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Insight into structural properties of viral G protein-coupled receptors and their role in the viral infection: IUPHAR Review 41.
Br J Pharmacol
January 2025
Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark.
G protein-coupled receptors (GPCRs) are pivotal in cellular signalling and drug targeting. Herpesviruses encode GPCRs (vGPCRs) to manipulate cellular signalling, thereby regulating various aspects of the virus life cycle, such as viral spreading and immune evasion. vGPCRs mimic host chemokine receptors, often with broader signalling and high constitutive activity.
View Article and Find Full Text PDFAdvancing the field of viroporins-Structure, function and pharmacology: IUPHAR Review 39.
Br J Pharmacol
November 2024
Molecular and Translational Pharmacology, Department of Biomedical Sciences, University of Copenhagen, Copenhagen, Denmark.
Viroporins possess important potential as antiviral targets due to their critical roles during virus life cycles, spanning from virus entry to egress. Although the antiviral amantadine targets the M2 viroporin of influenza A virus, successful progression of other viroporin inhibitors into clinical use remains challenging. These challenges relate in varying proportions to a lack of reliable full-length 3D-structures, difficulties in functionally characterising individual viroporins, and absence of verifiable direct binding between inhibitor and viroporin.
View Article and Find Full Text PDFInternational Union of Basic and Clinical Pharmacology. CXVI: NC-IUPHAR and : 30+ Years of Collaboration-Editorial.
Pharmacol Rev
August 2024
Personal Therapeutics Inc., Philadelphia, Pennsylvania, and Drexel University College of Medicine, Philadelphia, Pennsylvania
The affinity-efficacy problem: an essential part of pharmacology education.
R Soc Open Sci
July 2024
Neuroscience, Physiology and Pharmacology, University College London, London WC1E 6BT, UK.
A fundamental mistake in receptor theory has led to an enduring misunderstanding of how to estimate the affinity and efficacy of an agonist. These properties are inextricably linked and cannot be easily separated in any case where the binding of a ligand induces a conformation change in its receptor. Consequently, binding curves and concentration-response relationships for receptor agonists have no straightforward interpretation.
View Article and Find Full Text PDFInternational Union of Basic and Clinical Pharmacology CXV: The Class F of G Protein-Coupled Receptors.
Pharmacol Rev
October 2024
Karolinska Institutet, Department of Physiology & Pharmacology, Receptor Biology & Signaling, Biomedicum, Stockholm, Sweden
The class F of G protein-coupled receptors (GPCRs) consists of 10 Frizzleds (FZD) and Smoothened (SMO). FZDs bind and are activated by secreted lipoglycoproteins of the Wingless/Int-1 (WNT) family, and SMO is indirectly activated by the Hedgehog (Hh) family of morphogens acting on the transmembrane protein Patched. The advance of our understanding of FZDs and SMO as dynamic transmembrane receptors and molecular machines, which emerged during the past 14 years since the first-class F GPCR IUPHAR nomenclature report, justifies an update.
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