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EPR1  -  effector cell peptidase receptor 1 (non...

Homo sapiens

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Disease relevance of EPR1


High impact information on EPR1

  • Here we report that targeting a factor Xa receptor, designated effector cell protease receptor-1 (EPR-1), with antisense oligonucleotide or with a monoclonal antibody (mAB 2E1) inhibited CD3/T-cell receptor-dependent lymphocyte proliferation [4].
  • 125I-factor Xa binding was not affected by factor X, thrombin, or by DX9065, a direct inhibitor of factor Xa, but was inhibited by factor Xa (IC50 = 5.4+/-0.2 nM; n = 9) and by antibodies specific for the effector cell protease receptor 1 (EPR-1), a well-known receptor of factor Xa on various cell types [5].
  • When applied locally to air-injured rabbit carotid arteries, antibodies directed against EPR-1 (100 mug/ artery) strongly reduced myointimal proliferation 14 d after vascular injury (65-71% inhibition, P < 0.01) [5].
  • These findings indicate that SMCs express functional high affinity receptors for factor Xa related to EPR-1, which may be of importance in the regulation of homeostasis of the vascular wall and after vascular injury [5].
  • ECFC from patients with secondary (EP driven) polycythemia or anemia show two classes of EP-R (Kd = 0.18 and 1.10 nM, respectively) [6].

Biological context of EPR1

  • Splicing of the intervening sequence occurs in a cell type-specific fashion, as judged by the constitutive membrane overexpression of EPR-1 in certain leukemic B lymphocytes and monocytic cells [7].
  • One of the cellular binding sites for factor Xa, designated effector cell protease receptor-1 (EPR-1), has recently emerged as a novel potential regulator of factor Xa-mediated mitogenic signaling [8].
  • These findings suggest the existence of a potential EPR-1/survivin gene cluster and identify survivin as a new target for disrupting cell viability pathways in cancer [9].
  • Transient co-transfection of an EPR-1 cDNA potentially acting as a Survivin antisense with a lacZ reporter plasmid resulted in loss of viability of HeLa cells [9].
  • Weighted EPR-1 Score is positively correlated with apoptosis index, but is negatively related with proliferative index [2].

Anatomical context of EPR1

  • Monoclonal antibodies were generated against EPR-1+ MOLT13 lymphocytes and selected for reactivity with lymphocyte surface proteins by flow cytometry and with affinity-purified EPR-1 in Western blots [10].
  • Binding of the coagulation protease factor Xa to leukocytes is contributed by a recently identified molecule, denominated Effector cell Protease Receptor-1 (EPR-1) [10].
  • Furthermore, phenotypic analysis of cell lines stably transfected with functionally spliced or unspliced EPR-1 constructs suggests a potential role of intron cis-acting sequence(s) in splicing regulation [7].
  • In stably transfected HeLa cells, ZnSO4 induction of an EPR-1 mRNA under the control of a metallothionein promoter suppressed the expression of endogenous survivin [9].
  • In Northern blots, a single strand-specific probe identified a 1.3-kb EPR-1 mRNA broadly distributed in normal adult and fetal tissues, structurally distinct from the 1.9-kb Survivin transcript expressed in transformed cell lines [9].

Associations of EPR1 with chemical compounds

  • Effector cell protease receptor-1 (EPR-1) is a transmembrane glycoprotein receptor for factor Xa that contributes to cell surface assembly of proteolytic activities and leukocyte mitogenesis [7].
  • This strategy identified a monoclonal antibody (MAb) (EPR1) that blocks binding of titanium dioxide (TiO(2)) particles to the EC line which served as the immunogen (A549), as well as to other EC lines (Beas 2-B, HTB54, HeLa, and MDA-MB-435S) [11].
  • 125I-Labeled Factor Xa bound to endothelial cells in a dose-dependent saturable manner, and the binding was inhibited by antibody to EPR-1 [12].
  • Effector cell protease receptor (EPR-1) was identified as a novel leukocyte cell surface receptor recognizing the coagulation serine protease Factor Xa but not the precursor Factor X [12].
  • Factor Xa or catalytically inactive 5-dimethylaminonaphthalene-1sulfonyl (dansyl) Glu-Gly-Arg-(DEGR)-chloromethylketone-factor Xa bound indistinguishably to HUVEC and EPR-1 transfectants, and inhibited equally well the binding of 125I-factor Xa to these cells [13].

Regulatory relationships of EPR1

  • [125I]-factor Xa binding was inhibited by factor Xa but was not affected by factor X, thrombin or monoclonal antibodies against factor V, antithrombin-III or tissue factor pathway inhibitor (TFPI) but was inhibited by an antibody specific for the effector cell protease receptor-1 (EPR-1), a well-known receptor of factor Xa on various cell types [14].
  • These results suggest that EP receptor subtypes regulate acid extrusion mainly via NHE-1 through distinct signal transduction pathways in CHO cells [15].

Other interactions of EPR1

  • On the other hand, the average positive labeling index for Ki-67 (ki-67) in EPR-1-positive lymph node metastasis was 7.65%, which was significantly lower than that of 9.44% observed in EPR-1-negative lymph node metastasis [2].
  • To clarify the involvement of E-prostanoid (EP) receptors in the effect of prostaglandin E(2) on human monocyte-derived dendritic cell (MoDC) maturation, we examined the effect of four types of EP receptor-selective agonists on MoDC maturation [16].
  • These results may suggest that EP4 receptor plays an important role among four EP receptor subtypes for relaxation of smooth muscle in the human corpus cavernosum.International Journal of Impotence Research (2006) 18, 275-281. doi:10.1038/sj.ijir.3901408; published online 20 October 2005 [17].
  • Cyclooxygenase-2 (COX-2)-generated Prostaglandin-E(2) (PGE(2)), which signals through the PGE(2) receptor (EP receptor), as well as nitric oxide metabolites (NOx), appear to be important in postoperative immune dysfunction [18].
  • In addition to the 62-kDa effector cell protease receptor 1, mAb 2E1 bound the 32-kDa T cell adhesion receptor E2 (CD99) and the 86-kDa p80 subunit of the nuclear antigen complex Ku [19].

Analytical, diagnostic and therapeutic context of EPR1


  1. Downregulation of survivin expression by induction of the effector cell protease receptor-1 reduces tumor growth potential and results in an increased sensitivity to anticancer agents in human colon cancer. Yamamoto, T., Manome, Y., Nakamura, M., Tanigawa, N. Eur. J. Cancer (2002) [Pubmed]
  2. Significance of effector protease receptor-1 expression and its relationship with proliferation and apoptotic index in patients with primary advanced gastric adenocarcinoma. Yao, X.Q., Liu, F.K., Li, J.S., Qi, X.P., Wu, B., Yin, H.L., Ma, H.H., Shi, Q.L., Zhou, X.J. World J. Gastroenterol. (2004) [Pubmed]
  3. Protease receptors in Hodgkin's disease: expression of the factor Xa receptor, effector cell protease receptor-1, in Reed-Sternberg cells. Adida, C., Ambrosini, G., Plescia, J., Crotty, P.L., Costa, J., Altieri, D.C. Blood (1996) [Pubmed]
  4. In vivo immunosuppression by targeting a novel protease receptor. Duchosal, M.A., Rothermel, A.L., McConahey, P.J., Dixon, F.J., Altieri, D.C. Nature (1996) [Pubmed]
  5. Effector protease receptor 1 mediates the mitogenic activity of factor Xa for vascular smooth muscle cells in vitro and in vivo. Herbert, J., Bono, F., Herault, J., Avril, C., Dol, F., Mares, A., Schaeffer, P. J. Clin. Invest. (1998) [Pubmed]
  6. Erythropoietin receptors in polycythemia vera. Means, R.T., Krantz, S.B., Sawyer, S.T., Gilbert, H.S. J. Clin. Invest. (1989) [Pubmed]
  7. Splicing of effector cell protease receptor-1 mRNA is modulated by an unusual retained intron. Altieri, D.C. Biochemistry (1994) [Pubmed]
  8. Xa receptor EPR-1. Altieri, D.C. FASEB J. (1995) [Pubmed]
  9. Induction of apoptosis and inhibition of cell proliferation by survivin gene targeting. Ambrosini, G., Adida, C., Sirugo, G., Altieri, D.C. J. Biol. Chem. (1998) [Pubmed]
  10. Molecular cloning of effector cell protease receptor-1, a novel cell surface receptor for the protease factor Xa. Altieri, D.C. J. Biol. Chem. (1994) [Pubmed]
  11. Generation of a monoclonal antibody that blocks epithelial binding of unopsonized particles. Tao, F., Palecanda, A., Kumar, S., Kobzik, L. Hybrid. Hybridomics (2003) [Pubmed]
  12. Effector cell protease receptor-1 is a vascular receptor for coagulation factor Xa. Nicholson, A.C., Nachman, R.L., Altieri, D.C., Summers, B.D., Ruf, W., Edgington, T.S., Hajjar, D.P. J. Biol. Chem. (1996) [Pubmed]
  13. Activation-dependent exposure of the inter-EGF sequence Leu83-Leu88 in factor Xa mediates ligand binding to effector cell protease receptor-1. Ambrosini, G., Plescia, J., Chu, K.C., High, K.A., Altieri, D.C. J. Biol. Chem. (1997) [Pubmed]
  14. Human umbilical vein endothelial cells express high affinity receptors for factor Xa. Bono, F., Herault, J.P., Avril, C., Schaeffer, P., Lormeau, J.C., Herbert, J.M. J. Cell. Physiol. (1997) [Pubmed]
  15. Characteristics of acid extrusion from Chinese hamster ovary cells expressing different prostaglandin EP receptors. Okada, Y., Taniguchi, T., Morishima, S., Suzuki, F., Akagi, Y., Muramatsu, I. Life Sci. (2006) [Pubmed]
  16. E-prostanoid (EP)2/EP4 receptor-dependent maturation of human monocyte-derived dendritic cells and induction of helper T2 polarization. Kubo, S., Takahashi, H.K., Takei, M., Iwagaki, H., Yoshino, T., Tanaka, N., Mori, S., Nishibori, M. J. Pharmacol. Exp. Ther. (2004) [Pubmed]
  17. Gene and protein expression profiles of prostaglandin E2 receptor subtypes in the human corpus cavernosum. Komuro, M., Kamiyama, M., Furuya, Y., Takihana, Y., Araki, I., Takeda, M. Int. J. Impot. Res. (2006) [Pubmed]
  18. Altered cyclooxygenase-2 expression and nitric oxide metabolism following major elective surgery. Maddali, S., Stapleton, P.P., Freeman, T.A., Yan, Z., Duff, M., Smyth, G.P., Daly, J.M. J. Surg. Res. (2004) [Pubmed]
  19. High affinity cross-reacting mAb generated by minimal mimicry: implications for the pathogenesis of anti-nuclear autoantibodies and immunosuppression. Rothermel, A.L., Altieri, D.C. Proc. Natl. Acad. Sci. U.S.A. (1998) [Pubmed]
  20. Molecular dissection of effector cell protease receptor-1 recognition of factor Xa. Assignment of critical residues involved in antibody reactivity and ligand binding. Ambrosini, G., Altieri, D.C. J. Biol. Chem. (1996) [Pubmed]
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