Biological activity of antitumoural MGBG: the structural variable

The present study aims at determining the structure-activity relationships (SAR's) ruling the biological function of MGBG (methylglyoxal bis(guanylhydrazone)), a competitive inhibitor of S-adenosyl-l-methionine decarboxylase displaying anticancer activity, involved in the biosynthesis of the na...

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Veröffentlicht in:	Amino acids 2008-05, Vol.34 (4), p.555-564
Hauptverfasser:	Marques, M. P. M, Gil, F. P. S. C, Calheiros, R, Battaglia, V, Brunati, A. M, Agostinelli, E, Toninello, A
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosylmethionine Decarboxylase - antagonists & inhibitors Analytical Chemistry Animals Antineoplastic Agents - chemistry Antineoplastic Agents - metabolism Antineoplastic Agents - pharmacology Binding Sites Biochemical Engineering Biochemistry Biomedical and Life Sciences Calcium - antagonists & inhibitors Calcium - pharmacology Cell Membrane Permeability - drug effects Cell Membrane Permeability - physiology Computer Simulation DFT calculations Dose-Response Relationship, Drug Enzyme Inhibitors - chemistry Enzyme Inhibitors - metabolism Enzyme Inhibitors - pharmacology Hepatocytes - chemistry Hepatocytes - drug effects Hepatocytes - metabolism Hydrogen-Ion Concentration Life Sciences Male MGBG Mitochondria, Liver - drug effects Mitochondria, Liver - physiology Mitochondrial permeability transition (MPT) Mitoguazone - chemistry Mitoguazone - metabolism Mitoguazone - pharmacology Models, Biological Models, Molecular Neurobiology Original Article Physiological structures Polyamines Proteins Proteomics Quantum Theory Rats Rats, Wistar SAMDC Spermidine - antagonists & inhibitors Spermidine - pharmacology Spermine - antagonists & inhibitors Spermine - pharmacology Structure-Activity Relationship structure-activity relationships Time Factors
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Beschreibung
Zusammenfassung:	The present study aims at determining the structure-activity relationships (SAR's) ruling the biological function of MGBG (methylglyoxal bis(guanylhydrazone)), a competitive inhibitor of S-adenosyl-l-methionine decarboxylase displaying anticancer activity, involved in the biosynthesis of the naturally occurring polyamines spermidine and spermine. In order to properly understand its biochemical activity, MGBG's structural preferences at physiological conditions were ascertained, by quantum mechanical (DFT) calculations.
ISSN:	0939-4451 1438-2199
DOI:	10.1007/s00726-007-0009-2