Abstract:
INTRODUCTION:Na/K-ATPase is a heterodimeric transmembrane protein that regulates neuronal signaling, ion homeostasis, muscle contraction and substrate transportation. Modulators of Na/K-ATPase inhibit Na(+)/K(+) exchange and increase cytosolic Ca(2+) to induce inotropic activity in heart failure patients. Besides producing inotropic effects, the Na/K-ATPase acts as a signal transducer for the regulation of many cellular events, including those associated with tumor cell growth. This has aroused new interest for development of Na/K-ATPase inhibitors as anticancer agents. AREAS COVERED:This article summarizes the various Na/K-ATPase inhibitors that have shown biological importance in clinical study and drug development for inotropic and anticancer agents. EXPERT OPINION:The field of Na/K-ATPase modulators has attracted much interest in the past because of their clinical implication in heart failure treatments. Recent studies have shown that Na/K-ATPase modulators are capable of producing profound anticancer effects upon binding to the Na/K-ATPase. Interestingly, certain Na/K-ATPase isoforms are highly expressed in particular cancer cells, providing the opportunity for a Na/K-ATPase modulator to selectively target these cellular abnormalities. Indeed the most well-known Na/K-ATPase modulators, cardiac glycosides, have shown both strong binding affinity and moderate selectivity for isoforms. It is anticipated, in the future, that the further development of more selective and potent Na/K-ATPase modulators will take place, which in turn could lead to a more effective treatment for either heart failure or cancer.
journal_name
Expert Opin Ther Patjournal_title
Expert opinion on therapeutic patentsauthors
Wang HY,O'Doherty GAdoi
10.1517/13543776.2012.690033subject
Has Abstractpub_date
2012-06-01 00:00:00pages
587-605issue
6eissn
1354-3776issn
1744-7674journal_volume
22pub_type
杂志文章,评审abstract::The patent claims peptidic/nonpeptidic inhibitors of the ghrelin receptor, the growth hormone secretagogue receptor (GHSR) 1A. Among these compounds, it was disclosed that the addition in some compounds of a GlyMetAla tripeptide at the N-terminus of the ghrelin peptide agonists converts them into ghrelin receptor anta...
journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章
doi:10.1517/13543776.2012.684946
更新日期:2012-06-01 00:00:00
abstract:IMPORTANCE OF THE FIELD:c-Met kinase is the receptor for hepatocyte growth factor. Primarily expressed on epithelial and mesenchymal cells its normal function is associated with wound healing, liver regeneration and embryo development. However, dysregulation of c-Met through overexpression, gene amplification, mutation...
journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
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更新日期:2016-01-01 00:00:00
abstract:INTRODUCTION:Caffeic acid (CA) is broadly distributed in several species of the plant kingdom and is widely consumed in human diet. CA and derivatives have been extensively studied in the past years, which unveiled a broad spectrum of biological activities and potential therapeutic applications. As a result, there has ...
journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
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更新日期:2018-06-01 00:00:00
abstract::Cholesterol homeostasis maintenance is regulated by a cellular feedback system that senses cholesterol amount in cellular membranes. 3-hydroxy 3-methylglutaryl coenzyme A reductase (HMGR) plays a pivotal role in cholesterol metabolism as it is the key rate-limiting enzyme of its biosynthetic pathway; its inhibition pr...
journal_title:Expert opinion on therapeutic patents
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journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
doi:10.1080/13543776.2018.1414183
更新日期:2018-02-01 00:00:00
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journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章
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更新日期:2016-08-01 00:00:00
abstract:INTRODUCTION:Dendrimers were widely used in cancer diagnosis and therapy during the past decade. The surface functionalities allow bioactive molecules such as imaging probes, therapeutic compounds, targeting ligands to be present on dendrimer surface in a multivalent fashion. In addition, the interior pockets as well a...
journal_title:Expert opinion on therapeutic patents
pub_type: 杂志文章,评审
doi:10.1517/13543776.2013.761207
更新日期:2013-04-01 00:00:00
abstract:BACKGROUND:The application is in the field of neural stem cells (NSCs) and cellular therapy. OBJECTIVE:It aims at establishing conditions for the isolation and propagation of neural progenitor and stem cells from human fetal tissue, with high rate of growth and high yields of differentiation into the neuronal, astrogl...
journal_title:Expert opinion on therapeutic patents
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更新日期:2009-03-01 00:00:00
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abstract:INTRODUCTION:The alpha isoform of the class 1A family of phosphatidylinositol 3-kinases (PI3Kα) has been extensively studied and exploited as a target for cancer drugs. A large number of compounds, from a wide variety of structural scaffolds, are in development. There is an ongoing debate about the desirability for sel...
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abstract::In addition to its central role in haemostasis and wound healing, thrombin activates platelets and smooth muscle cells by proteolytic activation of cell surface protease-activated receptor-1 (PAR-1), which is also known as the thrombin receptor. Thrombin is the most potent activator of human platelets and, as such, a ...
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abstract:INTRODUCTION:Melatonin is a neurohormone involved in the regulation of circadian rhythms, with potent antioxidant activity. It has a wide functional repertoire, with effects almost on all tissues and organs. It is mainly used as a dietary supplement for sleep regulation and re-synchronization of disrupted circadian rhy...
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abstract:INTRODUCTION:New classes of synthetic and semi-synthetic β-glucan inhibitors have recently emerged, providing analogs that, in some cases, have been proven to have a high degree of activity against fungi, offering the prospect of alternatives to the commercially available lipopeptide/echinocandin agents caspofungin, mi...
journal_title:Expert opinion on therapeutic patents
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abstract::A series of 10 closely related patent applications define Theravance's approach to the development of long-acting M(3) selective antagonists for the treatment of chronic obstructive pulmonary disease. The applications illustrate a modular approach to the design of such agents, comprising a muscarinic pharmacophore att...
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abstract:INTRODUCTION:HIV/AIDS is one of the most devastating diseases in the world affecting > 40 million people worldwide. Morbidity and mortality from AIDS are significantly reduced due to the advent of highly active antiretroviral therapy (HAART). Long-term toxicity, emergence of drug resistant HIV strains and drug-drug int...
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