Biochemical pharmacology of the positive allosteric modulation of the GABAb receptor "in Vitro" and "in Vivo" [PDF]
, 2007 Allosteric modulators of G-protein coupled receptors (GPCRs) interact with binding sites on the receptor molecule that are topographically distinct from the classic orthosteric site.
Gjoni, Tina
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BMC Endocrine Disorders, 2021 Background Weight loss therapy is becoming more and more important, and two classes of molecules, namely amylin receptor and GLP-1 receptor agonists, have shown promise in this regard.
Anna Thorsø Larsen +4 more
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AMYLIN AND AMYLIN ANALOGS – FUTURE THERAPEUTIC STRATEGIES FOR THE TREATMENT OF TYPE 2 DIABETES AND OBESITY [PDF]
Journal of IMABAmylin is a peptide hormone co-synthesized with insulin in pancreatic beta cells at a ratio of 1:100. Notably, amylin has a pronounced tendency to form toxic amyloid fibrils, a characteristic relevant to its pathological role.
Nikolinka Koleva +2 more
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Selective non-steroidal glucocorticoid receptor agonists attenuate inflammation but do not impair intestinal epithelial cell restitution in vitro [PDF]
, 2012 Introduction: Despite the excellent anti-inflammatory and immunosuppressive action of glucocorticoids (GCs), their use for the treatment of inflammatory bowel disease (IBD) still carries significant risks in terms of frequently occurring severe side ...
Kerstin C Reuter +14 more
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Obesity and Type 2 Diabetes: Adiposopathy as a Triggering Factor and Therapeutic Options
Molecules, 2023 Obesity and type 2 diabetes (T2DM) are major public health concerns associated with serious morbidity and increased mortality. Both obesity and T2DM are strongly associated with adiposopathy, a term that describes the pathophysiological changes of the ...
Angelica Artasensi +4 more
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Inhibition of sequestration of human B-2 bradykinin receptor by phenylarsine oxide or sucrose allows determination of a receptor affinity shift and ligand dissociation in intact cells [PDF]
, 2004 Depending on their interaction with intracellular proteins, G proteincoupled receptors (GPCR) often display different affinities for agonists at 37degreesC. Determining the affinity at that temperature is often difficult in intact cells as most GPCRs are
Faussner, Alexander +3 more
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Biomedicines, 2022 Background: Dual Amylin and Calcitonin Receptor Agonists (DACRAs) are treatment candidates for obesity and type 2 diabetes. Recently, a once-weekly DACRA (KBP-A) showed promise, potentially due to its different exposure profile compared to daily DACRA ...
Nina Sonne +3 more
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Investigations on neuropeptide Y and histamine receptors by fluorescence-based and radiochemical methods [PDF]
, 2011 In the last three decades, a large amount of experimental data (for example Förster resonance energy transfer (FRET) at fluorescently labelled receptors) supported the hypothesis of the dimerization of G-protein-coupled receptors (GPCR), including ...
Lopuch, Miroslaw
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Molecular Metabolism, 2021 Objective: Dual amylin and calcitonin receptor agonists (DACRAs) are novel therapeutic agents that not only improve insulin sensitivity but also work as an adjunct to established T2DM therapies.
K.V. Andreassen +5 more
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Molecular pharmacology of an insect GABA receptor [PDF]
, 2010 Cys-loop receptors are ligand-gated ion channels that are involved in fast synaptic neurotransmission in the central and peripheral nervous system. The Cys-loop receptor RDL (‘resistant to dieldrin’) is a GABA-gated chloride channel from Drosophila ...
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