4.4 Editorial Material

Why is rapamycin not a rapalog?

Journal

GERONTOLOGY
Volume 69, Issue 6, Pages 657-659

Publisher

KARGER
DOI: 10.1159/000528985

Keywords

sirolimus; mTOR inhibitors; aging

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Rapamycin is an FDA-approved immunosuppressive drug and a leading candidate for targeting aging. It inhibits mTOR kinase by binding to FK506-binding proteins (FKBP) and has similar chemical structure with its analogs, which are referred to as 'rapalogs.' The development of rapalogs aimed to improve pharmacological properties of rapamycin.
Rapamycin (sirolimus) is an immunosuppressive drug approved by the Food and Drug Administration (FDA). It is also a leading candidate for targeting aging. Rapamycin and its analogs (everolimus, temsirolimus, ridaforolimus) inhibit the mammalian target of rapamycin (mTOR) kinase by binding to FK506-binding proteins (FKBP) and have a similar chemical structure that only differs in the functional group present at carbon-40. Analogs of rapamycin were developed to improve its pharmacological properties, such as low oral bioavailability and a long half-life. The analogs of rapamycin are referred to as 'rapalogs.' Rapamycin is the parent compound and should there with not be called a 'rapalog.'

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