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Fragment-Based Drug Discovery

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Apoptosis by Inhibition of Bcl-2 Family Proteins

Structure of Bcl-xl/Acyl-sulfonamide complex (PDB entry 1ysi)

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ABT-737


Using this acylsulfonamide-based ligand as a template, or pharmacophore, other drugs can be designed to have similar effects. has been shown to effectively inhibit the over-expression of this protein thereby inducing tumor regression and increasing chemo-sensitivity.


References

  1. Oltersdorf T., Elmore S.W., Shoemaker A.R. An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Vol 435|2 June 2005|doi:10.1038/nature03579

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