25 - antivirals - notes.docx

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Department
Molecular Genetics and Microbiology
Course
MGY378H1
Professor
Alan Cochrane
Semester
Winter

Description
ANTIVIRALS – March 23 CI index – lower the better – lower, more effective the drug – amount of drug used Delivery – delivered to site where needed in active form – not be metabolized Effective drug – Drug A and B – calculate the CI value – Drug A is more ffective – gives lower CI index Costly to develop – stages of research, so long time of development – also some drugs may never make it to the marketing stage At the end of the stages, very few make it through Human trials – phase one to four - phase IV – long term safety effects – still effective in the long run? Discovery of antiviral agents: - 1- both alpha herpes viruses – acyclovir inhibits - 2- do in vitro assay – inhibit activity in test tube - 3- screen for expression of gene – that block - 4- structure based approach – have structure of viral protein, and can look at it and figure out ways to inhibit it to design chemicals that fit in critical pocket of proteins – typically enzyme, Inhibitors can work at any stage of infection - 1 and 2 is attachment and entry – o Binding to host receptor or binding to viral protein that binds to host receptor  Ex. Inhibitor of HIV attachment – involves interaction with chemokine receptor – HIV associates with either CCR5 or CXCR4 in order to enter cells –  HIV drugs often used in combination b/c resistence develops quickly o Inhibitors that bind to virus  Disrupts function of capsid protein – do not attach to cell surface – pleconaril –  For HIV attachment and entry – fuzeon – binds glycoprotein – prevent conformational change needed for entry  HR1 and HR2  Fuzeon looks like piece of HR2 – blocks the normal HR1 and 2 interaction - 3 is uncoating o Channel forms for hydrogen ions – normally enter virion once in cell – changes pH in virion, changes conformation of matrix proteins in capsid – promotes release of nucleocapsid from envelope – nucleic acid gets released - 4 – viral gene expression o Interferons – small proteins that activate expression of antiviral genes – natural proteins that normally express  Not specific antiviral tr
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