Article
Cell Biology
Sergei Chavez-Abiega, Max L. B. Groenloh, Theodorus W. J. Gadella, Frank J. Bruggeman, Joachim Goedhart
Summary: This study reveals substantial cell-to-cell heterogeneity in kinase activity driven by GPCRs through imaging and analysis strategy.
JOURNAL OF CELL SCIENCE
(2022)
Article
Multidisciplinary Sciences
Kelsie J. Anson, Giulia A. Corbet, Amy E. Palmer
Summary: In this study, the researchers investigated how changes in intracellular zinc ion levels affect kinase signaling pathways using fluorescent biosensors and cell perturbations. The results showed that zinc ion fluctuations are not toxic and do not activate stress-dependent kinase signaling. Additionally, the study demonstrated that while zinc ions can inhibit phosphatases, ERK and Akt are primarily activated through upstream signaling pathways.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2021)
Article
Oncology
Mulu Geletu, Hanad Adan, Maximillian Niit, Rozanne Arulanandam, Esther Carefoot, Victoria Hoskin, Diana Sina, Bruce Elliott, Patrick Gunning, Leda Raptis
Summary: Cell-to-cell adhesion mediated by cadherins activates Stat3, while adhesion to the ECM activates FAK, Src, RTKs, PI3k/Akt, and Ras/Erk pathways. Cell density affects FAK and Akt activity, with FAK playing an important role in Akt activation.
EXPERIMENTAL CELL RESEARCH
(2021)
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)
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
Polymer Science
Tahir Mehmood, Rath Pichyangkura, Chatchai Muanprasat
Summary: This study demonstrates that chitosan oligosaccharide can reduce the diarrhea induced by afatinib and regulate the tight junctions and chloride secretion in intestinal epithelial cells by activating AMPK. This study provides a promising natural polymer-derived compound for further development of treatment for afatinib-associated diarrhea.
Article
Cell Biology
Ying Zhao, Haokun Liu, Mingzhen Fan, Yuyang Miao, Xiaoe Zhao, Qing Wei, Baohua Ma
Summary: Estrogen regulates the proliferation of goat mammary epithelial cells through the GPR30, MEK/ERK, and PI3K/AKT signaling pathways, providing a theoretical basis for researching estrogen sustained-release drugs promoting breast development and improving lactation performance.
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
Biochemistry & Molecular Biology
Mi Kyoung Kim, Won Chan Hwang, Do Sik Min
Summary: The study reveals that the PH domain of PLD2 acts as a negative regulator of PLD2 and FAK, inhibiting the migration and invasion of tumor cells, as well as tumor formation in a xenograft mouse model.
Review
Endocrinology & Metabolism
Fanhua Wang, Mingyao Liu, Ning Wang, Jian Luo
Summary: This review discusses the role of G-protein coupled receptors (GPCRs) in osteoarthritis (OA), including the pathophysiological processes involved, preclinical and clinical trial data, and the challenges in developing therapies targeting GPCRs for OA.
FRONTIERS IN ENDOCRINOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Santino Blando, Ivana Raffaele, Luigi Chiricosta, Andrea Valeri, Agnese Gugliandolo, Serena Silvestro, Federica Pollastro, Emanuela Mazzon
Summary: This study investigates the effect of cannabidiol (CBD) on neuronal differentiation at different concentrations and reveals a potential correlation between CBD, neurodifferentiation, and retinoic acid receptor-related orphan receptors (RORs).
Article
Chemistry, Multidisciplinary
Stefanie Kampen, Duc Duy Vo, Xiaoqun Zhang, Nicolas Panel, Yunting Yang, Mariama Jaiteh, Pierre Matricon, Per Svenningsson, Jose Brea, Maria Isabel Loza, Jan Kihlberg, Jens Carlsson
Summary: This study presents a structure-based strategy to design compounds with dual-target properties, which can both antagonize the A(2A) adenosine receptor and activate the D-2 dopamine receptor, showing promising potential as anti-parkinson drugs.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Biochemistry & Molecular Biology
Nadia Arang, Simone Lubrano, Damiano Cosimo Rigiracciolo, Daniela Nachmanson, Scott M. Lippman, Prashant Mali, Olivier Harismendy, J. Silvio Gutkind
Summary: G proteins and G protein-coupled receptors activate signal transduction pathways that promote cell growth and survival. This study found that G alpha q promotes PI3K/AKT signaling pathway activation, leading to resistance to FAK inhibition. These findings establish a novel link between G alpha q-driven signaling and the stimulation of PI3K, demonstrating the aberrant activation of signaling networks underlying the growth and survival of UM and other G alpha q-driven malignancies.
JOURNAL OF BIOLOGICAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Bianca Fiorillo, Valentina Sepe, Paolo Conflitti, Rosalinda Roselli, Michele Biagioli, Silvia Marchiano, Pasquale De Luca, Giuliana Baronissi, Pasquale Rapacciuolo, Chiara Cassiano, Bruno Catalanotti, Angela Zampella, Vittorio Limongelli, Stefano Fiorucci
Summary: GPCRs are important molecular targets for drug development, with potential for multitarget drugs. Compounds with dual activity towards CysLT(1)R and GPBAR1 show promise in treating inflammatory diseases such as colitis. The binding mode of these compounds reveals structural basis for future drug design studies.
JOURNAL OF MEDICINAL CHEMISTRY
(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.