Structure-based drug design targeting infectious disease [electronic resource] / Erin M. Duffy.

By: Duffy, Erin M [spk]Material type: FilmFilmSeries: Henry Stewart talksBiomedical & life sciences collection. Mechanisms of ribosome function : insights into protein synthesis: Publisher: London : Henry Stewart Talks, 2008Description: 1 online resource (1 streaming video file (45 min.) : color, sound)Subject(s): Anti-Bacterial Agents | Protein Biosynthesis | Ribosomal Proteins | RibosomesOnline resources: Click here to access online | Series
Contents:
Contents: Many antibiotics inhibit the ribosome -- Intelligent engine builds perpetual pipeline -- Crystallography shows 50S is a target-of-targets -- From new X-ray crystals to new leads -- Analog(Trade Mark) -- LINKER essentials: tethering two binding features -- BOMB essentials -- MUSIC essentials: core-swapping -- QikProp: calculating drug-like properties -- Structures + Analog(Trade Mark): balanced compounds -- Case study: enhanced oxazolidinones -- Structural foundations -- Path to enhanced oxazolidinones -- Pi contributions represent key interactions -- Probing selectivity of sparsomycin -- Seeking a new lead -- Difference density map showing rib-X prototype -- Perfect match -- A minimal scaffold for lead optimization -- Minimal scaffold binds effectively in A-site -- Activity against H. influenzae -- H. influenzae activity with time evolution -- H. flu model delivers differentiable oxazolidinones -- Moderate in vivo activity measured -- Predictive model for rat oral bioavailability -- First pool of drug candidates -- Structures + predictive models = time-saving filters.
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Animated audio-visual presentation with synchronized narration.

Title from title frames.

Contents: Many antibiotics inhibit the ribosome -- Intelligent engine builds perpetual pipeline -- Crystallography shows 50S is a target-of-targets -- From new X-ray crystals to new leads -- Analog(Trade Mark) -- LINKER essentials: tethering two binding features -- BOMB essentials -- MUSIC essentials: core-swapping -- QikProp: calculating drug-like properties -- Structures + Analog(Trade Mark): balanced compounds -- Case study: enhanced oxazolidinones -- Structural foundations -- Path to enhanced oxazolidinones -- Pi contributions represent key interactions -- Probing selectivity of sparsomycin -- Seeking a new lead -- Difference density map showing rib-X prototype -- Perfect match -- A minimal scaffold for lead optimization -- Minimal scaffold binds effectively in A-site -- Activity against H. influenzae -- H. influenzae activity with time evolution -- H. flu model delivers differentiable oxazolidinones -- Moderate in vivo activity measured -- Predictive model for rat oral bioavailability -- First pool of drug candidates -- Structures + predictive models = time-saving filters.

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