Article
Biochemistry & Molecular Biology
Hiroyuki Mizuguchi, Yuko Miyamoto, Takuma Terao, Haruka Yoshida, Wakana Kuroda, Yoshiaki Kitamura, Noriaki Takeda, Hiroyuki Fukui
Summary: Research reveals that histamine induces upregulation of the H1R gene in U-373 MG cells through activation of the PKC δ signaling pathway, with distinct molecular mechanisms and kinetics compared to HeLa cells. This suggests that compounds targeting PKC δ could potentially serve as peripheral type H1R-selective inhibitors without sedative effects.
CURRENT ISSUES IN MOLECULAR BIOLOGY
(2021)
Article
Pharmacology & Pharmacy
Iris Lim, Caio Christiansen, Russ Chess-Williams
Summary: This study aimed to investigate the effects of 17β-estradiol (E2) on ureteral contractility. The results showed that E2 increased the frequency of ureteral contractions through G protein-coupled estrogen receptor activation of potassium channels, while also decreasing the maximum amplitude of contractions via an unknown mechanism.
EUROPEAN 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.
Review
Cell Biology
Haoran Jiang, Daniella Galtes, Jialu Wang, Howard A. Rockman
Summary: This review explores the signaling pathways, dynamic structures, and physiological relevance of the three most important GPCR signaling effectors in the cardiovascular system: heterotrimeric G proteins, GPCR kinases (GRKs), and 8-arrestins. It summarizes their prominent roles in GPCR pharmacology before transitioning into less well-explored areas. The application of new technologies has contributed to an increasing understanding of GPCR structure and downstream effectors.
AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY
(2022)
Review
Pharmacology & Pharmacy
Nathalie Fuentes, Morgan McCullough, Reynold A. Panettieri, Kirk M. Druey
Summary: Asthma is a prevalent disorder characterized by chronic lung inflammation and reversible airways obstruction, with features including increased airway narrowing, excessive mucus secretion, airway remodeling, and airways hyperresponsiveness. Environmental factors such as allergens, viruses, and air pollution can promote asthma, leading to symptoms like cough, wheezing, and shortness of breath. G-protein-coupled receptors play a central role in asthma, with various treatments targeting these receptors to regulate airway smooth muscle tone and lung inflammation.
PHARMACOLOGY & THERAPEUTICS
(2021)
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
Multidisciplinary Sciences
Ruixue Xia, Na Wang, Zhenmei Xu, Yang Lu, Jing Song, Anqi Zhang, Changyou Guo, Yuanzheng He
Summary: The authors used cryo-EM to determine the complex structure of histamine-bound H1R/Gq and proposed a mechanism for ligand-induced receptor activation, providing insights for designing novel antihistamines.
NATURE COMMUNICATIONS
(2021)
Article
Multidisciplinary Sciences
Li Cheng, Cenglin Xu, Lu Wang, Dadao An, Lei Jiang, Yanrong Zheng, Yixin Xu, Yi Wang, Yujing Wang, Kuo Zhang, Xiaodong Wang, Xiangnan Zhang, Aimin Bao, Yudong Zhou, Jingyu Yang, Shumin Duan, Dick F. Swaab, Weiwei Hu, Zhong Chen
Summary: This study indicates that the deficiency of histamine H-1 receptor in cholinergic neurons in the basal forebrain is critical for sensorimotor gating deficit, social impairments, and anhedonia-like behavior in patients with schizophrenia. Deletion of the H1R gene in cholinergic neurons in mice resulted in functional deficiency of cholinergic projections and led to behavioral deficits, which could be rescued by re-expressing H1R or by chemogenetic activation of cholinergic neurons in the BF.
NATURE COMMUNICATIONS
(2021)
Article
Biochemistry & Molecular Biology
Eleonore W. E. Verweij, Reggie Bosma, Meichun Gao, Jelle van den Bor, Betty Al Araaj, Sabrina M. de Munnik, Xiaoyuan Ma, Rob Leurs, Henry F. Vischer
Summary: This study used bioluminescence resonance energy transfer (BRET)-based biosensors to measure the effects of different agonists on the H1R signaling pathway, and found that one of the agonists exhibited biased agonism.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Cell Biology
Abigail R. Walker, Camilla B. Larsen, Samit Kundu, Christina Stavrinidis, Sung Hye Kim, Asuka Inoue, David F. Woodward, Yun S. Lee, Roberta Migale, David A. Macntyre, Vasso Terzidou, Francesca Fanelli, Shirin Khanjani, Philip R. Bennet, Aylin C. Hanyaloglu
Summary: Current strategies to manage preterm labor focus on inhibiting uterine contractions, but do not improve neonatal outcomes. This study identifies a mechanism in which activated oxytocin receptor reprograms prostaglandin E2 receptor to promote pro-labor/inflammatory responses during human labor. It suggests a potential therapeutic solution by exploiting the functional associations between these receptors to delay preterm labor.
Article
Biochemistry & Molecular Biology
Julian A. Harris, Bryan Faust, Arisbel B. Gondin, Marc Andre Damgen, Carl-Mikael Suomivuori, Nicholas A. Veldhuis, Yifan Cheng, Ron O. Dror, David M. Thal, Aashish Manglik
Summary: The neuropeptide substance P activates the neurokinin-1 receptor through interactions deep within the receptor, while interactions between the neuropeptide and the receptor extracellular loops regulate G protein signaling selectivity. This study sheds light on how different stimuli can lead to distinct G protein signaling at the same receptor.
NATURE CHEMICAL BIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Diana Zindel, Patrick Mensat, Claire Vol, Zeinab Homayed, Fabienne Charrier-Savournin, Eric Trinquet, Jean-Louis Baneres, Jean-Philippe Pin, Julie Pannequin, Thomas Roux, Elodie Dupuis, Laurent Prezeau
Summary: The Hippo pathway is a key kinase cascade that regulates tissue homeostasis, cellular differentiation, and organ size. By studying the ghrelin receptor, a GPCR that activates Gq exclusively, researchers have shown that GPCRs can finely modulate YAP activity through the Gq pathway.
Article
Multidisciplinary Sciences
Li-Hua Zhao, Jingyu Lin, Su-Yu Ji, X. Edward Zhou, Chunyou Mao, Dan-Dan Shen, Xinheng He, Peng Xiao, Jinpeng Sun, Karsten Melcher, Yan Zhang, Xiao Yu, H. Eric Xu
Summary: This study presents the structures of CRF2R bound to UCN1 and coupled to G proteins G(11) and G(o), and compares them with the structure of CRF2R bound to G(s), uncovering the structural differences that determine the selective coupling of G protein subtypes by CRF2R.
NATURE COMMUNICATIONS
(2022)
Article
Cell Biology
Asma S. A. Alonazi, Jonathon M. Willets
Summary: Hypertension is associated with increased signaling through vasoconstrictor G protein-coupled receptors, leading to vascular smooth muscle cell proliferation and arterial contraction, contributing to the development of atherosclerosis and vascular remodeling. GRK2 expression is essential for promoting efficient PI3K-Akt signaling and facilitating vasoconstrictor-driven VSMC proliferation, highlighting its potential role in exacerbating hypertensive vascular remodeling.
CELLULAR SIGNALLING
(2021)
Article
Immunology
Shangze Gao, Keyue Liu, Wenhan Ku, Dengli Wang, Hidenori Wake, Handong Qiao, Kiyoshi Teshigawara, Masahiro Nishibori
Summary: Histamine induces the release of HMGB1 from vascular endothelial cells through H-1 receptor stimulation, and anti-HMGB1 therapy may provide a novel treatment for systemic allergies.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Cell Biology
Jonathon M. Willets, Craig A. Nash, Richard D. Rainbow, Carl P. Nelson, R. A. John Challiss
AMERICAN JOURNAL OF PHYSIOLOGY-CELL PHYSIOLOGY
(2015)
Editorial Material
Pharmacology & Pharmacy
Gary B. Willars, Andrew B. Tobin, R. A. John Challiss
BRITISH JOURNAL OF PHARMACOLOGY
(2015)
Article
Multidisciplinary Sciences
Jennifer L. Brignell, Matthew D. Perry, Carl P. Nelson, Jonathon M. Willets, R. A. John Challiss, Noel W. Davies
Article
Respiratory System
David Sweeney, Fay Hollins, Edith Gomez, Rajendra Mistry, Ruth Saunders, Robert Alfred John Challiss, Christopher Edward Brightling
BMC PULMONARY MEDICINE
(2015)
Article
Pharmacology & Pharmacy
Robert Jackson, Sean Brennan, Peter Fielding, Mark W. Sims, R. A. John Challiss, David Adlam, Iain B. Squire, Richard D. Rainbow
BRITISH JOURNAL OF PHARMACOLOGY
(2016)
Article
Biochemistry & Molecular Biology
Adrian J. Butcher, Sophie J. Bradley, Rudi Prihandoko, Simon M. Brooke, Adrian Mogg, Julie-Myrtille Bourgognon, Timothy Macedo-Hatch, Jennifer M. Edwards, Andrew R. Bottrill, R. A. John Challiss, Lisa M. Broad, Christian C. Felder, Andrew B. Tobin
JOURNAL OF BIOLOGICAL CHEMISTRY
(2016)
Letter
Allergy
Leonarda Di Candia, Edith Gomez, Emilie Venereau, Latifa Chachi, Davinder Kaur, Marco E. Bianchi, R. A. John Challiss, Christopher E. Brightling, Ruth M. Saunders
JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY
(2017)
Article
Pharmacology & Pharmacy
Khaled Alhosaini, Omar Bahattab, Heider Qassam, R. A. John Challiss, Gary B. Willars
MOLECULAR PHARMACOLOGY
(2018)
Article
Pharmacology & Pharmacy
Richard D. Rainbow, Sean Brennan, Robert Jackson, Alison J. Beech, Amal Bengreed, Helen Waldschmidt, John J. G. Tesmer, R. A. John Challiss, Jonathon M. Willets
MOLECULAR PHARMACOLOGY
(2018)
Article
Biochemistry & Molecular Biology
Susan W. Robinson, Julie-Myrtille Bourgognon, Jereme G. Spiers, Carlo Breda, Susanna Campesan, Adrian Butcher, Giovanna R. Mallucci, David Dinsdale, Nobuhiro Morone, Raj Mistry, Tim M. Smith, Maria Guerra-Martin, R. A. John Challiss, Flaviano Giorgini, Joern R. Steinert
Article
Cell Biology
Craig A. Nash, Carl P. Nelson, Rajendra Mistry, Christian Moeller-Olsen, Elena Christofidou, R. A. John Challiss, Jonathon M. Willets
CELLULAR SIGNALLING
(2018)
Article
Biochemistry & Molecular Biology
Sophie J. Bradley, Colin Molloy, Paulina Valuskova, Louis Dwomoh, Miriam Scarpa, Mario Rossi, Lisa Finlayson, Kjell A. Svensson, Eyassu Chernet, Vanessa N. Barth, Karolina Gherbi, David A. Sykes, Caroline A. Wilson, Rajendra Mistry, Patrick M. Sexton, Arthur Christopoulos, Adrian J. Mogg, Elizabeth M. Rosethorne, Shuzo Sakata, R. A. John Challiss, Lisa M. Broad, Andrew B. Tobin
NATURE CHEMICAL BIOLOGY
(2020)
Article
Pharmacology & Pharmacy
Xianguo Jiang, John Challiss, Paul Glynn
BIOCHEMICAL PHARMACOLOGY
(2020)
Article
Engineering, Multidisciplinary
S. B. Olsson, R. A. J. Challiss, M. Cole, J. G. E. Gardeniers, J. W. Gardner, A. Guerrero, B. S. Hansson, T. C. pearce
BIOINSPIRATION & BIOMIMETICS
(2015)
Article
Pharmacology & Pharmacy
David M. Pier, George S. G. Shehatou, Susan Giblett, Christine E. Pullar, Derek J. Trezise, Catrin A. Pritchard, R. A. John Challiss, John S. Mitcheson
MOLECULAR PHARMACOLOGY
(2014)