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Εξειδίκευση τύπου : Άρθρο σε επιστημονικό περιοδικό
Τίτλος: Na+/K+ ATPase inhibitors in cancer
Δημιουργός/Συγγραφέας: Alevizopoulos K.
[EL] Καλογεροπούλου, Θεοδώρα[EN] Calogeropoulou, Theodorasemantics logo
Lang F.
Stournaras C.
Εκδότης: Bentham Science Publishers
Ημερομηνία: 2014
Γλώσσα: Αγγλικά
ISSN: 1389-4501
DOI: 10.2174/1389450115666140908125025
Άλλο: PubMed ID: 25198786
Περίληψη: Sodium potassium pump (Na+/K+ ATPase) is a transmembrane protein complex found in all higher eukaryotes acting as a key energy-consuming pump maintaining ionic and osmotic balance in cells. Recently recognized as an important transducer and/or integrator of various signals as well as a protein-protein interaction scaffold forming receptor complexes with signaling properties, the most prominent pharmacological role of Na+/K+ ATPase inhibitors is the increase of myocardial contractility in pathologic conditions such as congestive heart failure. Consequently, modulators of Na+/K+ ATPase such as digoxin have been approved by regulatory authorities and are widely used in the treatment of cardiac failure since 1975. Initiating from early observations of reduction of cancer incidence in cardiac patients taking digoxin, recent epidemiological and other studies have consolidated the anti-cancer potential of Na+/K+ ATPase inhibitors in indications such as prostate, breast, lung cancer or leukemia. More importantly, a new series of pharmacologically optimized Na+/K+ ATPase inhibitors has recently shown strong anti-cancer activities in multiple preclinical assays and have reached early clinical trials. Altogether, these results suggest that Na+/K+ ATPase is an emerging cancer target that merits further investigation. In this review, we summarize key functional properties of the enzyme that are highly relevant for cancer cell selectivity, review the most prominent chemical classes of Na+/K+ ATPase inhibitors and analyze their downstream effectors. Moreover, we discuss overall development prospects of these candidate drugs on their way to becoming new effective treatments of cancer in patients.
Τίτλος πηγής δημοσίευσης: Current Drug Targets
Τόμος/Κεφάλαιο: 15
Τεύχος: 10
Σελίδες: 988-1000
Θεματική Κατηγορία: [EL] Φαρμακευτική χημεία[EN] Pharmaceutical chemistrysemantics logo
Λέξεις-Κλειδιά: Bufadienolides
Bufalin
Cancer therapy
Cardenolides
Cardiotonic steroids
Digoxin
Istaroxime
Na+/K+ ATPase
Sodium potassium ATPase
Steroidal Na+/K+ ATPase inhibitors
Αξιολόγηση από ομότιμους (peer reviewed): Ναι
Κάτοχος πνευματικών δικαιωμάτων: © 2014 Bentham Science Publishers.
Σημειώσεις: KA1526, KA3452
Εμφανίζεται στις συλλογές:Ινστιτούτο Χημικής Βιολογίας - Επιστημονικό έργο

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