Abstract
The molecular target of rapamycin (mTOR) is central to a complex intracellular signaling pathway and is involved in diverse processes including cell growth and proliferation, angiogenesis, autophagy, and metabolism. Although sirolimus (rapamycin), the oldest inhibitor of mTOR, was discovered more than 30 years ago, renewed interest in this pathway is evident by the numerous rapalogs recently developed. These newer agents borrow from the structure of sirolimus and, although there are some pharmacokinetic differences, they appear to differ little in terms of pharmacodynamic effects and overall tolerability. Given the multitude of potential applications for this class of agents and the decrease in cost that can be expected upon the expiration of sirolimus patents, renewed focus on this agent is warranted.
Publication types
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Research Support, N.I.H., Extramural
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Review
MeSH terms
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Animals
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Antifungal Agents / adverse effects
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Antifungal Agents / chemistry
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Antifungal Agents / pharmacokinetics
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Antifungal Agents / pharmacology*
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Antineoplastic Agents / adverse effects
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacokinetics
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Antineoplastic Agents / pharmacology*
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Drug Design
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Drug Interactions
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Everolimus
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Humans
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Immunosuppressive Agents / adverse effects
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Immunosuppressive Agents / chemistry
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Immunosuppressive Agents / pharmacokinetics
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Immunosuppressive Agents / pharmacology*
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Molecular Structure
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Protein Kinases / drug effects
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Signal Transduction / drug effects
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Sirolimus / adverse effects
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Sirolimus / analogs & derivatives*
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Sirolimus / chemistry
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Sirolimus / pharmacokinetics
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Sirolimus / pharmacology*
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Structure-Activity Relationship
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TOR Serine-Threonine Kinases
Substances
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Antifungal Agents
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Antineoplastic Agents
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Immunosuppressive Agents
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temsirolimus
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Everolimus
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Protein Kinases
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MTOR protein, human
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TOR Serine-Threonine Kinases
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Sirolimus