Search Results
119 items found for "short chain fatty acid"
- Integrative model of the FSH receptor reveals the structural role of the flexible hinge region
These models provide insights into the interface, important side-chain interactions, and activation mechanism
- Glyco-sulfo hotspots in the chemokine receptor system
linkage of other monosaccharides (Schjoldager KT et al. 2020), and usually capped by a single sialic acid phosphate 5’-phosphosulfate (PAPS) donor to the hydroxyl group of a tyrosine residue of the protein chain Removal of the terminal sialic acid was also shown to negatively impact signaling as previously appreciated
- HDX-MS-optimized approach to characterize nanobodies as tools for biochemical and structural ...
Here we describe the rapid and efficient characterization of multiple PI3Kγ binding single-chain camelid
- Dynamic recognition of naloxone, morphine and endomorphin1 in the same pocket of µ-opioid receptors
Reducing the side chain size of I322 (MORI322A) transformed naloxone from an inhibitor directly into
- Free-Energy Simulations Support a Lipophilic Binding Route for Melatonin Receptors
The side-chain flexibility of Tyr5.38 was significantly different in the two receptor subtypes, as assessed
- New role of β-arrestins in MOR signaling
under Gi/o activation-MOR, being crucial the formation of β-arrestin/ β2-adaptin and clathrin heavy chain Proc Natl Acad Sci U S A. 1993 Jun 15;90(12):5391-3. doi: 10.1073/pnas.90.12.5391.
- Cell Surface Calcium-Sensing Receptor Heterodimers: Mutant Gene Dosage Affects Ca 2+ Sensing but...
we generated CaSR-GABAB1 and CaSR-GABAB2 chimeras subject to GABAB -dependent endoplasmic reticulum sorting
- Microbial Metabolites Orchestrate a Distinct Multi-Tiered Regulatory Network in the Intestinal Epith
Recent studies revealed butyrate and secondary bile acids, produced by the intestinal microbiome, potentiate RNA sequencing of intestinal epithelial cells responding to butyrate and secondary bile acids in combination
- 📰 GPCR Weekly News, October 2 to 8, 2023
Actin in Neurotransmitter GPCR Signaling: Insights from Chronic Cholesterol Depletion Using Statin Side-Chain
- The Impact of CB1 Receptor on Nuclear Receptors in Skeletal Muscle Cells
Quantitative real-time probe-based polymerase chain reaction (qRT-PCR) assays are deployed in order to
- Decoding GPCR Function: The Role of Mutagenesis in Rational Drug Discovery
“ A substitution of one amino acid by another in a protein can have effects ranging from negligible to large-scale datasets, allowing researchers to determine the functional consequences of every possible amino acid ligand-receptor interactions, mutagenesis fills crucial knowledge gaps by revealing how specific amino acid
- Harnessing Deep Mutational Scanning for Enhanced Drug Discovery
By systematically mutating every amino acid in the protein and assessing the resulting phenotype, researchers Precision Medicine Finally, DMS aids in the advent of precision medicine by enabling a more detailed Finally, current sequencing technology restricts the mutagenizable region to about 300 amino acids, although this limitation has eased from an initial 25 amino acids and is expected to further diminish as sequencing
- Network pharmacological investigation into the mechanism of Kaixinsan powder for the treatment of...
Moreover, molecular docking results showed that Polygalaxanthone III, Girinimbine and Pachymic acid performed components in KXS, including Gomisin B, Asarone, Ginsenoside Rg1, Polygalaxanthone III and Pachymic acid
- Functional Characterization of the Venus Flytrap Domain of the Human TAS1R2 Sweet Taste Receptor
architecture, comprising a Venus Flytrap (VFT) module linked to the seven transmembrane domains (TMDs) by a short ligand affinities of hTAS1R2-VFT were drastically reduced through the introduction of single amino acid
- Decoding β-Arrestins: from Structure to function
X-ray protein crystallography yields high-resolution protein structures, illuminating side chain orientations Emerging strategies incorporate unnatural amino acids and crosslinking for structural data inference
- The NPXXY Motif Regulates β-Arrestin Recruitment by the CB1 Cannabinoid Receptor
G-protein coupled receptors (GPCRs) depends on different molecular mechanisms triggered by conserved amino acid
- 📰 GPCR Weekly News, September 25 to October 1, 2023
Drugs, and more Orthosteric ligand selectivity and allosteric probe dependence at Hydroxycarboxylic acid Developments at Aelis Farma Ion Channel Drug Developer Maxion Therapeutics Appoints Eva-Lotta Allan as Chair
- HBx induces hepatocellular carcinogenesis through ARRB1-mediated autophagy to drive the G 1/S cycle
immunohistochemistry; JAK1: Janus kinase 1; LOX: lysyl oxidase; MAP1LC3B/LC3: microtubule associated protein 1 light chain
- Molecular insights into psychedelic drug action
interest in the scientific understanding and translational potential of psychedelic drugs such as lysergic acid
- Recurrent high-impact mutations at cognate structural positions in class A G protein-coupled ...
cancer mutations across class A GPCRs and found a nonrandom distribution of positions with variant amino acid discovered that no single receptor drives this pattern, but rather multiple receptors contain amino acid
- Chemerin Forms: Their Generation and Activity
September 2022 "Chemerin is the product of the RARRES2 gene which is secreted as a precursor of 143 amino acids
- Molecular insights into regulation of constitutive activity by RNA editing 5HT2C serotonin receptor
post-transcriptional changes of mRNA nucleotides alter protein function through modification of the amino acid
- Unlocking Cell's Secrets: Spontaneous β-Arrestin-Membrane Preassociation Drives Receptor-Activation
trigger receptor internalization via interaction with the adaptor protein 2 (AP2) and clathrin heavy chain enabling it to independently reach clathrin-coated pits (CCPs) without solely relying on the initial and short-lived
- G protein coupling and activation of the metabotropic GABAB heterodimer
September 2022 "Metabotropic γ-aminobutyric acid receptor (GABABR), a class C G protein-coupled receptor
- Regulation of pulmonary surfactant by the adhesion GPCR GPR116/ADGRF5 requires a tethered agonist...
Using site-directed mutagenesis and species-swapping approaches, we identified key conserved amino acids
- The Gluopsins: Opsins without the Retinal Binding Lysine
Among them is a clade of 33 opsins that have the lysine replaced by glutamic acid.
- Addex and Indivior Extend GABAB Positive Allosteric Modulator Research Collaboration for...
agreement with Indivior PLC (LON: INDV) for discovering and developing novel oral gamma-aminobutyric acid
- 📰 GPCR Weekly News, November 6 to November 12, 2023
GPCR Binders, Drugs, and more Discovery of (S)-3-(4-(benzyloxy)phenyl)-2-(2-phenoxyacetamido)propanoic acid peptide receptors Molecular recognition of niacin and lipid-lowering drugs by the human hydroxycarboxylic acid