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Related Concept Videos

Overview of Protein Sorting and Transport01:45

Overview of Protein Sorting and Transport

Eukaryotic cells have different membrane-bound organelles with distinct protein requirements. The process by which proteins are targeted to a specific organelle is called protein sorting.
Protein sorting can be of two types: signal-based sorting and vesicle-based trafficking. In signal-based sorting, specific amino acid sequences called sorting signals target proteins to the proper location inside the cell either via gated transport or by protein translocation.  In gated transport, folded...
Regulation of Nuclear Protein Sorting01:45

Regulation of Nuclear Protein Sorting

Nuclear protein sorting regulates nucleus composition and gene expression, crucial for determining the fate of a eukaryotic cell. Hence, the entry and exit of molecules across the nuclear envelope is a tightly controlled process. Nuclear protein sorting can be inhibited by one of the following ways: 1) masking cargo signal sequences, 2) modifying the nuclear receptor's affinity for cargo, 3) controlling the nuclear pore size, 4) retaining the cargo during its transit to the cytosol or the...
Membrane Transporters01:31

Membrane Transporters

Transporters are essential membrane transport proteins with functions related to cell nutrition, homeostasis, communication, etc. Approximately 7% of all genes in the human genome code for transporters or transporter-related proteins.
Transporters are mainly composed of alpha-helices, built from bundles of ten or more helices traversing the plasma membrane. The solute-binding sites are located midway, where some of the helices are broken or distorted, making space for the binding site through...
Carrier-Mediated Transport01:06

Carrier-Mediated Transport

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...
Nuclear Protein Sorting01:34

Nuclear Protein Sorting

Nuclear protein sorting is the selective trafficking of histones, polymerases, gene regulatory proteins into the nucleus and exporting RNAs and ribosomes to the cytosol. It is a tightly controlled process that regulates gene expression within a cell.
Proteins targeted to the nucleus carry nuclear localization signals or NLS recognized by import receptors in the cytosol. Similarly, proteins with nuclear export signals are recognized by export receptors. Import and export receptors are...
Protein Transport to the Thylakoids01:22

Protein Transport to the Thylakoids

Thylakoids are membrane-bound sac-like structures within the chloroplast that serve as sites for photosynthesis. Thylakoid lumen contains many electron transport proteins and is enclosed by a thylakoid membrane rich in the light-harvesting complex. Proteins targeted to the thylakoids are transported as precursors and are sorted by the general TOC/TIC import pathway. Once the precursor reaches the stroma, stromal processing peptidases remove their transit signal and expose thylakoid signal...

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Related Experiment Video

Updated: Jun 2, 2026

Studying Protein Function and the Role of Altered Protein Expression by Antibody Interference and Three-dimensional Reconstructions
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Studying Protein Function and the Role of Altered Protein Expression by Antibody Interference and Three-dimensional Reconstructions

Published on: April 21, 2016

Controlling protein transport by small molecules.

Karl Gademann1

  • 1University of Basel, Department of Chemistry, St. Johanns-Ring 19, CH-4056 Basel, Switzerland. karl.gademann@unibas.ch

Current Drug Targets
|May 13, 2011
PubMed
Summary
This summary is machine-generated.

Nuclear export, crucial for cell function, can be blocked by small molecules inhibiting CRM1. This study reviews compounds that disrupt CRM1-cargo interactions, offering potential as anticancer agents.

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Area of Science:

  • Molecular Biology
  • Biochemistry
  • Pharmacology

Background:

  • Nuclear export of proteins to the cytoplasm is primarily mediated by exportin CRM1.
  • CRM1 recognizes cargo proteins via a leucine-rich nuclear export signal (NES).
  • Inhibition of CRM1-mediated nuclear export is a target for therapeutic intervention.

Purpose of the Study:

  • To review the chemistry and inhibitory mechanisms of various small molecules targeting CRM1.
  • To discuss the structural basis of CRM1 inhibition by compounds like leptomycin.
  • To evaluate the potential of these nuclear export inhibitors as anticancer agents.

Main Methods:

  • Literature review of studies on CRM1 inhibitors.
  • Analysis of the structural basis for CRM1-cargo interaction disruption.
  • Evaluation of chemical properties and biological activities of natural and synthetic compounds.

Main Results:

  • Several natural products and synthetic compounds inhibit CRM1-mediated nuclear export.
  • Leptomycin (LMB) inhibits export by disrupting the CRM1-cargo protein interaction.
  • A range of compounds including anguinomycin, goniothalamin, and synthetic molecules show inhibitory activity.

Conclusions:

  • Understanding the structural basis of CRM1 inhibition informs the design of novel export inhibitors.
  • Nuclear export inhibitors hold promise as anticancer therapeutics.
  • Further research into these compounds could lead to new cancer treatments.