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
Biochemistry & Molecular Biology
Angelo Felline, Sara Gentile, Francesca Fanelli
Summary: G protein coupled receptors (GPCRs) are important signal transduc-tion gatekeepers in eukaryotic cells and represent the largest protein superfamily in humans. They are involved in numerous human diseases and are targets of many drugs. Structure network analysis is a cutting-edge tool to study GPCR function, and psnGPCRdb is a unique database that stores structure networks and communication pathways of GPCR structures along with other information. It is a powerful resource for unraveling GPCR function and has implications in cell signaling and drug design.
JOURNAL OF MOLECULAR BIOLOGY
(2023)
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)
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
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)
Review
Pharmacology & Pharmacy
Bui San Thai, Ling Yeong Chia, Anh T. N. Nguyen, Chengxue Qin, Rebecca H. Ritchie, Dana S. Hutchinson, Andrew Kompa, Paul J. White, Lauren T. May
Summary: Heart failure remains a significant cause of morbidity and mortality worldwide. Current treatment options have limitations, leading to many patients progressing to advanced stages. Exploration of novel therapeutics targeting G protein-coupled receptors (GPCRs) has shown promise, but efficacy and unwanted effects remain as challenges.
BRITISH JOURNAL OF PHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Kazutoshi Hisano, Shiori Kawase, Tetsuhiko Mimura, Hironori Yoshida, Hiroki Yamada, Hisao Haniu, Tamotsu Tsukahara, Taiga Kurihara, Yoshikazu Matsuda, Naoto Saito, Takeshi Uemura
Summary: Structurally different LPE species, 16:0 LPE and 18:0 LPE, stimulate neurite outgrowth through distinct signaling cascades in cultured cortical neurons, involving different G protein-coupled receptors.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2021)
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
Biochemistry & Molecular Biology
Damian Jacenik, Pawel Hikisz, Ellen J. Beswick, Jakub Fichna
Summary: Among the various adhesion G protein-coupled receptors, ADGRF5 stands out with its unique domains in the N-terminal tail that play a critical role in cell-cell and cell-matrix interactions, as well as cell adhesion. Although the biology of ADGRF5 is still not fully understood, accumulating evidence suggests its fundamental importance in both health and disease. Recent studies have highlighted its potential diagnostic value in osteoporosis and cancers, and ongoing research indicates its relevance to other diseases as well. This article provides a comprehensive overview of the current understanding of ADGRF5 in human disease physiology and pathophysiology, emphasizing its potential as a novel therapeutic target in various areas.
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE
(2023)
Review
Biochemistry & Molecular Biology
Raudah Lazim, Donghyuk Suh, Jai Woo Lee, Thi Ngoc Lan Vu, Sanghee Yoon, Sun Choi
Summary: The presence of GPCR dimers has sparked research into their importance in disease pathogenesis and drug design, uncovering new signaling pathways and potential therapeutic targets. The increasing influence of computational methods in research is providing new avenues for understanding the functions and interactions of GPCRs.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Pharmacology & Pharmacy
Alastair C. Keen, Manuela Jorg, Michelle L. L. Halls
Summary: The ubiquitin-proteasome system is a major pathway for protein degradation in cells, and methods have been developed to exploit this system for targeted protein degradation. Targeted protein degraders have been useful tools in discovery research and are being developed as therapeutics. However, most targeted protein degrader technologies have been developed for cytosolic proteins, while examples for G protein-coupled receptor (GPCR) degradation are limited. This review discusses the strategies used for applying targeted protein degradation to GPCRs and explores alternative approaches used for degrading other integral membrane proteins.
BRITISH JOURNAL OF PHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Shuai Luo, Peng Zhang, Wei Miao, Jie Xiong
Summary: This study provides the first comprehensive genome-wide identification of GPCRs in ciliates, identifying 492 GPCRs in 24 ciliates. GPCRs in ciliates can be assigned to four families, with most belonging to family A. Gene duplication events play a role in the expansion of the GPCR superfamily in ciliates. This study improves our understanding of the evolution and function of GPCRs in ciliates.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Biochemistry & Molecular Biology
Roberto Maggio, Irene Fasciani, Francesco Petragnano, Maria Francesca Coppolino, Marco Scarselli, Mario Rossi
Summary: Unstructured regions in functional proteins, specifically the i3 loop and C-terminus in G protein-coupled receptors (GPCRs), have been recognized as crucial elements in GPCR function and regulation. They play critical roles in allosterically regulating GPCR activation, as autoregulators in receptor coupling specificity, and in facilitating receptor stability and interactions with intracellular protein partners.
Article
Pharmacology & Pharmacy
Jyrki P. Kukkonen
Summary: Recent data indicates cooperative effects between identical orthosteric binding sites in a G-protein-coupled receptor dimer. A mathematical model was created to test this concept, showing that even a neutral receptor ligand can allosterically affect agonist binding through the orthosteric binding site.
PHARMACOLOGICAL RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Yanan Tian, Chaohui Jiang, Yi Pan, Zhiqiang Guo, Weiwei Wang, Xumei Luo, Zheng Cao, Bing Zhang, Jingwen Yang, Ying Shi, Naiming Zhou, Xiaobai He
Summary: Two newly identified CCHamide receptors, BommoCCHaR-1 and -2, have been cloned and their specific endogenous ligands, CCHamide-1 and CCHamide-2, respectively, have been characterized. The receptors exhibit different signaling pathways upon activation, with BNGR-A14 eliciting increases in CRE-driven luciferase activity, intracellular Ca2+ mobilization, and ERK1/2 phosphorylation, while BNGR-A15 leads to intracellular accumulation of cAMP, Ca2+ mobilization, and ERK1/2 phosphorylation. Additionally, CCHamides are shown to require intrachain disulfide bonds for activation, and CCHamide-1 may regulate feeding behavior and growth through BNGR-A15, while CCHamide-2 plays a crucial role in multiple physiological processes.
INSECT BIOCHEMISTRY AND MOLECULAR BIOLOGY
(2021)
Article
Neurosciences
Mayra Moreno-Castillo, Roberto Meza, Jesus Romero-Vaca, Nayeli Huidobro, Abraham Mendez-Fernandez, Jaime Martinez-Castillo, Pedro Mabil, Amira Flores, Elias Manjarrez
FRONTIERS IN NEUROSCIENCE
(2020)
Article
Behavioral Sciences
Abraham Mendez-Fernandez, Mayra Moreno-Castillo, Nayeli Huidobro, Amira Flores, Elias Manjarrez
FRONTIERS IN INTEGRATIVE NEUROSCIENCE
(2020)
Article
Clinical Neurology
N. Huidobro, A. Gutierrez-Gomez, J. Gutierrez, I. Zea, I. Mendez-Balbuena, A. Flores, C. Trenado, E. Manjarrez
Article
Neurosciences
Pedro Mabil, Nayeli Huidobro, Oswaldo Torres-Ramirez, Jorge Flores-Hernandez, Amira Flores, Ranier Gutierrez, Elias Manjarrez
FRONTIERS IN NEUROSCIENCE
(2020)
Article
Neurosciences
Gustavo Hernandez-Carballo, Evelyn A. Ruiz-Luna, Gustavo Lopez-Lopez, Elias Manjarrez, Jorge Flores-Hernandez
Article
Physics, Multidisciplinary
Elias Manjarrez, Roberto Olmos, Lilia Cedillo, Humberto A. Salazar-lbarguen
FRONTIERS IN PHYSICS
(2020)
Article
Biology
Jesus A. Tapia, Argelia Reid, John Reid, Saul M. Dominguez-Nicolas, Elias Manjarrez
Summary: This study uses a mathematical model to demonstrate the potential transition of post-scratching locomotion in cats through shared neuronal circuits. The model replicates the experimental observations, revealing the mechanism of transition between two rhythmic movements and the flexible connectivity in the spinal cord circuitry.
Article
Medicine, General & Internal
Saul M. Dominguez-Nicolas, Elias Manjarrez
Summary: This study demonstrated that a 30-minute session of dorsal low-field thoracic magnetic stimulation (LF-ThMS) significantly increased SpO(2) levels in COVID-19 patients, with variables such as frequency, magnetic flux density, and temperature correlated to SpO(2) levels. Further research is needed to understand the physiological mechanisms behind these findings.
Article
Neurosciences
Ana Ramirez, Eduardo Monjaraz, Elias Manjarrez, Alejandro Moyaho, Jorge Cebada, Amira Flores
Summary: This study examined the role of NMDA receptors in the electrical signals of the chicken vestibular system at different developmental stages. The results showed that NMDA receptors mediate the spontaneous and mechanically evoked discharges of primary afferents, and their expression increases with development, reaching mature functionality close to hatching.
Editorial Material
Neurosciences
Giulia Curia, Erika Estrada-Camarena, Elias Manjarrez, Hidenobu Mizuno
FRONTIERS IN NEUROSCIENCE
(2022)
Review
Cell Biology
Mateo A. Herrera-Murillo, Mario Trevino, Elias Manjarrez
Summary: Random noise stimulation technique involves applying various forms of energy to the brain or sensory receptors to enhance sensory, motor, or cognitive functions. Recent studies have shown that transcranial random noise stimulation can increase corticospinal excitability, improve cognitive/motor performance, and produce positive effects at the behavioral and psychological levels. Random noise stimulation has potential uses in treating neurological disorders and further research is needed to discover optimal methods of application.
NEURAL REGENERATION RESEARCH
(2022)
Article
Medicine, General & Internal
Alma Fragoso, Brayan Martinez, Maria Elena Ceballos-Villegas, Elizabeth Herrera, Juan Jose Saldana, Ana Lilia Gutierrez-Lozano, Elias Manjarrez, Joel Lomeli
Summary: This study examined the neuroplastic effects of spinal manipulation with an Activator IV instrument on the bilateral H-reflex amplitude in dancers and non-dancers. The results showed that ten sessions of spinal manipulation did not cause significant changes in the H-reflex amplitude in either group. Furthermore, there was no significant difference in the effects of spinal manipulation between the two groups, despite their different baseline H-reflex amplitudes. Further research is needed to understand the mechanisms involved.
MEDICINA-LITHUANIA
(2022)
Proceedings Paper
Daniel Alejandro Lara-Lopez, Melissa Angelica Valdovinos-Zepeda, Jaime Martinez-Castillo, Jaime Martinez-Toribio, Oscar Chiquito-Coyotl, Mayra Moreno-Castillo, Elias Manjarrez
Summary: This report details the use of an OPT-101 photodetector and red light LED to detect DC-PPG signals in the spinal cord and brainstem, as well as the successful transmission of these signals wirelessly. By varying the distance between the photodetector and LED, the wireless system was able to detect all transmitted signals, with decreasing output and wireless potential observed at longer distances. Different arrangements of the device have the potential to detect hemodynamic responses in various animal models and human brain wirelessly.
2021 IEEE INTERNATIONAL CONFERENCE ON ENGINEERING VERACRUZ (IEEE ICEV 2021(R))
(2021)
Article
Neurosciences
Roberto Meza, Nayeli Huidobro, Mayra Moreno-Castillo, Abraham Mendez-Fernandez, Jorge Flores-Hernandez, Amira Flores, Elias Manjarrez
Article
Neurosciences
Yang He, Jun Tang, Meng Zhang, Junjie Ying, Dezhi Mu
Summary: This study investigated the protective effects and mechanisms of human placenta derived mesenchymal stem cells (hPMSCs) transplantation in a rat model of hypoxic-ischemic encephalopathy (HIE). The results showed that hPMSCs transplantation reduced apoptosis and improved long-term neurological prognosis. Furthermore, the downregulation of Sema 3A/NRP-1 expression and activation of the PI3K/Akt/mTOR signaling pathway played a key role in the protective effects of hPMSCs.
Article
Neurosciences
Emily L. Isenstein, Edward G. Freedman, Jiayi Xu, Ian A. DeAndrea-Lazarus, John J. Foxe
Summary: This study evaluated electrophysiological discrimination of parametric somatosensory stimuli in healthy young adults to understand how the brain processes the duration of tactile information. The results showed that participants did not electrophysiologically discriminate between 100 and 115 ms, but they exhibited distinct electrophysiological responses when the deviant stimuli were 130, 145, and 160 ms. These findings contribute to a better understanding of tactile sensitivity in different clinical conditions.
Article
Neurosciences
Juliana R. Souza, Ludmila Lima-Silveira, Daniela Accorsi-Mendonca, Benedito H. Machado
Summary: This study demonstrates that A2A receptors play a crucial role in modulating synaptic transmission in the NTS neurons and are required for the enhancement of glutamatergic transmission observed under short-term sustained hypoxia conditions.
Article
Neurosciences
Miki Hashizume, Rina Ito, Rie Suge, Yasushi Hojo, Gen Murakami, Takayuki Murakoshi
Summary: The basolateral amygdaloid complex (BLA) is closely involved in the formation of emotional memories, including both aversive memory and contextual fear memory. Acute sleep deprivation (SD) disrupts the acquisition of tone-associated fear memory in juvenile rats, but has no significant effect on contextual fear memory. Slow network oscillation in the amygdala contributes to the formation of amygdala-dependent fear memory in relation to sleep.
Article
Neurosciences
Qunxian Wang, Shipeng Guo, Dongjie Hu, Xiangjun Dong, Zijun Meng, Yanshuang Jiang, Zijuan Feng, Weihui Zhou, Weihong Song
Summary: GSDME plays a crucial role in the pathogenesis of Alzheimer's disease by regulating the switch from apoptosis to pyroptosis and participating in neuroinflammatory response. Knockdown of GSDME has been shown to improve cognitive impairments, indicating that GSDME could be a therapeutic target for Alzheimer's disease.