Neuropeptide receptor positive allosteric modulation in epilepsy: Galanin modulation revealed

Neuropeptide receptor positive allosteric modulation in epilepsy: galanin modulation revealed.

T he therapeutic potential of neuropeptides has long been recognized; some successes have been registered, for example, in the tachykinin, endothelin, somatostatin, angiotensin, calcitonin gene-related peptide (CGRP), orexin, or glucagon-like peptide 1 (GLP1) fields (1), primarily in peripheral applications. However, given the nature of receptor–ligand interactions at the orthosteric site of G ...

Allosteric modulation of peptide ligand binding to Neuropeptide Y receptor Y1 revealed by fluorescence-based assay

MicroRNAs (miRNAs) are short, 22–25 nucleotide long transcripts that may suppress entire signaling pathways by interacting with the 3’-untranslated region (3’-UTR) of coding mRNA targets, interrupting translation and inducing degradation of these targets. The long 3’-UTRs of brain transcripts compared to other tissues predict important roles for brain miRNAs. Supporting this notion, we found th...

Allosteric modulation of the cannabinoid CB1 receptor.

We investigated the pharmacology of three novel compounds, Org 27569 (5-chloro-3-ethyl-1H-indole-2-carboxylic acid [2-(4-piperidin-1-yl-phenyl)-ethyl]-amide), Org 27759 (3-ethyl-5-fluoro-1H-indole-2-carboxylic acid [2-94-dimethylamino-phenyl)-ethyl]-amide), and Org 29647 (5-chloro-3-ethyl-1H-indole-2-carboxylic acid (1-benzyl-pyrrolidin-3-yl)-amide, 2-enedioic acid salt), at the cannabinoid CB1...

Principles of NMDA Receptor Allosteric Modulation

Allosteric Modulation of the Calcium-Sensing Receptor

The calcium (Ca(2+))-sensing receptor (CaR) belongs to family C of the G-protein coupled receptors (GPCRs). The receptor is activated by physiological levels of Ca(2+) (and Mg(2+)) and positively modulated by a range of proteinogenic L-alpha-amino acids. Recently, several synthetic allosteric modulators of the receptor have been developed, which either act as positive modulators (termed calcimi...