Angiotensin (1–7) does not interact directly with MAS1, but can potently antagonize signaling from the AT1 receptor
Gaidarov, Ibragim, Adams, John, Frazer, John, Anthony, Todd, Chen, Xiaohua, Gatlin, Joel, Semple, Graeme, Unett, David J.
Published in Cellular signalling (01.10.2018)
Published in Cellular signalling (01.10.2018)
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Differential tissue and ligand-dependent signaling of GPR109A receptor: Implications for anti-atherosclerotic therapeutic potential
Gaidarov, Ibragim, Chen, Xiaohua, Anthony, Todd, Maciejewski-Lenoir, Dominique, Liaw, Chen, Unett, David J.
Published in Cellular signalling (01.10.2013)
Published in Cellular signalling (01.10.2013)
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Discovery of the First Potent and Orally Efficacious Agonist of the Orphan G-Protein Coupled Receptor 119
Semple, Graeme, Fioravanti, Beatriz, Pereira, Guillherme, Calderon, Imelda, Uy, Jane, Choi, Karoline, Xiong, Yifeng, Ren, Albert, Morgan, Michael, Dave, Vibha, Thomsen, William, Unett, David J, Xing, Charles, Bossie, Stuart, Carroll, Chris, Chu, Zhi-Liang, Grottick, Andrew J, Hauser, Erin K, Leonard, James, Jones, Robert M
Published in Journal of medicinal chemistry (11.09.2008)
Published in Journal of medicinal chemistry (11.09.2008)
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Discovery of a lead series of potent benzodiazepine 5-HT2C receptor agonists with high selectivity in functional and binding assays
Ren, Albert, Zhu, Xiuwen, Feichtinger, Konrad, Lehman, Juerg, Kasem, Michelle, Schrader, Thomas O., Wong, Amy, Dang, Huong, Le, Minh, Frazer, John, Unett, David J., Grottick, Andrew J., Whelan, Kevin T., Morgan, Michael E., Sage, Carleton R., Semple, Graeme
Published in Bioorganic & medicinal chemistry letters (01.03.2020)
Published in Bioorganic & medicinal chemistry letters (01.03.2020)
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Kinetics of 5-HT2B receptor signaling: profound agonist-dependent effects on signaling onset and duration
Unett, David J, Gatlin, Joel, Anthony, Todd L, Buzard, Daniel J, Chang, Steve, Chen, Chuan, Chen, Xiaohua, Dang, Huong T-M, Frazer, John, Le, Minh K, Sadeque, Abu J M, Xing, Charles, Gaidarov, Ibragim
Published in The Journal of pharmacology and experimental therapeutics (01.12.2013)
Published in The Journal of pharmacology and experimental therapeutics (01.12.2013)
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Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist for the Treatment of Chronic Pain
Han, Sangdon, Thoresen, Lars, Jung, Jae-Kyu, Zhu, Xiuwen, Thatte, Jayant, Solomon, Michelle, Gaidarov, Ibragim, Unett, David J, Yoon, Woo Hyun, Barden, Jeremy, Sadeque, Abu, Usmani, Amin, Chen, Chuan, Semple, Graeme, Grottick, Andrew J, Al-Shamma, Hussein, Christopher, Ronald, Jones, Robert M
Published in ACS medicinal chemistry letters (14.12.2017)
Published in ACS medicinal chemistry letters (14.12.2017)
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Embelin and its derivatives unravel the signaling, proinflammatory and antiatherogenic properties of GPR84 receptor
Gaidarov, Ibragim, Anthony, Todd, Gatlin, Joel, Chen, Xiaohua, Mills, David, Solomon, Michelle, Han, Sangdon, Semple, Graeme, Unett, David J.
Published in Pharmacological research (01.05.2018)
Published in Pharmacological research (01.05.2018)
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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
Tran, Thuy-Anh, Kramer, Bryan, Shin, Young-Jun, Vallar, Pureza, Boatman, P. Douglas, Zou, Ning, Sage, Carleton R, Gharbaoui, Tawfik, Krishnan, Ashwin, Pal, Biman, Shakya, Sagar R, Garrido Montalban, Antonio, Adams, John W, Ramirez, Juan, Behan, Dominic P, Shifrina, Anna, Blackburn, Anthony, Leakakos, Tina, Shi, Yunqing, Morgan, Michael, Sadeque, Abu, Chen, Weichao, Unett, David J, Gaidarov, Ibragim, Chen, Xiaohua, Chang, Steve, Shu, Hsin-Hui, Tung, Shiu-Feng, Semple, Graeme
Published in Journal of medicinal chemistry (09.02.2017)
Published in Journal of medicinal chemistry (09.02.2017)
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Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate‑1 Receptor
Buzard, Daniel J, Kim, Sun Hee, Lopez, Luis, Kawasaki, Andrew, Zhu, Xiuwen, Moody, Jeanne, Thoresen, Lars, Calderon, Imelda, Ullman, Brett, Han, Sangdon, Lehmann, Juerg, Gharbaoui, Tawfik, Sengupta, Dipanjan, Calvano, Lorene, Montalban, Antonio Garrido, Ma, You-An, Sage, Carleton, Gao, Yinghong, Semple, Graeme, Edwards, Jeff, Barden, Jeremy, Morgan, Michael, Chen, Weichao, Usmani, Khawja, Chen, Chuan, Sadeque, Abu, Christopher, Ronald J, Thatte, Jayant, Fu, Lixia, Solomon, Michelle, Mills, David, Whelan, Kevin, Al-Shamma, Hussien, Gatlin, Joel, Le, Minh, Gaidarov, Ibragim, Anthony, Todd, Unett, David J, Blackburn, Anthony, Rueter, Jaimie, Stirn, Scott, Behan, Dominic P, Jones, Robert M
Published in ACS medicinal chemistry letters (11.12.2014)
Published in ACS medicinal chemistry letters (11.12.2014)
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Journal Article
Discovery of a novel trans-1,4-dioxycyclohexane GPR119 agonist series
Han, Sangdon, Narayanan, Sanju, Kim, Sun Hee, Calderon, Imelda, Zhu, Xiuwen, Kawasaki, Andrew, Yue, Dawei, Lehmann, Juerg, Wong, Amy, Buzard, Daniel J., Semple, Graeme, Carroll, Chris, Chu, Zhi-Liang, Al-Sharmma, Hussein, Shu, Hsin-Hui, Tung, Shiu-Feng, Unett, David J., Behan, Dominic P., Yoon, Woo Hyun, Morgan, Michael, Usmani, Khawja A., Chen, Chuan, Sadeque, Abu, Leonard, James N., Jones, Robert M.
Published in Bioorganic & medicinal chemistry letters (01.08.2015)
Published in Bioorganic & medicinal chemistry letters (01.08.2015)
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Journal Article
Discovery of a new series of potent prostacyclin receptor agonists with in vivo activity in rat
Tran, Thuy-Anh, Shin, Young-Jun, Kramer, Bryan, Choi, Juyi, Zou, Ning, Vallar, Pureza, Martens, Peter, Douglas Boatman, P., Adams, John W., Ramirez, Juan, Shi, Yunqing, Morgan, Michael, Unett, David J., Chang, Steve, Shu, Hsin-Hui, Tung, Shiu-Feng, Semple, Graeme
Published in Bioorganic & medicinal chemistry letters (01.03.2015)
Published in Bioorganic & medicinal chemistry letters (01.03.2015)
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Journal Article
Discovery and optimization of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists
Buzard, Daniel J., Kim, Sun Hee, Lehmann, Juerg, Han, Sangdon, Calderon, Imelda, Wong, Amy, Kawasaki, Andrew, Narayanan, Sanju, Bhat, Rohit, Gharbaoui, Tawfik, Lopez, Luis, Yue, Dawei, Whelan, Kevin, Al-Shamma, Hussien, Unett, David J., Shu, Hsin-Hui, Tung, Shiu-Feng, Chang, Steve, Chuang, Ching-Fen, Morgan, Michael, Sadeque, Abu, Chu, Zhi-Liang, Leonard, James N., Jones, Robert M.
Published in Bioorganic & medicinal chemistry letters (01.09.2014)
Published in Bioorganic & medicinal chemistry letters (01.09.2014)
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Discovery of 1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a] pentalen-4-carboxamides as potent and selective CB2 receptor agonists
Han, Sangdon, Thoresen, Lars, Zhu, Xiuwen, Narayanan, Sanju, Jung, Jae-Kyu, Strah-Pleynet, Sonja, Decaire, Marc, Choi, Karoline, Xiong, Yifeng, Yue, Dawei, Semple, Graeme, Thatte, Jayant, Solomon, Michelle, Fu, Lixia, Whelan, Kevin, Al-Shamma, Hussien, Gatlin, Joel, Chen, Ruoping, Dang, Huong, Pride, Cameron, Gaidarov, Ibragim, Unett, David J., Behan, Dominic P., Abu Sadeque, Usmani, Khawja A., Chen, Chuan, Edwards, Jeffrey, Morgan, Michael, Jones, Robert M.
Published in Bioorganic & medicinal chemistry letters (15.01.2015)
Published in Bioorganic & medicinal chemistry letters (15.01.2015)
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Discovery of APD371: Identification of a Highly Potent and Selective CB 2 Agonist for the Treatment of Chronic Pain
Han, Sangdon, Thoresen, Lars, Jung, Jae-Kyu, Zhu, Xiuwen, Thatte, Jayant, Solomon, Michelle, Gaidarov, Ibragim, Unett, David J, Yoon, Woo Hyun, Barden, Jeremy, Sadeque, Abu, Usmani, Amin, Chen, Chuan, Semple, Graeme, Grottick, Andrew J, Al-Shamma, Hussein, Christopher, Ronald, Jones, Robert M
Published in ACS medicinal chemistry letters (14.12.2017)
Published in ACS medicinal chemistry letters (14.12.2017)
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Journal Article
(7‑Benzyloxy-2,3-dihydro-1H-pyrrolo[1,2‑a]indol-1-yl)acetic Acids as S1P1 Functional Antagonists
Buzard, Daniel J, Lopez, Luis, Moody, Jeanne, Kawasaki, Andrew, Schrader, Thomas O, Kasem, Michelle, Johnson, Ben, Zhu, Xiuwen, Thoresen, Lars, Kim, Sun Hee, Gharbaoui, Tawfik, Sengupta, Dipanjan, Calvano, Lorene, Krishnan, Ashwin, Gao, Yinghong, Semple, Graeme, Edwards, Jeff, Barden, Jeremy, Morgan, Michael, Usmani, Khawja, Chen, Chuan, Sadeque, Abu, Chen, Weichao, Christopher, Ronald J, Thatte, Jayant, Fu, Lixia, Solomon, Michelle, Whelan, Kevin, Al-Shamma, Hussien, Gatlin, Joel, Gaidarov, Ibragim, Anthony, Todd, Le, Minh, Unett, David J, Stirn, Scott, Blackburn, Anthony, Behan, Dominic P, Jones, Robert M
Published in ACS medicinal chemistry letters (11.12.2014)
Published in ACS medicinal chemistry letters (11.12.2014)
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Design of a new series of potent and selective beta-3 adrenergic receptor (β3-AdrR) antagonists for the treatment of acute decompensated heart failure
Tran, Thuy-Anh, Kramer, Bryan, Shin, Young-Jun, Do, Quyen-Quyen, Ullman, Brett, Sagi, Vasudeva, Adams, John W., Shi, Yunqing, Shu, Hsin-Hui, Unett, David J., Gatlin, Joel, Morgan, Michael E., Reuter, Jaimie, Blackburn, Anthony, Sage, Carleton R., Semple, Graeme
Published in Results in Chemistry (01.01.2022)
Published in Results in Chemistry (01.01.2022)
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Functional assays for screening GPCR targets
Thomsen, William, Frazer, John, Unett, David
Published in Current opinion in biotechnology (01.12.2005)
Published in Current opinion in biotechnology (01.12.2005)
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Journal Article
A Role for β-Cell-Expressed G Protein-Coupled Receptor 119 in Glycemic Control by Enhancing Glucose-Dependent Insulin Release
Chu, Zhi-Liang, Jones, Robert M, He, Hongmei, Carroll, Chris, Gutierrez, Veronica, Lucman, Annette, Moloney, Molly, Gao, Hui, Mondala, Helen, Bagnol, Didier, Unett, David, Liang, Yin, Demarest, Keith, Semple, Graeme, Behan, Dominic P, Leonard, James
Published in Endocrinology (Philadelphia) (01.06.2007)
Published in Endocrinology (Philadelphia) (01.06.2007)
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Journal Article
N-Oleoyldopamine Enhances Glucose Homeostasis through the Activation of GPR119
Chu, Zhi-Liang, Carroll, Chris, Chen, Ruoping, Alfonso, Jean, Gutierrez, Veronica, He, Hongmei, Lucman, Annette, Xing, Charles, Sebring, Kristen, Zhou, Jinyao, Wagner, Brandee, Unett, David, Jones, Robert M, Behan, Dominic P, Leonard, James
Published in Molecular endocrinology (Baltimore, Md.) (01.01.2010)
Published in Molecular endocrinology (Baltimore, Md.) (01.01.2010)
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