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Related Concept Videos

Recycling Endosomes and Transcytosis00:58

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The recycling endosome, also known as the endosomal recycling compartment (ERC), is a part of the slow-recycling process of the endocytic pathway. Molecules internalized through receptor-mediated endocytosis are either degraded in the lysosomes or are recycled to the plasma membrane through the fast- or slow-recycling route.
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Receptor-mediated endocytosis is when bulk amounts of specific molecules are imported into a cell after binding to cell surface receptors. The molecules bound to these receptors are taken into the cell through inward folding of the cell surface membrane, which is eventually pinched off into a vesicle within the cell. Structural proteins, such as clathrin, coat the budding vesicle.
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Eukaryotic cells use different mechanisms to eliminate toxic waste obsolete and worn-out substances. Lysosomes play a pivotal role in this, and hence, these substances are carried to the lysosome from other parts of the cell and extracellular space through different pathways. The most elaborately studied pathways to the lysosome are the endocytic pathways.
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Introduction to Membrane Traffic01:44

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Essential proteins such as insulin or low-density lipoprotein (LDL) and micronutrients such as iron enter a eukaryotic cell through receptor-mediated endocytosis. Subsequently, the early endosomes fuse with the vesicles containing such receptor-ligand complexes and play a vital role in sorting the incoming ligands and receptors. While the ligands are either degraded inside the vesicle or released into the cytosol, their receptors are returned to the plasma membrane for further rounds of...
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Vesicular transport is a cellular process that encompasses the engulfment of particles or dissolved substances by cells. It involves endocytosis, transcytosis, and exocytosis.
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Small molecules targeting endocytic uptake and recycling pathways.

Giampaolo Placidi1,2, Clara Mattu2, Gianluca Ciardelli2,3

  • 1Italian Institute for Genomic Medicine, Candiolo, Italy.

Frontiers in Cell and Developmental Biology
|March 27, 2023
PubMed
Summary

Small molecules targeting endocytosis and endocytic recycling are crucial for understanding cell physiology and treating diseases like cancer and neurodegeneration. This review details inhibitors blocking these essential cellular transport pathways.

Keywords:
endocytic recyclingendocytosisinhibitorsmechanism of actionsmall molecules

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Area of Science:

  • Cell Biology
  • Pharmacology

Background:

  • Intracellular trafficking is vital for cell functions like sensing, communication, and migration.
  • Dysregulation of endocytic pathways contributes to diseases such as cancer and neurodegeneration.

Purpose of the Study:

  • To review small molecule inhibitors targeting endocytosis and endocytic recycling.
  • To characterize these inhibitors based on specificity, affinity, and efficacy.

Main Methods:

  • Literature review of existing and novel small molecules.
  • Analysis of pharmacological properties and biological activity.
  • Evaluation of efficacy in in vitro and in vivo models.

Main Results:

  • Identification of key drugs and novel small molecules blocking endocytosis and recycling.
  • Characterization of target specificity, molecular affinity, and biological activity.
  • Assessment of in vitro and in vivo efficacy of identified inhibitors.

Conclusions:

  • Small molecule inhibitors offer therapeutic potential for diseases linked to endocytic pathway dysregulation.
  • Targeted inhibition of endocytosis and endocytic recycling is a promising strategy for disease intervention.