Sabine Albold
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Metabotropic glutamate receptor 5 (mGlu<sub>5</sub>)‐positive allosteric modulators differentially induce or potentiate desensitization of mGlu<sub>5</sub> signaling in recombinant cells and neurons Open
Allosteric modulators of metabotropic glutamate receptor 5 (mGlu 5 ) are a promising therapeutic strategy for a number of neurological disorders. Multiple mGlu 5 ‐positive allosteric modulator (PAM) chemotypes have been discovered that act…
Structure-based discovery of selective positive allosteric modulators of antagonists for the M <sub>2</sub> muscarinic acetylcholine receptor Open
Significance The orthosteric binding sites of the five muscarinic acetylcholine receptor (mAChR) subtypes are highly conserved, making the development of selective antagonists challenging. The allosteric sites of these receptors are more v…
Coincident activation of adenosine A1 receptors and metabotropic glutamate receptor 5 differentially influences signalling in primary brain cell cultures Open
G protein-coupled receptors (GPCRs) are highly 'druggable' proteins and represent the largest class of current therapeutic targets. Two distinct neuromodulatory GPCRs, the adenosine A1 receptor (A1AR) and the metabotropic glutamate recepto…
Structure-Based Design and Discovery of New M<sub>2</sub>Receptor Agonists Open
Muscarinic receptor agonists are characterized by apparently strict restraints on their tertiary or quaternary amine and their distance to an ester or related center. On the basis of the active state crystal structure of the muscarinic M2 …
β2-Adrenoceptors on tumor cells play a critical role in stress-enhanced metastasis in a mouse model of breast cancer Open
Chronic stress accelerates metastasis - the main cause of death in cancer patients - through the activation of β-adrenoceptors (βARs). We have previously shown that β2AR signaling in MDA-MB-231(HM) breast cancer cells, facilitates invadopo…