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Beyond DNA binding - a review of the potential mechanisms mediating quinacrine's therapeutic activities in parasitic infections, inflammation, and cancers.

Ehsanian R, Van Waes C, Feller SM - Cell Commun. Signal (2011)

Bottom Line: This is an in-depth review of the history of quinacrine as well as its pharmacokinetic properties and established record of safety as an FDA-approved drug.The potential uses of quinacrine as an anti-cancer agent are discussed with particular attention to its actions on nuclear proteins, the arachidonic acid pathway, and multi-drug resistance, as well as its actions on signaling proteins in the cytoplasm.In particular, quinacrine's role on the NF-κB, p53, and AKT pathways are summarized.

View Article: PubMed Central - HTML - PubMed

Affiliation: Tumor Biology Section, Head and Neck Surgery Branch, National Institute on Deafness and Other Communication Disorders, National Institutes of Health, Bethesda, MD, USA. rezae@stanford.edu.

ABSTRACT
This is an in-depth review of the history of quinacrine as well as its pharmacokinetic properties and established record of safety as an FDA-approved drug. The potential uses of quinacrine as an anti-cancer agent are discussed with particular attention to its actions on nuclear proteins, the arachidonic acid pathway, and multi-drug resistance, as well as its actions on signaling proteins in the cytoplasm. In particular, quinacrine's role on the NF-κB, p53, and AKT pathways are summarized.

No MeSH data available.


Structures of acridine and the acridine family member quinacrine. (A) Chemical structure of the acridine family member quinacrine. (B) Chemical structure of acridine.
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Figure 1: Structures of acridine and the acridine family member quinacrine. (A) Chemical structure of the acridine family member quinacrine. (B) Chemical structure of acridine.

Mentions: Quinacrine (IUPAC name 4-N-(6-chloro-2-methoxyacridin-9-yl)-1-N,1-N-diethylpentane-1,4-diamine) is a heterocyclic three-ring compound (Figure 1A), and an acridine (Figure 1B) derivative (9-aminoacridine). It is readily available as quinacrine dihydrochloride, the dihydrochloride salt of quinacrine, for clinical use. The interest in quinacrine stems from its long history of therapeutic uses, as will be discussed in the following sections, and in particular its potential antineoplastic activities.


Beyond DNA binding - a review of the potential mechanisms mediating quinacrine's therapeutic activities in parasitic infections, inflammation, and cancers.

Ehsanian R, Van Waes C, Feller SM - Cell Commun. Signal (2011)

Structures of acridine and the acridine family member quinacrine. (A) Chemical structure of the acridine family member quinacrine. (B) Chemical structure of acridine.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3117821&req=5

Figure 1: Structures of acridine and the acridine family member quinacrine. (A) Chemical structure of the acridine family member quinacrine. (B) Chemical structure of acridine.
Mentions: Quinacrine (IUPAC name 4-N-(6-chloro-2-methoxyacridin-9-yl)-1-N,1-N-diethylpentane-1,4-diamine) is a heterocyclic three-ring compound (Figure 1A), and an acridine (Figure 1B) derivative (9-aminoacridine). It is readily available as quinacrine dihydrochloride, the dihydrochloride salt of quinacrine, for clinical use. The interest in quinacrine stems from its long history of therapeutic uses, as will be discussed in the following sections, and in particular its potential antineoplastic activities.

Bottom Line: This is an in-depth review of the history of quinacrine as well as its pharmacokinetic properties and established record of safety as an FDA-approved drug.The potential uses of quinacrine as an anti-cancer agent are discussed with particular attention to its actions on nuclear proteins, the arachidonic acid pathway, and multi-drug resistance, as well as its actions on signaling proteins in the cytoplasm.In particular, quinacrine's role on the NF-κB, p53, and AKT pathways are summarized.

View Article: PubMed Central - HTML - PubMed

Affiliation: Tumor Biology Section, Head and Neck Surgery Branch, National Institute on Deafness and Other Communication Disorders, National Institutes of Health, Bethesda, MD, USA. rezae@stanford.edu.

ABSTRACT
This is an in-depth review of the history of quinacrine as well as its pharmacokinetic properties and established record of safety as an FDA-approved drug. The potential uses of quinacrine as an anti-cancer agent are discussed with particular attention to its actions on nuclear proteins, the arachidonic acid pathway, and multi-drug resistance, as well as its actions on signaling proteins in the cytoplasm. In particular, quinacrine's role on the NF-κB, p53, and AKT pathways are summarized.

No MeSH data available.