Related Experiment Video

Updated: Jul 13, 2026

Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors
08:45

Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors

Published on: July 17, 2020

Inhibition of tumor metastasis by a growth factor receptor bound protein 2 Src homology 2 domain-binding antagonist

Alessio Giubellino1, Yang Gao, Sunmin Lee

  • 1Urologic Oncology Branch, Medical Oncology Branch, National Cancer Institute, Bethesda, Maryland 20892-1107, USA.

Cancer Research
|July 10, 2007
PubMed

Insights

A novel compound, C90, effectively inhibits cancer metastasis in aggressive tumor models by targeting Growth factor receptor binding protein 2 (Grb2). This discovery offers a promising strategy to reduce tumor spread and improve patient survival rates.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Development

Background:

  • Metastasis is the primary cause of cancer mortality.
  • Understanding the molecular mechanisms of metastasis is crucial for developing effective treatments.
  • Growth factor receptor binding protein 2 (Grb2) is implicated in cell growth, morphogenesis, and angiogenesis.

Purpose of the Study:

  • To investigate the role of Grb2 in cancer metastasis.
  • To evaluate the efficacy of C90, a Grb2 antagonist, in inhibiting metastasis in vivo.
  • To establish the potential of C90 as an anti-metastatic therapeutic.

Main Methods:

  • Utilized two aggressive tumor models to study metastasis in vivo.
  • Administered C90, a Grb2 antagonist, to assess its impact on metastatic spread.
  • Monitored primary tumor growth rate alongside metastatic progression.

Main Results:

  • C90 significantly inhibited metastasis in vivo in two aggressive tumor models.
  • C90 did not affect the growth rate of primary tumors.
  • Demonstrated a critical role for Grb2 Src homology-2 domain-mediated interactions in metastasis.

Conclusions:

  • C90 shows potential as a therapeutic agent to reduce metastatic spread.
  • Targeting Grb2-mediated interactions offers a promising strategy for cancer treatment.
  • Further research into Grb2 antagonists could lead to improved cancer survival rates.

Related Concept Videos

Mitogens and the Cell Cycle02:38

Mitogens and the Cell Cycle

Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
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 specific...
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...
Receptor Downregulation in MVBs01:15

Receptor Downregulation in MVBs

Multivesicular bodies (MVBs) are mature endosomes that sort ubiquitinated proteins and then fuse with lysosomes to degrade the sorted proteins. Epidermal growth factor (EGF) and its receptor (EGFR) form a complex that can be internalized through endocytosis, sorted into an MVB, and later degraded.
The EGFR can initiate signaling pathways that  lead to cell proliferation, migration, and differentiation. Overexpression of EGFR  stimulates cells to proliferate. Excessive  EGFR activation may...
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...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include: