Related Experiment Video

Updated: Jan 28, 2026

Use of Label-free Optical Biosensors to Detect Modulation of Potassium Channels by G-protein Coupled Receptors
10:59

Use of Label-free Optical Biosensors to Detect Modulation of Potassium Channels by G-protein Coupled Receptors

Published on: February 10, 2014

10.7K

Pocket similarity identifies selective estrogen receptor modulators as microtubule modulators at the taxane site

Yu-Chen Lo1, Olga Cormier2, Tianyun Liu1,3

  • 1Department of Bioengineering, Stanford University, Stanford, CA, USA.

Nature Communications
|March 6, 2019
PubMed

Insights

Selective estrogen receptor modulators (SERMs) unexpectedly interact with the beta-tubulin taxane binding site. These compounds stabilize microtubules and inhibit cancer cell proliferation, offering a new therapeutic avenue beyond traditional taxanes.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Oncology

Background:

  • Taxanes like paclitaxel and docetaxel are vital anticancer drugs targeting beta-tubulin.
  • Current taxane therapies face limitations due to severe adverse effects and toxicity.

Purpose of the Study:

  • To identify novel taxane site modulators.
  • To explore potential new anticancer agents by screening drug-like pockets.

Main Methods:

  • Computational binding site similarity screening of over 14,000 protein pockets from the Protein Data Bank (PDB).
  • Evaluation of selective estrogen receptor modulators (SERMs) using cellular and biochemical assays.

Main Results:

  • An unexpected structural similarity was found between the estrogen receptor and the beta-tubulin taxane binding pocket.
  • Nine tested SERMs demonstrated interaction with the taxane binding site.
  • SERMs induced microtubule stabilization and inhibited cancer cell proliferation.

Conclusions:

  • Selective estrogen receptor modulators (SERMs) can modulate microtubule assembly.
  • SERMs show potential as anticancer agents through an estrogen receptor-independent mechanism.

More Related Videos

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators07:41

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

9.5K
Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay09:07

Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay

Published on: December 19, 2018

6.8K

Related Concept Videos

Microtubules01:35

Microtubules

There are three types of cytoskeletal structures in eukaryotic cells—microfilaments, intermediate filaments, and microtubules. With a diameter of about 25 nm, microtubules are the thickest of these fibers. Microtubules carry out a variety of functions that include cell structure and support, transport of organelles, cell motility (movement), and the separation of chromosomes during cell division.
98.8K
Microtubules01:18

Microtubules

Microtubules are the thickest cytoskeletal filaments with a diameter of 25 nm. In prokaryotic organisms, microtubules are commonly found in locomotory appendages like cilia and flagella. In eukaryotic cells, microtubules form specialized extensions for moving fluid over the surface, like those found in cells lining the intestine.
Microtubules have two structurally similar globular protein subunits: α and β tubulins. In the cytosol, the α and β tubulins form a heterodimer....
10.6K
Internal Receptors01:31

Internal Receptors

Many cellular signals are hydrophilic and therefore cannot pass through the plasma membrane. However, small or hydrophobic signaling molecules can cross the hydrophobic core of the plasma membrane and bind to internal, or intracellular, receptors that reside within the cell. Many mammalian steroid hormones use this mechanism of cell signaling, as does nitric oxide (NO) gas.
74.6K
Causes of Similarity-Dissimilarity Effect01:26

Causes of Similarity-Dissimilarity Effect

The similarity-dissimilarity effect, a fundamental concept in social psychology, explains how interpersonal similarities and differences influence attraction and social interactions. This effect is supported by three key psychological perspectives: balance theory, social comparison theory, and consensual validation.Balance Theory and Cognitive ConsistencyBalance theory, developed by Fritz Heider, posits that individuals seek cognitive consistency in their relationships. When two people share...
258
Antiepileptic Drugs: Modulators of Neurotransmitter Release Mediated by SV2A Protein01:20

Antiepileptic Drugs: Modulators of Neurotransmitter Release Mediated by SV2A Protein

Antiepileptic drugs, such as levetiracetam (Keppra) and brivaracetam (Briviact), have emerged as crucial tools in managing epilepsy. These medications exert their therapeutic effects by targeting the synaptic vesicle protein SV2A, a transmembrane glycoprotein primarily found in the brain.
SV2A is a transmembrane glycoprotein located predominantly in the brain, modulating the release of neurotransmitters for neuronal communication. Both levetiracetam and brivaracetam exhibit a high affinity for...
886
Factors Influencing Attraction III: Similarity01:23

Factors Influencing Attraction III: Similarity

The similarity hypothesis suggests that individuals are more likely to form relationships with others who share similar attitudes, beliefs, values, and interests. This concept has been widely studied in social psychology, demonstrating that perceived similarity fosters interpersonal attraction. In an experiment supporting this hypothesis, participants were presented with fabricated information indicating that strangers held attitudes similar to their own. The results showed that participants...
747