Targeting mTOR Pathway: An Overview of Rapamycin and Rapalogs


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Kılıç B., Kuzu B. , Şahan Fırat S.

İnternational 9. Drug Chemistry Congress, Antalya, Turkey, 8 - 11 April 2021, pp.39

  • Publication Type: Conference Paper / Summary Text
  • City: Antalya
  • Country: Turkey
  • Page Numbers: pp.39

Abstract

The mammalian target of rapamycin (mTOR), a serine/threonine protein kinase, is the central controller of cell growth, proliferation and metabolism. mTOR acts as a “master switch” of cellular anabolic and catabolic processes, regulating the rate of cell growth and proliferation by virtue of its ability to sense mitogen, energy and nutrient levels. As the name implies, the history of the target of rapamycin is closely linked to the discovery of rapamycin. Rapamycin, a secondary lipophilic macrolide metabolite, with the chemical formula of C51H79NO13, produced by Streptomyces hygroscopicus, was first isolated in the 1970s in the soil of Easter Island (Rapa Nui). The best-known mTOR inhibitor, rapamycin was first discovered as a potent antifungal agent, but it has also been shown to exhibit antitumor and immunosuppressant effects . Rapamycin was approved due to immunosuppressive activity by FDA firstly. Because of their significant antiproliferative, neuroprotective/neuroregenerative and cellular effects, new semi-synthetic rapamycin analogues with similar and more specific pharmacological properties have been developed.