Rapamycin: Difference between revisions
added links, tried to sort out references |
added references |
||
| Line 1: | Line 1: | ||
= Rapamycin = | = Rapamycin = | ||
Rapamycin can be used as a targeted anti-cancer drug and works as a [[Non- | Rapamycin can be used as a targeted anti-cancer drug and works as a [[Non-competitive inhibitor|non-competitive enzyme inhibitor]]<ref>9. Gajanan V. Sherbet. Molecular Approach to Cancer Management. 1st Edition. Published 2017. Available at: https://books.google.co.uk/books?id=gpBYDgAAQBAJ&amp;pg=PA145&amp;lpg=PA145&amp;dq=rapamycin+mtorc1+noncompetitive&amp;source=bl&amp;ots=fXw8f3mry-&amp;sig=zOzOgq9Xb9sXWyCGYe9XPLoQnM4&amp;hl=en&amp;sa=X&amp;ved=0ahUKEwiR7tzQlcnXAhWLJ8AKHY2CBOAQ6AEIWzAH#v=onepage&amp;q=rapamycin%20mtorc1%20noncompetitive&amp;f=false</ref>. | ||
Rapamycin binds to the FKBP protein at an [[ | Rapamycin binds to the FKBP protein at an [[Allosteric Enzyme|allosteric site]]. The FKBP is bound to an [[MTOR|mTOR enzyme]] and the binding of rapamycin to FKBP changes the shape of the 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 30ml tube of ointment containing only one rapamycin tablet can cost up to $3000<ref>11. 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>. | Rapamycin, although very efficient and powerful at targetting cancer, is not used too often due to the cost. One 30ml tube of ointment containing only one rapamycin tablet can cost up to $3000<ref>11. 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>. | ||
== References == | |||
1. Gajanan V. Sherbet. Molecular Approach to Cancer Management. 1st Edition. Published 2017. Available at: https://books.google.co.uk/books?id=gpBYDgAAQBAJ&pg=PA145&lpg=PA145&dq=rapamycin+mtorc1+noncompetitive&source=bl&ots=fXw8f3mry-&sig=zOzOgq9Xb9sXWyCGYe9XPLoQnM4&hl=en&sa=X&ved=0ahUKEwiR7tzQlcnXAhWLJ8AKHY2CBOAQ6AEIWzAH#v=onepage&q=rapamycin%20mtorc1%20noncompetitive&f=false | |||
2. 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. | |||
3. 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/<br> <br> | |||
Revision as of 15:05, 28 November 2017
Rapamycin
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 30ml tube of ointment containing only one rapamycin tablet can cost up to $3000[3].
References
1. Gajanan V. Sherbet. Molecular Approach to Cancer Management. 1st Edition. Published 2017. Available at: https://books.google.co.uk/books?id=gpBYDgAAQBAJ&pg=PA145&lpg=PA145&dq=rapamycin+mtorc1+noncompetitive&source=bl&ots=fXw8f3mry-&sig=zOzOgq9Xb9sXWyCGYe9XPLoQnM4&hl=en&sa=X&ved=0ahUKEwiR7tzQlcnXAhWLJ8AKHY2CBOAQ6AEIWzAH#v=onepage&q=rapamycin%20mtorc1%20noncompetitive&f=false
2. 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.
3. 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/
- ↑ 9. Gajanan V. Sherbet. Molecular Approach to Cancer Management. 1st Edition. Published 2017. Available at: https://books.google.co.uk/books?id=gpBYDgAAQBAJ&pg=PA145&lpg=PA145&dq=rapamycin+mtorc1+noncompetitive&source=bl&ots=fXw8f3mry-&sig=zOzOgq9Xb9sXWyCGYe9XPLoQnM4&hl=en&sa=X&ved=0ahUKEwiR7tzQlcnXAhWLJ8AKHY2CBOAQ6AEIWzAH#v=onepage&q=rapamycin%20mtorc1%20noncompetitive&f=false
- ↑ 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.
- ↑ 11. 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/