Review
Cell Biology
Jeffrey L. Benovic
Summary: Agonist activation of G protein-coupled receptors leads to sequential interaction with G proteins, GRKs, and arrestins. GRKs play a central role in mediating the switch from G protein to arrestin interaction and controlling processes like receptor desensitization. Early studies on GRK identification and cloning laid the foundation for understanding the structure and function of these enzymes.
Editorial Material
Biochemistry & Molecular Biology
Arun K. Shukla
Summary: This Special Issue of The FEBS Journal presents a series of review articles focusing on recent developments in the field of GPCR biology, with particular emphasis on novel paradigms of their activation, signaling, and regulation. These articles cover a wide range of cellular, physiological, and structural aspects related to GPCRs and their interactions with signal transducers, allosteric modulation, and emerging technologies for studying receptor signaling and regulation.
Review
Biochemistry & Molecular Biology
Gizem Kayki-Mutlu, Walter J. Koch
Summary: Cardiac diseases, especially heart failure, are the leading cause of morbidity and mortality globally. The loss of beta-adrenoceptor-mediated inotropic reserve and the elevated activities of G protein-coupled receptor kinases and beta-arrestins after heart injury/stress play significant roles in heart failure. Nitric oxide produced by NO synthase enzymes modulates GPCR regulators profoundly through S-nitrosylation, independent of its canonical signaling pathway.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Pharmacology & Pharmacy
Sam Groom, Nina K. Blum, Alexandra E. Conibear, Alexander Disney, Rob Hill, Stephen M. Husbands, Yangmei Li, Lawrence Toll, Andrea Kliewer, Stefan Schulz, Graeme Henderson, Eamonn Kelly, Chris P. Bailey
Summary: This study confirmed that Compound 1 is a G protein-biased mu agonist that can induce substantial rapid receptor desensitisation in mammalian neurons. However, contrary to previous assumptions, the desensitisation effect of Compound 1 is dependent on G protein-coupled receptor kinase (GRK).
BRITISH JOURNAL OF PHARMACOLOGY
(2023)
Review
Endocrinology & Metabolism
Camila Oliveira de Souza, Xuenan Sun, Dayoung Oh
Summary: Seven transmembrane receptors, also known as G protein-coupled receptors, are common targets for therapeutic drugs. Studies suggest that different members of the GPCR superfamily may be potential targets for treating metabolic disorders like obesity and type 2 diabetes.
FRONTIERS IN ENDOCRINOLOGY
(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
Medicine, General & Internal
Rocio Alcantara-Hernandez, David A. Hernandez-Espinosa, Luz del C. Medina, Jesus A. Garcia-Sainz
Summary: This review focuses on G protein-coupled receptors, the most diverse and abundant family of receptors that recognize and mediate the action of various endogenous ligands. Understanding their structure and function is crucial due to their involvement in disease pathogenesis and targeting by a significant percentage of clinical medications. X-ray crystallography and molecular modeling provide essential tools for studying receptor-ligand binding and supporting the development of specific drugs.
GACETA MEDICA DE MEXICO
(2022)
Article
Hematology
Jean Marie N. Mwiza, Robert H. Lee, David S. Paul, Lori A. Holle, Brian C. Cooley, Bernhard Nieswandt, Wyatt J. Schug, Tomohiro Kawano, Nigel Mackman, Alisa S. Wolberg, Wolfgang Bergmeier
Summary: Platelets play a critical role in venous thrombosis, and their activation through G protein-coupled receptors and immunoreceptor tyrosine-based activation motifs is important in this process. Strong inhibition of these signaling pathways can reduce venous thrombosis.
Article
Meteorology & Atmospheric Sciences
Ren Wang, Longhui Li, Lijuan Chen, Liang Ning, Linwang Yuan, Guonian Lu
Summary: Climate change has led to an increase in drought in most global land areas. The contributions of decreased precipitation and increased potential evapotranspiration to long-term drought duration and intensity vary by region, but overall, changes in precipitation play a more significant role in the increase of long-term drought.
INTERNATIONAL JOURNAL OF CLIMATOLOGY
(2022)
Article
Biotechnology & Applied Microbiology
Sara Capolla, Federico Colombo, Luca De Maso, Prisca Mauro, Paolo Bertoncin, Thilo Kahne, Alexander Engler, Luis Nunez, Ruben Spretz, Gustavo Larsen, Michele Dal Bo, Giuseppe Toffoli, Paolo Macor
Summary: Nanoparticles have great potential in medical field, but their interactions with blood proteins limit their clinical translation. Mouse and human serum proteins bind differently to nanoparticles, and the presence of a targeting antibody affects complement activation. However, both targeted and untargeted nanoparticles are similarly recognized and eliminated by macrophages.
JOURNAL OF NANOBIOTECHNOLOGY
(2023)
Review
Immunology
Reza Akbarzadeh, Antje Mueller, Jens Y. Humrich, Gabriela Riemekasten
Summary: Systemic sclerosis (SSc) is a chronic autoimmune disease with complex features such as autoimmunity, vasculopathy, and fibrosis. Antibodies targeting G protein-coupled receptors (GPCRs) have been found to play a role in SSc pathologies. Understanding the effects of GPCR antibodies in SSc could contribute to the development of therapeutic strategies targeting these receptors.
FRONTIERS IN IMMUNOLOGY
(2023)
Article
Water Resources
Hafzullah Aksoy, Mahmut Cetin, Ebru Eris, Halil Ibrahim Burgan, Yonca Cavus, Isilsu Yildirim, Murugesu Sivapalan
Summary: A methodology using the standardised precipitation index is proposed to develop critical drought intensity-duration-frequency (IDF) curves, with the generalised extreme value probability distribution function found to best fit the critical drought severity. The critical drought intensity decreases linearly with increasing drought duration, while the return period increases exponentially as the drought becomes more severe. The site-specific IDF curves allow one to characterise the drought by its return period, providing a physically easier understanding for stakeholders and decision makers.
HYDROLOGICAL SCIENCES JOURNAL
(2021)
Article
Cardiac & Cardiovascular Systems
Ji Yoon Kim, Jimi Choi, Sin Gon Kim, Nam Hoon Kim
Summary: This study aimed to evaluate the optimal statin therapy for patients with type 2 diabetes. The findings suggest that the duration of statin therapy is as important or even more crucial than statin intensity or achieved LDL-C level in reducing cardiovascular risk. Longer treatment duration was associated with a lower risk of major adverse cardiovascular events. Adequate control of LDL-C levels with moderate to high-intensity statins also contributed to a lower cardiovascular risk.
CARDIOVASCULAR DIABETOLOGY
(2022)
Article
Chemistry, Inorganic & Nuclear
Beiyi Zhang, Junqi Li, Qianqian Song, Xiaotao Xu, Wenfei Hou, Hui Liu
Summary: The research introduces a feasible strategy for designing an excellent acidic and alkaline hydrogen evolution electrocatalyst using the MoS2@Mo-S-C3N4 heterostructure with transferable active centers. Mo-S-C3N4 is regarded as a synergistic catalyst for acidic hydrogen evolution, while MoS2 acts as a co-catalyst for alkaline hydrogen evolution. The coordination of electrons between interfaces achieves a synergistic balance, providing optimal sites for reactant adsorption. This electrocatalyst shows better overpotentials in acidic and alkaline media compared to previous reports.
INORGANIC CHEMISTRY
(2021)
Article
Cell & Tissue Engineering
Ryan C. McDonough, Christopher Price
Summary: The study demonstrated the effects of long-term CNO stimulation on hM3Dq [Ca2+] (i) signaling dynamics, proliferation, and protein deposition in 2D ATDC5 cultures. Prolonged culturing under repeated CNO stimulation modified the temporal dynamics of hM3Dq [Ca2+] (i) signaling, increased cell proliferation, enhanced matrix production, and triggered the formation of cartilaginous neotissue structures.
TISSUE ENGINEERING PART A
(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
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
M. Perez-Aso, V. Segura, F. Monto, D. Barettino, M. A. Noguera, G. Milligan, P. D'Ocon
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH
(2013)
Article
Biochemistry & Molecular Biology
Brian D. Hudson, Maria E. Due-Hansen, Elisabeth Christiansen, Anna Mette Hansen, Amanda E. Mackenzie, Hannah Murdoch, Sunil K. Pandey, Richard J. Ward, Rudi Marquez, Irina G. Tikhonova, Trond Ulven, Graeme Milligan
JOURNAL OF BIOLOGICAL CHEMISTRY
(2013)
Article
Chemistry, Medicinal
Elisabeth Christiansen, Maria E. Due-Hansen, Christian Urban, Manuel Grundmann, Johannes Schmidt, Steffen V. F. Hansen, Brian D. Hudson, Mohamed Zaibi, Stine B. Markussen, Ellen Hagesaether, Graeme Milligan, Michael A. Cawthorne, Evi Kostenis, Matthias U. Kassack, Trond Ulven
JOURNAL OF MEDICINAL CHEMISTRY
(2013)
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)
Article
Cell & Tissue Engineering
Lynsey Howard, Ruth M. Mackenzie, Nikolay A. Pchelintsev, Tony McBryan, John D. McClure, Martin W. McBride, Nicole M. Kane, Peter D. Adams, Graeme Milligan, Andrew H. Baker
STEM CELL RESEARCH & THERAPY
(2013)
Article
Pharmacology & Pharmacy
Brian D. Hudson, Bharat Shimpukade, Amanda E. Mackenzie, Adrian J. Butcher, John D. Pediani, Elisabeth Christiansen, Helen Heathcote, Andrew B. Tobin, Trond Ulven, Graeme Milligan
MOLECULAR PHARMACOLOGY
(2013)
Meeting Abstract
Biochemistry & Molecular Biology
Amanda Elaine Mackenzie, Zaynab Neetoo-Isseljee, Craig Southern, Jeff Jerman, Edward G. McIver, Brian D. Hudson, Debra L. Taylor, Graeme Milligan
Meeting Abstract
Biochemistry & Molecular Biology
Brian Hudson, Bharat Shimpukade, Trond Ulven, Graeme Milligan
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)