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Selected Publications

EXAMPLES OF PAST AND CURRENT RESEARCH

•    Al-Shamma, H., Lehmann-Bruinsma, K., Carroll, C., Solomon, M., Komori, H.K., Peyrin-Biroulet, L., Adams, J.  The Selective Sphingosine 1-phosphate Receptor Modulator Etrasimod Regulates Lymphocyte Trafficking and Alleviates Experimental Colitis. J Pharmacol Exp Ther. 2019 Mar 14. pii: jpet.118.254268. doi: 10.1124/jpet.118.254268.

•    Gaidarov, I., Adams, J., Frazer, J., Anthony, T., Chen, X., Gatlin, J., Semple, G., Unett, D.J. Angiotensin (1-7) does not interact directly with MAS1, but can potently antagonize signaling from the AT1 receptor. Cell Signal. 2018 Oct; 50:9-24. doi: 10.1016/j.cellsig.2018.06.007.

•    Gaidarov, I., Anthony, T., Gatlin, J., Chen, X., Mills, D., Solomon, M., Han, S., Semple, G., Unett, D.J. Embelin and its derivatives unravel the signaling, proinflammatory and antiatherogenic properties of GPR84 receptor. Pharmacol Res. 2018 May; 131:185-198. doi: 10.1016/j.phrs.2018.02.021.

•    Han, S., Thoresen, L., Jung, J.-K., Zhu, X., Thatte, J., Solomon, M., Gaidarov, I., Unett, D.J., Yoon, W.H., Barden, J., Sadeque, A., Usmani, A., Chen, C., Semple, G., Grottick, A.J., Al-Shamma, H., Christopher, R., Jones, R.M., 2017. Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist  for the Treatment of Chronic Pain. ACS Med Chem Lett 8, 1309–1313. doi:10.1021/acsmedchemlett.7b00396


•    Tran, T.-A., Kramer, B., Shin, Y.-J., Vallar, P., Boatman, P.D., Zou, N., Sage, C.R., Gharbaoui, T., Krishnan, A., Pal, B., Shakya, S.R., Garrido Montalban, A., Adams, J.W., Ramirez, J., Behan, D.P., Shifrina, A., Blackburn, A., Leakakos, T., Shi, Y., Morgan, M., Sadeque, A., Chen, W., Unett, D.J., Gaidarov, I., Chen, X., Chang, S., Shu, H.-H., Tung, S.-F., Semple, G., 2017. Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)- carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension. J Med Chem 60, 913–927. doi:10.1021/acs.jmedchem.6b00871


•    Grottick, A.J., Whelan, K., Sanabria, E.K., Behan, D.P., Morgan, M., Sage, C., 2015. Investigating interactions between phentermine, dexfenfluramine, and 5-HT2C agonists, on food intake in the rat. Psychopharmacology (Berl) 232, 1973–1982. doi:10.1007/s00213-014-3829-2


•    Buzard, D.J., Kim, S.H., Lopez, L., Kawasaki, A., Zhu, X., Moody, J., Thoresen, L., Calderon, I., Ullman, B., Han, S., Lehmann, J., Gharbaoui, T., Sengupta, D., Calvano, L., Montalban, A.G., Ma, Y.-A., Sage, C., Gao, Y., Semple, G., Edwards, J., Barden, J., Morgan, M., Chen, W., Usmani, K., Chen, C., Sadeque, A., Christopher, R.J., Thatte, J., Fu, L., Solomon, M., Mills, D., Whelan, K., Al-Shamma, H., Gatlin, J., Le, M., Gaidarov, I., Anthony, T., Unett, D.J., Blackburn, A., Rueter, J., Stirn, S., Behan, D.P., Jones, R.M., 2014. Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor. ACS Med Chem Lett 5, 1313–1317. doi:10.1021/ml500389m


•    Gaidarov, I., Chen, X., Anthony, T., Maciejewski-Lenoir, D., Liaw, C., Unett, D.J., 2013. Differential tissue and ligand-dependent signaling of GPR109A receptor: implications for anti-atherosclerotic therapeutic potential. Cell Signal 25, 2003–2016. doi:10.1016/j.cellsig.2013.06.008


•    Unett, D.J., Gatlin, J., Anthony, T.L., Buzard, D.J., Chang, S., Chen, C., Chen, X., Dang, H.T.-M., Frazer, J., Le, M.K., Sadeque, A.J.M., Xing, C., Gaidarov, I., 2013. Kinetics of 5-HT2B receptor signaling: profound agonist-dependent effects on signaling onset and duration. J Pharmacol Exp Ther 347, 645–659. doi:10.1124/jpet.113.207670


•    Bagnol, D., Al-Shamma, H.A., Behan, D., Whelan, K., Grottick, A.J., 2012. Diet-induced models of obesity (DIO) in rodents. Curr Protoc Neurosci Chapter 9, Unit 9.38.1-13. doi:10.1002/0471142301.ns0938s59


•    Boatman, P.D., Lauring, B., Schrader, T.O., Kasem, M., Johnson, B.R., Skinner, P., Jung, J.-K., Xu, J., Cherrier, M.C., Webb, P.J., Semple, G., Sage, C.R., Knudsen, J., Chen, R., Luo, W.-L., Caro, L., Cote, J., Lai, E., Wagner, J., Taggart, A.K., Carballo-Jane, E., Hammond, M., Colletti, S.L., Tata, J.R., Connolly, D.T., Waters, M.G., Richman, J.G., 2012. (1aR,5aR)1a,3,5,5a-Tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid (MK-1903): a potent GPR109a agonist that lowers free fatty acids in humans. J Med Chem 55, 3644–3666. doi:10.1021/jm2010964


•    Lauring, B., Taggart, A.K.P., Tata, J.R., Dunbar, R., Caro, L., Cheng, K., Chin, J., Colletti, S.L., Cote, J., Khalilieh, S., Liu, J., Luo, W.-L., Maclean, A.A., Peterson, L.B., Polis, A.B., Sirah, W., Wu, T.-J., Liu, X., Jin, L., Wu, K., Boatman, P.D., Semple, G., Behan, D.P., Connolly, D.T., Lai, E., Wagner, J.A., Wright, S.D., Cuffie, C., Mitchel, Y.B., Rader, D.J., Paolini, J.F., Waters, M.G., Plump, A., 2012. Niacin lipid efficacy is independent of both the niacin receptor GPR109A and free fatty acid suppression. Sci Transl Med 4, 148ra115. doi:10.1126/scitranslmed.3003877


•    Semple, G., Santora, V.J., Smith, J.M., Covel, J.A., Hayashi, R., Gallardo, C., Ibarra, J.B., Schultz, J.A., Park, D.M., Estrada, S.A., Hofilena, B.J., Smith, B.M., Ren, A., Suarez, M., Frazer, J., Edwards, J.E., Hart, R., Hauser, E.K., Lorea, J., Grottick, A.J., 2012. Identification of biaryl sulfone derivatives as antagonists of the histamine H(3) receptor: discovery of (R)-1-(2-(4’-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916). Bioorg Med Chem Lett 22, 71–75. doi:10.1016/j.bmcl.2011.11.075


•    Al-Shamma, H.A., Anderson, C., Chuang, E., Luthringer, R., Grottick, A.J., Hauser, E., Morgan, M., Shanahan, W., Teegarden, B.R., Thomsen, W.J., Behan, D., 2010. Nelotanserin, a novel selective human 5-hydroxytryptamine2A inverse agonist for the treatment of insomnia. J Pharmacol Exp Ther 332, 281–290. doi:10.1124/jpet.109.160994


•    Chu, Z.-L., Carroll, C., Chen, R., Alfonso, J., Gutierrez, V., He, H., Lucman, A., Xing, C., Sebring, K., Zhou, J., Wagner, B., Unett, D., Jones, R.M., Behan, D.P., Leonard, J., 2010. N-oleoyldopamine enhances glucose homeostasis through the activation of GPR119. Mol Endocrinol 24, 161–170. doi:10.1210/me.2009-0239
•    Przyklenk, K., Frelinger, A.L. 3rd, Linden, M.D., Whittaker, P., Li, Y., Barnard, M.R., Adams, J., Morgan, M., Al-Shamma, H., Michelson, A.D., 2010. Targeted inhibition of the serotonin 5HT2A receptor improves coronary patency in  an in vivo model of recurrent thrombosis. J Thromb Haemost 8, 331–340. doi:10.1111/j.1538-7836.2009.03693.x


•    Adams, J.W., Ramirez, J., Shi, Y., Thomsen, W., Frazer, J., Morgan, M., Edwards, J.E., Chen, W., Teegarden, B.R., Xiong, Y., Al-Shamma, H., Behan, D.P., Connolly, D.T., 2009. APD791, a Novel 5-HT2A Receptor Antagonist: Pharmacological Profile, Pharmacokinetics, Platelet and Vascular Biology. J Pharmacol Exp Ther 331, 96–103. doi:10.1124/jpet.109.153189


•    Lai, E., Waters, M.G., Tata, J.R., Radziszewski, W., Perevozskaya, I., Zheng, W., Wenning, L., Connolly, D.T., Semple, G., Johnson-Levonas, A.O., Wagner, J.A., Mitchel, Y., Paolini, J.F., 2008. Effects of a niacin receptor partial agonist, MK-0354, on plasma free fatty acids, lipids, and cutaneous flushing in humans. J Clin Lipidol 2, 375–383. doi:10.1016/j.jacl.2008.08.445


•    Semple, G., Fioravanti, B., Pereira, G., Calderon, I., Uy, J., Choi, K., Xiong, Y., Ren, A., Morgan, M., Dave, V., Thomsen, W., Unett, D.J., Xing, C., Bossie, S., Carroll, C., Chu, Z.-L., Grottick, A.J., Hauser, E.K., Leonard, J., Jones, R.M., 2008a. Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. J Med Chem 51, 5172–5175. doi:10.1021/jm8006867


•    Semple, G., Skinner, P.J., Gharbaoui, T., Shin, Y.-J., Jung, J.-K., Cherrier, M.C., Webb, P.J., Tamura, S.Y., Boatman, P.D., Sage, C.R., Schrader, T.O., Chen, R., Colletti, S.L., Tata, J.R., Waters, M.G., Cheng, K., Taggart, A.K., Cai, T.-Q., Carballo-Jane, E., Behan, D.P., Connolly, D.T., Richman, J.G., 2008b. 3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): a partial agonist of the nicotinic acid receptor, G-protein coupled receptor 109a, with antilipolytic but no vasodilatory activity in mice. J Med Chem 51, 5101–5108. doi:10.1021/jm800258p


•    Smith, B.M., Smith, J.M., Tsai, J.H., Schultz, J.A., Gilson, C.A., Estrada, S.A., Chen, R.R., Park, D.M., Prieto, E.B., Gallardo, C.S., Sengupta, D., Dosa, P.I., Covel, J.A., Ren, A., Webb, R.R., Beeley, N.R.A., Martin, M., Morgan, M., Espitia, S., Saldana, H.R., Bjenning, C., Whelan, K.T., Grottick, A.J., Menzaghi, F., Thomsen, W.J., 2008. Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity. J Med Chem 51, 305–313. doi:10.1021/jm0709034


•    Richman, J.G., Kanemitsu-Parks, M., Gaidarov, I., Cameron, J.S., Griffin, P., Zheng, H., Guerra, N.C., Cham, L., Maciejewski-Lenoir, D., Behan, D.P., Boatman, D., Chen, R., Skinner, P., Ornelas, P., Waters, M.G., Wright, S.D., Semple, G., Connolly, D.T., 2007. Nicotinic acid receptor agonists differentially activate downstream effectors. J Biol Chem 282, 18028–18036. doi:10.1074/jbc.M701866200


•    Smith, B.M., Thomsen, W.J., Grottick, A.J., 2006. The potential use of selective 5-HT2C agonists in treating obesity. Expert Opin Investig Drugs 15, 257–266. doi:10.1517/13543784.15.3.257


•    Fletcher, P.J., Grottick, A.J., Higgins, G.A., 2002. Differential effects of the 5-HT(2A) receptor antagonist M100907 and the 5-HT(2C) receptor antagonist SB242084 on cocaine-induced locomotor activity, cocaine self-administration and cocaine-induced reinstatement of responding. Neuropsychopharmacology 27, 576–586. doi:10.1016/S0893-133X(02)00342-1