Protease-Activated Receptor F2R Is a Potential Target for New Diagnostic/Prognostic and Treatment Applications for

Riya Khetan1, Noor A Lokman2, Preethi Eldi3

  • 1Centre of Pharmaceutical Innovation, UniSA Clinical and Health Sciences, University of South Australia, Adelaide, SA 5000, Australia.

Insights

Coagulation factor II receptor (F2R) is elevated in ovarian cancers, correlating with metastasis and resistance to chemotherapy. Targeting F2R may offer new theranostic strategies for advanced ovarian cancer.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • Ovarian cancer treatment faces challenges due to late detection and chemotherapy resistance.
  • Novel molecular targets are crucial for developing advanced theranostic approaches.

Purpose of the Study:

  • To investigate the coagulation factor II receptor/protease-activated receptor 1 (F2R/PAR1) as a diagnostic/prognostic biomarker and therapeutic target in ovarian cancer.

Main Methods:

  • Analysis of public RNA sequence and DNA microarray data for F2R gene expression.
  • Confirmation of F2R protein expression using flow cytometry, immunofluorescence, and immunohistochemistry (IHC).
  • Functional assays to assess the impact of F2R suppression on ovarian cancer cell behavior and drug sensitivity.

Main Results:

  • Elevated F2R mRNA and protein expression were observed in ovarian cancers, particularly in metastatic and chemotherapy-resistant cases.
  • High F2R protein levels were associated with reduced progression-free survival.
  • Suppression of F2R decreased tumor cell motility, invasion, spheroid formation, and metabolism, while increasing carboplatin sensitivity.

Conclusions:

  • F2R represents a promising diagnostic/prognostic biomarker and therapeutic target for ovarian cancer.
  • Targeting F2R could lead to novel theranostic strategies for chemotherapy-resistant and metastatic ovarian cancer.
  • Further research into F2R-targeting therapies, such as antibody-drug conjugates, is warranted.

Related Concept Videos

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:
3.9K
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...
4.6K
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...
7.7K
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