Herein, we demonstrate that a thiophene modification at the C8 position in the common adenine scaffold Structural analysis revealed that the introduced thiophene modification restricted receptor conformational

Precise Spatiotemporal Control of Serotonin Receptor 2C Signaling GPCRs in Oncology and Immunology CaaX-motif-adjacent

path searching Heterotrimeric G protein signaling without GPCRs: the Gα-binding-and-activating (GBA) motif

Signaling Constitutive internalisation of EP2 differentially regulates G protein signalling ArreSTick motif

Classifying tetraspanins: A universal system for numbering residues and a proposal for naming structural motifs

Allosteric modulation of conserved motifs and helices in 5HT2BR: Advances drug discovery and therapeutic

phosphorylation of BLT1 defines complex assemblies with β-arrestin serving distinct functions Phosphorylation motif

spectrometry, BRET, pull down, and transwell cell migration assays to investigate the effects of these modifications Computational analyses indicated that these modifications favor the nucleotide-free state of Gαi.

disorders, today announced it is advancing TRV045 into clinical development, following receipt of a notification

Systematic modification of 1 was performed to produce compounds with improved potency and ADME properties

Moreover, it enables reversibly photocontrolling zebrafish motility on a timescale of seconds and allows

a process by which post-transcriptional changes of mRNA nucleotides alter protein function through modification

The careful structural modifications during the lead optimization phase led to a compound with high biological

G-protein signaling activates the MAPK Fus3, which phosphorylates the RGS; however, the role of this modification

receptors as key regulators of transcriptional programmes will be introduced as well as epigenetic modifications

Our study provides mechanistic insights into the regulation of aGPCRs via post-translational modifications

September 2022 "The function of the actin cytoskeleton in cellular motility and trafficking has been

phosphopeptides of different GPCRs using cryo-EM, and discovered a significantly conserved phosphorylation motif

teaching purpose, the TeachOpenCADD material can serve as starting point for users’ project-directed modifications

incapable of promoting cell migration, a phenomenon which is likely to be mediated by changes in the cell motility

models like AlphaFold3, which can predict complex protein-molecule interactions and post-translational modifications

in GPCR Research Solvent accessibility of a GPCR transmembrane domain probed by in-membrane chemical modification

endoplasmic reticulum, GPCRs are transported to the Golgi apparatus to undergo additional post-translational modifications

intracellular signaling Therapeutic potential of allosteric modulators for the treatment of gastrointestinal motility

association, dissociation, or both, of an orthosteric ligand; 2) efficacy modulation where there are modifications

In the genito-urinary system, the activation of ORs was shown to influence the motility of spermatozoa

incapable of promoting cell migration, a phenomenon which is likely to be mediated by changes in the cell motility

negatively charged residues, as a consequence of the negatively charged aminoacids and post-translational modifications