Related Experiment Video

Updated: Nov 15, 2025

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
10:29

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors

Published on: May 9, 2025

1.8K

The FDA-Approved Antiviral Raltegravir Inhibits Fascin1-Dependent Invasion of Colorectal Tumor Cells In Vitro and In

Begoña Alburquerque-González1, Ángel Bernabé-García2, Manuel Bernabé-García3

  • 1Department of Pathology and Histology, Campus de los Jerónimos, UCAM Universidad Católica San Antonio de Murcia, s/n, 30107 Murcia, Spain.

Cancers
|March 6, 2021
PubMed
Abstract

Insights

The antiretroviral drug RAL effectively inhibits colorectal cancer invasion and metastasis by targeting the Fascin1 protein. This study demonstrates RAL

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Fascin1 is a key actin-bundling protein driving cancer invasion and metastasis.
  • High Fascin1 expression correlates with poor prognosis across various cancer types.

Purpose of the Study:

  • To identify potential Fascin1 inhibitors using virtual screening.
  • To evaluate the efficacy of the identified inhibitor, RAL, against colorectal cancer metastasis.

Main Methods:

  • Virtual screening identified RAL, an HIV-1 integrase inhibitor, as a potential Fascin1 inhibitor.
  • Biophysical methods (NMR, DSF) confirmed RAL's interaction with Fascin1.
  • In vitro (cell lines HCT-116, DLD-1) and in vivo (zebrafish model) assays assessed RAL's impact on cancer cell migration, invasion, and actin organization.

Main Results:

  • RAL binding to Fascin1 was confirmed, leading to actin structure disorganization.
  • RAL treatment inhibited lamellipodia protrusion, migration, and invasion of colorectal cancer cells.
  • In vivo studies showed RAL significantly impaired colorectal tumor cell invasion without cytotoxicity.

Conclusions:

  • The antiretroviral drug RAL demonstrates in vitro and in vivo efficacy in inhibiting human colorectal cancer cell invasion and metastasis.
  • RAL's anti-metastatic effects are mediated through a Fascin1-dependent mechanism.
Keywords:
Fascin1colorectal cancerinvasionmigrastatinmigrationraltegravirzebrafish xenograft

More Related Videos

A High-throughput Cre-Lox Activated Viral Membrane Fusion Assay to Identify Inhibitors of HIV-1 Viral Membrane Fusion07:22

A High-throughput Cre-Lox Activated Viral Membrane Fusion Assay to Identify Inhibitors of HIV-1 Viral Membrane Fusion

Published on: August 14, 2018

6.7K
Portal Vein Injection of Colorectal Cancer Organoids to Study the Liver Metastasis Stroma07:59

Portal Vein Injection of Colorectal Cancer Organoids to Study the Liver Metastasis Stroma

Published on: September 3, 2021

6.7K

Related Concept Videos

Rous Sarcoma Virus (RSV) and Cancer01:03

Rous Sarcoma Virus (RSV) and Cancer

Rous Sarcoma virus or RSV was discovered by F. Peyton Rous in the year 1911 as a filterable transmissible agent that could cause tumors in chickens. He won a Nobel Prize for this discovery in 1966. His experiments clearly demonstrated that some cancers could be caused by infectious agents and led to the discovery of many more cancer-causing viruses in animals as well as humans.
RSV is a retrovirus that contains two copies of a plus-strand  RNA genome. Its genome consists of four main open...
5.8K
Drugs for Treatment of Ulcerative Colitis in IBD01:29

Drugs for Treatment of Ulcerative Colitis in IBD

Ulcerative colitis is a chronic inflammatory condition primarily affecting the colon and rectum. The primary drugs used in the treatment of ulcerative colitis are aminosalicylates. They exhibit anti-inflammatory and immunosuppressive properties. They modulate inflammatory mediators and inhibit the activity of nuclear factor κB (NF-κB). Aminosalicylates also reduce inflammation by inhibiting prostaglandin and leukotriene production and decreasing neutrophil chemotaxis and superoxide...
303
Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists01:27

Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists

5-HT3 receptor antagonists, such as dolasetron, granisetron (Kytril), ondansetron (Zofran), and palonosetron (Axoli), are crucial in managing chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea. These drugs selectively block 5-HT3 receptors in the visceral vagal and spinal afferent nerves, chemoreceptor trigger zone, and the vomiting center. They have a rapid onset of action and can be given as a single dose before chemotherapy. Ondansetron and granisetron, in particular,...
444
Mechanisms of Retrovirus-induced Cancers01:51

Mechanisms of Retrovirus-induced Cancers

Retroviruses are RNA viruses that have been shown to cause cancers in diverse species, including chickens, mice, cats, and monkeys. The RNA genomes of these viruses are first reverse-transcribed into single and then double-stranded DNA (dsDNA) copies. This dsDNA called proviral DNA then integrates into the host genome. Subsequently, the host cell transcribes the proviral DNA in concert with the chromosomal DNA. This leads to the production of viral RNA and proteins that assemble at the host...
5.8K