Physiology and Pathophysiology of Proteinase-Activated Receptors (PARs): Regulation of the Expression of PARs
The level of receptors expressed on the cell surface determines the cellular responsiveness to agonists. Proteinase-activated receptors (PARs) have been reported to be either upregulated or down-regulated in response to various types of stimulation and pathological situations. In addition, the trans...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Elsevier
2005-01-01
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| Series: | Journal of Pharmacological Sciences |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S134786131932290X |
| _version_ | 1818417490864111616 |
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| author | Katsuya Hirano Tatsuya Yufu Mayumi Hirano Junji Nishimura Hideo Kanaide |
| author_facet | Katsuya Hirano Tatsuya Yufu Mayumi Hirano Junji Nishimura Hideo Kanaide |
| author_sort | Katsuya Hirano |
| collection | DOAJ |
| description | The level of receptors expressed on the cell surface determines the cellular responsiveness to agonists. Proteinase-activated receptors (PARs) have been reported to be either upregulated or down-regulated in response to various types of stimulation and pathological situations. In addition, the transcriptional regulation plays a major role in the alteration of the expression of PARs under pathological conditions, while post-translational mechanisms such as phosphorylation, arresting-binding, internalization, and lysosomal degradation, which desensitize activated PARs and terminate intracellular signaling, also play an important role in regulating the expression of PARs and the cellular responsiveness to the agonists. Elucidating the mechanisms related to the expression of PARs is a critical step to understand the pathophysiology of various diseases and establish new therapeutic strategies. However, the molecular mechanism regulating the expression of PARs still remains to be elucidated. This minireview discusses our current understanding of the mechanisms regulating the expression of PARs. The transcription factors and the regulatory elements in the promoter regions, and the proteins that interact with the receptors and thereby regulate their trafficking and desensitization are the main problems that need to be elucidated. Keywords:: expression, transcription, trafficking, proteinase-activated receptor |
| first_indexed | 2024-12-14T12:07:37Z |
| format | Article |
| id | doaj.art-1ceff26db7944a808359989e877cd54e |
| institution | Directory Open Access Journal |
| issn | 1347-8613 |
| language | English |
| last_indexed | 2024-12-14T12:07:37Z |
| publishDate | 2005-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Journal of Pharmacological Sciences |
| spelling | doaj.art-1ceff26db7944a808359989e877cd54e2022-12-21T23:01:50ZengElsevierJournal of Pharmacological Sciences1347-86132005-01-019713137Physiology and Pathophysiology of Proteinase-Activated Receptors (PARs): Regulation of the Expression of PARsKatsuya Hirano0Tatsuya Yufu1Mayumi Hirano2Junji Nishimura3Hideo Kanaide4Division of Molecular Cardiology, Research Institute of Angiocardiology, Graduate School of Medical Sciences, Kyushu University andDivision of Molecular Cardiology, Research Institute of Angiocardiology, Graduate School of Medical Sciences, Kyushu University andDivision of Molecular Cardiology, Research Institute of Angiocardiology, Graduate School of Medical Sciences, Kyushu University andDivision of Molecular Cardiology, Research Institute of Angiocardiology, Graduate School of Medical Sciences, Kyushu University andDivision of Molecular Cardiology, Research Institute of Angiocardiology, Graduate School of Medical Sciences, Kyushu University and; Kyushu University COE Program on Lifestyle-Related Diseases, 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, Japan; Corresponding author (affiliation #1). FAX: +81-92-642-5552 E-mail: kanaide@molcar.med.kyushu-u.ac.jpThe level of receptors expressed on the cell surface determines the cellular responsiveness to agonists. Proteinase-activated receptors (PARs) have been reported to be either upregulated or down-regulated in response to various types of stimulation and pathological situations. In addition, the transcriptional regulation plays a major role in the alteration of the expression of PARs under pathological conditions, while post-translational mechanisms such as phosphorylation, arresting-binding, internalization, and lysosomal degradation, which desensitize activated PARs and terminate intracellular signaling, also play an important role in regulating the expression of PARs and the cellular responsiveness to the agonists. Elucidating the mechanisms related to the expression of PARs is a critical step to understand the pathophysiology of various diseases and establish new therapeutic strategies. However, the molecular mechanism regulating the expression of PARs still remains to be elucidated. This minireview discusses our current understanding of the mechanisms regulating the expression of PARs. The transcription factors and the regulatory elements in the promoter regions, and the proteins that interact with the receptors and thereby regulate their trafficking and desensitization are the main problems that need to be elucidated. Keywords:: expression, transcription, trafficking, proteinase-activated receptorhttp://www.sciencedirect.com/science/article/pii/S134786131932290X |
| spellingShingle | Katsuya Hirano Tatsuya Yufu Mayumi Hirano Junji Nishimura Hideo Kanaide Physiology and Pathophysiology of Proteinase-Activated Receptors (PARs): Regulation of the Expression of PARs Journal of Pharmacological Sciences |
| title | Physiology and Pathophysiology of Proteinase-Activated Receptors (PARs): Regulation of the Expression of PARs |
| title_full | Physiology and Pathophysiology of Proteinase-Activated Receptors (PARs): Regulation of the Expression of PARs |
| title_fullStr | Physiology and Pathophysiology of Proteinase-Activated Receptors (PARs): Regulation of the Expression of PARs |
| title_full_unstemmed | Physiology and Pathophysiology of Proteinase-Activated Receptors (PARs): Regulation of the Expression of PARs |
| title_short | Physiology and Pathophysiology of Proteinase-Activated Receptors (PARs): Regulation of the Expression of PARs |
| title_sort | physiology and pathophysiology of proteinase activated receptors pars regulation of the expression of pars |
| url | http://www.sciencedirect.com/science/article/pii/S134786131932290X |
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