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Insights into the binding of Phenyltiocarbamide (PTC) agonist to its target human TAS2R38 bitter receptor

Biarnés, Xevi ; Marchiori, Alessandro ; Giorgetti, Alejandro ; Lanzara, Carmela ; Gasparini, Paolo ; Carloni, Paolo ; Born, Stephan ; Brockhoff, Anne ; Behrens, Maik ; Meyerhof, Wolfgang

PloS one, 25 August 2010, Vol.5(8), pp.e12394 [Peer Reviewed Journal]

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Chemogenomic analysis of G-protein coupled receptors and their ligands deciphers locks and keys governing diverse aspects of signalling

Wichard, Jörg D ; Ter Laak, Antonius ; Krause, Gerd ; Heinrich, Nikolaus ; Kühne, Ronald ; Kleinau, Gunnar

PloS one, 04 February 2011, Vol.6(2), pp.e16811 [Peer Reviewed Journal]

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Label-free phenotypic profiling identified D-luciferin as a GPR35 agonist

Hu, Haibei ; Deng, Huayun ; Fang, Ye

PloS one, 2012, Vol.7(4), pp.e34934 [Peer Reviewed Journal]

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Characterization of the modes of binding between human sweet taste receptor and low-molecular-weight sweet compounds

Masuda, Katsuyoshi ; Koizumi, Ayako ; Nakajima, Ken-Ichiro ; Tanaka, Takaharu ; Abe, Keiko ; Misaka, Takumi ; Ishiguro, Masaji

PloS one, 2012, Vol.7(4), pp.e35380 [Peer Reviewed Journal]

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A potent class of GPR40 full agonists engages the enteroinsular axis to promote glucose control in rodents

Luo, Jian ; Swaminath, Gayathri ; Brown, Sean P ; Zhang, Jane ; Guo, Qi ; Chen, Michael ; Nguyen, Kathy ; Tran, Thanhvien ; Miao, Lynn ; Dransfield, Paul J ; Vimolratana, Marc ; Houze, Jonathan B ; Wong, Simon ; Toteva, Maria ; Shan, Bei ; Li, Frank ; Zhuang, Run ; Lin, Daniel C-H

PloS one, 2012, Vol.7(10), pp.e46300 [Peer Reviewed Journal]

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Novel Zn2+ Modulated GPR39 Receptor Agonists Do Not Drive Acute Insulin Secretion in Rodents

Fjellström, Ola ; Larsson, Niklas ; Yasuda, Shin-Ichiro ; Tsuchida, Takuma ; Oguma, Takahiro ; Marley, Anna ; Wennberg-Huldt, Charlotte ; Hovdal, Daniel ; Fukuda, Hajime ; Yoneyama, Yukimi ; Sasaki, Kazuyo ; Johansson, Anders ; Lundqvist, Sara ; Brengdahl, Johan ; Isaacs, Richard J ; Brown, Daniel ; Geschwindner, Stefan ; Benthem, Lambertus ; Priest

PloS one, 2015, Vol.10(12), pp.e0145849 [Peer Reviewed Journal]

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The red imported fire ant (Solenopsis invicta Buren) kept Y not F: predicted sNPY endogenous ligands deorphanize the short NPF (sNPF) receptor

Bajracharya, Prati ; Lu, Hsiao-Ling ; Pietrantonio, Patricia V

PloS one, 2014, Vol.9(10), pp.e109590 [Peer Reviewed Journal]

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A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1

Yabuki, Chiori ; Komatsu, Hidetoshi ; Tsujihata, Yoshiyuki ; Maeda, Risa ; Ito, Ryo ; Matsuda-Nagasumi, Kae ; Sakuma, Kensuke ; Miyawaki, Kazumasa ; Kikuchi, Naoya ; Takeuchi, Koji ; Habata, Yugo ; Mori, Masaaki

PloS one, 2013, Vol.8(10), pp.e76280 [Peer Reviewed Journal]

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9
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Novel Small Molecule Agonist of TGR5 Possesses Anti-Diabetic Effects but Causes Gallbladder Filling in Mice

Briere, Daniel A ; Ruan, Xiaoping ; Cheng, Christine C ; Siesky, Angela M ; Fitch, Thomas E ; Dominguez, Carmen ; Sanfeliciano, Sonia Gutierrez ; Montero, Carlos ; Suen, Chen S ; Xu, Yanping ; Coskun, Tamer ; Michael, M Dodson

PloS one, 2015, Vol.10(8), pp.e0136873 [Peer Reviewed Journal]

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The human bitter taste receptor T2R38 is broadly tuned for bacterial compounds

Verbeurgt, Christophe ; Veithen, Alex ; Carlot, Sébastien ; Tarabichi, Maxime ; Dumont, Jacques E ; Hassid, Sergio ; Chatelain, Pierre

PloS one, 2017, Vol.12(9), pp.e0181302 [Peer Reviewed Journal]

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Discovery and cardioprotective effects of the first non-Peptide agonists of the G protein-coupled prokineticin receptor-1

Gasser, Adeline ; Brogi, Simone ; Urayama, Kyoji ; Nishi, Toshishide ; Kurose, Hitoshi ; Tafi, Andrea ; Ribeiro, Nigel ; Désaubry, Laurent ; Nebigil, Canan G

PloS one, 2015, Vol.10(4), pp.e0121027 [Peer Reviewed Journal]

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Estradiol and GPER Activation Differentially Affect Cell Proliferation but Not GPER Expression in the Hippocampus of Adult Female Rats

Duarte-Guterman, Paula ; Lieblich, Stephanie E ; Chow, Carmen ; Galea, Liisa A M

PloS one, 2015, Vol.10(6), pp.e0129880 [Peer Reviewed Journal]

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GPR40 partial agonists and AgoPAMs: Differentiating effects on glucose and hormonal secretions in the rodent

Pachanski, Michele J ; Kirkland, Melissa E ; Kosinski, Daniel T ; Mane, Joel ; Cheewatrakoolpong, Boonlert ; Xue, Jiyan ; Szeto, Daphne ; Forrest, Gail ; Miller, Corin ; Bunzel, Michelle ; Plummer, Christopher W ; Chobanian, Harry R ; Miller, Michael W ; Souza, Sarah ; Thomas-Fowlkes, Brande S ; Ogawa, Aimie M ; Weinglass, Adam B ; Di Salvo, Jerry ; Li, Xiaoyan ; Feng

PloS one, 2017, Vol.12(10), pp.e0186033 [Peer Reviewed Journal]

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G-protein-coupled estrogen receptor agonist suppresses airway inflammation in a mouse model of asthma through IL-10

Itoga, Masamichi ; Konno, Yasunori ; Moritoki, Yuki ; Saito, Yukiko ; Ito, Wataru ; Tamaki, Mami ; Kobayashi, Yoshiki ; Kayaba, Hiroyuki ; Kikuchi, Yuta ; Chihara, Junichi ; Takeda, Masahide ; Ueki, Shigeharu ; Hirokawa, Makoto

PloS one, 2015, Vol.10(3), pp.e0123210 [Peer Reviewed Journal]

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15
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A GPBAR1 (TGR5) small molecule agonist shows specific inhibitory effects on myeloid cell activation in vitro and reduces experimental autoimmune encephalitis (EAE) in vivo

Lewis, Nuruddeen D ; Patnaude, Lori A ; Pelletier, Josephine ; Souza, Donald J ; Lukas, Susan M ; King, F James ; Hill, Jonathan D ; Stefanopoulos, Dimitria E ; Ryan, Kelli ; Desai, Sudha ; Skow, Donna ; Kauschke, Stefan G ; Broermann, Andre ; Kuzmich, Daniel ; Harcken, Christian ; Hickey, Eugene R ; Modis, Louise K

PloS one, 2014, Vol.9(6), pp.e100883 [Peer Reviewed Journal]

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16
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Synthesis and characterization of tricarbonyl-Re/Tc(I) chelate probes targeting the G protein-coupled estrogen receptor GPER/GPR30

Burai, Ritwik ; Ramesh, Chinnasamy ; Nayak, Tapan K ; Dennis, Megan K ; Bryant, Bj K ; Prossnitz, Eric R ; Arterburn, Jeffrey B

PloS one, 2012, Vol.7(10), pp.e46861 [Peer Reviewed Journal]

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17
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AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents

Lin, Daniel C-H ; Zhang, Jane ; Zhuang, Run ; Li, Frank ; Nguyen, Kathy ; Chen, Michael ; Tran, Thanhvien ; Lopez, Edwin ; Lu, Jenny Ying Lin ; Li, Xiaoyan Nina ; Tang, Liang ; Tonn, George R ; Swaminath, Gayathri ; Reagan, Jeff D ; Chen, Jin-Long ; Tian, Hui ; Lin, Yi-Jyun ; Houze, Jonathan B ; Luo, Jian

PloS one, 2011, Vol.6(11), pp.e27270 [Peer Reviewed Journal]

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18
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High-throughput screening for GPR119 modulators identifies a novel compound with anti-diabetic efficacy in db/db mice

Zhang, Meng ; Feng, Yang ; Wang, Jia ; Zhao, Jianwei ; Li, Ting ; He, Min ; Yang, Dehua ; Nosjean, Olivier ; Boutin, Jean ; Renard, Pierre ; Wang, Ming-Wei

PloS one, 2013, Vol.8(5), pp.e63861 [Peer Reviewed Journal]

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19
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Chronic activation of the G protein-coupled receptor 30 with agonist G-1 attenuates heart failure

Kang, Shoulei ; Liu, Ying ; Sun, Di ; Zhou, Chunle ; Liu, Aiying ; Xu, Chuanying ; Hao, Yanling ; Li, Dongye ; Yan, Changdong ; Sun, Hong

PloS one, 2012, Vol.7(10), pp.e48185 [Peer Reviewed Journal]

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20
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Improvement of vascular function by acute and chronic treatment with the GPR30 agonist G1 in experimental diabetes mellitus

Li, Zi-Lin ; Liu, Jin-Cheng ; Liu, Shui-Bing ; Li, Xiao-Qiang ; Yi, Ding-Hua ; Zhao, Ming-Gao

PloS one, 2012, Vol.7(6), pp.e38787 [Peer Reviewed Journal]

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21
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The acute glucose lowering effect of specific GPR120 activation in mice is mainly driven by glucagon-like peptide 1

Sundström, Linda ; Myhre, Susanna ; Sundqvist, Monika ; Ahnmark, Andrea ; Mccoull, William ; Raubo, Piotr ; Groombridge, Sam D ; Polla, Magnus ; Nyström, Ann-Christin ; Kristensson, Lisbeth ; Någård, Mats ; Winzell, Maria Sörhede

PloS one, 2017, Vol.12(12), pp.e0189060 [Peer Reviewed Journal]

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22
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A New Signaling Pathway for HCV Inhibition by Estrogen: GPR30 Activation Leads to Cleavage of Occludin by MMP-9

Ulitzky, Laura ; Lafer, Manuel M ; Kukuruga, Mark A ; Silberstein, Erica ; Cehan, Nicoleta ; Taylor, Deborah R

PloS one, 2016, Vol.11(1), pp.e0145212 [Peer Reviewed Journal]

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23
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3,5-Dihydroxybenzoic acid, a specific agonist for hydroxycarboxylic acid 1, inhibits lipolysis in adipocytes

Liu, Changlu ; Kuei, Chester ; Zhu, Jessica ; Yu, Jingxue ; Zhang, Li ; Shih, Amy ; Mirzadegan, Taraneh ; Shelton, Jonathan ; Sutton, Steven ; Connelly, Margery A ; Lee, Grace ; Carruthers, Nicholas ; Wu, Jiejun ; Lovenberg, Timothy W

The Journal of pharmacology and experimental therapeutics, June 2012, Vol.341(3), pp.794-801 [Peer Reviewed Journal]

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24
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Phenobarbital and Insulin Reciprocate Activation of the Nuclear Receptor Constitutive Androstane Receptor through the Insulin Receptor

Yasujima, Tomoya ; Saito, Kosuke ; Moore, Rick ; Negishi, Masahiko

The Journal of pharmacology and experimental therapeutics, May 2016, Vol.357(2), pp.367-74 [Peer Reviewed Journal]

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25
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Discovery and validation of novel peptide agonists for G-protein-coupled receptors

Shemesh, Ronen ; Toporik, Amir ; Levine, Zurit ; Hecht, Iris ; Rotman, Galit ; Wool, Assaf ; Dahary, Dvir ; Gofer, Eyal ; Kliger, Yossef ; Soffer, Michal Ayalon ; Rosenberg, Avi ; Eshel, Dani ; Cohen, Yossi

The Journal of biological chemistry, 12 December 2008, Vol.283(50), pp.34643-9 [Peer Reviewed Journal]

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26
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Superagonism at G protein-coupled receptors and beyond

Schrage, R ; De Min, A ; Hochheiser, K ; Kostenis, E ; Mohr, K

British journal of pharmacology, October 2016, Vol.173(20), pp.3018-27 [Peer Reviewed Journal]

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27
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Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40

Lu, Jun ; Byrne, Noel ; Wang, John ; Bricogne, Gerard ; Brown, Frank K ; Chobanian, Harry R ; Colletti, Steven L ; Di Salvo, Jerry ; Thomas-Fowlkes, Brande ; Guo, Yan ; Hall, Dawn L ; Hadix, Jennifer ; Hastings, Nicholas B ; Hermes, Jeffrey D ; Ho, Thu ; Howard, Andrew D ; Josien, Hubert ; Kornienko, Maria ; Lumb, Kevin J ; Miller

Nature structural & molecular biology, July 2017, Vol.24(7), pp.570-577 [Peer Reviewed Journal]

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28
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A novel method for analyzing extremely biased agonism at G protein-coupled receptors

Stahl, Edward L ; Zhou, Lei ; Ehlert, Frederick J ; Bohn, Laura M

Molecular pharmacology, May 2015, Vol.87(5), pp.866-77 [Peer Reviewed Journal]

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29
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Molecular pharmacology of G protein-coupled receptors

Summers, R J

British journal of pharmacology, October 2016, Vol.173(20), pp.2931-3 [Peer Reviewed Journal]

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30
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Safety and Pharmacokinetics of DS-8500a, a Novel GPR119 Agonist, After Multiple Oral Doses in Healthy Japanese Males

Kato, Manabu ; Furuie, Hidetoshi ; Kamiyama, Emi ; Shiosakai, Kazuhito ; Yoshihara, Kazutaka ; Taguchi, Takashi

Clinical drug investigation, June 2018, Vol.38(6), pp.519-525 [Peer Reviewed Journal]

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31
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Quantitative Measure of Receptor Agonist and Modulator Equi-Response and Equi-Occupancy Selectivity

Zhang, Rumin ; Kavana, Michael

Scientific reports, 27 April 2016, Vol.6, pp.25158 [Peer Reviewed Journal]

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32
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Advances in Computational Techniques to Study GPCR-Ligand Recognition

Ciancetta, Antonella ; Sabbadin, Davide ; Federico, Stephanie ; Spalluto, Giampiero ; Moro, Stefano

Trends in pharmacological sciences, December 2015, Vol.36(12), pp.878-890 [Peer Reviewed Journal]

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33
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Avenues for the development of therapeutics that target trace amine associated receptor 1 (TAAR1)

Miller, Gregory M

Journal of medicinal chemistry, 08 March 2012, Vol.55(5), pp.1809-14 [Peer Reviewed Journal]

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34
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Identification of the GPR55 agonist binding site using a novel set of high-potency GPR55 selective ligands

Kotsikorou, Evangelia ; Madrigal, Karla E ; Hurst, Dow P ; Sharir, Haleli ; Lynch, Diane L ; Heynen-Genel, Susanne ; Milan, Loribelle B ; Chung, Thomas D Y ; Seltzman, Herbert H ; Bai, Yushi ; Caron, Marc G ; Barak, Larry ; Abood, Mary E ; Reggio, Patricia H

Biochemistry, 28 June 2011, Vol.50(25), pp.5633-47 [Peer Reviewed Journal]

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35
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Tactical Approaches to Interconverting GPCR Agonists and Antagonists

Dosa, Peter I ; Amin, Elizabeth Ambrose

Journal of medicinal chemistry, 11 February 2016, Vol.59(3), pp.810-40 [Peer Reviewed Journal]

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36
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Allosteric modulation and functional selectivity of G protein-coupled receptors

Gao, Zhan-Guo ; Jacobson, Kenneth A

Drug discovery today. Technologies, 2013, Vol.10(2), pp.e237-43 [Peer Reviewed Journal]

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37
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When simple agonism is not enough: emerging modalities of GPCR ligands

Smith, Nicola J ; Bennett, Kirstie A ; Milligan, Graeme

Molecular and cellular endocrinology, 15 January 2011, Vol.331(2), pp.241-7 [Peer Reviewed Journal]

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