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Related Concept Videos

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-Receptor Bonds01:25

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Drug-receptor bonds are formed through various chemical forces when drugs interact with target cells. Covalent bonds, strong and irreversible, are exemplified by DNA-alkylating anticancer agents that inhibit cell division. However, such irreversible drug binding lacks selectivity and can modify the DNA of the surrounding healthy cells. Covalent binding often contributes to tissue toxicity, as seen with chloroform and paracetamol metabolites binding to the liver, causing hepatotoxicity.
In...
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Multi-pass Transmembrane Proteins and β-barrels01:09

Multi-pass Transmembrane Proteins and β-barrels

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In multi-pass transmembrane proteins, the polypeptide chain crosses the membrane more than once. The transmembrane polypeptide chain either forms an α-helix or β-strand structure. α-Helix containing multi-pass transmembrane proteins are ubiquitous, whereas β-strand containing ones are mainly found in gram-negative bacteria, mitochondria, and chloroplasts.
α-Helix containing multi-pass transmembrane proteins
Multi-pass transmembrane proteins such as...
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Protein Diffusion in the Membrane01:24

Protein Diffusion in the Membrane

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Proteins show rotational as well as lateral diffusion across the membrane. The lateral diffusion of proteins was confirmed through the cell fusion experiment where mouse and human cells were fused, resulting in hybrid cells. When the human and mouse cells fused, the specific membrane proteins on human and mouse cells were marked with the red and green-fluorescent markers, respectively. Initially, the red and green fluorescence was located on the respective hemisphere of the cell. As time...
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Cellular Membranes and Drug Transport01:24

Cellular Membranes and Drug Transport

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Drugs must traverse multiple biological barriers, such as multi-layered skin, single-layered intestinal epithelium, and the plasma membrane, to reach their target sites within the body. The plasma membrane, a highly structured composite of phospholipids, carbohydrates, and proteins, is the cell's protective boundary, facilitating selective substance exchange.
Phospholipids arrange themselves into a bilayer, with hydrophilic heads oriented outward and hydrophobic tails facing inward.
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Mechanisms of Membrane Domain Formation00:59

Mechanisms of Membrane Domain Formation

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Different physical properties of lipids and proteins allow them to localize and form distinct islands or domains in the membrane. Some membrane domains are formed due to protein-protein interactions, whereas others are formed due to the presence of specific lipids such as sphingolipids and sterols—for example, large proteins, such as bacteriorhodopsin, aggregate and create distinct domains.
Another mechanism for membrane domain formation involves membrane proteins interacting with...
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Updated: Mar 26, 2026

Native Cell Membrane Nanoparticles System for Membrane Protein-Protein Interaction Analysis
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Native Cell Membrane Nanoparticles System for Membrane Protein-Protein Interaction Analysis

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Drugging Membrane Protein Interactions.

Hang Yin1,2,3, Aaron D Flynn2,4

  • 1Department of Chemistry and Biochemistry.

Annual Review of Biomedical Engineering
|February 12, 2016
PubMed
Summary
This summary is machine-generated.

New technologies enable targeting previously undruggable membrane proteins for drug discovery. This review explores high-throughput screening and rational design for novel pharmacotherapies against these critical targets.

Keywords:
curvature sensingdrug discoveryhigh-throughput screeningrational designtransmembrane domains

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Molecular Biology

Background:

  • Membrane proteins are crucial cellular components involved in signaling, transport, and catalysis.
  • Most therapeutics currently target accessible membrane proteins.
  • Conventionally undruggable regions of membrane proteins present a challenge in drug discovery.

Purpose of the Study:

  • To review the state-of-the-art in high-throughput screening and rational design for membrane protein targets.
  • To evaluate advances enabling the targeting of unorthodox membrane protein regions.
  • To discuss the future of pharmacotherapy against challenging membrane protein targets.

Main Methods:

  • Survey of current high-throughput screening methodologies.
  • Analysis of rational drug design strategies.
  • Evaluation of emerging biological understanding and technological advancements.

Main Results:

  • Newly devised technologies facilitate the drugging of previously inaccessible membrane protein regions.
  • Modulation of protein-protein, protein-lipid, and protein-nucleic acid interactions is now achievable.
  • Significant progress has been made in understanding and targeting complex membrane proteins.

Conclusions:

  • Advances in technology and biological understanding are expanding the scope of druggable membrane proteins.
  • This progress promises to drive pharmacotherapy forward against unorthodox membrane protein targets.
  • The review highlights the potential for novel therapeutics by targeting previously intractable membrane proteins.