Blog Archives

Hot Topics: Time to FRET about GPCR activation dynamics?

G protein coupled receptors (GPCRs) are crucial for the transduction of extracellular stimuli to the intracellular space. Upon activation, GPCRs undergo large conformational changes to engage transducers and stimulate intracellular responses. However, the kinetics of agonist induced GPCR conformational changes

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Hot Topic: Structural details for coupling of the agonist-occupied ยต opioid receptor (amongst others) to the Gi protein

Every few years in the field of receptor pharmacology, a technological advance occurs that drives the field forward in terms of insight and understanding. Over the past couple of years, the cryo-EM technique (the development of which won the 2017

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Database release 2018.2

Our second database release of the year, 2018.2, is now available. This update contains the following new features and content changes: Content updates GPCRs: 5-Hydroxytryptamine receptors Adenosine receptors Adrenoceptors Histamine receptors Opioid receptors Lysophospholipid (S1P) receptors Prostanoid receptors NHRs: Mineralocorticoid

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Posted in Database updates, Guide to Malaria Pharmacology

Hot topic: Engineered mini G proteins provide a useful tool for studying the activation of GPCRs in living cells

In order to stabilize the GPCR-G protein complex, an agonist must be bound to the receptor and the alpha subunit of the heterotrimer must be in a nucleotide-free state. Ground-breaking work by expert crystallographers made use of so-called mini G

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Hot topic: The G Protein-Coupled Receptors deorphanization landscape.

Within the vast GPCR superfamily, orphans are described as receptors devoid of known endogenous ligands. They have been labeled as 7 transmembrane proteins by sequence homology and dispatched accordingly in the different GPCR subfamilies. They have attracted much attention given

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Hot topic: Pharmacogenomics of GPCR Drug Targets

A system of rigorous clinical trials and regulation exist to ensure that a new drug is safe and effective when reaching the market. However, natural human genetic variation(s) may cause individuals to respond differently to the same medication. A collaboration

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Hot topic: Trends in GPCR drug discovery: new agents, targets and indications

New avenues for GPCR drug discovery have emerged owing to recent advances in receptor pharmacology, technological breakthroughs in structural biology and innovations in biotechnology. A collaboration between the Department of Drug Design and Pharmacology, University of Copenhagen (home of the

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