Related Experiment Video

Updated: Jun 9, 2026

The Establishment of a Lung Colonization Assay for Circulating Tumor Cell Visualization in Lung Tissues
07:39

The Establishment of a Lung Colonization Assay for Circulating Tumor Cell Visualization in Lung Tissues

Published on: June 16, 2018

Enzastaurin inhibits invasion and metastasis in lung cancer by diverse molecules

A Körner1, G Mudduluru, C Manegold

  • 1Department of Experimental Surgery Mannheim/Molecular Oncology of Solid Tumors (German Cancer Research Center-DKFZ-Heidelberg), Mannheim Medical Faculty, Ruprecht-Karls-University Heidelberg, Mannheim 68167, Germany.

British Journal of Cancer
|August 26, 2010
PubMed
Abstract

Insights

Enzastaurin inhibits non-small cell lung cancer (NSCLC) invasion and metastasis by targeting urokinase-type plasminogen activator receptor (u-PAR). U-PAR also serves as a novel marker for Enzastaurin response in NSCLC.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Enzastaurin is a kinase inhibitor targeting the protein kinase C (PKC)beta/AKT pathway.
  • Its efficacy in inhibiting cancer invasion and metastasis requires further elucidation.

Purpose of the Study:

  • To investigate the effect of Enzastaurin on non-small cell lung cancer (NSCLC) cell migration, invasion, and metastasis.
  • To identify molecular targets of Enzastaurin in NSCLC.

Main Methods:

  • Utilized RT-PCR validated microarray, Matrigel invasion assays, and in vivo chorionallantoic membrane (CAM) assays.
  • Investigated gene expression changes and molecular mechanisms using luciferase/chromatin immunoprecipitation analysis and siRNA knockdown.

Main Results:

  • Enzastaurin significantly reduced migration, invasion, and metastasis in NSCLC cell lines.
  • Enzastaurin altered the expression of key genes involved in cancer progression and tumor suppression.
  • Enzastaurin transcriptionally inhibits urokinase-type plasminogen activator receptor (u-PAR) expression, and u-PAR knockdown re-sensitized resistant cells.

Conclusions:

  • Enzastaurin inhibits NSCLC metastasis by targeting u-PAR and modulating other progression-related and tumor-suppressor genes.
  • Urokinase-type plasminogen activator receptor (u-PAR) is identified as a novel marker for Enzastaurin response.
  • These findings support molecularly tailored clinical studies of Enzastaurin in NSCLC therapy.

More Related Videos

Lung Tumor Cell Recruitment Assay04:28

Lung Tumor Cell Recruitment Assay

Published on: February 26, 2019

Related Concept Videos

Metastasis02:30

Metastasis

Metastasis is the spread of cancer cells from the original site to distant locations in the body. Cancer cells can spread via blood vessels (hematogenous) as well as lymph vessels in the body.
Epithelial-to-Mesenchymal Transition
The epithelial-to-mesenchymal transition or EMT is a developmental process commonly observed in wound healing, embryogenesis, and cancer metastasis. EMT is induced by transforming growth factor-beta (TGF-β) or receptor tyrosine kinase (RTK) ligands, which further...
Cancer Cell Migration through Invadopodia01:35

Cancer Cell Migration through Invadopodia

Invadosome is a broad category of cell surface structures with proteolytic activity that  degrades the extracellular matrix (ECM). Invadosomes are present in normal cell types, including macrophages, endothelial cells, and neurons, as well as tumor cells. Although the macrophage podosomes and tumor cell invadopodia are classified as invadosomes, they have different structures, molecular pathways, and functions. Podosomes are short structures that last for a few minutes. However, invadopodia can...
Drugs that Destabilize Microtubules01:10

Drugs that Destabilize Microtubules

Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...
Drugs that Stabilize Microtubules01:15

Drugs that Stabilize Microtubules

Microtubules are dynamic structures that undergo cycles of catastrophe and rescue. The microtubules play a central role in cell division by forming the spindle apparatus for segregating the chromosomes. This makes them ideal targets for regulating dividing cells in tumors and malignant cancer cells. Microtubule stabilizing drugs help stabilize the microtubule formation and promote its polymerization. Paclitaxel was the first microtubule stabilizing agent used as anticancer drug in chemotherapy...
Antiasthma Drugs: Leukotriene Modifiers01:19

Antiasthma Drugs: Leukotriene Modifiers

Leukotriene modifiers, or cysteinyl leukotriene receptor antagonists, are medications used to manage chronic asthma. These agents target specific inflammatory mediators produced during arachidonic acid metabolism, an essential process in generating inflammation in the body.
Leukotriene modifiers work through two distinct mechanisms:
The Tumor Microenvironment02:17

The Tumor Microenvironment

Every normal cell or tissue is embedded in a complex local environment called stroma, consisting of different cell types, a basal membrane, and blood vessels. As normal cells mutate and develop into cancer cells, their local environment also changes to allow cancer progression. The tumor microenvironment (TME) consists of a complex cellular matrix of stromal cells and the developing tumor. The cross-talk between cancer cells and surrounding stromal cells is critical to disrupt normal tissue...