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Bioengineering and ...
Bioengineering and Semisynthesis of an Optimized Cyclophilin Inhibitor for Treatment of Chronic Viral Infection.
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- Hansson, Magnus (author)
- Lund University,Lunds universitet,Klinisk neurofysiologi,Sektion IV,Institutionen för kliniska vetenskaper, Lund,Medicinska fakulteten,Klinisk fysiologi, Lund,Sektion V,Institutionen för kliniska vetenskaper, Lund,Clinical Neurophysiology,Section IV,Department of Clinical Sciences, Lund,Faculty of Medicine,Clinical Physiology (Lund),Section V,Department of Clinical Sciences, Lund
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Moss, Steven James (author)
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Bobardt, Michael (author)
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Chatterji, Udayan (author)
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Coates, Nigel (author)
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Garcia-Rivera, Jose A (author)
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- Elmer, Eskil (author)
- Lund University,Lunds universitet,Klinisk neurofysiologi,Sektion IV,Institutionen för kliniska vetenskaper, Lund,Medicinska fakulteten,Clinical Neurophysiology,Section IV,Department of Clinical Sciences, Lund,Faculty of Medicine
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Kendrew, Steve (author)
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Leyssen, Pieter (author)
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Neyts, Johan (author)
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Nur-E-Alam, Mohammad (author)
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Warneck, Tony (author)
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Wilkinson, Barrie (author)
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Gallay, Philippe (author)
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Gregory, Matthew Alan (author)
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(creator_code:org_t)
- Elsevier BV, 2015
- 2015
- English.
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In: Chemistry and Biology. - : Elsevier BV. - 1879-1301 .- 1074-5521. ; 22:2, s. 285-292
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Abstract
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- Inhibition of host-encoded targets, such as the cyclophilins, provides an opportunity to generate potent high barrier to resistance antivirals for the treatment of a broad range of viral diseases. However, many host-targeted agents are natural products, which can be difficult to optimize using synthetic chemistry alone. We describe the orthogonal combination of bioengineering and semisynthetic chemistry to optimize the drug-like properties of sanglifehrin A, a known cyclophilin inhibitor of mixed nonribosomal peptide/polyketide origin, to generate the drug candidate NVP018 (formerly BC556). NVP018 is a potent inhibitor of hepatitis B virus, hepatitis C virus (HCV), and HIV-1 replication, shows minimal inhibition of major drug transporters, and has a high barrier to generation of both HCV and HIV-1 resistance.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Lungmedicin och allergi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Respiratory Medicine and Allergy (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Neurologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Neurology (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Kardiologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Cardiac and Cardiovascular Systems (hsv//eng)
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- By the author/editor
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Hansson, Magnus
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Moss, Steven Jam ...
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Bobardt, Michael
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Chatterji, Udaya ...
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Coates, Nigel
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Garcia-Rivera, J ...
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show more...
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Elmer, Eskil
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Kendrew, Steve
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Leyssen, Pieter
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Neyts, Johan
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Nur-E-Alam, Moha ...
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Warneck, Tony
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Wilkinson, Barri ...
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Gallay, Philippe
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Gregory, Matthew ...
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show less...
- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Clinical Medicin ...
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and Respiratory Medi ...
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Clinical Medicin ...
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and Neurology
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Clinical Medicin ...
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and Cardiac and Card ...
- Articles in the publication
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Chemistry and Bi ...
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Lund University