Polyoxometalates as Versatile Enzyme Inhibitors
Identifieur interne : 001279 ( Main/Exploration ); précédent : 001278; suivant : 001280Polyoxometalates as Versatile Enzyme Inhibitors
Auteurs : Holger Stephan [Allemagne] ; Manja Kubeil ; Franziska Emmerling [Allemagne] ; Christa E. Müller [Allemagne]Source :
- European Journal of Inorganic Chemistry [ 1434-1948 ] ; 2013-04-01.
English descriptors
- Teeft :
- Acid phosphatase, Anderson structure, Anticancer, Anticancer activities, Anticancer effects, Antidiabetic activities, Antitumour activity, Antiviral, Aqueous solution, Bacterial ntpdase, Biochem, Biological activities, Cancer cells, Cell membranes, Cell surfaces, Cellular uptake, Chem, Covalent attachment, Dalton trans, Different structures, Encapsulation, Enzyme, Enzyme inhibition, Extracellular, Extracellular localization, Extracellular space, Gmbh, Heteropoly compounds, Highest oxidation state, Histone deacetylases, Holger stephan, Hydrolytic stability, Imaging agents, Inhibition, Inhibitor, Inorg, Intracellular targets, Isopoly compounds, Keggin, Keggin structure, Kegginderived sandwich, Kgaa, Kinase, Large number, Ligand, Lindqvist structure, Medical applications, Membrane proteins, Micromolar concentrations, Microreview, Nanomolar concentrations, Octahedral triples, Octahedron, Organic ligands, Other poms, Oxygen atoms, Pharmacenter bonn, Pharmaceutical chemistry, Phosphatase, Phosphoglycerate mutase, Physiological conditions, Polymerase, Polyoxometalates, Pom, Protease, Protein kinase, Protein tyrosine phosphatase, Stephan, Target proteins, Transcriptase, Tumour cells, Various poms, Verlag, Verlag gmbh, Wang, Weinheim, Weinheim microreview figure, Weinheim microreview table, Yamase.
Abstract
Polyoxometalates (POMs) are inorganic cluster compounds that have been shown to possess a number of pharmacological properties, including antidiabetic, antibacterial, antiprotozoal, antiviral and anticancer activities. Their molecular mechanism of action is largely unknown. However, several studies indicate that many of their activities may be due to the inhibition of enzymes, in particular, of those enzymes that are accessible from the extracellular space and do not require the penetration of cell membranes. In this review, we describe the recent progress in the preparation and optimization of POMs, and an evaluation of their use as inhibitors of different families of enzymes. The next important steps in this area of research will be to gain a better understanding of the interactions of POMs with enzymes on a structural level through an X‐ray crystallographic study of enzyme–POM complexes and the analysis of structure–activity relationships. Furthermore, POMs with increased stability and in vivo half‐lives have to be prepared. Surface modification may allow the targeting of POM drugs at their sites of action.
Polyoxometalates (POMs) are metal cluster compounds with a broad range of pharmacological properties, including antidiabetic, antibacterial, antiprotozoal, antiviral and anticancer activities. The inhibition of enzymes, in particular those accessible from the extracellular space, may constitute an important biological mechanism of action of POMs.
Url:
DOI: 10.1002/ejic.201201224
Affiliations:
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Le document en format XML
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<front><div type="abstract" xml:lang="en">Polyoxometalates (POMs) are inorganic cluster compounds that have been shown to possess a number of pharmacological properties, including antidiabetic, antibacterial, antiprotozoal, antiviral and anticancer activities. Their molecular mechanism of action is largely unknown. However, several studies indicate that many of their activities may be due to the inhibition of enzymes, in particular, of those enzymes that are accessible from the extracellular space and do not require the penetration of cell membranes. In this review, we describe the recent progress in the preparation and optimization of POMs, and an evaluation of their use as inhibitors of different families of enzymes. The next important steps in this area of research will be to gain a better understanding of the interactions of POMs with enzymes on a structural level through an X‐ray crystallographic study of enzyme–POM complexes and the analysis of structure–activity relationships. Furthermore, POMs with increased stability and in vivo half‐lives have to be prepared. Surface modification may allow the targeting of POM drugs at their sites of action.</div>
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