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Related Concept Videos

Aquaporins01:25

Aquaporins

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Aquaporins or AQPs are a family of integral membrane proteins whose primary function is to transport water, while some called aquaglyceroporins also transport glycerol. In addition, aquaporins have also been suspected to be involved in transporting volatile substances, such as carbon dioxide and ammonia, across membranes. Such AQPs that act as gas channels are often highly expressed in cells involved in the gaseous exchange, such as red blood cells, epithelial cells, and pulmonary capillaries.
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Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

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Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
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Pore Transport and Ion-Pair Transport01:17

Pore Transport and Ion-Pair Transport

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Pore transport and ion-pair formation are critical mechanisms for the absorption and distribution of drugs in the body.
Pore transport, also known as convective transport, is a process where small molecules like urea, water, and sugars rapidly cross cell membranes as though there were channels or pores in the membrane. Although direct microscopic evidence is limited  but the concept of pores or channels is widely accepted based on physiological evidence. Despite the lack of direct...
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Drug Elimination by Renal Route: Tubular Secretion01:15

Drug Elimination by Renal Route: Tubular Secretion

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Once the process of glomerular filtration is completed, blood carrying unfiltered drug molecules traverses through efferent arterioles and makes its way into the peritubular capillaries in the proximal tubule. A variety of carriers play a pivotal role in actively secreting drugs from these peritubular capillaries into the tubular fluid. The organic anion transporter transfers acidic drugs, against an electrochemical gradient, from the peritubular capillaries into the renal tubule cells and...
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Reabsorption and Secretion in the DCT and Collecting Duct01:26

Reabsorption and Secretion in the DCT and Collecting Duct

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The early phase of the DCT manages the reabsorption of approximately 10-15% of filtered water, 5–10% of filtered sodium, and 5–10% of filtered chloride. This process is facilitated by Na+–Cl− symporters in apical membranes and sodium-potassium pumps, as well as Cl− leakage channels in basolateral membranes. The early DCT also stands out as a site where parathyroid hormone (PTH) stimulates calcium reabsorption, depending on the body's requirements.
The distal...
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Drug Elimination by Renal Route: Tubular Reabsorption01:22

Drug Elimination by Renal Route: Tubular Reabsorption

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During the process of renal excretion, as the glomerular filtrate progresses to the distal convoluted tubule (DCT), drugs that are highly permeable, lipophilic, and nonionized undergo passive reabsorption from the tubular fluid into the surrounding peritubular capillaries. This reabsorption process restricts their elimination through the kidneys. However, the majority of drugs are either weak acids or weak bases, and their ionization level is dependent on pH. By altering the pH of urine, the...
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Updated: Jul 31, 2025

Culturing Primary Rat Inner Medullary Collecting Duct Cells
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Drugging aquaporins.

Roslyn M Bill1

  • 1College of Health and Life Sciences, Aston University, Aston Triangle, Birmingham B4 7ET, UK.

Biochimica Et Biophysica Acta. Biomembranes
|May 5, 2023
PubMed
Summary
This summary is machine-generated.

Aquaporins, water channels crucial for cell function, are implicated in diseases but lack targeted drugs. Developing these medicines remains a significant challenge for treating water homeostasis disorders.

Keywords:
Aquaporin water channelsDiseaseHealthInhibitorsMembrane proteins

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Area of Science:

  • Biophysics
  • Molecular Biology
  • Cell Biology

Background:

  • Water is vital for cellular and tissue function in all organisms.
  • Aquaporins (AQPs) facilitate rapid water transport across cell membranes, excluding protons.
  • The discovery of AQPs has advanced understanding of membrane transport and their roles in various diseases.

Purpose of the Study:

  • To review the current understanding of aquaporin structure and function.
  • To highlight the implication of human aquaporins in various pathologies.
  • To address the challenge of developing aquaporin-targeted drugs for unmet clinical needs.

Main Methods:

  • Literature review of aquaporin research since the 2003 Nobel Prize.
  • Analysis of established knowledge on aquaporin structure-function relationships.
  • Examination of aquaporin involvement in human diseases and drug development efforts.

Main Results:

  • Detailed understanding of aquaporin-mediated water and solute transport mechanisms.
  • Identification of thirteen human aquaporins linked to diseases like edema, epilepsy, and cancer.
  • Absence of any aquaporin-targeted drugs currently in clinical use.

Conclusions:

  • Despite detailed knowledge, aquaporins are considered challenging drug targets.
  • Developing drugs for aquaporin-related disorders presents an unmet clinical need.
  • Success in aquaporin drug discovery could benefit millions with life-threatening conditions.