Results 251 to 260 of about 34,307 (290)

Bivalent HIV-1 fusion inhibitors based on peptidomimetics

Bioorganic and Medicinal Chemistry, 2020
Membrane fusion is a valid target for inhibition of HIV-1 replication. A 34-mer fragment peptide (C34), which is contained in the HIV-1 envelope protein gp41, has significant anti-HIV activity. Previously, a dimeric derivative of C34 linked by a disulfide bridge at its C-terminus was found to have more potent anti-HIV activity than the C34 peptide ...
Takuya Kobayakawa, Kohei Tsuji, Nami Ohashi   +2 more
exaly   +3 more sources

HIV fusion inhibitors

Reviews in Medical Virology, 2009
AbstractDrugs based on amino acid sequence of Heptad Repeats of gp41 of HIV have been explored in search of anti‐HIV drugs acting by inhibition of the gp41 6‐helix formation and subsequent cellular infection. These are classified under a distinct discipline called HIV fusion inhibitors.
M I, Qadir, S A, Malik
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Development of HIV fusion inhibitors

Journal of Peptide Science, 2005
AbstractIn the past 25 years, the worldwide AIDS epidemic has grown such that roughly 38 million people were estimated to be living with the disease worldwide at the end of 2003. The introduction of antiretroviral‐based therapies, beginning in 1987, has enabled many to live with HIV as a chronic, rather than terminal, disease.
Stephen E, Schneider, Brian L, Bray, Catherine J, Mader, Paul E, Friedrich, Mark W, Anderson, Tracy S, Taylor, Natalia, Boshernitzan, Toivo E, Niemi, Brian C, Fulcher, Sheila R, Whight, Jonathan M, White, Reagan J, Greene, Larry E, Stoltenberg, Maynard, Lichty   +13 more
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HIV-1 anchor inhibitors and membrane fusion inhibitors target distinct but overlapping steps in virus entry

Journal of Biological Chemistry, 2019
HIV-1 entry into cells is mediated by the envelope glycoprotein (Env) and represents an attractive target for therapeutic intervention. Two drugs that inhibit HIV entry are approved for clinical use: the membrane fusion-inhibitor T20 (Fuzeon, enfuvirtide)
Dirk Eggink, Ilja Bontjer, Steven W De Taeye   +2 more
exaly   +2 more sources

HIV entry and fusion inhibitors

Expert Opinion on Emerging Drugs, 2004
Human immunodeficiency virus (HIV) is a retrovirus that is the causative agent of acquired immunodeficiency syndrome (AIDS). Current HIV therapy is based on targeting two critical enzymes in the viral replication machinery: reverse transcriptase and a virally encoded protease. Although mortality rates due to HIV infection have been dramatically reduced,
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Enfuvirtide: A fusion inhibitor for the treatment of HIV infection

Clinical Therapeutics, 2004
Drug resistance continues to be a major challenge in the treatment of HIV-1 infection. Virtually all currently available antiretroviral medications inhibit the viral reverse transcriptase or protease. Enfuvirtide is the first fusion inhibitor approved by the US Food and Drug Administration for use in combination with other antiretroviral agents for the
Horatio B, Fung, Yi, Guo
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Sifuvirtide, a potent HIV fusion inhibitor peptide

Biochemical and Biophysical Research Communications, 2009
Enfuvirtide (ENF) is currently the only FDA approved HIV fusion inhibitor in clinical use. Searching for more drugs in this category with higher efficacy and lower toxicity seems to be a logical next step. In line with this objective, a synthetic peptide with 36 amino acid residues, called Sifuvirtide (SFT), was designed based on the crystal structure ...
Rui-Rui, Wang, Liu-Meng, Yang, Yun-Hua, Wang, Wei, Pang, Siu-Cheung, Tam, Po, Tien, Yong-Tang, Zheng   +6 more
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Peptide and Non-peptide HIV Fusion Inhibitors

Current Pharmaceutical Design, 2002
Fusion of the HIV envelope with the target cell membrane is a critical step of HIV entry into the target cell. The HIV envelope glycoprotein gp41 plays an important role in the fusion of viral and target cell membranes and serves as an attractive target for development of HIV fusion inhibitors.
Shibo, Jiang, Qian, Zhao, Asim K, Debnath   +2 more
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Enfuvirtide: the first HIV fusion inhibitor

Expert Opinion on Pharmacotherapy, 2005
Highly active antiretroviral therapy, a combination of antiretrovirals to treat HIV-infected individuals, may fail for a number of reasons, including the selection of genetic mutations which confer resistance to the antiretroviral drugs, and poor adherence or treatment discontinuation resulting from drug toxicity.
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Are Fusion Inhibitors Active against All HIV Variants?

AIDS Research and Human Retroviruses, 2004
Genetic sequence alignment of the transmembrane region from HIV-1 group O and HIV-2 isolates was performed to examine their potential susceptibility to fusion inhibitors enfuvirtide (T-20) and T-1249. A high genetic diversity within the HRI and HR2 domains was found, which should compromise any antiviral effect of T-20 on HIV-2 and HIV-1 group O ...
Eva, Poveda, Berta, Rodes, Carlos, Toro, Vincent, Soriano   +3 more
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