Review
Immunology
Nan Li, Shan Shan, Xiu-Qin Li, Ting-Ting Chen, Meng Qi, Sheng-Nan Zhang, Zi-Ying Wang, Ling-Ling Zhang, Wei Wei, Wu-Yi Sun
Summary: G protein-coupled receptor kinase 2 (GRK2) plays important roles in regulating signaling pathways associated with fibrotic diseases. Recent research suggests that GRK2 could be a potential therapeutic target for fibrotic diseases.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Neurosciences
Mariela Mitre, Khalil Saadipour, Kevin Williams, Latika Khatri, Robert C. Froemke, Moses V. Chao
Summary: The study shows that oxytocin can enhance the activity of BDNF in neurons by transactivating the TrkB receptor. This finding is important for understanding the mechanism of oxytocin and its relationship with neural development and social behaviors.
FRONTIERS IN MOLECULAR NEUROSCIENCE
(2022)
Review
Biology
Terry W. Moody, Irene Ramos-Alvarez, Robert T. Jensen
Summary: Cancer growth is regulated by receptor tyrosine kinases (RTKs) and G-protein-coupled receptors (GPCRs). Different mutations in EGFR and NTSR1 can lead to abnormal cancer proliferation. The use of tyrosine kinase inhibitors and SR48692 as antagonists can impair the transactivation process and inhibit cancer growth.
Article
Biochemistry & Molecular Biology
Matej Gazdarica, Judith Noda, Oleh Durydivka, Vendula Novosadova, Ken Mackie, Jean-Philippe Pin, Laurent Prezeau, Jaroslav Blahos
Summary: CB1R signaling is regulated by receptor desensitization and the protein SGIP1, which plays an important role in controlling CB1R function and its involvement in pathological conditions.
JOURNAL OF NEUROCHEMISTRY
(2022)
Article
Developmental Biology
Farah Saad, David R. Hipfner
Summary: The Hedgehog (Hh) pathway is regulated by G protein-coupled receptors (GPCRs) in Drosophila, with Mthl5 identified as a modulator of this pathway. This suggests potential crosstalk between GPCRs and the Hh pathway in mammals as well.
Article
Biochemistry & Molecular Biology
Jesus Bertran-Gonzalez, Caroline Dinale, Miriam Matamales
Summary: Multidisciplinary evidence suggests that the control of voluntary action is mediated by two major forms of behavioral processing: cognitively guided and autonomously guided. Brain-state irregularities, such as aging, often shift control towards the latter, but the neural mechanisms responsible are still unknown. By combining instrumental conditioning, cell-specific mapping, and chemogenetics, this study investigated strategies to enhance goal-directed control in aged mice. The findings suggest that desensitization of D2-SPN signaling in the striatum can shift behavior towards vigorous, goal-directed action and enhance cognitive functioning in habit-prone brains.
Review
Chemistry, Medicinal
Ningning Sun, Kyeong-Man Kim
Summary: The desensitization of G protein-coupled receptors can occur through various mechanisms including phosphorylation-dependent desensitization at the receptor level and downstream mechanisms involving the sequestration of G proteins. These mechanisms involve GRKs, arrestins, and deubiquitinated arrestins to regulate GPCR signaling and prevent G-protein activation. Further studies are needed on the interesting mechanism of arrestin deubiquitination in GPCR desensitization.
ARCHIVES OF PHARMACAL RESEARCH
(2021)
Article
Multidisciplinary Sciences
Paul H. Taghert
Summary: In this study, the incidence and conservation of beta-arrestin binding sites (BBS's) among the C terminal tails of Drosophila melanogaster neuropeptide GPCRs were evaluated. The results showed great diversity in the profile of BBS's, with some GPCRs lacking conserved BBS sequences. Additionally, certain GPCRs displayed multiple conserved compound BBS's, and BBS-like sequences were found in the intracellular loop domains. This research lays the initial foundation for future genetic analyses to investigate the roles of arrestins in neuropeptide GPCR desensitization, trafficking, and signaling in Drosophila.
Article
Pharmacology & Pharmacy
Sweta Adhikary, Omar Koita, Joseph J. Lebowitz, William T. Birdsong, John T. Williams
Summary: This study suggests that chronic opioid treatment alters kinase regulation of nonopioid GPCRs, highlighting the importance of sustained opioid receptor signaling in initiating adaptive processes downstream.
MOLECULAR PHARMACOLOGY
(2022)
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
Biochemistry & Molecular Biology
Sandra Berndt, Ines Liebscher
Summary: SFKs are crucial regulators of cell proliferation, differentiation, and survival, with their expression strongly linked to cancer development and tumor progression. The regulation of SFKs through GPCR-mediated pathways is complex and may involve direct protein interactions or allosteric regulation by arrestins and G proteins. The potential direct interaction between GPCRs and SFKs could lead to a novel mechanism of SFK signaling and identification of new GPCR-SFK interactions.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biology
Ramon Cierco Jimenez, Nil Casajuana-Martin, Adrian Garcia-Recio, Lidia Alcantara, Leonardo Pardo, Mercedes Campillo, Angel Gonzalez
Summary: The study analyzed 119,069 natural variants in human olfactory receptors, revealing a significant diversity of natural variations in the olfactory gene repertoire between individuals and populations, with a considerable number of changes occurring at the structurally conserved regions. Mutations in positions linked to the conserved GPCR activation mechanism were highlighted, which could imply phenotypic variation in olfactory perception.
Article
Medicine, General & Internal
Gerd Wallukat, Stephan Mattecka, Katrin Wenzel, Wieland Schroedl, Birgit Vogt, Patrizia Brunner, Ahmed Sheriff, Rudolf Kunze
Summary: This study found that C-reactive protein (CRP) affects intracellular calcium signaling and blood pressure. When CRP is combined with GPCR agonists in cardiomyocytes, it can interfere with the desensitization of GPCRs, regardless of the type of GPCR, but dependent on the concentration of CRP.
JOURNAL OF CLINICAL MEDICINE
(2022)
Article
Clinical Neurology
Thais Rafael Guimaraes, Eric Swanson, Julia Kofler, Amantha Thathiah
Summary: The study identifies a link between G protein-coupled receptor kinases (GRKs) and the pathological phosphorylation and accumulation of tau in Alzheimer's disease (AD), as well as a novel role in regulating the disease's pathological hallmarks. The expression patterns of different GRKs vary in AD patients compared to control subjects, indicating potential involvement in tau phosphorylation and NFT formation.
NEUROPATHOLOGY AND APPLIED NEUROBIOLOGY
(2021)
Article
Biology
Carolina Franco Nitta, Ellen W. Green, Elton D. Jhamba, Justine M. Keth, Irais Ortiz-Caraveo, Rachel M. Grattan, David J. Schodt, Aubrey C. Gibson, Ashwani Rajput, Keith A. Lidke, Bridget S. Wilson, Mara P. Steinkamp, Diane S. Lidke
Summary: Crosstalk between EGFR and RON is unidirectional, with EGFR phosphorylating RON to activate RON-directed signaling, which requires the formation of a signaling competent EGFR dimer. Nanoscale imaging reveals association of EGFR and RON in common plasma membrane microdomains, while two-color single particle tracking captures the formation of complexes between RON and EGF-bound EGFR.
Article
Pharmacology & Pharmacy
Carla Sosa-Alvarado, Aurelio Hernandez-Mendez, M. Teresa Romero-Avila, Omar B. Sanchez-Reyes, Yoshinori Takei, Gozoh Tsujimoto, Akira Hirasawa, J. Adolfo Garcia-Sainz
EUROPEAN JOURNAL OF PHARMACOLOGY
(2015)
Correction
Biotechnology & Applied Microbiology
Mitra Khumbatta, Bahrom Firozgary, David John Tweardy, Joel Weinstock, Gohar Firozgary, Zal Bhatena, Tushar Bulsara, Ricardo Siller, Prema Robinson
BIOMED RESEARCH INTERNATIONAL
(2015)
Article
Pharmacology & Pharmacy
Marco A. Alfonzo-Mendez, Jean A. Castillo-Badillo, M. Teresa Romero-Avila, Richard Rivera, Jerold Chun, J. Adolfo Garcia-Sainz
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
(2016)
Article
Pharmacology & Pharmacy
Marco A. Alfonzo-Mendez, David A. Hernandez-Espinosa, Gabriel Carmona-Rosas, M. Teresa Romero-Avila, Guadalupe Reyes-Cruz, J. Adolfo Garcia-Sainz
MOLECULAR PHARMACOLOGY
(2017)
Article
Biochemistry & Molecular Biology
S. Villegas-Comonfort, Y. Takei, G. Tsujimoto, A. Hirasawa, J. A. Garcia-Sainz
PROSTAGLANDINS LEUKOTRIENES AND ESSENTIAL FATTY ACIDS
(2017)
Article
Multidisciplinary Sciences
Jean A. Castillo-Badillo, Omar B. Sanchez-Reyes, Marco A. Alfonzo-Mendez, Teresa Romero-Avila, Guadalupe Reyes-Cruz, J. Adolfo Garcia-Sainz
Article
Biochemistry & Molecular Biology
Juan Carlos Martinez-Morales, M. Teresa Romero-Avila, Guadalupe Reyes-Cruz, J. Adolfo Garcia-Sainz
BIOSCIENCE REPORTS
(2018)
Article
Cell Biology
Gabriel Carmona-Rosas, David A. Hernandez-Espinosa, Rod Alcantara-Hernandez, Marco A. Alfonzo-Mendez, J. Adolfo Garcia-Sainz
CELLULAR SIGNALLING
(2019)
Review
Biochemistry & Molecular Biology
Karina Helivier Solis, M. Teresa Romero-Avila, Alejandro Guzman-Silva, J. Adolfo Garcia-Sainz
Summary: This review provides a comprehensive overview of the function regulation, signaling pathways activation, and structural characteristics of the LPA(3) receptor, highlighting the current knowledge gap in its functional regulation to stimulate further experimental work.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Pharmacology & Pharmacy
Juan Carlos Martinez-Morales, M. Teresa Romero-Avila, Guadalupe Reyes-Cruz, Jesus Adolfo Garcia-Sainz
Summary: The phosphorylation and endosomal traffic of G protein-coupled receptors play a significant role in receptor responsiveness, cellular localization, and fate, with important implications in pharmacology and therapy.
MOLECULAR PHARMACOLOGY
(2022)
Article
Cell Biology
Alejandro Guzman-Silva, Juan Carlos Martinez-Morales, Luz del Carmen Medina, M. Teresa Romero-Avila, Socrates Villegas-Comonfort, Karina Helivier Solis, J. Adolfo Garcia-Sainz
Summary: The phosphorylation sites of Free fatty acid receptor 1 were studied using mutants. The identified sites were found to play important roles in receptor phosphorylation, signaling, and internalization.
MOLECULAR AND CELLULAR ENDOCRINOLOGY
(2022)
Review
Medicine, Research & Experimental
Juan Carlos Martinez-Morales, K. Helivier Solis, M. Teresa Romero-Avila, Guadalupe Reyes-Cruz, J. Adolfo Garcia-Sainz
Summary: G protein-coupled receptors (GPCRs) are membrane proteins that function as sensors and play significant roles in various physiological and pathological processes. This review provides an overview of the current understanding of the structure, signaling, internalization, and recycling of GPCRs.
ARCHIVES OF MEDICAL RESEARCH
(2022)
Article
Cell Biology
Juan Carlos Martinez-Morales, Karla D. Gonzalez-Ruiz, M. Teresa Romero-Avila, Ruth Rincon-Heredia, Guadalupe Reyes-Cruz, Jesus Adolfo Garcia-Sainz
Summary: LPA1 receptor internalization was studied using FRET to analyze the interaction between LPA1 and Rab proteins under different stimuli. The results showed that LPA-induced internalization was rapid and transient, while PMA-induced internalization was slower but sustained. LPA stimulated the interaction between LPA1 and Rab5 rapidly but transiently, while PMA showed a rapid but sustained interaction. LPA1-Rab9 interaction was only observed at 60 min, and LPA1-Rab7 interaction was observed after 5 min with LPA and after 60 min with PMA. LPA triggered immediate but transient rapid recycling, while PMA showed slower but sustained recycling. Our findings suggest that LPA1 receptor internalization varies depending on the stimuli.
MOLECULAR AND CELLULAR ENDOCRINOLOGY
(2023)
Review
Biochemistry & Molecular Biology
Marco A. Alfonzo-Mendez, Rocio Alcantara-Hernandez, J. Adolfo Garcia-Sainz
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2017)
Article
Pharmacology & Pharmacy
Jessica B. Nascimento-Viana, Aline R. Carvalho, Luiz Eurico Nasciutti, Rocio Alcantara-Hernandez, Fernanda Chagas-Silva, Pedro A. R. Souza, Luiz Antonio S. Romeiro, J. Adolfo Garcia-Sainz, Francois Noel, Claudia Lucia Martins Silva
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
(2016)