Article
Biochemistry & Molecular Biology
Melissa Girard, Steve Dagenais Bellefeuille, Emilie Eiselt, Guillaume Arguin, Jean-Michel Longpre, Philippe Sarret, Fernand-Pierre Gendron
Summary: This study found that endosomal trafficking plays an important role in G protein-coupled receptor (GPCR) signaling. UDP selectively activates GPCR P2Y6 as a signaling molecule. The study found that MRS2693 and UDP have different effects on the internalization of the P2Y6 receptor, with MRS2693 inducing P2Y6 internalization through an independent caveolin-dependent mechanism. This study provides insights for the development of bias ligands that can influence P2Y6 signaling.
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH
(2023)
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
Pharmacology & Pharmacy
Vincent B. Luscombe, Luis Alberto Baena-Lopez, Carole J. R. Bataille, Angela J. Russell, David R. Greaves
Summary: In this study, heterologous cell lines with low GPR84 expression levels were developed to mimic the response of primary cells in a label-free cell electrical impedance sensing system. It was found that DL-175 exhibited a delayed impedance response, a delayed and suppressed activation of Akt, and impaired ability to internalise GPR84 from the plasma membrane compared to 6-OAU. These signalling differences were transient and occurred only at early time points in the low expressing cell lines, highlighting the importance of receptor number and kinetic readouts when evaluating signalling bias. These findings provide new insights into GPR84 signalling and the evaluation of newly developed agonists.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2023)
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
Hugo Avila, Anh Truong, David Tyrpak, Shin-Jae Park, Siqi Lei, Yaocun Li, Curtis Okamoto, Sarah Hamm-Alvarez, J. Andrew MacKay
Summary: A novel tool based on ELP technology can modulate the structure of DNM2 quickly, precisely, and reversibly, forming distinct temperature-dependent structures with potential applications in dynamin-dependent biology.
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.
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
Pharmacology & Pharmacy
Eliud Morales Davila, Felipe Patricio, Mariana Rebolledo-Bustillo, David Garcia-Gomez, Juan Carlos Garcia Hernandez, Brenda L. Sanchez-Gaytan, Ilhuicamina Daniel Limon, Jose Manuel Perez-Aguilar
Summary: Cannabidiol (CBD) has shown beneficial pharmacological effects in the treatment of neurological disorders and modulates receptors in the endocannabinoid system. The specific mechanisms by which CBD functions as both an agonist and antagonist remain unclear. Computational methods were used to investigate the interactions of CBD with GPR55 and CB1 receptors, revealing different functional features. This research provides insight into the molecular pharmacology of CBD and its potential therapeutic use.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Immunology
Katharina M. Glaser, Teresa K. Tarrant, Tim Laemmermann
Summary: G-protein coupled receptor kinases (GRKs) participate in the regulation of chemokine receptors, but they also have other functions beyond GPCR desensitization in primary immune cells. The interplay between different GRK family members and their effects on different immune cell types and GPCRs are complex and unpredictable. This study demonstrates the importance of studying GRK functions in primary immune cells to understand their specific roles.
FRONTIERS IN IMMUNOLOGY
(2022)
Review
Pharmacology & Pharmacy
Kate F. Byrne, Ajay Pal, James F. Curtin, John C. Stephens, Gemma K. Kinsella
Summary: The focus of the review is on G-protein-coupled receptor (GPCR) targets, with chemokine, cannabinoid, and dopamine receptors showing promise. Further research is needed on potential targets such as MC4R, adhesion receptors, LPA, and Smo receptors to develop new drug-screening strategies for safe and effective GBM therapies.
DRUG DISCOVERY TODAY
(2021)
Review
Biochemistry & Molecular Biology
Dekel David, Ziv Bentulila, Merav Tauber, Yair Ben-Chaim
Summary: GPCRs are involved in signal transduction processes, and although they span the cell membrane, they have not been considered to be regulated by membrane potential. Recent studies, however, have shown that several GPCRs are voltage regulated. This review discusses the advances in understanding the voltage dependence of GPCRs, the suggested molecular mechanisms, and the possible physiological roles.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Cell Biology
Jane C. Ammon, Danielle Valls, Mohamed Eldemerdash, Jigisha R. Patel, Philip D. Tran, Lifeng Feng, Michael Gi, Trang T. Gonzalez, Chuc Phan, Ashley E. Zendejas, Christopher H. So
Summary: The study demonstrates that GRK2 modulates the response of cancer cells to cisplatin by interacting with NOX4, affecting the levels of NADPH and NADP, and potentially impacting the efficacy of cisplatin-based regimens.
MOLECULAR AND CELLULAR BIOCHEMISTRY
(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.
Review
Chemistry, Medicinal
Joshua W. Conner, Daniel P. Poole, Manuela Jorg, Nicholas A. Veldhuis
Summary: This review addresses the key challenges, synthesis approaches, and structure-activity relationships in recent fluorescent small molecule studies for GPCRs, and discusses the advantages of using high-resolution GPCR structures to inform conjugation strategies.
FUTURE MEDICINAL CHEMISTRY
(2021)
Review
Pharmacology & Pharmacy
Sergi Ferre, Francisco Ciruela, Carmen W. Dessauer, Javier Gonzalez-Maeso, Terence E. Hebert, Ralf Jockers, Diomedes E. Logothetis, Leonardo Pardo
Summary: The study proposes the concept of GPCR-effect assemblies (GEMMAs), which are pre-assembled before receptor activation and allow more efficient interactions between specific signaling components. This offers an alternative model to the conventional collision coupling model and explains the differential properties of GPCRs in different cellular environments.
PHARMACOLOGY & THERAPEUTICS
(2022)
Article
Biochemistry & Molecular Biology
Eugenia Sergeev, Anders Hojgaard Hansen, Sunil K. Pandey, Amanda E. MacKenzie, Brian D. Hudson, Trond Ulven, Graeme Milligan
JOURNAL OF BIOLOGICAL CHEMISTRY
(2016)
Article
Biochemistry & Molecular Biology
Elisa Alvarez-Curto, Asuka Inoue, Laura Jenkins, Sheikh Zahir Raihan, Rudi Prihandoko, Andrew B. Tobin, Graeme Milligan
JOURNAL OF BIOLOGICAL CHEMISTRY
(2016)
Article
Biochemistry & Molecular Biology
John D. Pediani, Richard J. Ward, Antoine G. Godin, Sara Marsango, Graeme Milligan
JOURNAL OF BIOLOGICAL CHEMISTRY
(2016)
Article
Immunology
Nurul A. S. Binti Mohd Amir, Amanda E. Mackenzie, Laura Jenkins, Karim Boustani, Marston C. Hillier, Tomoko Tsuchiya, Graeme Milligan, James E. Pease
JOURNAL OF IMMUNOLOGY
(2018)
Review
Neurosciences
Sara Marsango, Richard J. Ward, Elisa Alvarez-Curto, Graeme Milligan
Article
Biochemistry & Molecular Biology
Suparna Patowary, Elisa Alvarez-Curto, Tian-Rui Xu, Jessica D. Holz, Julie A. Oliver, Graeme Milligan, Valerica Raicu
BIOCHEMICAL JOURNAL
(2013)
Article
Biotechnology & Applied Microbiology
R. W. Horobin, F. Rashid-Doubell, J. D. Pediani, G. Milligan
BIOTECHNIC & HISTOCHEMISTRY
(2013)
Review
Biochemistry & Molecular Biology
Elizabeth Scott, Komal Loya, Joanne Mountford, Graeme Milligan, Andrew H. Baker
FREE RADICAL BIOLOGY AND MEDICINE
(2013)
Review
Endocrinology & Metabolism
Brian D. Hudson, Hannah Murdoch, Graeme Milligan
MOLECULAR ENDOCRINOLOGY
(2013)
Article
Multidisciplinary Sciences
Vanessa Segura, Miguel Perez-Aso, Fermi Monto, Elena Carceller, Maria Antonia Noguera, John Pediani, Graeme Milligan, Ian Christie McGrath, Pilar D'Ocon
Article
Chemistry, Medicinal
Elisabeth Christiansen, Steffen V. F. Hansen, Christian Urban, Brian D. Hudson, Edward T. Wargent, Manuel Grundmann, Laura Jenkins, Mohamed Zaibi, Claire J. Stocker, Susanne Ullrich, Evi Kostenis, Matthias U. Kassack, Graeme Milligan, Michael A. Cawthorne, Trond Ulven
ACS MEDICINAL CHEMISTRY LETTERS
(2013)
Review
Cardiac & Cardiovascular Systems
Carolyn Clarke, Monica Flores-Munoz, Clare A. McKinney, Graeme Milligan, Stuart A. Nicklin
Review
Pharmacology & Pharmacy
Graeme Milligan
BRITISH JOURNAL OF PHARMACOLOGY
(2018)
Article
Pharmacology & Pharmacy
Amanda E. MacKenzie, Gianluigi Caltabiano, Toby C. Kent, Laura Jenkins, Jennifer E. McCallum, Brian D. Hudson, Stuart A. Nicklin, Lindsay Fawcett, Rachel Markwick, Steven J. Charlton, Graeme Milligan
MOLECULAR PHARMACOLOGY
(2014)
Review
Chemistry, Medicinal
Brian D. Hudson, Trond Ulven, Graeme Milligan
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2013)