Article
Pharmacology & Pharmacy
Nicole B. Servant, Mark E. Williams, Paul F. Brust, Huixian Tang, Melissa S. Wong, Qing Chen, Marketa Lebl-Rinnova, Sara L. Adamski-Werner, Catherine Tachdjian, Guy Servant
Summary: The sweet taste receptor is unique and complex, and it is still unclear if different cell-based assays can accurately report its molecular potency and efficacy. A new assay for the human sweet taste receptor was developed in this study, revealing that non-physiological coupling can influence the potency and efficacy of sweet taste receptor ligands.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Multidisciplinary Sciences
Lisa Forster, Steffen Pockes
Summary: In this study, the successful application of DMR technology to CHO-Kl cells expressing the human dopamine D-2(long) receptor was reported. The results showed that DMR can be used to characterize D2R ligands and distinguish different types of agonists. Furthermore, the study identified G alpha(i/o) protein as the main trigger of the observed DMR response, highlighting the importance of DMR technology in GPCR research.
SCIENTIFIC REPORTS
(2022)
Article
Chemistry, Multidisciplinary
Bettina Lengger, Emma E. Hoch-Schneider, Christina N. Jensen, Tadas Jakociunas, Anja A. Petersen, Thomas M. Frimurer, Emil Jensen, Michael K. Jensen
Summary: This study systematically assessed the signaling of various serotonin GPCRs and successfully achieved high-resolution quantification of serotonin using a yeast platform. The study also characterized serotonin GPCR polymorphisms in human populations and observed differences in signaling among these polymorphisms.
Article
Biology
Annemarie Boleij, Payam Fathi, William Dalton, Ben Park, Xinqun Wu, David Huso, Jawara Allen, Sepideh Besharati, Robert A. Anders, Franck Housseau, Amanda E. Mackenzie, Laura Jenkins, Graeme. Milligan, Shaoguang Wu, Cynthia L. Sears
Summary: GPR35 plays a crucial role in the response of colonic epithelial cells to BFT, and GPR35 deficiency can reduce the mortality and disease severity induced by ETBF in mice.
COMMUNICATIONS BIOLOGY
(2021)
Review
Pharmacology & Pharmacy
Rina Pokhrel, Alexandra L. Morgan, Harley R. Robinson, Martin J. Stone, Simon R. Foster
Summary: G protein-coupled receptor (GPCR) activation triggers complex intracellular signalling networks, which have important implications for receptor biology and drug discovery. Phosphoproteomics has emerged as a powerful tool for investigating these networks and accelerating the discovery of new therapeutic targets.
BRITISH JOURNAL OF PHARMACOLOGY
(2023)
Article
Chemistry, Medicinal
Li-Chiung Lin, Tezz Quon, Susanna Engberg, Amanda E. Mackenzie, Andrew B. Tobin, Graeme Milligan
Summary: Experimental studies using various mouse models and a humanized GPR35 mouse model suggest that activation of the GPR35 receptor can effectively prevent and reverse lipid accumulation induced by liver X receptor stimulation. This finding highlights the potential value of targeting GPR35 in the treatment of fatty liver diseases.
ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE
(2021)
Article
Biochemistry & Molecular Biology
Nina Divorty, Laura Jenkins, Amlan Ganguly, Adrian J. Butcher, Brian D. Hudson, Stefan Schulz, Andrew B. Tobin, Stuart A. Nicklin, Graeme Milligan
Summary: G protein-coupled receptor 35 (GPR35) plays diverse roles in lower gut inflammation and pain. The phosphorylation of specific sites in GPR35a is crucial for its interaction with arrestin-3 and the internalization of the receptor. Phospho-site-specific antisera can effectively detect the activation status of GPR35 and be used in drug discovery and target validation programs.
JOURNAL OF BIOLOGICAL CHEMISTRY
(2022)
Article
Peripheral Vascular Disease
Hainan Li, Huong Nguyen, Sai Pranathi Meda Venkata, Jia Yi Koh, Anjaneyulu Kowluru, Li Li, Noreen F. Rossi, Wei Chen, Jie-Mei Wang
Summary: Inhibition of GPR35 was found to enhance endothelial cell functions and promote angiogenesis while reducing intracellular superoxide levels, resulting in improved vasodilation and decreased blood pressure in male mice. These findings suggest that antagonizing GPR35 activity could be a potential therapeutic approach to restore endothelial function and maintain hemodynamic homeostasis, particularly in the context of hypertension.
Article
Neurosciences
Sam R. J. Hoare, Paul H. Tewson, Shivani Sachdev, Mark Connor, Thomas E. Hughes, Anne Marie Quinn
Summary: Neurons integrate inputs over different time and space scales, combining fast and slow signals to produce behavior. Measuring signaling kinetics in live cells using fluorescent biosensors and dyes provides a deeper understanding of G-protein-coupled receptor signaling and therapeutic mechanisms in the nervous system.
FRONTIERS IN CELLULAR NEUROSCIENCE
(2022)
Review
Biochemistry & Molecular Biology
Libin Ye, Xudong Wang, Aidan McFarland, Jesper J. Madsen
Summary: Advances in X-ray crystallography and cryoelectron microscopy have provided insights into GPCR activation processes, but these static structures have limitations in revealing dynamics and conformational transitions. Developing NMR techniques can lead to a more comprehensive understanding of signaling processes, but challenges remain.
Article
Pharmacology & Pharmacy
Estefania Moreno, Nil Casajuana-Martin, Michael Coyle, Baruc Campos Campos, Ewa Galaj, Claudia Llinas del Torrent, Arta Seyedian, William Rea, Ning-Sheng Cai, Alessandro Bonifazi, Benjamin Floran, Zheng-Xiong Xi, Xavier Guitart, Vicent Casado, Amy H. Newman, Christopher Bishop, Leonardo Pardo, Sergi Ferre
Summary: This study provides evidence that heteromerization of G protein-coupled receptors (GPCRs), specifically dopamine D1 and D3 receptors, can influence the pharmacological properties of selective ligands. In vivo experiments support the involvement of D1R-D3R heteromers in the development of L-DOPA-induced dyskinesia in Parkinson's disease, suggesting the potential of targeting GPCR heteromers for drug development.
PHARMACOLOGICAL RESEARCH
(2022)
Article
Pharmacology & Pharmacy
Stephen P. H. Alexander, Arthur Christopoulos, Anthony P. Davenport, Eamonn Kelly, Alistair Mathie, John A. Peters, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Adam J. Pawson, Christopher Southan, Jamie A. Davies, Maria Pia Abbracchio, Wayne Alexander, Khaled Al-hosaini, Magnus Baeck, Nicholas M. Barnes, Ross Bathgate, Jean-Martin Beaulieu, Kenneth E. Bernstein, Bernhard Bettler, Nigel J. M. Birdsall, Victoria Blaho, Francois Boulay, Corinne Bousquet, Hans Braeuner-Osborne, Geoffrey Burnstock, Girolamo Calo, Justo P. Castano, KevinJ Catt, Stefania Ceruti, Paul Chazot, Nan Chiang, Bice Chini, Jerold Chun, Antonia Cianciulli, Olivier Civelli, Lucie H. Clapp, Rejean Couture, Zsolt Csaba, Claes Dahlgren, Gordon Dent, Khuraijam Dhanachandra Singh, Steven D. Douglas, Pascal Dournaud, Satoru Eguchi, Emanuel Escher, Edward J. Filardo, Tung Fong, Marta Fumagalli, Raul R. Gainetdinov, Marc de Gasparo, Craig Gerard, Marvin Gershengorn, Fernand Gobeil, Theodore L. Goodfriend, Cyril Goudet, Karen J. Gregory, Andrew L. Gundlach, Joerg Hamann, Julien Hanson, Richard L. Hauger, Debbie L. Hay, Akos Heinemann, Morley D. Hollenberg, Nicholas D. Holliday, Mastgugu Horiuchi, Daniel Hoyer, Laszlo Hunyady, Ahsan Husain, Adriaan P. IJzerman, Tadashi Inagami, Kenneth A. Jacobson, Robert T. Jensen, Ralf Jockers, Deepa Jonnalagadda, Sadashiva Karnik, Klemens Kaupmann, Jacqueline Kemp, Charles Kennedy, Yasuyuki Kihara, Takio Kitazawa, Pawel Kozielewicz, Hans-Juergen Kreienkamp, Jyrki P. Kukkonen, Tobias Langenhan, Katie Leach, Davide Lecca, John D. Lee, Susan E. Leeman, Jerome Leprince, Xaria X. Li, Tom Lloyd Williams, Stephen J. Lolait, Amelie Lupp, Robyn Macrae, Janet Maguire, Jean Mazella, Craig A. McArdle, Shlomo Melmed, Martin C. Michel, Laurence J. Miller, Vincenzo Mitolo, Bernard Mouillac, Christa E. Mueller, Philip Murphy, Jean-Louis Nahon, Tony Ngo, Xavier Norel, Duuamene Nyimanu, Anne-Marie Ocarroll, Stefan Offermanns, Maria Antonietta Panaro, Marc Parmentier, Roger G. Pertwee, Jean-Philippe Pin, Eric R. Prossnitz, Mark Quinn, Rithwik Ramachandran, Manisha Ray, Rainer K. Reinscheid, Philippe Rondard, G. Enrico Rovati, Chiara Ruzza, Gareth J. Sanger, Torsten Schoeneberg, Gunnar Schulte, Stefan Schulz, Deborah L. Segaloff, Charles N. Serhan, Leigh A. Stoddart, Yukihiko Sugimoto, Roger Summers, Valerie P. Tan, David Thal, Walter (Wally) Thomas, PieterB M. W. M. Timmermans, Kalyan Tirupula, Giovanni Tulipano, Hamiyet Unal, Thomas Unger, Celine Valant, Patrick Vanderheyden, David Vaudry, Hubert Vaudry, Jean-Pierre Vilardaga, Christopher S. Walker, Ji Ming Wang, Donald T. Ward, Hans-Juergen Wester, Gary B. Willars, Trent M. Woodruff, Chengcan Yao, Richard D. Ye
Summary: The Concise Guide to PHARMACOLOGY 2021/22 presents concise overviews of nearly 1900 human drug targets with an emphasis on selective pharmacology, along with links to a more detailed knowledgebase. It serves as a permanent, citable record for researchers, providing useful information in the field of pharmacology.
BRITISH JOURNAL OF PHARMACOLOGY
(2021)
Review
Pharmacology & Pharmacy
Reid H. J. Olsen, Justin G. English
Summary: Enzymatic and cellular signaling biosensors are powerful tools for understanding complex biological systems. G protein-coupled receptors (GPCRs) are extensively studied using biosensors, which have expanded our knowledge of this important class of proteins. Transducer biosensors that measure receptor coupling and selectivity, with a focus on receptor association and activation of heterotrimeric signaling complexes, are of particular importance.
BRITISH JOURNAL OF PHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Nur Diyana Jamaluddin, Nur-Fadhilah Mazlan, Ling Ling Tan, Nurul Yuziana Mohd Yusof, Bahariah Khalid
Summary: In this study, an acrylic micropolymer-based RNA biosensor was developed to detect viral RNA using a G-quadruplex DNA probe. The biosensor showed a rapid response time and high sensitivity, allowing real-time detection of DENV2 in non-invasive human fluid samples.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2022)
Review
Pharmacology & Pharmacy
Mydirah Littlepage-Saunders, Michael J. Hochstein, Doris S. Chang, Kari A. Johnson
Summary: Dopamine transmission in the striatum is regulated by various G protein-coupled receptors (GPCRs) that bind neuromodulators, including dopamine itself. These GPCRs can modulate dopamine release by acting on different components of the dopaminergic circuitry and can have distinct effects on behavior and psychoactive drug actions. This review discusses the mechanisms by which GPCRs regulate dopaminergic transmission and their relevance to the effects of psychoactive drugs on physiology and behavior.
BRITISH JOURNAL OF PHARMACOLOGY
(2023)
Article
Chemistry, Analytical
Huayun Deng, Chaoming Wang, Ming Su, Ye Fang
ANALYTICAL CHEMISTRY
(2012)
Article
Physics, Applied
Ann M. Ferrie, Oberon D. Deichmann, Qi Wu, Ye Fang
APPLIED PHYSICS LETTERS
(2012)
Article
Biochemical Research Methods
Elizabeth Tran, Haiyan Sun, Ye Fang
ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES
(2012)
Article
Chemistry, Medicinal
Huayun Deng, Jieyu Hu, Haibei Hu, Mingqian He, Ye Fang
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2012)
Review
Pharmacology & Pharmacy
Ye Fang
EXPERT OPINION ON DRUG DISCOVERY
(2012)
Article
Biochemistry & Molecular Biology
Florence Verrier, Songon An, Ann M. Ferrie, Haiyan Sun, Minjoung Kyoung, Huayun Deng, Ye Fang, Stephen J. Benkovic
NATURE CHEMICAL BIOLOGY
(2011)
Article
Pharmacology & Pharmacy
Huayun Deng, Ye Fang
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
(2012)
Article
Pharmacology & Pharmacy
Huayun Deng, Ye Fang
Article
Multidisciplinary Sciences
Vasiliy Goral, Yan Jin, Haiyan Sun, Ann M. Ferrie, Qi Wu, Ye Fang
Article
Biochemistry & Molecular Biology
Huayun Deng, Ye Fang
Article
Chemistry, Medicinal
Huayun Deng, Ye Fang
ACS MEDICINAL CHEMISTRY LETTERS
(2012)
Article
Chemistry, Medicinal
Huayun Deng, Haibei Hu, Shizhang Ling, Ann M. Ferrie, Ye Fang
ACS MEDICINAL CHEMISTRY LETTERS
(2012)
Article
Multidisciplinary Sciences
Huayun Deng, Haibei Hu, Ye Fang
SCIENTIFIC REPORTS
(2012)
Article
Pharmacology & Pharmacy
Ye Fang
JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS
(2013)
Article
Biochemical Research Methods
Sadashiva Pai, Florence Verrier, Haiyan Sun, Haibei Hu, Ann M. Ferrie, Azita Eshraghi, Ye Fang
JOURNAL OF BIOMOLECULAR SCREENING
(2012)
