Search Results
176 items found for "Metabolomic alterations"
- Regulators of G-protein signaling: essential players in GPCR signaling
specific and tightly regulated; mutations in the RGS domain and other structural motifs have been shown to alter
- TM5-TM6: structural switches that modulate the coupling of serotonin receptors to Gs or Gi
orthosteric binding pocket is of great importance in GPCRs field as it supports the development of alternatives
- 📰 GPCR Weekly News, March 27 to April 4, 2023
Deficiency of G protein-coupled receptor Gpr111/Adgrf2 causes enamel hypomineralization in mice by alteration
- Chemokine receptor-targeted drug discovery: progress and challenges
Therefore, an alternative approach is to make use of chemokine receptors redundancy and the fact that
- An overview of the compartmentalized GPCR Signaling: Relevance and Implications
Tagging molecules may alter the conformation or activity of GPCRs, leading to unintended effects on downstream
- 📰 GPCR Weekly News, October 30 to November 4, 2023
opportunities for therapeutic targeting Recent progress in degradation of membrane proteins by PROTACs and alternative
- Fentanyl activates ovarian cancer and alleviates chemotherapy-induced toxicity via opioid...
Methods Proliferation, migration and apoptosis assays were performed in ovarian cancer cells after
- C1-inhibitor influence on platelet activation by thrombin receptors agonists
Flow-cytometric measurements were performed in 5, 10 and 15 min after activation."
- Synthesis and characterization of an orally bioavailable small molecule agonist of the apelin recept
summary, a potent and selective APJ agonist suitable for in vivo studies of APJ in peripheral tissues after
- High hedgehog signaling is transduced by a multikinase-dependent switch controlling the...
We provide evidence that HH promotes the stabilization of SMO by switching its fate after endocytosis
- GPR108 is required for gambogic acid inhibiting NF-κB signaling in cancer
Notably, TNFα activation of NF-κB was totally impaired after GPR108 knockout.
- Cholesterol occupies the lipid translocation pathway to block phospholipid scrambling by a GPCR
rhodopsin-like) G protein-coupled receptors (GPCRs) are constitutive phospholipid scramblases as evinced after
- Self-docking and cross-docking simulations of G protein-coupled receptor-ligand complexes
absence of extensive resampling of the input GPCR structure, and only limited sidechain flexibility after Receptor conformational sampling in advance of docking or receptor conformational adjustment after docking
- Ode to GPCRs
the various hormones, including adrenaline secreted from the anterior pituitary lobe, in carbohydrate metabolism 39] In their work, the duo further investigated the work of Gerty Cori and Carl Cori on carbohydrate metabolism Later on, Kobilka joined in with Lefkowitz to identify the shared architecture of the β-adrenergic receptor
- Drug Discovery Picks Up the Pace, Stays on Target
After all, he also complained that the perfect is the enemy of the good.
- In vivo detection of GPCR-dependent signaling using fiber photometry and FRET-based biosensors
After several weeks to allow biosensor expression, fiber photometry is used in order to record drug responses
- Addex Raises $10 Million In Equity Financing
The Unregistered Warrants have an exercise price of $6.50 per ADS, will become exercisable in 60 days after
- GB83, an Agonist of PAR2 with a Unique Mechanism of Action Distinct from Trypsin and PAR2-AP
Moreover, the recovery of the localization and function of PAR2 was significantly delayed after stimulation
- Unlocking the Therapeutic Potential of Previously Undruggable GPCRs
seven membrane-spanning α-helices, comprising the transmembrane (TM) domain of the receptor, joined by alternating the receptor, leading to the binding and activation of cytosolic effector proteins: the G proteins after
- Addex raises $4.2 million in equity financing
The Unregistered Warrants have an exercise price of $1.90 per ADS, will become exercisable in 60 days after
- Structural landscape of the Chemokine Receptor system
inactive states of CCR5, it becomes evident that there are four distinct pathways through which structural alterations
- APEX2/AUR Biosensor: A Powerful Tool for Protein Interaction and Trafficking
After the labeling reaction, the researchers purified and biotinylated proteins (those that have been
- Neurocrine Biosciences Presents Data on Treatment of Adolescent Patients with Classic Congenital ...
Hyperplasia at ENDO 2022 "06/13/22 - Substantial Reductions in Key Hormones and Hormone Precursors Observed After
- Artificial intelligence – faster, smarter, cheaper GPCR drug discovery
data comprising millions of parameters, becoming infeasible for a human to interpret, in contrast with alternative
- Differences across sexes on head-twitch behavior and 5-HT2A receptor signaling in C57BL/6J mice
properties of DOI differed among sexes - brain and plasma concentrations of DOI were lower 30 and 60 min after
- GPR125 (ADGRA3) is an autocleavable adhesion GPCR that traffics with Dlg1 to the basolateral...
., the N-terminal and C-terminal fragments, seem to remain associated after self-proteolysis, as observed
- Lack of Oestrogen Receptor Expression in Breast Cancer Cells Does Not Correlate with Kisspeptin...
signalling and physiological output in the hormone receptor-negative MDA-MB-231 and BT-20 cell lines after
- Novel interaction between neurotrophic factor-α1/carboxypeptidase E and serotonin receptor, 5-HTR1E,
Furthermore, after phosphorylating the C-terminal tail and intracellular loop 3 (ICL3) of NF-α1/CPE-5