Fragment-Based Drug Discovery
From Proteopedia
(Difference between revisions)
| Line 1: | Line 1: | ||
| - | + | == 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. 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 has been show to effectively inhibit the over-expression of this protein thereby inducing tumor regression and increasing chemo-sensitivity. |
| Line 24: | Line 24: | ||
| align="center" | <scene name='Sandbox_reserved_394/Phe109_and_ala108/1'>Ala108</scene> || align="center" | <scene name='Sandbox_reserved_394/Tyrosine_105/1'>Tyr105</scene> || align="center" | <scene name='Sandbox_reserved_394/Phe_101/1'>Phe101</scene> || align="center" | <scene name='Sandbox_reserved_394/Glycine_142/1'>Gly142</scene> | | align="center" | <scene name='Sandbox_reserved_394/Phe109_and_ala108/1'>Ala108</scene> || align="center" | <scene name='Sandbox_reserved_394/Tyrosine_105/1'>Tyr105</scene> || align="center" | <scene name='Sandbox_reserved_394/Phe_101/1'>Phe101</scene> || align="center" | <scene name='Sandbox_reserved_394/Glycine_142/1'>Gly142</scene> | ||
|} | |} | ||
| + | |||
| + | |||
</StructureSection> | </StructureSection> | ||
| + | == References == | ||
| + | {{Reflist}} | ||
Revision as of 18:36, 26 September 2012
Paclitaxel in Apoptosis
| |||||||||||
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
