Fragment-Based Drug Discovery

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Using this acylsulfonamide-based ligand as a template, or pharmacophore, other drugs can be designed to have similar effects. <scene name='Sandbox_reserved_394/Abt-737/1'>ABT-737</scene> has been shown to effectively inhibit the over-expression of this protein thereby inducing tumor regression and increasing chemo-sensitivity.
Using this acylsulfonamide-based ligand as a template, or pharmacophore, other drugs can be designed to have similar effects. <scene name='Sandbox_reserved_394/Abt-737/1'>ABT-737</scene> has been shown to effectively inhibit the over-expression of this protein thereby inducing tumor regression and increasing chemo-sensitivity.
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== References ==
== References ==
{{Reflist}}
{{Reflist}}

Revision as of 18:29, 3 October 2012

Apoptosis by Inhibition of Bcl-2 Family Proteins

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

Drag the structure with the mouse to rotate

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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