Recent Advances in the Development of Polyamine Analogues as Antitumor Agents

Casero, Robert A.; Woster, Patrick M.

doi:10.1021/jm900187v

Cited by 156 publications

(125 citation statements)

References 159 publications

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“…Previously, polyamine analogues were designed, synthesized, and tested as anticancer agents (Casero and Woster 2009) as well as in neurodegenerative processes (Minarini et al 2010), antiparasitic compounds, neurotransmitter receptor neuroprotectants, and multitargetdirected ligands for multifactorial diseases. Murray- Stewart et al (2013) report the effects of an antitumor polyamine analogue as an inhibitor of LSD1 in acute myeloid leukemia (AML).…”

Section: Editorialmentioning

confidence: 99%

Polyamines and transglutaminases: biological, clinical, and biotechnological perspectives

Agostinelli

2014

Amino Acids

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Section: Editorialmentioning

confidence: 99%

Polyamines and transglutaminases: biological, clinical, and biotechnological perspectives

Agostinelli

2014

Amino Acids

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“…Therefore, they can bind to the negatively charged nucleic acid either by electrostatic interactions and/or by hydrogen bonding. [16][17][18][19][20][21] Several other polycationic dendrimers such as poly(amidoamine) and poly(propyleneimine) have been synthesised. [22][23][24] Due to their unique one-dimensional structure and remarkable mechanical, thermal, optical and electronic properties, carbon nanotubes (CNTs), [25][26][27][28][29][30] can be considered as attractive candidates in diverse nanotechnological applications ranging from molecular electronics and quantum computing to materials science and biomedicine.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of mesitylene-based polyamine dendrimer for functionalisation of single-walled carbon nanotubes

Singh

2013

Journal of Experimental Nanoscience

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We have synthesised first generation (G1) of mesitylene-based polyamine dendrimer by following the convergent approach. The polyamine dendrimer was characterised by the usual spectroscopic techniques including liquid chromatography coupled with mass spectrometry. To develop polycationic functionalised carbon nanotubes (f-CNTs) as advanced systems for the delivery of nucleic acid, we attached G1 polyamine dendrimer onto the surface of single-walled CNTs (SWCNTs). The f-SWCNTs were characterised by thermogravimetric analysis and transmission electron microscopy. The nanotubes after functionalisation with polyamine dendrimer showed good dispersibility in highly polar solvents.

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“…These compounds, together with the enzymes involved in their biosynthesis, are present at high levels in rapidly proliferating cells, including cancer cells and protozoan parasites Casero and Woster, 2009). The physiological roles of polyamines are not completely understood (Jänne et al, 2004).…”

Section: Introductionmentioning

confidence: 99%

“…Nevertheless, there is significant interest in targeting polyamine synthesis as a basis for chemotherapy; e.g. the polyamine biosynthesis inhibitor -difluoromethylornithine (DFMO, Ornidyl) is used for the treatment of West African sleeping sickness caused by the parasite Trypanosoma brucei gambiense (Bacchi et al, 1990), and DFMO is also under investigation as an anticancer agent (Casero and Woster, 2009). …”

Section: Introductionmentioning

confidence: 99%

Polyamine uptake by the intraerythrocytic malaria parasite, Plasmodium falciparum

Niemand

Louw

Birkholtz

et al. 2012

International Journal for Parasitology

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Polyamines and the enzymes involved in their biosynthesis are present at high levels in rapidly proliferating cells, including cancer cells and protozoan parasites. Inhibition of polyamine biosynthesis in asexual blood-stage malaria parasites causes cytostatic arrest of parasite development under in vitro conditions, but does not cure infections in vivo. This may be due to replenishment of the parasite's intracellular polyamine pool via salvage of exogenous polyamines from the host. However the mechanism(s) of polyamine uptake by the intra-erythrocytic parasite are not well understood. In this study, the uptake of the polyamines putrescine and spermidine into Plasmodium falciparum parasites functionally isolated from their host erythrocyte were investigated using radioisotope flux techniques. Both putrescine and spermidine were taken up into isolated parasites via a temperature-dependent process that showed cross-competition between different polyamines. There was also some inhibition of polyamine uptake by basic amino acids. Inhibition of polyamine biosynthesis led to an increase in the total amount of putrescine and spermidine taken up from the extracellular medium. The uptake of putrescine and spermidine by isolated parasites was independent of extracellular Na + but increased with increasing external pH. Uptake also showed a marked dependence on the parasite's membrane potential, decreasing with membrane depolarization and increasing with membrane hyperpolarization. The data are consistent with polyamines being taken up into the parasite via an electrogenic uptake process, energized by the parasite's inwardly negative membrane potential.

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Recent Advances in the Development of Polyamine Analogues as Antitumor Agents

Cited by 156 publications

References 159 publications

Polyamines and transglutaminases: biological, clinical, and biotechnological perspectives

Polyamines and transglutaminases: biological, clinical, and biotechnological perspectives

Synthesis of mesitylene-based polyamine dendrimer for functionalisation of single-walled carbon nanotubes

Polyamine uptake by the intraerythrocytic malaria parasite, Plasmodium falciparum

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