Rapamycin: Difference between revisions
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Rapamycin can be used as a targeted anti-cancer drug and works as a | <p>Rapamycin can be used as a targeted anti-cancer drug and works as a <a href="Non-competitive inhibitor">non-competitive enzyme inhibitor</a><span class="fck_mw_ref" _fck_mw_customtag="true" _fck_mw_tagname="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;amp;amp;amp;amp;pg=PA145&amp;amp;amp;amp;amp;lpg=PA145&amp;amp;amp;amp;amp;dq=rapamycin+mtorc1+noncompetitive&amp;amp;amp;amp;amp;source=bl&amp;amp;amp;amp;amp;ots=fXw8f3mry-&amp;amp;amp;amp;amp;sig=zOzOgq9Xb9sXWyCGYe9XPLoQnM4&amp;amp;amp;amp;amp;hl=en&amp;amp;amp;amp;amp;sa=X&amp;amp;amp;amp;amp;ved=0ahUKEwiR7tzQlcnXAhWLJ8AKHY2CBOAQ6AEIWzAH#v=onepage&amp;amp;amp;amp;amp;q=rapamycin%20mtorc1%20noncompetitive&amp;amp;amp;amp;amp;f=false</span>. | ||
</p><p>Rapamycin binds to the FKBP protein at an <a href="Allosteric Enzyme">allosteric site</a>. The FKBP is bound to an <a href="MTOR">mTOR enzyme</a> and the binding of rapamycin to FKBP changes the shape of the <a href="ATP binding site">ATP binding site</a> of the mTOR so <a href="Phosphorylation">phosphorylation</a> no longer occurs and the <a href="Kinase">kinase</a> has been inhibited<span class="fck_mw_ref" _fck_mw_customtag="true" _fck_mw_tagname="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.</span>. | |||
Rapamycin binds to the FKBP protein at an | </p><p>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<span class="fck_mw_ref" _fck_mw_customtag="true" _fck_mw_tagname="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/</span>.<br /> | ||
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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>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/</ | <h3> References </h3> | ||
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Revision as of 16:09, 5 December 2017
Rapamycin can be used as a targeted anti-cancer drug and works as a <a href="Non-competitive inhibitor">non-competitive enzyme inhibitor</a>9. Gajanan V. Sherbet. Molecular Approach to Cancer Management. 1st Edition. Published 2017. Available at: https://books.google.co.uk/books?id=gpBYDgAAQBAJ&amp;amp;amp;amp;pg=PA145&amp;amp;amp;amp;lpg=PA145&amp;amp;amp;amp;dq=rapamycin+mtorc1+noncompetitive&amp;amp;amp;amp;source=bl&amp;amp;amp;amp;ots=fXw8f3mry-&amp;amp;amp;amp;sig=zOzOgq9Xb9sXWyCGYe9XPLoQnM4&amp;amp;amp;amp;hl=en&amp;amp;amp;amp;sa=X&amp;amp;amp;amp;ved=0ahUKEwiR7tzQlcnXAhWLJ8AKHY2CBOAQ6AEIWzAH#v=onepage&amp;amp;amp;amp;q=rapamycin%20mtorc1%20noncompetitive&amp;amp;amp;amp;f=false.
Rapamycin binds to the FKBP protein at an <a href="Allosteric Enzyme">allosteric site</a>. The FKBP is bound to an <a href="MTOR">mTOR enzyme</a> and the binding of rapamycin to FKBP changes the shape of the <a href="ATP binding site">ATP binding site</a> of the mTOR so <a href="Phosphorylation">phosphorylation</a> no longer occurs and the <a href="Kinase">kinase</a> has been inhibited8. 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..
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 $300011. 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/.
References