Kim S, Chavan SS, Cai C, Li T, Szoleczky P, Szabo C, Tracey KJ, Billiar TR.
PMID: 26349060
Mol Med. 2015 Dec;21(1):749-757. doi: 10.2119/molmed.2015.00197. Epub 2015 Sep 02.

Extracellular high-mobility group box 1 (HMGB1) (disulfide form), via activation of toll-like receptor 4 (TLR4)-dependent signaling, is a strong driver of pathologic inflammation in both acute and chronic conditions. Identification of selective inhibitors of HMGB1-TLR4 signaling could offer novel...

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Pribis JP, Al-Abed Y, Yang H, et al. The HIV Protease Inhibitor Saquinavir Inhibits HMGB1-Driven Inflammation by Targeting the Interaction of Cathepsin V with TLR4/MyD88. Mol Med. 2015;21(1):749-757doi: 10.2119/molmed.2015.00197.
Pribis, J. P., Al-Abed, Y., Yang, H., Gero, D., Xu, H., Montenegro, M. F., Bauer, E. M., Kim, S., Chavan, S. S., Cai, C., Li, T., Szoleczky, P., Szabo, C., Tracey, K. J., & Billiar, T. R. (2015). The HIV Protease Inhibitor Saquinavir Inhibits HMGB1-Driven Inflammation by Targeting the Interaction of Cathepsin V with TLR4/MyD88. Molecular medicine (Cambridge, Mass.), 21(1), 749-757. https://doi.org/10.2119/molmed.2015.00197
Pribis, John P, et al. "The HIV Protease Inhibitor Saquinavir Inhibits HMGB1-Driven Inflammation by Targeting the Interaction of Cathepsin V with TLR4/MyD88." Molecular medicine (Cambridge, Mass.) vol. 21,1 (2015): 749-757. doi: https://doi.org/10.2119/molmed.2015.00197
Pribis JP, Al-Abed Y, Yang H, Gero D, Xu H, Montenegro MF, Bauer EM, Kim S, Chavan SS, Cai C, Li T, Szoleczky P, Szabo C, Tracey KJ, Billiar TR. The HIV Protease Inhibitor Saquinavir Inhibits HMGB1-Driven Inflammation by Targeting the Interaction of Cathepsin V with TLR4/MyD88. Mol Med. 2015 Dec;21(1):749-757. doi: 10.2119/molmed.2015.00197. Epub 2015 Sep 02. PMID: 26349060; PMCID: PMC4749497.
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HIV protease inhibitors in pulmonary hypertension: rationale and design of a pilot trial in idiopathic pulmonary arterial hypertension.

Pulmonary circulation

Li Y, Li XH, Yu ZX, Cai JJ, Billiar TR, Chen AF, Lv B, Chen ZY, Huang ZJ, Yang GP, Song J, Liu B, Yuan H.
PMID: 26401255
Pulm Circ. 2015 Sep;5(3):538-46. doi: 10.1086/682426.

We propose an exploratory clinical study, the first of its kind to our knowledge, to determine the safety and potential clinical benefit of the combination of the HIV protease inhibitors (HIV-PIs) saquinavir and ritonavir (SQV+RIT) in patients with idiopathic...

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Li Y, Li XH, Yu ZX, et al. HIV protease inhibitors in pulmonary hypertension: rationale and design of a pilot trial in idiopathic pulmonary arterial hypertension. Pulm Circ. 2015;5(3):538-46doi: 10.1086/682426.
Li, Y., Li, X. H., Yu, Z. X., Cai, J. J., Billiar, T. R., Chen, A. F., Lv, B., Chen, Z. Y., Huang, Z. J., Yang, G. P., Song, J., Liu, B., & Yuan, H. (2015). HIV protease inhibitors in pulmonary hypertension: rationale and design of a pilot trial in idiopathic pulmonary arterial hypertension. Pulmonary circulation, 5(3), 538-46. https://doi.org/10.1086/682426
Li, Ying, et al. "HIV protease inhibitors in pulmonary hypertension: rationale and design of a pilot trial in idiopathic pulmonary arterial hypertension." Pulmonary circulation vol. 5,3 (2015): 538-46. doi: https://doi.org/10.1086/682426
Li Y, Li XH, Yu ZX, Cai JJ, Billiar TR, Chen AF, Lv B, Chen ZY, Huang ZJ, Yang GP, Song J, Liu B, Yuan H. HIV protease inhibitors in pulmonary hypertension: rationale and design of a pilot trial in idiopathic pulmonary arterial hypertension. Pulm Circ. 2015 Sep;5(3):538-46. doi: 10.1086/682426. PMID: 26401255; PMCID: PMC4556505.
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Role of novel retroviruses in chronic liver disease: assessing the link of human betaretrovirus with primary biliary cirrhosis.

Current infectious disease reports

Sharon D, Mason AL.
PMID: 25754451
Curr Infect Dis Rep. 2015 Feb;17(2):460. doi: 10.1007/s11908-014-0460-7.

A human betaretrovirus resembling mouse mammary tumor virus has been characterized in patients with primary biliary cirrhosis. The agent triggers a disease-specific phenotype in vitro with aberrant cell-surface expression of mitochondrial antigens. The presentation of a usually sequestered self-protein...

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Sharon D, Mason AL. Role of novel retroviruses in chronic liver disease: assessing the link of human betaretrovirus with primary biliary cirrhosis. Curr Infect Dis Rep. 2015;17(2):460doi: 10.1007/s11908-014-0460-7.
Sharon, D., & Mason, A. L. (2015). Role of novel retroviruses in chronic liver disease: assessing the link of human betaretrovirus with primary biliary cirrhosis. Current infectious disease reports, 17(2), 460. https://doi.org/10.1007/s11908-014-0460-7
Sharon, David, and Mason, Andrew L. "Role of novel retroviruses in chronic liver disease: assessing the link of human betaretrovirus with primary biliary cirrhosis." Current infectious disease reports vol. 17,2 (2015): 460. doi: https://doi.org/10.1007/s11908-014-0460-7
Sharon D, Mason AL. Role of novel retroviruses in chronic liver disease: assessing the link of human betaretrovirus with primary biliary cirrhosis. Curr Infect Dis Rep. 2015 Feb;17(2):460. doi: 10.1007/s11908-014-0460-7. PMID: 25754451; PMCID: PMC4353873.
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Second generation HIV protease inhibitors against resistant virus.

Expert opinion on drug discovery

Lu Z.
PMID: 23496220
Expert Opin Drug Discov. 2008 Jul;3(7):775-86. doi: 10.1517/17460441.3.7.775.

BACKGROUND: The AIDS epidemic has spread around the world at an alarming rate. Although the first generation of HIV protease inhibitors, including indinavir, nelfinavir, saquinavir, ritonavir and amprenavir, were initially effective against HIV infection, the fast emerging resistance to...

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Lu Z. Second generation HIV protease inhibitors against resistant virus. Expert Opin Drug Discov. 2008;3(7):775-86doi: 10.1517/17460441.3.7.775.
Lu, Z. (2008). Second generation HIV protease inhibitors against resistant virus. Expert opinion on drug discovery, 3(7), 775-86. https://doi.org/10.1517/17460441.3.7.775
Lu, Zhijian. "Second generation HIV protease inhibitors against resistant virus." Expert opinion on drug discovery vol. 3,7 (2008): 775-86. doi: https://doi.org/10.1517/17460441.3.7.775
Lu Z. Second generation HIV protease inhibitors against resistant virus. Expert Opin Drug Discov. 2008 Jul;3(7):775-86. doi: 10.1517/17460441.3.7.775. PMID: 23496220.
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Farnesyltransferase inhibitors prevent HIV protease inhibitor (lopinavir/ritonavir)-induced lipodystrophy and metabolic syndrome in mice.

Experimental and therapeutic medicine

Tanaka T, Nakazawa H, Kuriyama N, Kaneki M.
PMID: 29434718
Exp Ther Med. 2018 Feb;15(2):1314-1320. doi: 10.3892/etm.2017.5526. Epub 2017 Nov 17.

Highly active antiretroviral therapy (HAART) has successfully reduced the mortality rate of patients with human immune deficiency virus (HIV) and HIV protease inhibitors (HIV PIs) are key components of HAART. Complications of HAART, particularly those associated with HIV PIs...

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Tanaka T, Nakazawa H, Kuriyama N, et al. Farnesyltransferase inhibitors prevent HIV protease inhibitor (lopinavir/ritonavir)-induced lipodystrophy and metabolic syndrome in mice. Exp Ther Med. 2017;15(2):1314-1320doi: 10.3892/etm.2017.5526.
Tanaka, T., Nakazawa, H., Kuriyama, N., & Kaneki, M. (2018). Farnesyltransferase inhibitors prevent HIV protease inhibitor (lopinavir/ritonavir)-induced lipodystrophy and metabolic syndrome in mice. Experimental and therapeutic medicine, 15(2), 1314-1320. https://doi.org/10.3892/etm.2017.5526
Tanaka, Tomokazu, et al. "Farnesyltransferase inhibitors prevent HIV protease inhibitor (lopinavir/ritonavir)-induced lipodystrophy and metabolic syndrome in mice." Experimental and therapeutic medicine vol. 15,2 (2018): 1314-1320. doi: https://doi.org/10.3892/etm.2017.5526
Tanaka T, Nakazawa H, Kuriyama N, Kaneki M. Farnesyltransferase inhibitors prevent HIV protease inhibitor (lopinavir/ritonavir)-induced lipodystrophy and metabolic syndrome in mice. Exp Ther Med. 2018 Feb;15(2):1314-1320. doi: 10.3892/etm.2017.5526. Epub 2017 Nov 17. PMID: 29434718; PMCID: PMC5774418.
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