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Fragment-Based Drug Discovery
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| - | == Paclitaxel in Apoptosis == | + | —== Paclitaxel in Apoptosis == |
<StructureSection load='1ysi' size='500' side='right' caption='Structure of HMG-CoA reductase (PDB entry [[1ysi]])' scene=''> | <StructureSection load='1ysi' size='500' side='right' caption='Structure of HMG-CoA reductase (PDB entry [[1ysi]])' scene=''> | ||
This represents the binding of the anti-cancer drug, paclitaxel, to the anti-apoptotic protein, Bcl-xl. The protein includes seven <scene name='Sandbox_reserved_394/Alpha_helices/1'>alpha helices</scene> and no beta sheets. | This represents the binding of the anti-cancer drug, paclitaxel, to the anti-apoptotic protein, Bcl-xl. The protein includes seven <scene name='Sandbox_reserved_394/Alpha_helices/1'>alpha helices</scene> and no beta sheets. | ||
| - | Bcl-xl is a protein that is over-expressed in many forms of cancers and is an initiator of tumor formation.<ref>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</ref> There is also evidence that Bcl-xl expression may also contribute to chemo-resistance. Paclitaxel has been show to effectively inhibit the over-expression of this protein thereby inducing tumor regression and increasing chemo-sensitivity. | + | Bcl-xl is a protein that is over-expressed in many forms of cancers and is an initiator of tumor formation.<ref>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</ref> There is also evidence that Bcl-xl expression may also contribute to chemo-resistance. Paclitaxel, a member of the <scene name='Sandbox_reserved_394/Abt-737/1'>ABT-737</scene> family, has been show to effectively inhibit the over-expression of this protein thereby inducing tumor regression and increasing chemo-sensitivity. |
Revision as of 17:54, 1 October 2012
—== Paclitaxel in Apoptosis ==
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References
- ↑ 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
