Rapamycin: Difference between revisions
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Rapamycin can be used as a targeted anti-cancer drug and works as a [[ | Rapamycin can be used as a targeted anti-cancer drug and works as a [[Non-competitive enzyme inhibitor|non-competitive enzyme inhibitor]]<ref>Gajanan V. Sherbet. Molecular Approach to Cancer Management. 1st Edition. Published 2017.</ref>. | ||
Rapamycin binds to the FKBP protein at an [[ | Rapamycin binds to the FKBP protein at an [[Allosteric site|allosteric site]]. The FKBP is bound to an [[MTOR enzyme|mTOR enzyme]] and the binding of rapamycin to FKBP changes the shape of the [[ATP binding site|ATP binding site]] of the mTOR so [[Phosphorylation|phosphorylation]] no longer occurs and the [[Kinase|kinase]] has been inhibited<ref>8. Tao Z, Barker J, Shi SD, Gehring M, Sun S. Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes. Biochemistry. Published 2010. Volume 49, Issue 39, Pages 8488-98.</ref>. | ||
Rapamycin, although very efficient and powerful at targetting cancer, is not used too often due to the cost. One 30 ml tube of the ointment containing only one rapamycin tablet can cost up to $3000<ref> | Rapamycin, although very efficient and powerful at targetting cancer, is not used too often due to the cost. One 30 ml tube of the ointment containing only one rapamycin tablet can cost up to $3000<ref>Bhushan Madke. Topical rapamycin (sirolimus) for facial angiofibromas. Indian Dermatol Online J. Published 2013. Volume 4, Issue 1, Pages 54-57. Available at: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3573457/</ref>.<br> | ||
=== References === | === References === | ||
<references /><br> | <references /><br> | ||
Revision as of 19:57, 5 December 2017
Rapamycin can be used as a targeted anti-cancer drug and works as a non-competitive enzyme inhibitor[1].
Rapamycin binds to the FKBP protein at an allosteric site. The FKBP is bound to an mTOR enzyme and the binding of rapamycin to FKBP changes the shape of the ATP binding site of the mTOR so phosphorylation no longer occurs and the kinase has been inhibited[2].
Rapamycin, although very efficient and powerful at targetting cancer, is not used too often due to the cost. One 30 ml tube of the ointment containing only one rapamycin tablet can cost up to $3000[3].
References
- ↑ Gajanan V. Sherbet. Molecular Approach to Cancer Management. 1st Edition. Published 2017.
- ↑ 8. Tao Z, Barker J, Shi SD, Gehring M, Sun S. Steady-state kinetic and inhibition studies of the mammalian target of rapamycin (mTOR) kinase domain and mTOR complexes. Biochemistry. Published 2010. Volume 49, Issue 39, Pages 8488-98.
- ↑ Bhushan Madke. Topical rapamycin (sirolimus) for facial angiofibromas. Indian Dermatol Online J. Published 2013. Volume 4, Issue 1, Pages 54-57. Available at: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3573457/