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There are three known thrombin receptors (ThrR), termed PAR1, PAR3 and PAR4 (PAR for protease-activated receptor). G-protein-coupled receptors that are responsible for the coagulation effects and responses of thrombin on cells are known as protease-activated receptors, or PARs. These receptors are members of the 7-transmembrane g protein-coupled family of receptors, however, their method of activation is unique. Unlike most G-protein-coupled receptors, PARs are irreversibly activated by proteolytic mechanism and therefore, are strictly regulated.

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  • There are three known thrombin receptors (ThrR), termed PAR1, PAR3 and PAR4 (PAR for protease-activated receptor). G-protein-coupled receptors that are responsible for the coagulation effects and responses of thrombin on cells are known as protease-activated receptors, or PARs. These receptors are members of the 7-transmembrane g protein-coupled family of receptors, however, their method of activation is unique. Unlike most G-protein-coupled receptors, PARs are irreversibly activated by proteolytic mechanism and therefore, are strictly regulated. Thrombin is an allosteric serine protease that is an essential effector of coagulation that is produced at sites of vascular injury and plays a critical role in cellular response to blood-related diseases. It binds to and cleaves the extracellular N-terminal domain of the receptor. A tethered ligand corresponding to the new N-terminus, SFLLRN, is then unmasked, binding to the second extracellular loop of the receptor and activating it. (en)
  • トロンビン受容体(トロンビンじゅようたい、英: thrombin receptor、略称: ThrR)は3種類が知られており、PAR1、PAR3、PAR4と命名されている(PARはプロテアーゼ活性化受容体(protease-activated receptor)を意味する)。 これらの受容体はGタンパク質共役7回膜貫通受容体ファミリーのメンバーであるが、これらの活性化方法は独特である。セリンプロテアーゼであるトロンビンは、受容体の細胞外のN末端ドメインに結合して切断を行う。その結果、新たに形成されたN末端のSFLLRNが露出し、これがテザードリガンド(係留リガンド)として受容体の2番目の細胞外ループに結合して活性化を行う。 (ja)
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  • トロンビン受容体(トロンビンじゅようたい、英: thrombin receptor、略称: ThrR)は3種類が知られており、PAR1、PAR3、PAR4と命名されている(PARはプロテアーゼ活性化受容体(protease-activated receptor)を意味する)。 これらの受容体はGタンパク質共役7回膜貫通受容体ファミリーのメンバーであるが、これらの活性化方法は独特である。セリンプロテアーゼであるトロンビンは、受容体の細胞外のN末端ドメインに結合して切断を行う。その結果、新たに形成されたN末端のSFLLRNが露出し、これがテザードリガンド(係留リガンド)として受容体の2番目の細胞外ループに結合して活性化を行う。 (ja)
  • There are three known thrombin receptors (ThrR), termed PAR1, PAR3 and PAR4 (PAR for protease-activated receptor). G-protein-coupled receptors that are responsible for the coagulation effects and responses of thrombin on cells are known as protease-activated receptors, or PARs. These receptors are members of the 7-transmembrane g protein-coupled family of receptors, however, their method of activation is unique. Unlike most G-protein-coupled receptors, PARs are irreversibly activated by proteolytic mechanism and therefore, are strictly regulated. (en)
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  • トロンビン受容体 (ja)
  • Thrombin receptor (en)
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