Fragment-Based Drug Discovery
From Proteopedia
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<StructureSection load='1ysi' size='500' side='right' caption='Structure of Bcl-xl/Acyl-sulfonamide complex (PDB entry [[1ysi]])' scene=''> | <StructureSection load='1ysi' size='500' side='right' caption='Structure of Bcl-xl/Acyl-sulfonamide complex (PDB entry [[1ysi]])' scene=''> | ||
Apoptosis, or programmed cell death, is a natural mechanism in which a damaged cell dies in order to prevent further damage to the multicellular organism. The absence of apoptosis in damaged cells can lead to many types of cancers and other diseases. In certain types of cancers, a family of proteins, known as the Bcl-2 family, has been observed as being over-expressed compared to normal, healthy cells.<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 to suggest that Bcl-2 over-expression may also contribute to chemo-resistance. | Apoptosis, or programmed cell death, is a natural mechanism in which a damaged cell dies in order to prevent further damage to the multicellular organism. The absence of apoptosis in damaged cells can lead to many types of cancers and other diseases. In certain types of cancers, a family of proteins, known as the Bcl-2 family, has been observed as being over-expressed compared to normal, healthy cells.<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 to suggest that Bcl-2 over-expression may also contribute to chemo-resistance. | ||
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=== Bcl-xl: a member of the Bcl-2 family === | === Bcl-xl: a member of the Bcl-2 family === | ||
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| - | Bcl-xl is a member of the Bcl-2 family. The protein includes seven <scene name='Sandbox_reserved_394/Alpha_helices/1'>alpha helices</scene> and no beta sheets. | ||
| - | Inhibition of the over-expression of this protein has been shown to be effective at inducing tumor regression and increasing chemo-sensitivity. This represents the binding of an <scene name='Sandbox_reserved_394/Paclitaxel/1'>acyl-sulfonamide</scene> to the anti-apoptotic protein, | + | <scene name='Sandbox_reserved_394/Bcl-xl/1'>Bcl-xl</scene> is a member of the Bcl-2 family. The protein includes seven <scene name='Sandbox_reserved_394/Alpha_helices/1'>alpha helices</scene> and no beta sheets. |
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| + | Inhibition of the over-expression of this protein has been shown to be effective at inducing tumor regression and increasing chemo-sensitivity. This represents the binding of an <scene name='Sandbox_reserved_394/Paclitaxel/1'>acyl-sulfonamide</scene> to the anti-apoptotic protein, . | ||
Revision as of 01:14, 3 October 2012
Apoptosis by Inhibition of Bcl-2 Family Proteins
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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
