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226 items found for "InterAx Biotech"
- Regulators of G-protein signaling: essential players in GPCR signaling
Role of RGS proteins in regulating GPCR signaling: Recent studies have revealed that the interaction The interaction between RGS proteins and GPCRs is highly specific and tightly regulated; mutations in domain and other structural motifs have been shown to alter the specificity and potency of the RGS-GPCR interaction For example, μ opioid receptor (MOR) interacts with Gαi/o and Gαz subunits, which have a slow enzymatic
- Overview of adhesion GPCRs self-activation
characterize by a long extracellular region of adhesion-like domains which modulate protein-protein interactions As occurs with other GPCRs in an active state, in aGPCRs the rearrangements induced by the interaction Overall the count of interactions between the last eight αH5 residues of each G protein with the receptor showed that there are more polar interactions in Gq/Gs engagements than in G1/G12 engagements; where Gi had the fewest hydrophobic and polar interactions with the receptor and the αH5 tilt of G12 towards
- Functional Characterization of the Venus Flytrap Domain of the Human TAS1R2 Sweet Taste Receptor
molecular docking and site-directed mutagenesis studies have revealed that the VFT, CRR and TMD of TAS1R3 interact feasibility of producing milligram quantities of hTAS1R2-VFT to further characterize the mechanism of binding interaction
- 📰 GPCR Weekly News, December 18 to 31, 2023
Activation and Signaling Palmitoylation of the Glucagon-like Peptide-1 Receptor Modulates Cholesterol Interactions at the Receptor-Lipid Microenvironment Basal interaction of the orphan receptor GPR101 with arrestins leads to constitutive internalization Identification of G Protein-Coupled Receptors (GPCRs) Associated NLRP3 degradation Methods & Updates in GPCR Research Direct Binding Methods to Measure Receptor-Ligand Interactions Meetings, and Webinars January 16 - 19, 2024 | 23rd Annual PEP Talk February 3 - 7, 2024 | SLAS2024 International
- Chemokine receptor-targeted drug discovery: progress and challenges
ligand-binding and signaling patterns, by modulating ligand binding, as well as G-protein coupling or interaction These larger interfaces represent the typical protein-protein interactions which are difficult to modulate . 2009; Wang and Norcross 2008); and are also too small to be engaged by antibodies, which can only interact
- Illuminating GPCR Research: FRET and BRET-Based Sensors Shed Light on Cellular Signaling
Transfer (BRET), has revolutionized the study of GPCRs by enabling real-time monitoring of protein-protein interactions Galés, C., et al., Real-time monitoring of receptor and G-protein interactions in living cells. Eidne, Bioluminescence resonance energy transfer (BRET) for the real-time detection of protein-protein interactions
- Cell Surface Calcium-Sensing Receptor Heterodimers: Mutant Gene Dosage Affects Ca 2+ Sensing but...
Surface Calcium-Sensing Receptor Heterodimers: Mutant Gene Dosage Affects Ca 2+ Sensing but Not G Protein Interaction However, the nature of interactions between VFT units and HH bundles, and the impacts of heterozygous
- Specific Functions of Melanocortin 3 Receptor (MC3R)
appetite control, 2) the control of growth, puberty, and circadian rhythm, and, 3) its protein-protein interactions
- 📰 GPCR Weekly News, July 10 to 16, 2023
The potent BECN2-ATG14 coiled-coil interaction is selectively critical for endolysosomal degradation NEW MPGPCR Conference (November 15 -17, 2023) Structure, Mechanism, and Drug Interactions of GPCRs, Ion
- N-terminal alterations turn the gut hormone GLP-2 into an antagonist with gradual loss of GLP-2 ...
GLP-2 into an antagonist with gradual loss of GLP-2 receptor selectivity towards more GLP-1 receptor interaction
- G protein-coupled receptor signaling: transducers and effectors
their function and mechanism of action, there is a greater understanding of how effector molecules interact
- 📰 GPCR Weekly News, January 29 to February 4, 2024
Gunnar Schulte et al. on the study of the interaction of Clostridioides difficile toxin B and FZD7. bias: an emerging framework for opioid drug development Structural and functional insight into the interaction unravel neurotransmitter dynamics MFD-GDrug: multimodal feature fusion-based deep learning for GPCR-drug interaction
- Molecular basis for ligand modulation of the cannabinoid CB 1 receptor
in different functional states have significantly improved our molecular understanding of CB1 ligand interactions
- The expression and clinical significance of GPR39 in colon cancer
GPR39 is a GPCR which can interact with Zn and modulate the colonocytes' survival.
- Arginine 125 Is an Essential Residue for the Function of MRAP2
It is expressed in the paraventricular nucleus of the hypothalamus, where it interacts with various G
- Dimerization of β2-adrenergic receptor is responsible for the constitutive activity subjected to inv
A Gαs preferentially interacts with dimeric β2-AR, but not monomeric β2-AR, in a resting state, resulting
- Adhesion GPCR Consortium Newsletter - May 2024
Transitioning to study Latrophilins, I decided to test the interaction of neurexins with Latrophilins New Insights Members Torsten Schöneberg and Ines Liebscher present an interactive browser-based application PMID: 38311610 Member Dimitris Placantonakis’s identifies extended synaptotagmin 1 as an intracellular interaction
- 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 The interface indicates a strong involvement of the connecting loop.
- Identification of hub genes in the subacute spinal cord injury in rats
analysis (WGCNA) were performed using R software, and functional enrichment analysis and protein–protein interaction
- Isoform-and ligand-specific modulation of adhesion GPCR ADGRL3/Latrophilin3 by a synthetic binder
In cellular-adhesion assays, LK30 specifically broke the trans-cellular interaction of ADGRL3 with teneurin
- All Aboard the GPCR Express: Your Weekly Update is here! Oct 14-20, 2024
Gunnar Schulte for his excellent work on International Union of Basic and Clinical Pharmacology CXV: receptors reveal a discrete cellular mechanism of endosomal G protein activation Amylin receptor subunit interactions locomotive behaviors in C. elegans GPCRs in Oncology and Immunology In Silico Design of Novel RGS2-Galpha-q Interaction to Detect Intracellular Ligands for the Chemokine Receptors CCR6 and CXCR1 Reviews, GPCRs, and more International
- Endogenous ligand recognition and structural transition of a human PTH receptor
A comparison of the PTH-bound and PTHrP-bound structures reveals distinct ligand-receptor interactions
- 📰 GPCR Weekly News, July 17 to July 23, 2023
Orion Biotechnology Completes Discovery of First-in-Class Molecule Against Undrugged GPCR Target in Four MPGPCR Conference (November 15 -17, 2023) Structure, Mechanism, and Drug Interactions of GPCRs, Ion Channels
- GPCRs steer G i and G s selectivity via TM5-TM6 switches as revealed by structures of serotonin...
, we discover specific residues within TM5 and TM6 that function as micro-switches to form specific interactions
- G protein coupling and activation of the metabotropic GABAB heterodimer
We find that the inactive GP first interacts with TM3, which further leads to the TMD rearrangement and
- C3aR plays both sides in regulating resistance to bacterial infections
the complement pathway results in the production of bioactive C3a, a product of C3 cleavage, which interacts
- Endogenous ligand recognition and structural transition of a human PTH receptor
A comparison of the PTH-bound and PTHrP-bound structures reveals distinct ligand-receptor interactions
- Membrane Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case Study of...
observed differences in the binding affinity and cooperativity arise from the functional groups that interact