Abstract

Aquaporins (AQPs) are a family of water channel proteins distributed in various human tissues, responsible for the transport of small solutes such as glycerol, even gas and ions. The expression of AQPs has been found in more than 20 human cancer types and is significantly correlated with the severity of histological tumors and prognosis of patients with cancer. More recent evidence showed that AQPs could also play a role in tumor-associated edema, tumor cell proliferation and migration, and tumor angiogenesis in solid and hematological tumors. Inhibitors of AQPs in tumor cells and microvessels have been suggested as new therapeutic strategies. The present review overviews AQPs structures, expression variation among normal tissues and tumors, AQPs functions and roles in the development of cancer with special focuses on lung, colorectal, liver, brain and breast cancers, and potential AQPs-target inhibitors. We call the special attention to consider AQPs important as diagnostic and therapeutic biomarkers. It may be a novel anticancer therapy by the AQPs inhibition.

Highlights

  • The aquaporins (AQPs) are a family of small, transmembrane, water-transport proteins distributed in various human tissues [1]

  • AQP1, AQP2, AQP4, AQP5, or AQP8 are exclusively selective for water, while AQP3, AQP7, AQP9, or AQP10 proposed as aquaglyceroporins can transport water and small neutral solutes such as glycerol [2]

  • AQPs expression in normal and cancer tissues Human AQPs distribute in different normal tissue and most of them are located in epithelium and endothelium, as well as some other typical cells such as erythrocytes, astrocytes, adipocytes and skeletal muscle [28]

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Summary

Introduction

The aquaporins (AQPs) are a family of small, transmembrane, water-transport proteins distributed in various human tissues [1]. The present review overviews AQPs structures, AQPs expression in normal and tumor tissues, AQPs functions and specific roles in cancer development, and potential AQPs-target anticancer drugs. AQP monomer contains independently water pore and assembles as homotetramers to contribute to fluid transport [20] (Figure 1B). AQPs expression in normal and cancer tissues Human AQPs distribute in different normal tissue and most of them are located in epithelium and endothelium, as well as some other typical cells such as erythrocytes, astrocytes, adipocytes and skeletal muscle [28]. AQPs regulate brain water homeostasis, exocrine gland secretion, urine concentration, skin moisturization, fat metabolism or neural signal transduction. In the CNS, AQP4 plays a principle role in the regulation of blood-brain barrier (BBB) water permeability while AQP1 facilitates cerebrospinal fluid

Tumor type
Findings
Cervical cancer
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