Alendronate: Difference between revisions
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== Target Proteins and Bone == | == Target Proteins and Bone == | ||
Alendronate not only targets several proteins, but also directly binds to a bone mineral (hydroxyapatite), which causes the inhibition of bone resorption. The mechanism for this has not been elucidated.<ref>http://www.ncbi.nlm.nih.gov/pubmed/20209564</ref> | Alendronate not only targets several proteins, but also directly binds to a bone mineral (hydroxyapatite), which causes the inhibition of bone resorption. The mechanism for this has not been elucidated.<ref>http://www.ncbi.nlm.nih.gov/pubmed/20209564</ref><ref>http://www.ncbi.nlm.nih.gov/pubmed/16046206</ref> | ||
=== Protein-Tyrosine-Phosphatases (PTP) === | === Protein-Tyrosine-Phosphatases (PTP) === | ||
Initial reports indicated that alendronate inhibited several types of PTPs, though specific mechanisms are not known. The data does suggest that alendronate works as an antagonist, which means that, when bound, the alendronate does not elicit a response from the protein but rather disallows the binding of an agonist which would cause a change (likely activating) in the protein.<ref>http://www.drugbank.ca/drugs/DB00630</ref> | Initial reports indicated that alendronate inhibited several types of PTPs, though specific mechanisms are not known. The data does suggest that alendronate works as an antagonist, which means that, when bound, the alendronate does not elicit a response from the protein but rather disallows the binding of an agonist which would cause a change (likely activating) in the protein.<ref>http://www.drugbank.ca/drugs/DB00630</ref><ref>http://www.ncbi.nlm.nih.gov/pubmed/8610169</ref><ref>http://www.ncbi.nlm.nih.gov/pubmed/9310349</ref> | ||
=== Farnesyl Pyrophosphate Synthase (FPPS) === | === Farnesyl Pyrophosphate Synthase (FPPS) === | ||
<Structure load='2f92' size='450' frame='true' align='right' caption='Shown: The asymmetric subunit of FPPS, not the assumed biological molecule.' scene='Insert optional scene name here' /> | <Structure load='2f92' size='450' frame='true' align='right' caption='Shown: The asymmetric subunit of FPPS, not the assumed biological molecule.' scene='Insert optional scene name here' /> | ||
FPPS is considered the main target protein of aminobisphosphonates (including alendronate). | |||
<scene name='Sandbox_59/Fpps/2'>FPPS</scene> is considered the main target protein of aminobisphosphonates (including alendronate). | |||
<scene name='Sandbox_59/Alen_in_secondary_struct/2'>Bound Alendronate</scene> | <scene name='Sandbox_59/Alen_in_secondary_struct/2'>Bound Alendronate</scene> | ||
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<scene name='Sandbox_59/Fpps_hydrophobic/1'>hydrphobic FPPS</scene> | <scene name='Sandbox_59/Fpps_hydrophobic/1'>hydrphobic FPPS</scene> | ||
