Related Experiment Video

Updated: Jan 1, 2026

Tumor Treating Field Therapy in Combination with Bevacizumab for the Treatment of Recurrent Glioblastoma
06:15

Tumor Treating Field Therapy in Combination with Bevacizumab for the Treatment of Recurrent Glioblastoma

Published on: October 27, 2014

27.8K

Battling Glioblastoma: A Novel Tyrosine Kinase Inhibitor with Multi-Dimensional Anti-Tumor Effect (Running Title:

Anisha Viswanathan1, Aliyu Musa2, Akshaya Murugesan1,3

  • 1Molecular Signaling Lab, Faculty of Medicine and Health Technology, Tampere University, BioMeditech and Tays Cancer Center, Tampere University Hospital, P.O. Box 553, 33101 Tampere, Finland.

Cells
|December 18, 2019
PubMed

Insights

Novel thioester compounds show potent anti-glioblastoma activity, offering a new therapeutic avenue. These compounds exhibit strong cytotoxic and anti-angiogenic effects, challenging glioblastoma pathogenesis.

Area of Science:

  • Medicinal Chemistry
  • Oncology
  • Molecular Biology

Background:

  • Glioblastoma (GB) is a highly heterogeneous and chemoresistant grade IV glioma.
  • Multidimensional therapeutic strategies are required to effectively combat glioblastoma.
  • Thioesters have shown potential as antitumor agents.

Purpose of the Study:

  • To investigate novel thioester compounds as potent anti-glioblastoma agents.
  • To evaluate the cytotoxic, anti-angiogenic, and molecular mechanisms of action of these compounds against glioblastoma.

Main Methods:

  • Synthesis and bio-evaluation of 12 novel thioester compounds.
  • In vitro toxicity studies including cell viability, apoptosis, oxidative stress, and caspase activation assays.
  • RNA-sequencing analysis, docking, and immunoblotting to elucidate molecular targets and pathways.

Main Results:

  • Five novel thioester analogs demonstrated superior cytotoxic profiles compared to cisplatin.
  • The most effective compound showed IC50 values of 27 μM (U87) and 23 μM (LN229) against glioblastoma cells.
  • Significant downregulation of angiogenic pathways (MAPK, JAK-STAT, VEGF) and inhibition of tyrosine kinase cascades were observed.
  • Promotion of apoptotic genes and cell cycle arrest genes, with EGFR identified as a potential target.

Conclusions:

  • Orthothioesters represent a promising class of multi-dimensional chemotherapeutics against glioblastoma.
  • These compounds exhibit significant cytotoxic, anti-angiogenic, and chemo-sensitization activities.
  • Targeting glioblastoma pathogenesis through these novel agents warrants further investigation.
Keywords:
anti-angiogenesisglioblastomathioestertyrosine kinase inhibitor

More Related Videos

A Rapid Screening Workflow to Identify Potential Combination Therapy for GBM using Patient-Derived Glioma Stem Cells05:29

A Rapid Screening Workflow to Identify Potential Combination Therapy for GBM using Patient-Derived Glioma Stem Cells

Published on: March 28, 2021

3.1K
Generation of CAR T Cells for Adoptive Therapy in the Context of Glioblastoma Standard of Care12:55

Generation of CAR T Cells for Adoptive Therapy in the Context of Glioblastoma Standard of Care

Published on: February 16, 2015

22.0K

Related Concept Videos

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
8.6K
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
5.8K
PI3K/mTOR/AKT Signaling Pathway01:22

PI3K/mTOR/AKT Signaling Pathway

The mammalian target of rapamycin  (mTOR) is a serine/threonine kinase that regulates growth, proliferation, and cell survival in response to hormones, growth factors, or nutrient availability. This kinase exists in two structurally and functionally distinct forms: mTOR complex 1  (mTORC1) and mTOR complex 2  (mTORC2). The first form (mTORC1) is composed of a rapamycin-sensitive Raptor and proline-rich Akt substrate, PRAS40. In contrast,  mTORC2 consists of a...
5.2K
mTOR Signaling and Cancer Progression03:03

mTOR Signaling and Cancer Progression

The mammalian target of rapamycin or mTOR protein was discovered in 1994 due to its direct interaction with rapamycin. The protein gets its name from a yeast homolog called TOR. The mTOR protein complex in mammalian cells plays a major role in balancing anabolic processes such as the synthesis of proteins, lipids, and nucleotides and catabolic processes, such as autophagy in response to environmental cues, such as availability of nutrients and growth factors.
The mTOR pathway or the...
4.5K
Tumor Immunotherapy01:27

Tumor Immunotherapy

Immunotherapy is a treatment that boosts or manipulates the immune system to fight diseases, including cancer. For instance, by stimulating an immune response through vaccinations against viruses that cause cancers, like hepatitis B virus and human papillomavirus, these diseases can be prevented. Nonetheless, some cancer cells can avoid the immune system due to their rapid mutation and division. The immune response to many cancers involves three phases: elimination, equilibrium, and escape.
1.7K