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)
Article
Biochemistry & Molecular Biology
Carina Hoering, Marcus Conrad, Christian A. Soldner, Jinan Wang, Heinrich Sticht, Andrea Strasser, Yinglong Miao
Summary: In this study, the coupling profiles of histamine receptors H2R and H4R to engineered mini-G proteins were investigated using cellular experimental assays and Gaussian accelerated molecular dynamics (GaMD) simulations. The results revealed that H2R and H4R preferentially bind to different types of G proteins, providing insights into the signaling mechanisms of histamine receptors.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Shingo Nojima, Yoko Fujita, Kanako Terakado Kimura, Norimichi Nomura, Ryoji Suno, Kazushi Morimoto, Masaki Yamamoto, Takeshi Noda, So Iwata, Hideki Shigematsu, Takuya Kobayashi
Summary: EP4, a class A GPCR, is a common drug target in various disorders. The structure features of EP4-Gs binding are formed by specific conserved residues, which may be important for understanding the binding mechanism of G protein.
Article
Pharmacology & Pharmacy
Joachim Neumann, Rafaela Voss, Ulrich Laufs, Christian Werner, Ulrich Gergs
Summary: Histamine exerts cAMP-dependent positive inotropic effects (PIE) on the left and right atria of transgenic mice which overexpress the human H-2-receptor, with PDE 3 and PDE 4 regulating the effects on inotropic response, while PDE 2 and PDE 4 play a role in regulating the positive chronotropic effects on heart beat rate.
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
(2021)
Review
Pharmacology & Pharmacy
Xiaoqing Guo, Qin Li, Shulan Pi, Yuanpeng Xia, Ling Mao
Summary: P2Y receptors are a critical group of G protein-coupled receptors that signal through dimers, playing diverse roles in physiology and pathology. Research has shown the significance of dimerization between P2Y receptors and other receptors in cardiovascular and cerebrovascular processes.
BIOCHEMICAL PHARMACOLOGY
(2021)
Article
Pharmacology & Pharmacy
Lyndsay R. Watkins, Cesare Orlandi
Summary: Members of the GPCR family, including many less-studied orphan receptors, play important physiological roles and serve as attractive drug targets. A novel approach has been developed to detect G protein coupling in unliganded orphan GPCRs, shedding light on the pathophysiological processes associated with certain orphan receptors. This platform provides a valuable tool for ongoing studies in orphan receptor signalling and de-orphanization efforts.
BRITISH JOURNAL OF PHARMACOLOGY
(2021)
Review
Chemistry, Medicinal
Joachim Neumann, Britt Hofmann, Uwe Kirchhefer, Stefan Dhein, Ulrich Gergs
Summary: Histamine can affect cardiac contraction force and beating rate in mammals, including humans, but there are significant differences between species and regions. The mammalian heart produces and contains histamine, which may have autocrine or paracrine effects. Cardiomyocytes express histamine receptors, including H-1 and H-2, but their functional role is not fully understood. This review aims to identify gaps in knowledge and highlight the potential of histamine H-1 receptors as therapeutic targets in the human heart, particularly in diseases.
Article
Pharmacology & Pharmacy
Andrea N. Beltran Gonzalez, Manuel I. Lopez Pazos, Mariana del Vas, Daniel J. Calvo
Summary: Histamine can function as a neurotransmitter and neuromodulator in addition to its role as a mediator of the immune response. It was previously shown to act as a positive modulator on various GABAA receptor subtypes, but its effects on GABA(A)rho 1 receptors had not been studied. This research demonstrated that histamine inhibits GABAA.1 receptor-mediated responses through competitive antagonism on GABA(A rho)1 receptors.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Kamil J. Kuder, Magdalena Kotanska, Katarzyna Szczepanska, Kamil Mika, David Reiner-Link, Holger Stark, Katarzyna Kiec-Kononowicz
Summary: Researchers designed a series of dual acting histamine H-3 receptor ligands, with compound 16 demonstrating strong antioxidant properties and moderate hH(3)R affinity. These compounds could serve as potential tools for treating neurological disorders.
Article
Cell Biology
Laura M. Chamness, Nathan B. Zelt, Haley R. Harrington, Charles P. Kuntz, Brian J. Bender, Wesley D. Penn, Joshua J. Ziarek, Jens Meiler, Jonathan P. Schlebach
Summary: Mammalian forms of the gonadotropin-releasing hormone receptor exhibit apparent instability due to specific residue variations, affecting membrane integration and function. Evolutionary trends suggest that changes in residue polarity track with reproductive phenotypes, highlighting the importance of cotranslational folding in tuning membrane protein fitness.
Article
Genetics & Heredity
Min Li, Yuting Cao, Biswojit Debnath, Hongjuan Yang, Xiaohua Kui, Dongliang Qiu
Summary: In this study, the full-length cDNA sequence of F3'5'H gene from Brunfelsia acuminata was obtained, and its protein characteristics were analyzed. Real-time quantitative PCR analysis showed differential expression of the gene in petals on different days.
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
Multidisciplinary Sciences
Margaret Driscoll, Steven N. Buchert, Victoria Coleman, Morgan McLaughlin, Amanda Nguyen, Divya Sitaraman
Summary: Sleep is an important behavioral state regulated by biogenic amines across species, but the precise neurocircuitry underlying how amines control sleep, arousal, and wakefulness remains unclear. Investigating the neural circuits in fruit flies provides insight into the balance of sleep, wakefulness, and arousal in organisms.
SCIENTIFIC REPORTS
(2021)
Review
Biochemistry & Molecular Biology
Jace Jones-Tabah
Summary: Parkinson's disease (PD) is a progressive neurodegenerative disease characterized by the deterioration of dopaminergic neurons and motor impairment. Although there is no cure for PD, dopamine replacement therapies like L-DOPA can alleviate motor symptoms. However, non-motor symptoms and the progression of neurodegeneration still lack effective treatments. This review focuses on G protein-coupled receptors (GPCRs) as potential targets for treating PD and discusses various therapeutic strategies.
JOURNAL OF MOLECULAR BIOLOGY
(2023)
Article
Chemistry, Medicinal
Steffen Pockes, Katharina Tropmann
Summary: Radioligands have been a powerful tool in investigating the histamine H-2 receptor (H2R) and its functions, with tritium labeling primarily used for in vitro assays and carbon-14 labeling preferred for metabolic studies. The recent development of a G protein-biased radioligand represents a step forward in understanding the potentially unknown role of H2R in the central nervous system through future studies.
FUTURE MEDICINAL CHEMISTRY
(2021)