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Structure of class B GPCR corticotropin-releasing factor receptor 1
Structural analysis of class B G-protein-coupled receptors (GPCRs), cell-surface proteins that respond to peptide hormones, has been restricted to the amino-terminal extracellular domain, thusExpand
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Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain
Metabotropic glutamate receptors are class C G-protein-coupled receptors which respond to the neurotransmitter glutamate. Structural studies have been restricted to the amino-terminal extracellularExpand
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Saccharomyces cerevisiae Sin3p facilitates DNA double-strand break repair.
There are two main pathways in eukaryotic cells for the repair of DNA double-strand breaks: homologous recombination and nonhomologous end joining. Because eukaryotic genomes are packaged inExpand
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Extra-helical binding site of a glucagon receptor antagonist
Glucagon is a 29-amino-acid peptide released from the α-cells of the islet of Langerhans, which has a key role in glucose homeostasis. Glucagon action is transduced by the class B G-protein-coupledExpand
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Thermostabilisation of an Agonist-Bound Conformation of the Human Adenosine A2A Receptor
The adenosine A2A receptor (A2AR) is a G-protein-coupled receptor that plays a key role in transmembrane signalling mediated by the agonist adenosine. The structure of A2AR was determined recently inExpand
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Intracellular allosteric antagonism of the CCR9 receptor
Chemokines and their G-protein-coupled receptors play a diverse role in immune defence by controlling the migration, activation and survival of immune cells. They are also involved in viral entry,Expand
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Crystal structure of the GLP-1 receptor bound to a peptide agonist
Glucagon-like peptide 1 (GLP-1) regulates glucose homeostasis through the control of insulin release from the pancreas. GLP-1 peptide agonists are efficacious drugs for the treatment of diabetes. ToExpand
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The properties of thermostabilised G protein-coupled receptors (StaRs) and their use in drug discovery
G protein-coupled receptors (GPCRs) are one of the most important target classes in the central nervous system (CNS) drug discovery, however the fact they are integral membrane proteins and areExpand
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Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).
Fragment screening of a thermostabilized mGlu5 receptor using a high-concentration radioligand binding assay enabled the identification of moderate affinity, high ligand efficiency (LE) pyrimidineExpand
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Structure of the complement C5a receptor bound to the extra-helical antagonist NDT9513727
The complement system is a crucial component of the host response to infection and tissue damage. Activation of the complement cascade generates anaphylatoxins including C5a and C3a. C5a exerts aExpand
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