Biased signaling: potential agonist and antagonist of PAR2

References

• Alonso, N., Monczor, F., Echeverría, E., Davio, C., Shayo, C., & Fernández, N. (2014). Signal transduction mechanism of biased ligands at histamine H2 receptors. Biochemical Journal, 459, 117–126.10.1042/BJ20131226
   PubMed Web of Science ®Google Scholar
• Bachelerie, F., Ben-Baruch, A., Combadiere, C., Farber, J. M., Graham, G. J., Horuk, R., … Zlotnik, A. (2014). Chemokine receptors, introduction. Retrieved October 31, from IUPHAR/BPS Guide to PHARMACOLOGY. http://www.guidetopharmacology.org/GRAC/FamilyIntroductionForward?familyId
   Google Scholar
• Bäck, M., Shimizu, T., Yokomizo, T., Rovati, G. E., Serhan, C. N., Dahlén, S. E., … Powell, W. (2013). Leukotriene receptors, introduction. Retrieved October 8, 2013, from http://www.iuphar-db.org/DATABASE/FamilyIntroductionForward?familyId=35
   Google Scholar
• Barrington, W. W., Jacobson, K. A., & Stiles, G. L. (1989). Demonstration of distinct agonist and antagonist conformations of the A1 adenosine receptor. Journal of Biological Chemistry, 264, 13157–13164.
   PubMed Web of Science ®Google Scholar
• Berger, A. (2000). PAR2 antagonists – The next generation of anti-inflammatories? British Medical Journal, 320, 334.10.1136/bmj.320.7231.334
   PubMed Web of Science ®Google Scholar
• Capra, V., Ravasi, S., Accomazzo, M. R., Citro, S., Grimoldi, M., Abbracchio, M. P., & Rovati, G. E. (2005). CysLT1 receptor is a target for extracellular nucleotide-induced heterologous desensitization: A possible feedback mechanism in inflammation. Journal of Cell Science, 118, 5625–5636.10.1242/jcs.02668
   PubMed Web of Science ®Google Scholar
• Cavasotto, C. N., Orry, A. J. W., Murgolo, N. J., Czarniecki, M. F., Kocsi, S. A., Hawes, B. E., … Monsma, F. J. (2008). Discovery of novel antagonist chemotypes to a G-protein coupled receptor through ligand-steered homology modeling and structure-based virtual screening. Journal of Medicinal Chemistry, 51, 581–588.10.1021/jm070759m
   PubMed Web of Science ®Google Scholar
• Charfi, I., Audet, N., Bagheri Tudashki, H., & Pineyro, G. (2015). Identifying ligand-specific signalling within biased responses: Focus on δ opioid receptor ligands. British Journal of Pharmacology, 172, 435–448.10.1111/bph.2015.172.issue-2
   PubMed Web of Science ®Google Scholar
• Chen, V. B., Arendall, W. B., Headd, J. J., Keedy, D. A., Immormino, R. M., Kapral, G. J., … Richardson, D. C. (2010). MolProbity: All-atom structure validation for macromolecular crystallography. Acta Crystallographica, D66, 12–21.
   Web of Science ®Google Scholar
• Ciana, P., Fumagalli, M., Trincavelli, M. L., Verderio, C., Rosa, P., Lecca, D., … Abbracchio, M. P. (2006). The orphan receptor GPR17 identified as a new dual uracil nucleotides/cysteinyl-leukotrienes receptor. The EMBO Journal, 25, 4615–4627.10.1038/sj.emboj.7601341
   PubMed Web of Science ®Google Scholar
• Diaz, P., Phatak, S., Xu, J., Diaz, F.-A., Cavasotto, C. N., & Naguib, M. (2009a). 6-methoxy-n-alkyl isatin acylhydrazone derivatives as a novel series of potent selective cannabinoid receptor 2 inverse agonists: Design, synthesis, and binding mode prediction. Journal of Medicinal Chemistry, 52, 433–444.
   PubMed Web of Science ®Google Scholar
• Diaz, P., Phatak, S. S., Xu, J., Fronczek, F., Astruc-Diaz, F., Thompson, C., … Naguib, M. (2009b). 2,3-dihydro-1-benzofuran derivatives as a novel series of potent selective cannabinoid receptor 2 agonists: Design, synthesis, and binding mode prediction through ligand-steered modeling. ChemMedChem, 4, 1615–1629.
   PubMed Web of Science ®Google Scholar
• Deupi, X., & Kobilka, B. K. (2010). Energy landscapes as a tool to integrate GPCR structure, dynamics, and function. Physiology (Bethesda), 25, 293–303.10.1152/physiol.00002.2010
   PubMed Web of Science ®Google Scholar
• Eswar, N., Eramian, D., Webb, B., Shen, M. Y., & Sali, A. (2008). Protein structure modeling with MODELLER. Methods in Molecular Biology, 426, 145–159.10.1007/978-1-60327-058-8
   PubMedGoogle Scholar
• Fernandes, L., Fortes, Z. B., Nigro, D., Tostes, R. C., Santos, R. A., & Catelli De Carvalho, M. H. (2001). Potentiation of bradykinin by angiotensin-(1-7) on arterioles of spontaneously hypertensive rats studied in vivo. Hypertension, 37, 703–709.10.1161/01.HYP.37.2.703
   PubMed Web of Science ®Google Scholar
• Friesner, R. A., Banks, J. L., Murphy, R. B., Halgren, T. A., Klicic, J. J., Mainz, D. T., … Shenkin, P. S. (2004). Glide: A new approach for rapid, accurate docking and scoring. Method and assessment of docking accuracy. Journal of Medicinal Chemistry, 47, 1739–1749.10.1021/jm0306430
   PubMed Web of Science ®Google Scholar
• Friesner, R. A., Murphy, R. B., Repasky, M. P., Frye, L. L., Greenwood, J. R., Halgren, T. A., … Mainz, D. T. (2006). Extra precision glide: Docking and scoring incorporating a model of hydrophobic enclosure for protein-ligand complexes. Journal of Medicinal Chemistry, 49, 6177–6196.10.1021/jm051256o
   PubMed Web of Science ®Google Scholar
• Garza, L. A., Liu, Y., Yang, Z. Z., Alagesan, B., Lawson, J. A., Norberg, S. M., … Cotsarelis, G. (2012). Prostaglandin D2 inhibits hair growth and is elevated in bald scalp of men with androgenetic alopecia. Science Translational Medicine, 4, 126ra34. doi:10.1126/scitranslmed.3003122
   PubMed Web of Science ®Google Scholar
• Gatica, E. A., & Cavasotto, C. N. (2012). Ligand and decoy sets for docking to G protein-coupled receptors. Journal of Chemical Information and Modeling, 52(1), 1–6.10.1021/ci200412p
   PubMed Web of Science ®Google Scholar
• Hassan, I., & Haji, M. L. (2014). Understanding itch: An update on mediators and mechanisms of pruritus. Indian Journal of Dermatology, Venereology and Leprology, 80, 106–114.10.4103/0378-6323.129377
   PubMed Web of Science ®Google Scholar
• Hollenberg, M. D., & Compton, S. J. (2002). International Union of Pharmacology. XXVIII. Proteinase-activated receptors. Pharmacological Reviews, 54, 203–217.
   PubMed Web of Science ®Google Scholar
• Hollenberg, M. D., Mihara, K., Polley, D., Suen, J. Y., Han, A., Fairlie, D. P., & Ramachandran, R. (2014). Biased signalling and proteinase-activated receptors (PARs): Targeting inflammatory disease. British Journal of Pharmacology, 171, 1180–1194.10.1111/bph.12544
   PubMed Web of Science ®Google Scholar
• Holst, B., Mokrosinski, J., Lang, M., Brandt, E., Nygaard, R., Frimurer, T. M., … Schwartz, T. W., (2007). Identification of an efficacy switch region in the ghrelin receptor responsible for interchange between agonism and inverse agonism. Journal of Biological Chemistry, 282, 15799–15811.10.1074/jbc.M609796200
   PubMed Web of Science ®Google Scholar
• Jaakola, V. P., Griffith, M. T., Hanson, M. A., Cherezov, V., Chien, E. Y., Lane, J. R., … Stevens, R. C. (2008). The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist. Science, 322, 1211–1217.10.1126/science.1164772
   PubMed Web of Science ®Google Scholar
• Kahsai, A. W., Xiao, K., Rajagopal, S., Ahn, S., Shukla, A. K., Sun, J., … Lefkowitz, R. J. (2011). Multiple ligand-specific conformations of the β2-adrenergic receptor. Nature Chemical Biology, 7, 692–700. doi:10.1038/nchembio.634
   PubMed Web of Science ®Google Scholar
• Kakarala, K. K., Jamil, K., & Devaraji, V. (2014). Structure and putative signaling mechanism of protease activated receptor 2 (PAR2) – A promising target for breast cancer. Journal of Molecular Graphics and Modelling, 53, 179–199.10.1016/j.jmgm.2014.07.012
   PubMed Web of Science ®Google Scholar
• Kenakin, T. (2002). Efficacy at G-protein-coupled receptors. Nature Reviews Drug Discovery, 1, 103–110.10.1038/nrd722
   PubMed Web of Science ®Google Scholar
• Kenakin, T. (2011). Functional selectivity and biased receptor signaling. Journal of Pharmacology and Experimental Therapeutics, 336, 296–302.10.1124/jpet.110.173948
   PubMed Web of Science ®Google Scholar
• Kenakin, T. K. (2012). Biased signalling and allosteric machines: New vistas and challenges for drug discovery. British Journal of Pharmacology, 165, 1659–1669.10.1111/j.1476-5381.2011.01749.x
   PubMed Web of Science ®Google Scholar
• Kuntal, B. K., Aparoy, P., & Reddanna, P. (2010). EasyModeller: A graphical interface to MODELLER. BMC Research Notes, 3, 226. doi:10.1186/1756-0500-3-22610.1186/1756-0500-3-226
   PubMedGoogle Scholar
• Laskowski, R. A., MacArthur, M. W., Moss, D. S., & Thornton, J. M. (2005). PROCHECK: A program to check the stereo chemical quality of protein structures. Journal of Applied Crystallography, 26, 283–291.
   Web of Science ®Google Scholar
• Li, Z., Zhang, X. J., Xu, H. X., Sung, J. J., & Bian, Z. X. (2009). Intracolonical administration of protease-activated receptor-2 agonists produced visceral hyperalgesia by up-regulating serotonin in the colon of rats. European Journal of Pharmacology, 606, 199–204.10.1016/j.ejphar.2009.01.031
   PubMed Web of Science ®Google Scholar
• Liu, Y., & Mueller, B. M. (2006). Protease-activated receptor-2 regulates vascular endothelial growth factor expression in MDA-MB-231 cells via MAPK pathways. Biochemical and Biophysical Research Communications, 344, 1263–1270. Epub 2006 Apr 19.10.1016/j.bbrc.2006.04.005
   PubMed Web of Science ®Google Scholar
• Macfarlane, S. R., Seatter, M. J., Kanke, T., Hunter, G. D., & Plevin, R. (2001). Proteinase-activated receptors. Pharmacological Reviews, 53, 245–282.
   PubMed Web of Science ®Google Scholar
• Magnusson, C., Liu, J., Ehrnström, R., Manjer, J., Jirström, K., Andersson, T., & Sjölander, A. (2011). Cysteinyl leukotriene receptor expression pattern affects migration of breast cancer cells and survival of breast cancer patients. International Journal of Cancer, 129, 9–22.10.1002/ijc.v129.1
   PubMed Web of Science ®Google Scholar
• Matej, R., Mandakova, P., Netikova, I., Pouckova, P., & Olejar, T. (2007). Proteinase-activated receptor-2 expression in breast cancer and the role of trypsin on growth and metabolism of breast cancer cell line MDAMB-231. Physiological Research, 56, 475–484.
   PubMed Web of Science ®Google Scholar
• Maudsley, S., Patel, S. A., Park, S. S., Luttrell, L. M., & Martin, B. (2012). Functional signaling biases in G protein-coupled receptors: Game theory and receptor dynamics. Mini-reviews in Medicinal Chemistry, 12, 831–840.10.2174/138955712800959071
   PubMed Web of Science ®Google Scholar
• Morris, D. R., Ding, Y., Ricks, T. K., Gullapalli, A., Wolfe, B. L., & Trejo, J. (2006). Protease-activated receptor-2 is essential for factor VIIa and Xa-induced signaling, migration, and invasion of breast cancer cells. Cancer Research, 66, 307–314.10.1158/0008-5472.CAN-05-1735
   PubMed Web of Science ®Google Scholar
• Nonaka, Y., Hiramoto, T., & Fujita, N. (2005). Identification of endogenous surrogate ligands for human P2Y12 receptors by in silico and in vitro methods. Biochemical and Biophysical Research Communications, 337, 281–288.10.1016/j.bbrc.2005.09.052
   PubMed Web of Science ®Google Scholar
• Nystedt, S., Emilsson, K., Wahlestedt, C., & Sundelin, J. (1994). Molecular cloning of a potential proteinase activated receptor. Proceedings of the National Academy of Sciences, 91, 9208–9212.10.1073/pnas.91.20.9208
   PubMed Web of Science ®Google Scholar
• Orry, A. J. W., Abagyan, R., & Cavasotto, C. N. (2006). Structure-based development of target-specific compound libraries. Drug Discovery Today, 11, 261–266.10.1016/S1359-6446(05)03717-7
   PubMed Web of Science ®Google Scholar
• Perez, D. M., & Karnik, S. S. (2005). Multiple signaling states of G-protein-coupled receptors. Pharmacological Reviews, 57, 147–161.10.1124/pr.57.2.2
   PubMed Web of Science ®Google Scholar
• Phatak, S. S., Gatica, E. A., & Cavasotto, C. N. (2010). Ligand-steered modeling and docking: A benchmarking study in class A G-protein-coupled receptors. Journal of Chemical Information and Modeling, 50, 2119–2128.10.1021/ci100285f
   PubMed Web of Science ®Google Scholar
• Phatak, S. S., Stephan, C. C., & Cavasotto, C. N. (2009). High-throughput and in silico screenings in drug discovery. Expert Opinion on Drug Discovery, 4, 947–959.10.1517/17460440903190961
   PubMed Web of Science ®Google Scholar
• Preininger, A. M., Meiler, J., & Hamm, H. E. (2013). Conformational flexibility and structural dynamics in GPCR-mediated G protein activation: A perspective. Journal of Molecular Biology, 425, 2288–2298.10.1016/j.jmb.2013.04.011
   PubMed Web of Science ®Google Scholar
• Ramachandran, R., & Hollenberg, M. D. (2008). Proteinases and signalling: Pathophysio-logical and therapeutic implications via PARs and more. British Journal of Pharmacology, 153, S263–S282.
   Web of Science ®Google Scholar
• Rasmussen, U. B., Gachet, C., Schlesinger, Y., Hanau, D., Ohlmann, P., Van Obberghen-Schilling, E., … Pavirani, A. (1993). A peptide ligand of the human thrombin receptor antagonizes alpha-thrombin and partially activates platelets. Journal of Biological Chemistry, 268, 14322–14328.
   PubMed Web of Science ®Google Scholar
• Raval, A., Piana, S., Eastwood, M. P., Dror, R. O., & Shaw, D. E. (2012). Refinement of protein structure homology models via long, all-atom molecular dynamics simulations. Proteins, 80, 2071–2079.
   PubMed Web of Science ®Google Scholar
• Reiner, S., Ambrosio, M., Hoffmann, C., & Lohse, M. J. (2010). Differential signaling of the endogenous agonists at the 2-adrenergic receptor. Journal of Biological Chemistry, 285, 36188–36198.10.1074/jbc.M110.175604
   PubMed Web of Science ®Google Scholar
• Sastry, M., Lowrie, J. F., Dixon, S. L., & Sherman, W. (2010). Large-scale systematic analysis of 2D fingerprint methods and parameters to improve virtual screening enrichments. Journal of Chemical Information and Modeling, 50, 771–784.10.1021/ci100062n
   PubMed Web of Science ®Google Scholar
• Staus, D. P., Wingler, L. M., Strachan, R. T., Rasmussen, S. G., Pardon, E., Ahn, S., … Lefkowitz, R. J. (2014). Regulation of β2-adrenergic receptor function by conformationally selective single-domain intrabodies. Molecular Pharmacology, 85, 472–481.10.1124/mol.113.089516
   PubMed Web of Science ®Google Scholar
• Storey, R. F., Judge, H. M., Wilcox, R. G., & Heptinstall, S. (2002). Inhibition of ADP-induced P-selectin expression and platelet–leukocyte conjugate formation by clopidogrel and the P2Y12 receptor antagonist AR-C69931MX but not aspirin. Thrombosis and Haemostasis, 88, 488–494.
   PubMed Web of Science ®Google Scholar
• Su, X., Camerer, E., Hamilton, J. R., Coughlin, S. R., & Matthay, M. A. (2005). Protease-activated receptor-2 activation induces acute lung inflammation by neuropeptide-dependent mechanisms. The Journal of Immunology, 175, 2598–2605.10.4049/jimmunol.175.4.2598
   PubMed Web of Science ®Google Scholar
• Su, S., Li, Y., Luo, Y., Sheng, Y., Su, Y., Padia, R. N., … Huang, S. (2009). Proteinase-activated receptor 2 expression in breast cancer and its role in breast cancer cell migration. Oncogene, 28, 3047–3057.10.1038/onc.2009.163
   PubMed Web of Science ®Google Scholar
• Suen, J. Y., Barry, G. D., Lohman, R. J., Halili, M. A., Cotterell, A. J., Le, G. T., & Fairlie, D. P. (2012). Modulating human proteinase activated receptor 2 with a novel antagonist (GB88) and agonist (GB110). British Journal of Pharmacology, 165, 1413–1423.10.1111/j.1476-5381.2011.01610.x
   PubMed Web of Science ®Google Scholar
• Suen, J. Y., Gardiner, B., Grimmond, S., & Fairlie, D. P. (2010). Profiling gene expression induced by protease-activated receptor 2 (PAR2) activation in human kidney cells. PLoS One, 5, e13809. doi:10.1371/journal.pone.001380910.1371/journal.pone.0013809
   Google Scholar
• Tanaka, H., Yoshida, T., Miyamoto, N., Motoike, T., Kurosu, H., Shibata, K., … Yanagisawa, M. (2003). Characterization of a family of endogenous neuropeptide ligands for the G protein-coupled receptors GPR7 and GPR8. Proceedings of the National Academy of Sciences, 100, 6251–6256.10.1073/pnas.0837789100
   PubMed Web of Science ®Google Scholar
• Tautermann, C. S., Seeliger, D., & Kriegl, J.M. (2015). What can we learn from molecular dynamics simulations for GPCR drug design? Computational and Structural Biotechnology Journal, 13, 111–121.10.1016/j.csbj.2014.12.002
   PubMed Web of Science ®Google Scholar
• Urban, J. D., Clarke, W. P., von Zastrow, M., Nichols, D. E., Kobilka, B., Weinstein, H., … Mailman, R. B. (2007). Functional selectivity and classical concepts of quantitative pharmacology. Journal of Pharmacology and Experimental Therapeutics, 320(1), 1–13.
   PubMed Web of Science ®Google Scholar
• Warszycki, D., Mordalski, S., Kristiansen, K., Kafel, R., Sylte, I., Chilmonczyk, Z., & Bojarski, A. J. (2013). A linear combination of pharmacophore hypotheses as a new tool in search of new active compounds – An application for 5-HT1A receptor ligands. PLoS One, 8, e84510. doi:10.1371/journal.pone.0084510
   PubMed Web of Science ®Google Scholar
• Wiederstein, & Sippl. (2007). ProSA-web: Interactive web service for the recognition of errors in three-dimensional structures of proteins. Nucleic Acids Research, 35, W407–W410.10.1093/nar/gkm290
   PubMed Web of Science ®Google Scholar
• Yosten, G. L., Kolar, G. R., Redlinger, L. J., & Samson, W. K. (2013). Evidence for an interaction between proinsulin C-peptide and GPR146. Journal of Endocrinology, 218, B1–B8.10.1530/JOE-13-0203
   Google Scholar
• Zhang, C., Srinivasan, Y., Arlow, D. H., Fung, J. J., Palmer, D., Zheng, Y., … Kobilka, B. K. (2012). High-resolution crystal structure of human protease-activated receptor 1. Nature, 492, 387–392.10.1038/nature11701
   PubMed Web of Science ®Google Scholar