Article
Multidisciplinary Sciences
Matthew T. Dickerson, Prasanna K. Dadi, Karolina E. Zaborska, Arya Y. Nakhe, Charles M. Schaub, Jordyn R. Dobson, Nicole M. Wright, Joshua C. Lynch, Claire F. Scott, Logan D. Robinson, David A. Jacobson
Summary: The study demonstrates that G(i/o)-GPCRs hyperpolarize beta-cell membrane potential by activating Na+/K(+)ATPases, leading to decreased insulin secretion. NKAs play a crucial role in this process, regulating electrical excitability, Ca2+ handling, and insulin secretion through a NKA-mediated mechanism.
NATURE COMMUNICATIONS
(2022)
Article
Biochemistry & Molecular Biology
Mu Li, Xintong Zhang, Sixiang Chen, Hanhe Liu, Yuan-Wei Zhang
Summary: This study reveals a novel structural characteristic of the neurotransmitter sodium symporter (NSS) family, specifically in TuriSERT, and demonstrates the unique substrate binding site and 1:1 stoichiometry of sodium-substrate binding.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Kate Dunning, Adeline Martz, Francisco Andres Peralta, Federico Cevoli, Eric Boue-Grabot, Vincent Compan, Fanny Gautherat, Patrick Wolf, Thierry Chataigneau, Thomas Grutter
Summary: Activation of P2X7 receptors leads to various physiological responses, such as the secretion of pro-inflammatory cytokines and modulation of cell death. Current facilitation and macropore formation involve functional complexes that increase P2X7 open probability and mediate large molecule permeation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Karolina E. Kolaczynska, Jan Thomann, Marius C. Hoener, Matthias E. Liechti
Summary: Pyrovalerone cathinones are potent DAT and NET inhibitors with high selectivity, potentially leading to strong psychostimulant effects and high abuse liability.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
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)
Article
Multidisciplinary Sciences
Bo Hyun Lee, Bertil Hille, Duk-Su Koh
Summary: The pineal gland secretes melatonin at night, regulated by sympathetic nerve terminals. The secretion of 5-HT is primarily through a specific transporter, and activation of receptors on pinealocytes affects melatonin release.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2021)
Article
Multidisciplinary Sciences
Miriam Hernandez-Morales, Victor Han, Richard H. Kramer, Chunlei Liu
Summary: FeRIC is a magnetogenetic technique using RF alternating magnetic fields to activate TRPV channels and increase cytosolic Ca2+ levels. The interaction between RF and ferritin increases free cytosolic iron levels, triggering the activation of specific pathological channels.
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
Multidisciplinary Sciences
Xudong Wang, Chris Neale, Soo-Kyung Kim, William A. Goddard, Libin Ye
Summary: Understanding the roles of intermediate states in GPCR signaling is crucial for studying the activation processes. In this study, conformation-biased mutants were used to enrich the populations of discrete states along the activation pathway of A(2A)R. The results reveal important structural interactions and propose a GPCR activation process modulated by these interactions.
NATURE COMMUNICATIONS
(2023)
Article
Pharmacology & Pharmacy
Zhengnan Ren, Xiaohua Pan, Jiahong Li, Xiaoliang Dong, Xing Tu, Li Long Pan, Jia Sun
Summary: GPR41 is found to be involved in the progression of pulmonary fibrosis, and its knockout attenuates fibrosis and decreases collagen secretion. This suggests that GPR41 could be a potential therapeutic target for pulmonary fibrosis.
PHARMACOLOGICAL RESEARCH
(2023)
Article
Thermodynamics
Shadi Zaheri, Fatemeh Hassanipour
Summary: Mathematical modeling of membrane transporters and ion channels helps researchers gain a comprehensive understanding of the complex regulation process, estimate changes and uncertainties in mechanisms, and study how disorders may lead to diseases. A unified mathematical framework makes it easier for scientists to choose the appropriate model, saving time and resources.
INTERNATIONAL JOURNAL OF HEAT AND MASS TRANSFER
(2021)
Article
Biochemistry & Molecular Biology
Juergen Einsiedel, Maximilian F. Schmidt, Harald Huebner, Peter Gmeiner
Summary: A broadly applicable synthesis method was developed for peptides incorporating mixed disulfides between cysteine and homocysteine and cysteamine. The method was successfully applied to pharmacologically relevant GPCR ligands and showed covalent binding to neurotensin receptor 1 in a radioligand depletion study.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Gastroenterology & Hepatology
Kiyoaki Ito, Akinori Okumura, Junko S. Takeuchi, Koichi Watashi, Rieko Inoue, Taeko Yamauchi, Kazumasa Sakamoto, Yukiko Yamashita, Yusuke Iguchi, Mizuho Une, Takaji Wakita, Kazuo Umezawa, Masashi Yoneda
Summary: This study investigated inhibitory effects of bile acid (BA) derivatives on HBV infection, highlighting the strong inhibitory effect of INT-767, possibly achieved through inhibiting HBV entry and stimulating FXR signaling. In a chimeric mouse model with humanized liver, INT-767 significantly delayed the rise of HBV markers.
Editorial Material
Biochemistry & Molecular Biology
Elena O. Gracheva, Sviatoslav N. Bagriantsev
Summary: David Julius and Ardem Patapoutian were awarded this year's Nobel Prize in Physiology or Medicine for explaining the molecular basis for sensing heat, cold and mechanical force, marking the end of a scientific journey to identify the mechanisms in the somatosensory system mediating the detection of internal and external environments.