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Related Concept Videos

Carrier-Mediated Transport01:06

Carrier-Mediated Transport

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Carrier-mediated transport is a pivotal process in drug absorption, particularly for lipid-insoluble drugs, and encompasses facilitated diffusion and active transport. Facilitated diffusion allows drugs to move along their concentration gradient without energy expenditure, while active transport utilizes ATP to drive drug movement against this gradient.
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
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Thiols are prepared using the hydrosulfide anion as a nucleophile in a nucleophilic substitution reaction with alkyl halides. For instance, bromobutane reacts with sodium hydrosulfide to give butanethiol.
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Facilitated Diffusion01:16

Facilitated Diffusion

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The plasma membrane, a critical structure in cellular biology, houses an array of transporters, or carrier proteins, interspersed within its lipid bilayer. These proteins play a crucial role in solute transport through facilitated diffusion, a form of passive diffusion that uses transporters to move the molecules across the membrane.
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Overview
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Drugs need to permeate cell membranes to reach their target sites after administration. Orally administered drugs must transcend intestinal epithelial membrane barriers to infiltrate the systemic circulation. Drugs with a molecular weight of less than 500 Daltons diffuse through gaps between neighboring cells, called paracellular pathways.
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Drug Absorption Mechanism: Carrier-Mediated Membrane Transport01:19

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Certain large, lipid-insoluble drug molecules that resemble amino acids, peptides, or glucose, require specialized carrier proteins to facilitate their diffusion across cell membranes. This transport can occur through either facilitated diffusion, which does not require energy input, or active transport, which does require energy input.
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Thiol-Mediated Uptake.

Quentin Laurent1, Rémi Martinent1, Bumhee Lim1

  • 1Department of Organic Chemistry, University of Geneva, 1211 Geneva, Switzerland.

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Summary
This summary is machine-generated.

Thiol-mediated uptake involves cell entry via oligochalcogenides, inhibited by thiol-reactive agents. Cell-penetrating poly(disulfide)s and cyclic oligochalcogenides are key scaffolds, with inhibitors showing antiviral potential.

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Area of Science:

  • Biochemistry
  • Cell Biology
  • Medicinal Chemistry

Background:

  • Thiol-mediated uptake describes substrate entry into cells facilitated by specific sulfur compounds.
  • Oligochalcogenides and their mimics, particularly disulfides, play a crucial role in this process.
  • Thiol-reactive agents can inhibit this uptake mechanism.

Purpose of the Study:

  • To provide a chronological overview of thiol-mediated uptake research.
  • To summarize cell-penetrating poly(disulfide)s (CPDs) and cyclic oligochalcogenides (COCs) as essential scaffolds.
  • To explore potential antiviral applications of thiol-mediated uptake inhibitors.

Main Methods:

  • Reviewing historical observations and current literature on thiol-mediated uptake.
  • Analyzing the chemical properties of various sulfur-containing compounds (e.g., COCs, disulfides).
  • Investigating the role of factors like acidity, ring tension, and exchange reactions.

Main Results:

  • CPDs and COCs are identified as privileged scaffolds for thiol-mediated uptake.
  • Inhibitors of thiol-mediated uptake demonstrate promise as antiviral agents.
  • Potential mechanisms involving micellar pores, lipid ion channels, and specific membrane proteins are discussed.

Conclusions:

  • Thiol-mediated uptake is a complex process influenced by sulfur chemistry and cellular structures.
  • Understanding these mechanisms can lead to the development of novel antiviral therapies.
  • Specific membrane proteins like CLIC1, TMEM16F, EGFR, and PDI are implicated targets.