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Updated: May 23, 2026

Characterizing Modulators of Protease-Activated Receptors with a Calcium Mobilization Assay Using a Plate Reader
Published on: May 24, 2024
Proteinase-activated receptors (PARs) and calcium signaling in cancer
Roland Kaufmann1, Morley D Hollenberg
1Experimental Transplantation Surgery, Department of General, Visceral and Vascular Surgery, Jena University Hospital, Erlanger Allee 101, D-07747, Jena, Germany. roland.kaufmann@med.uni-jena.de
Abstract:
Proteinase activated receptors (PARs), a small subfamily of G protein-coupled receptors with four members, PAR₁, PAR₂, PAR₃ and PAR₄, are expressed in various tumours from epithelial origin and can play an important role in tumour progression and metastasis. Within the complex intracellular PAR signaling networks triggered by PARs, an elevation in intracellular free calcium ion concentrations represents a key second messenger system. In this review, we summarize current information about the mechanisms whereby PARs can signal via intracellular calcium in the setting of cancer and we discuss possibilities for using the PAR-[Ca(2+)](i) signaling pathway as a target for the therapy of epithelial cancer.
Insights
Proteinase activated receptors (PARs) are involved in epithelial cancer progression. Targeting PAR signaling pathways, specifically calcium ion concentrations, offers potential therapeutic strategies for cancer treatment.
Area of Science:
- Oncology
- Cell Signaling
- G protein-coupled receptors
Background:
- Proteinase activated receptors (PARs) are a subfamily of G protein-coupled receptors.
- PARs are expressed in various epithelial cancers and influence tumor progression and metastasis.
- Intracellular calcium ion concentration is a critical second messenger in PAR signaling networks.
Purpose of the Study:
- To review the mechanisms of PAR signaling via intracellular calcium in cancer.
- To discuss the therapeutic potential of targeting the PAR-calcium signaling pathway in epithelial cancers.
Main Methods:
- Literature review of current research on PARs and calcium signaling in cancer.
- Analysis of signaling pathways involved in PAR activation and calcium mobilization.
- Discussion of potential therapeutic applications.
Main Results:
- PARs activate intracellular signaling cascades that lead to elevated intracellular calcium levels.
- This calcium signaling plays a role in tumor progression and metastasis.
- The PAR-calcium pathway is a promising target for novel cancer therapies.
Conclusions:
- PARs significantly contribute to epithelial cancer development and spread through calcium signaling.
- Targeting the PAR-calcium pathway presents a viable therapeutic strategy for epithelial cancers.
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