Search Results - "Kong, Jimmy"

An inverse agonist of orphan receptor GPR61 acts by a G protein-competitive allosteric mechanism by Lees, Joshua A., Dias, João M., Rajamohan, Francis, Fortin, Jean-Philippe, O’Connor, Rebecca, Kong, Jimmy X., Hughes, Emily A. G., Fisher, Ethan L., Tuttle, Jamison B., Lovett, Gabrielle, Kormos, Bethany L., Unwalla, Rayomand J., Zhang, Lei, Dechert Schmitt, Anne-Marie, Zhou, Dahui, Moran, Michael, Stevens, Kimberly A., Fennell, Kimberly F., Varghese, Alison E., Maxwell, Andrew, Cote, Emmaline E., Zhang, Yuan, Han, Seungil

“…GPR61 is an orphan GPCR related to biogenic amine receptors. Its association with phenotypes relating to appetite makes it of interest as a druggable target to…”
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Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss by Garnsey, Michelle R., Smith, Aaron C., Polivkova, Jana, Arons, Autumn L., Bai, Guoyun, Blakemore, Caroline, Boehm, Markus, Buzon, Leanne M., Campion, Sarah N., Cerny, Matthew, Chang, Shiao-Chi, Coffman, Karen, Farley, Kathleen A., Fonseca, Kari R., Ford, Kristen K., Garren, Jeonifer, Kong, Jimmy X., Koos, Martin R. M., Kung, Daniel W., Lian, Yajing, Li, Monica M., Li, Qifang, Martinez-Alsina, Luis A., O’Connor, Rebecca, Ogilvie, Kevin, Omoto, Kiyoyuki, Raymer, Brian, Reese, Matthew R., Ryder, Tim, Samp, Lacey, Stevens, Kimberly A., Widlicka, Daniel W., Yang, Qingyi, Zhu, Kaicheng, Fortin, Jean-Philippe, Sammons, Matthew F.

“…The melanocortin-4 receptor (MC4R) is a centrally expressed, class A GPCR that plays a key role in the regulation of appetite and food intake. Deficiencies in…”
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Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity by Liu, Kevin K.-C., Cornelius, Peter, Patterson, Terrell A., Zeng, Yuan, Santucci, Stephanie, Tomlinson, Elizabeth, Gibbons, Colleen, Maurer, Tristan S., Marala, Ravi, Brown, Janice, Kong, Jimmy X., Lee, Eunsun, Werner, Wendy, Wenzel, Zane, Vage, Chandra

“…A series of novel conformationally-restricted 5HT2c receptor agonists with 2-piperazin-azaindane scaffold were designed. Orally-active compounds were…”
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Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity by Liu, Kevin K.-C., Lefker, Bruce A., Dombroski, Mark A., Chiang, Phoebe, Cornelius, Peter, Patterson, Terrell A., Zeng, Yuan, Santucci, Stephanie, Tomlinson, Elizabeth, Gibbons, Colleen P., Marala, Ravi, Brown, Janice A., Kong, Jimmy X., Lee, Eunsun, Werner, Wendy, Wenzel, Zane, Giragossian, Craig, Chen, Hou, Coffey, Steven B.

“…Brain-penetrable proline amides were developed as 5HT2c agonists with more than 1000-fold binding selectivity against 5HT2b receptor. After medicinal chemistry…”
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Zoniporide: a potent and highly selective inhibitor of human Na +/H + exchanger-1 by Marala, Ravi B, Brown, Janice A, Kong, Jimmy X, Tracey, W.Ross, Knight, Delvin R, Wester, Ronald T, Sun, Dexue, Kennedy, Scott P, Hamanaka, Ernest S, Ruggeri, Roger B, Hill, Roger J

“…We evaluated the in vitro pharmacological profile of a novel, potent and highly selective Na +/H + exchanger-1 (NHE-1) inhibitor,…”
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Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate by Bhattacharya, Samit K, Andrews, Kim, Beveridge, Ramsay, Cameron, Kimberly O, Chen, Chiliu, Dunn, Matthew, Fernando, Dilinie, Gao, Hua, Hepworth, David, Jackson, V. Margaret, Khot, Vishal, Kong, Jimmy, Kosa, Rachel E, Lapham, Kimberly, Loria, Paula M, Londregan, Allyn T, McClure, Kim F, Orr, Suvi T. M, Patel, Jigna, Rose, Colin, Saenz, James, Stock, Ingrid A, Storer, Gregory, VanVolkenburg, Maria, Vrieze, Derek, Wang, Guoqiang, Xiao, Jun, Zhang, Yingxin

“…The identification of potent, highly selective orally bioavailable ghrelin receptor inverse agonists from a spiro-azetidino-piperidine series is described…”
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Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor by McClure, Kim F., Jackson, Margaret, Cameron, Kimberly O., Kung, Daniel W., Perry, David A., Orr, Suvi T.M., Zhang, Yingxin, Kohrt, Jeffrey, Tu, Meihua, Gao, Hua, Fernando, Dilinie, Jones, Ryan, Erasga, Noe, Wang, Guoqiang, Polivkova, Jana, Jiao, Wenhua, Swartz, Roger, Ueno, Hirokazu, Bhattacharya, Samit K., Stock, Ingrid A., Varma, Sam, Bagdasarian, Victoria, Perez, Sylvie, Kelly-Sullivan, Dawn, Wang, Ruduan, Kong, Jimmy, Cornelius, Peter, Michael, Laura, Lee, Eunsun, Janssen, Ann, Steyn, Stefanus J., Lapham, Kimberly, Goosen, Theunis

“…The optimization for selectivity and central receptor occupancy for a series of spirocyclic azetidine–piperidine inverse agonists of the ghrelin receptor is…”
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3‘-Aminoadenosine-5‘-uronamides:  Discovery of the First Highly Selective Agonist at the Human Adenosine A3 Receptor by DeNinno, Michael P, Masamune, Hiroko, Chenard, Lois K, DiRico, Kenneth J, Eller, Cynthia, Etienne, John B, Tickner, Jeanene E, Kennedy, Scott P, Knight, Delvin R, Kong, Jimmy, Oleynek, Joseph J, Tracey, W. Ross, Hill, Roger J

“…Selective adenosine A3 agonists have potential utility for the prevention of perioperative myocardial ischemic injury. Herein, we report on the discovery and…”
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The synthesis of highly potent, selective, and water-soluble agonists at the human adenosine A3 receptor by DENINNO, Michael P, MASAMUNE, Hiroko, OLEYNEK, Joseph J, TRACEY, W. Ross, HILL, Roger J, CHENARD, Lois K, DIRICO, Kenneth J, ELLER, Cynthia, ETIENNE, John B, TICKNER, Jeanene E, KENNEDY, Scott P, KNIGHT, Delvin R, KONG, Jimmy

“…Using a combination of parallel and directed synthesis, the discovery of a highly potent and selective series of adenosine A3 agonists was achieved. High…”
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Expression of the Rat Adrenomedullin Receptor or a Putative Human Adrenomedullin Receptor Does Not Correlate with Adrenomedullin Binding or Functional Response by Kennedy, Scott P., Sun, Dexue, Oleynek, Joseph J., Hoth, Christopher F., Kong, Jimmy, Hill, Roger J.

“…There has been considerable difficulty in defining distinct adrenomedullin (AM) binding sites and functionin vivo.However, a rat adrenomedullin receptor (rAMR)…”
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The synthesis of highly potent, selective, and water-soluble agonists at the human adenosine A 3 receptor by DeNinno, Michael P., Masamune, Hiroko, Chenard, Lois K., DiRico, Kenneth J., Eller, Cynthia, Etienne, John B., Tickner, Jeanene E., Kennedy, Scott P., Knight, Delvin R., Kong, Jimmy, Oleynek, Joseph J., Tracey, W. Ross, Hill, Roger J.

“…Using a combination of parallel and directed synthesis, the discovery of a highly potent and selective series of adenosine A 3 agonists was achieved. High…”
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The synthesis of highly potent, selective, and water-soluble agonists at the human adenosine A sub(3) receptor by DeNinno, Michael P, Masamune, Hiroko, Chenard, Lois K, DiRico, Kenneth J, Eller, Cynthia, Etienne, John B, Tickner, Jeanene E, Kennedy, Scott P, Knight, Delvin R, Kong, Jimmy, Oleynek, Joseph J, Tracey, WRoss, Hill, Roger J

“…Using a combination of parallel and directed synthesis, the discovery of a highly potent and selective series of adenosine A sub(3) agonists was achieved. High…”
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3‘-Aminoadenosine-5‘-uronamides:  Discovery of the First Highly Selective Agonist at the Human Adenosine A 3 Receptor by DeNinno, Michael P., Masamune, Hiroko, Chenard, Lois K., DiRico, Kenneth J., Eller, Cynthia, Etienne, John B., Tickner, Jeanene E., Kennedy, Scott P., Knight, Delvin R., Kong, Jimmy, Oleynek, Joseph J., Tracey, W. Ross, Hill, Roger J.

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A novel sodium-hydrogen exchanger isoform-1 inhibitor, zoniporide, reduces ischemic myocardial injury in vitro and in vivo by Knight, D R, Smith, A H, Flynn, D M, MacAndrew, J T, Ellery, S S, Kong, J X, Marala, R B, Wester, R T, Guzman-Perez, A, Hill, R J, Magee, W P, Tracey, W R

“…The cardioprotective efficacy of zoniporide (CP-597,396), a novel, potent, and selective inhibitor of the sodium-hydrogen exchanger isoform 1 (NHE-1), was…”
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