Related Experiment Video

Updated: Feb 3, 2026

Detection of Copy Number Alterations Using Single Cell Sequencing
09:45

Detection of Copy Number Alterations Using Single Cell Sequencing

Published on: February 17, 2017

12.2K

Alteration of Androgen Receptor Protein Stability by Triptolide in LNCaP Cells

Wei Li1,2, Bi-De Liu3, Kai Liao4,5

  • 1Translational Medicine Research Institute, College of Medicine, Yangzhou University, Yangzhou 225001, China. weili@yzu.edu.cn.

Medicina (Kaunas, Lithuania)
|October 23, 2018
PubMed

Insights

Triptolide reduces prostate cancer progression by decreasing androgen receptor (AR) protein stability. This occurs through calpain activation and increased intracellular calcium, leading to AR protein breakdown in LNCaP cells.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • Prostate cancer (PCa) remains a significant health concern, with the androgen receptor (AR) driving its development and progression, even post-castration.
  • Triptolide demonstrates efficacy against PCa, yet its precise mechanism of action requires elucidation.
  • Understanding AR regulation is crucial for developing targeted PCa therapies.

Purpose of the Study:

  • To investigate the impact of triptolide on androgen receptor (AR) protein stability.
  • To elucidate the molecular mechanism by which triptolide affects AR protein levels.
  • To explore the role of calpains and intracellular calcium in triptolide's action on AR.

Main Methods:

  • Utilized cycloheximide (CHX) to block protein synthesis and assess AR protein stability via western blot assay.
  • Employed calpain inhibitors and calcium (Ca2+) chelators to investigate the involvement of calpains in triptolide-induced AR degradation.
  • Conducted experiments on LNCaP cells, a human prostate cancer cell line.

Main Results:

  • Triptolide significantly reduced AR protein levels in the presence of CHX, indicating decreased AR protein stability.
  • Co-treatment with calpain inhibitors or Ca2+ chelators restored AR protein levels, highlighting the critical role of calpains.
  • Triptolide was shown to decrease AR protein stability, leading to its breakdown.

Conclusions:

  • Triptolide activates calpain, likely by promoting intracellular Ca2+ accumulation.
  • This calpain activation leads to decreased androgen receptor (AR) protein stability and subsequent protein breakdown in LNCaP cells.
  • The findings provide a mechanistic basis for triptolide's anti-prostate cancer effects, targeting AR stability.
Keywords:
androgen receptorcalpainprotein stabilitytriptolide

More Related Videos

Immunostaining-Based Detection of Dynamic Alterations in Red Blood Cell Proteins10:07

Immunostaining-Based Detection of Dynamic Alterations in Red Blood Cell Proteins

Published on: March 17, 2023

2.4K
Studying Protein Function and the Role of Altered Protein Expression by Antibody Interference and Three-dimensional Reconstructions11:57

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

Published on: April 21, 2016

7.0K

Related Concept Videos

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.
74.7K
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
132.0K
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
17.0K
RNA Stability01:53

RNA Stability

Intact DNA strands can be found in fossils, while scientists sometimes struggle to keep RNA intact under laboratory conditions. The structural variations between RNA and DNA underlie the differences in their stability and longevity. Because DNA is double-stranded, it is inherently more stable. The single-stranded structure of RNA is less stable but also more flexible and can form weak internal bonds. Additionally, most RNAs in the cell are relatively short, while DNA can be up to 250 million...
35.7K
Alterations in Respiration II01:30

Alterations in Respiration II

There are numerous types of normal and abnormal respiration. Based on ventilatory movements, breathing patterns are classified as regular, deep, or shallow. Examples include Biot's breathing, Cheyne-Stokes respiration, Kussmaul's breathing, hyperventilation, and hypoventilation. Each pattern is clinically significant and aids in evaluating patients.
In Biot's breathing, the respiratory rate and depth are irregular, alternating between periods of deep gasping and apnea. Common causes...
1.8K
Nuclear Stability03:18

Nuclear Stability

Protons and neutrons, collectively called nucleons, are packed together tightly in a nucleus. With a radius of about 10−15 meters, a nucleus is quite small compared to the radius of the entire atom, which is about 10−10 meters. Nuclei are extremely dense compared to bulk matter, averaging 1.8 × 1014 grams per cubic centimeter. If the earth’s density were equal to the average nuclear density, the earth’s radius would be only about 200 meters.
To hold positively charged protons together...
23.3K