Related Experiment Video

Updated: Feb 5, 2026

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
10:49

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia

Published on: September 18, 2013

18.6K

Effects of Sunitinib and Other Kinase Inhibitors on Cells Harboring a

Martin Sramek1,2,3, Jakub Neradil4,5,6, Petra Macigova7,8

  • 1Laboratory of Tumor Biology, Department of Experimental Biology, Faculty of Science, Masaryk University, 61137 Brno, Czech Republic. martin.sramek@mail.muni.cz.

International Journal of Molecular Sciences
|September 12, 2018
PubMed

Insights

Sunitinib shows promise in treating infantile myofibromatosis by reducing platelet-derived growth factor receptor beta (PDGFR-beta) phosphorylation in tumor cells with the p.R561C mutation.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Infantile myofibromatosis is a common childhood tumor requiring better treatments for drug-resistant cases.
  • The p.R561C mutation in platelet-derived growth factor receptor beta (PDGFR-beta) is linked to infantile myofibromatosis.
  • Targeted therapies, particularly protein kinase inhibitors, offer a potential treatment strategy.

Purpose of the Study:

  • To analyze kinase phosphorylation in the NSTS-47 cell line from a patient with infantile myofibromatosis and a PDGFR-beta p.R561C mutation.
  • To investigate the impact of specific protein kinase inhibitors on cell signaling and proliferation in this cell line.

Main Methods:

  • Utilized the NSTS-47 cell line derived from infantile myofibromatosis tumor tissue.
  • Analyzed phosphorylation levels of PDGFR-beta, ERK1/2, and other kinases.
  • Assessed the effects of sunitinib and other protein kinase inhibitors on cell signaling and proliferation.

Main Results:

  • The NSTS-47 cell line exhibited high phosphorylation of PDGFR-beta, ERK1/2, and other kinases.
  • Sunitinib effectively reduced PDGFR-beta phosphorylation in tumor cells.
  • MEK1/2 and ERK1/2 remained constitutively phosphorylated despite sunitinib and other inhibitor treatments.

Conclusions:

  • Sunitinib demonstrates potential as a therapeutic agent for infantile myofibromatosis with the PDGFR-beta p.R561C mutation.
  • Further research is warranted to explore combination therapies targeting both PDGFR-beta and downstream signaling pathways.
Keywords:
FR180204U0126erlotinibinfantile myofibromatosisplatelet-derived growth factor receptorprotein kinase inhibitorsreceptor tyrosine kinasessunitinibtargeted therapy

More Related Videos

A Simple Method to Identify Kinases That Regulate Embryonic Stem Cell Pluripotency by High-throughput Inhibitor Screening07:18

A Simple Method to Identify Kinases That Regulate Embryonic Stem Cell Pluripotency by High-throughput Inhibitor Screening

Published on: May 12, 2017

6.8K
Protein Kinase C-delta Inhibitor Peptide Formulation using Gold Nanoparticles06:06

Protein Kinase C-delta Inhibitor Peptide Formulation using Gold Nanoparticles

Published on: March 9, 2019

5.9K

Related Concept Videos

Protein Kinases and Phosphatases02:54

Protein Kinases and Phosphatases

Proteins undergo chemical modifications that trigger changes in the charge, structure, and conformation of the proteins. Phosphorylation, acetylation, glycosylation, nitrosylation, ubiquitination, lipidation, methylation, and proteolysis are various protein modifications that regulate protein activity. Such modifications are usually enzyme-driven.
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
15.2K
Protein Kinases and Phosphatases02:54

Protein Kinases and Phosphatases

4.5K
Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers01:26

Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers

Receptor tyrosine kinase inhibitors (TKIs) and calcium channel blockers (CCBs) are two critical categories of drugs employed in the treatment of pulmonary artery hypertension (PAH). PAH is a disease that causes high blood pressure in the pulmonary arteries, resulting in chest pain, fatigue, and shortness of breath.
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...
544
Eukaryotic Transcription Inhibitors01:52

Eukaryotic Transcription Inhibitors

Certain biochemical processes, such as embryonic development and cell growth regulation, depend on the repression of specific genes. DNA binding proteins known as eukaryotic transcription inhibitors regulate the repression of gene expression in eukaryotes. The presence of these inhibitors at the required location and time in the cell is triggered by the presence of hormones and additional signals from other cells.
Eukaryotic transcription inhibitors usually contain two distinct domains, a...
11.0K
Receptor Tyrosine Kinases01:26

Receptor Tyrosine Kinases

Receptor tyrosine kinases or RTKs are membrane-bound receptors that phosphorylate specific tyrosine on protein substrates. RTKs regulate cellular growth, differentiation, survival, and migration. They contain an extracellular ligand binding domain, a transmembrane domain, and a cytosolic tail with intrinsic kinase activity. Several extracellular signaling molecules activate RTKs in one or more ways and relay the signal downstream. Ligands such as platelet-derived growth factor (PDGF) or...
18.8K
Buffer Effectiveness02:19

Buffer Effectiveness

Buffer solutions do not have an unlimited capacity to keep the pH relatively constant . Instead, the ability of a buffer solution to resist changes in pH relies on the presence of appreciable amounts of its conjugate weak acid-base pair. When enough strong acid or base is added to substantially lower the concentration of either member of the buffer pair, the buffering action within the solution is compromised.
The buffer capacity is the amount of acid or base that can be added to a given volume...
55.4K