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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Is the Multifunctional Na+/H+ Exchanger Isoform 1 a Potential Therapeutic Target in Cancer?

Author(s): C. Stock, F.T. Ludwig and A. Schwab

Volume 19 , Issue 5 , 2012

Page: [647 - 660] Pages: 14

DOI: 10.2174/092986712798992101

Price: $65


The Na+/H+ exchanger isoform 1 (NHE1) is a ubiquitously expressed transporter fulfilling a variety of cell physiological tasks. By importing Na+ and exporting H+, NHE1 contributes to regulatory volume increase and cytoplasmic pH homeostasis. In addition it anchors the cytoskeleton in the plasma membrane. NHE1 plays a critical role in mediating the progression of reperfusion injuries after ischemia. Moreover, it is upregulated and/or overexpressed in a number of tumour cells. In many cases an elevated NHE1 activity can be correlated with an increase in cell motility and malignancy. Consequently, NHE1 including its regulators may represent potential targets in anticancer therapy. Different NHE1 inhibitors are compared and possible clinical exploitations of NHE1 inhibition are discussed.

Keywords: Cancer treatment, cariporide (HOE642), growth factors, Na+/H+ exchanger, NHE1, pH, tumour microenvironment, physiological tasks, cytoplasmic pH homeostasis, plasma membrane, malignancy

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