8 pages. Imatinib X-Ray Crystallography

| December 22, 2015

Intro – Cover the motivation for discussing imatinib (clinically), and for the use of X-ray crystallography. Also the advantage of rational drug design (efficient targeting of resources etc – could have a table/figure listing these in bullet points additionally)
1. Identification of the problem (Chronic Myeloid Leukaemia), and the biology of the problem (chromosomal translocation/BCR-ABL/excessive signalling etc). No harm in discussing some patient statistics/prognosis. In this section, you can justify why the specific kinase should be inhibited, bringing in the point about specificity of binding
2. Identification of the target (BCR-ABL) – Can discuss how the structure was determined, with some details of the methods/experiments. Selection of appropriate binding site. You can start to discuss how the spatial configuration of the binding site might help in finding a specific drug.
3. Designing the drug (Imatinib)
4. Demonstrating the drug acts on the target (might find some of the papers I’ve attached helpful for this – bring in X-ray crystallography again) Make sure to discuss experiments/modelling that shows this, and critically analyse
5. Showing that the drug is effective in patients (this is the overall aim, after all)
Conclusion – Summarise very briefly, and answer the questions you have highlighted clearly

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Category: Pharmacology

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