Development of HIV fusion inhibitors
| Autor: | Brian L. Bray, Jonathan M. White, Sheila R. Whight, Reagan J. Greene, Natalia Boshernitzan, Brian C. Fulcher, Stephen E. Schneider, Tracy S. Taylor, Catherine J. Mader, Maynard Lichty, Larry E. Stoltenberg, Mark W. Anderson, Paul Erickson Friedrich, Toivo E. Niemi |
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| Rok vydání: | 2005 |
| Předmět: |
Enfuvirtide
Human immunodeficiency virus (HIV) HIV Infections Disease medicine.disease_cause Gp41 Biochemistry chemistry.chemical_compound Acquired immunodeficiency syndrome (AIDS) Structural Biology HIV Fusion Inhibitors Drug Discovery medicine Peptide synthesis HIV fusion inhibitors Humans Molecular Biology Pharmacology Molecular Structure business.industry Organic Chemistry General Medicine medicine.disease Solution phase Virology HIV Envelope Protein gp41 Peptide Fragments chemistry Drug Design Molecular Medicine business medicine.drug |
| Zdroj: | Journal of peptide science : an official publication of the European Peptide Society. 11(11) |
| ISSN: | 1075-2617 |
| Popis: | In 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. However, the emergence and spread of drug-resistant strains highlights the continued need for new therapies with novel modes of action. In 2003, the FDA and EMEA approved enfuvirtide (Fuzeon), a 36 amino acid peptide derived from the natural gp41 HR2 sequence, as the first HIV fusion inhibitor. T-1249, a 39 amino acid fusion inhibitor, is active against viruses that develop resistance to enfuvirtide. The development of FIs and the processes to manufacture enfuvirtide and T-1249 on an unprecedented scale for peptide therapeutics are presented. Synthetic routes based on a combination of solid phase peptide synthesis and solution phase fragment condensation as well as the analytical controls necessary to insure a robust process are discussed. |
| Databáze: | OpenAIRE |
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