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- Architecture of the ribosome RNA-protein machine assembly
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2. Assembly of the 30S ribosomal subunit in vitro and in cells
- Prof. James Williamson
- Decoding and peptide bond formation
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3. How aminoacyl-tRNA synthetases translate the genetic code
- Dr. Stephen Cusack
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5. Elongation of protein synthesis: structural basis of the process of decoding
- Prof. Marina Rodnina
- Initiation of protein synthesis
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7. Factor independent initiation of protein synthesis by IRES RNAs
- Prof. Jeffrey Kieft
- Elongation and termination of protein synthesis
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8. Translocation: movement of tRNA and mRNA through the ribosome
- Prof. Harry Noller
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9. Recoding: getting more out of the message by shifting reading frame and redefining codon meaning
- Prof. John Atkins
- Prof. Raymond Gesteland
- Co-translational protein secretion
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10. Mechanism of translocon function: current insights and models
- Prof. Arnold Driessen
- How antibiotics target the ribosome
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12. Antibiotic inhibition of ribosome function
- Dr. Daniel Wilson
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13. Structure-based drug design targeting infectious disease
- Dr. Erin Duffy
- Archived Lectures *These may not cover the latest advances in the field
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15. Introduction to the ribosome
- Prof. Anders Liljas
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16. The structure of the intact ribosome and ribosomal subunit interactions
- Dr. Jamie H. Doudna Cate
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17. Structural insights into decoding of mRNA by the ribosome
- Prof. Venki Ramakrishnan
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18. Chemistry of peptide bond formation
- Prof. Rachel Green
Printable Handouts
Navigable Slide Index
- Introduction
- Many antibiotics inhibit the ribosome
- Intelligent engine builds perpetual pipeline (1)
- Crystallography shows 50s is a target-of-targets
- From new X-ray crystals to new leads
- AnalogTM
- LINKER essentials: tethering two binding features
- BOMB essentials: grow
- BOMB essentials: grow, search
- BOMB essentials: score, refine
- MUSIC essentials: core-swapping
- QikProp - calculating drug-like properties
- Structures + AnalogTM: balanced compounds
- Case study: enhanced oxazolidinones
- Structural foundations
- Path to enhanced oxazolidinones
- Py contributions represent key interactions
- Probing selectivity of sparsomycin
- Seeking a new lead
- The results (1)
- Difference density map showing rib-X prototype
- Modeling - a perfect match
- The results (2)
- 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
- Intelligent engine builds perpetual pipeline (2)
- Acknowledgments
Topics Covered
- 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
Links
Series:
Categories:
Therapeutic Areas:
Talk Citation
Duffy, E. (2008, May 15). Structure-based drug design targeting infectious disease [Video file]. In The Biomedical & Life Sciences Collection, Henry Stewart Talks. Retrieved March 21, 2025, from https://doi.org/10.69645/ISPB8442.Export Citation (RIS)
Publication History
- Published on May 15, 2008
Financial Disclosures
- Dr. Erin Duffy has not informed HSTalks of any commercial/financial relationship that it is appropriate to disclose.