Physiology and pathophysiology of proteinase-activated receptors (PARs): Regulation of the expression of PARs

Katsuya Hirano, Tatsuya Yufu, Mayumi Hirano, Junji Nishimura, Hideo Kanaide

    Research output: Contribution to journalShort survey

    16 Citations (Scopus)

    Abstract

    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 up-regulated 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.

    Original languageEnglish
    Pages (from-to)31-37
    Number of pages7
    JournalJournal of Pharmacological Sciences
    Volume97
    Issue number1
    DOIs
    Publication statusPublished - Jan 1 2005

      Fingerprint

    All Science Journal Classification (ASJC) codes

    • Molecular Medicine
    • Pharmacology

    Cite this