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377 items found for "Marcelo G Kazanietz"

  • 📰 GPCR Weekly News, July 10 to 16, 2023

    GPCRs in Oncology and Immunology Ovarian cancer G protein-coupled receptor 1 (OGR1) deficiency exacerbates Responses to Human β2AR Using Native Mass Spectrometry. psnGPCRdb: The Structure-network Database of G Reviews, GPCRs, and more Optical approaches for investigating neuromodulation and G Protein-Coupled Receptor Structural basis for the ubiquitination of G protein βγ subunits by KCTD5/Cullin3 E3 ligase.

  • The NPXXY Motif Regulates β-Arrestin Recruitment by the CB1 Cannabinoid Receptor

    August 2022 "Background: Activation of signaling effectors by G-protein coupled receptors (GPCRs) depends Although studies have focused on the G-protein signaling state, the mechanism for β-arrestin signaling

  • Overview of adhesion GPCRs self-activation

    Among the different families of G-protein-coupled receptors (GPCRs), adhesion GPCRs (aGPCRs) represent Lphns have promiscuous behavior, where in a constitutive state Lphns signal through different types of G form stable complexes with Gs, Gi, Gq, and G12, where like other GPCRs, the distal αH5 region of the G the αH5 tilt of G12 towards TM3/TM5 of the receptor is more pronounced compared to the rest of the G From a structural perspective, the -4 position of αH5 was key for the selectivity of G-protein coupling

  • 📰 GPCR Weekly News, February 12 to 18, 2024

    from February 12th to 18th, 2024 GPCR Activation and Signaling Fine-tuning activation specificity of G-protein-coupled receptors via automated path searching Heterotrimeric G protein signaling without GPCRs: the Gα-binding-and-activating downstream of CXCR3 depending on their subcellular localization Investigating selectivity and bias for G for the atypical chemokine receptor ACKR3 GPCRs in Cardiology, Endocrinology, and Taste The Role of G and Exhibition June 2 - 7, 2024 | Chemotactic Cytokines June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein

  • In vitro assays for the functional characterization of (psychedelic) substances at the serotonin...

    More specifically, this review covers assays to monitor the canonical G protein signaling pathway (e.g . measuring G protein recruitment/activation, inositol phosphate accumulation, or Ca2+ mobilization), assays to monitor non-canonical G protein signaling (such as arachidonic acid release), assays to monitor

  • 📰 GPCR Weekly News, June 26 to July 2, 2023

    Signaling Trans-palmitoleic acid, a dairy fat biomarker, stimulates insulin secretion and activates G GPCRs in Cardiology, Endocrinology, and Taste Adipocyte G Protein-Coupled Receptors as Potential Targets GPCRs in Neuroscience Fine-tuning GPCR-mediated neuromodulation by biasing signaling through different G G protein-coupled receptor-targeting antibody-drug conjugates: Current status and future directions. G protein-coupled receptors as targets for transformative neuropsychiatric therapeutics.

  • 📰 GPCR Weekly News, May 20 to 26, 2024

    Adhesion GPCRs Adhesion G Protein-Coupled Receptor Gpr126 (Adgrg6) Expression Profiling in Diseased Mouse , Rat, and Human Kidneys GPCR Activation and Signaling Differential regulation of G protein-coupled receptor-associated interactome in primary human cells Exploiting Cell-Based Assays to Accelerate Drug Development for G Protein Sciences as a Key to Success in Drug Discovery’ June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein

  • Decoding GPCR Function: The Role of Mutagenesis in Rational Drug Discovery

    This technique has uncovered fundamental aspects of the G protein-coupled receptor (GPCR) function, including G-protein coupled receptors: models, mutagenesis, and drug design. G., Irwin, J. J., Shoichet, B. K., & Jacobson, K. A. (2010). G. (2017).

  • Harnessing Deep Mutational Scanning for Enhanced Drug Discovery

    G., Coyote-Maestas, W., & Aashish Manglik. (2024). Molecular basis of proton-sensing by G protein-coupled receptors. BioRxiv (Cold Spring Harbor Laboratory) . https://doi.org/10.1101/2024.04.17.590000 Pines, G., Fankhauser G., & Eckert, C. A. (2020). Predicting Drug Resistance Using Deep Mutational Scanning.

  • 📰 GPCR Weekly News, May 22 to 28, 2023

    GPCR Activation and Signaling The adhesion GPCRs CELSR1-3 and LPHN3 engage G proteins via distinct activation Multiple Subthreshold GPCR Signals Combined by the G-Proteins Gαq and Gαs Activate the Caenorhabditis Bioorthogonal Tethering Enhances Drug Fragment Affinity for G Protein-Coupled Receptors in Live Cells GPCRs in Cardiology, Endocrinology, and Taste Pathophysiology and pharmacology of G protein-coupled receptors

  • 📰 GPCR Weekly News, February 26 to March 3, 2024

    Structure-guided engineering of biased-agonism in the human niacin receptor via single amino acid substitution G Bicarbonate signalling via G protein-coupled receptor regulates ischaemia-reperfusion injury GPCRs in Commentary: Analyzing invertebrate bitopic cadherin G protein-coupled receptors that bind cry toxins and Exhibition June 2 - 7, 2024 | Chemotactic Cytokines June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein

  • 📰 GPCR Weekly News, March 27 to April 4, 2023

    The adhesion G-protein-coupled receptor VLGR1/ADGRV1 controls autophagy. Regulator of G-Protein Signalling 4 (RGS4) negatively modulates nociceptin/orphanin FQ opioid receptor Methods & Updates in GPCR Research Discovery and design of G protein-coupled receptor targeting antibodies Developmental and homeostatic signaling transmitted by the G-protein coupled receptor FPR2. The impact of cryo-EM on determining allosteric modulator-bound structures of G protein-coupled receptors

  • Ode to GPCRs

    Edwin G. Edwin G. Alfred G. Alfred G. G. G protein-dependent and –independent signaling pathways and their impact on cardiac function.

  • Structure of the vasopressin hormone-V2 receptor-β-arrestin1 ternary complex

    October 2022 "Arrestins interact with G protein-coupled receptors (GPCRs) to stop G protein activation

  • 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 Understanding the mechanism by which MRAP2 regulates G protein-coupled receptors helps in elucidating

  • GPCR Buzz of the Week | Sep 23 - 29, 2024

    Postdoc in GPCR mechanosensing   Postdoctoral Position Postdoctoral research position Adhesion GPCRs The G in Oncology and Immunology Aberrant hormone receptors regulate a wide spectrum of endocrine tumors G structural representations identifies candidate drugs for pain Reviews, GPCRs, and more The role of G protein-coupled receptors and their ligands in animal domestication The repertoire of G-protein-coupled

  • Structures of oxysterol sensor EBI2/GPR183, a key regulator of the immune response

    Mutations within the oxysterol binding site and the Gαi interface attenuate G protein signaling and abolish oxysterol-mediated cell migration indicating that G protein signaling directly involves in the oxysterol-EBI2

  • 📢 Early Bird Registration Ends Tomorrow! | Sep 16 - 22, 2024

    Sakmar , Vladimir Katanaev , Helen Su , et al. for their fantastic work on Germline mutations in a G GPCR Event Spotlight Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled Postdoctoral Position Postdoctoral research position GPCR Activation and Signaling Germline mutations in a G between the anti-allodynic effects of fingolimod (FTY720) and desensitization of S1P1 receptor-mediated G-protein

  • Activation of the human chemokine receptor CX3CR1 regulated by cholesterol

    Thus, our data deepen the understanding of cholesterol modulation in GPCR (G protein-coupled receptor ) signaling and provide insights into the diversity of G protein coupling."

  • 📰 GPCR Weekly News, July 3 to 9, 2023

    GPCR Activation and Signaling G protein activation via chemokine (C-X-C motif) receptor 4 and α1b -adrenoceptor The G protein-coupled receptor GPRC5C is a saccharide sensor with a novel "off" response. Mammalian type Opsin 5 preferentially activates G14 in Gq-type G proteins triggering intracellular calcium

  • PLC-IP3-ORAI pathway participates in the activation of the MRGPRB2 receptor in mouse peritoneal...

    in the activation of the MRGPRB2 receptor in mouse peritoneal mast cells "A novel mast cell-specific G-protein-coupled receptor (GPCR), known as Mas-related G protein-coupled receptor-B2 (MRGPRB2), plays important roles

  • 📰 GPCR Weekly News, September 18 to 24, 2023

    GPCR Activation and Signaling Rules and mechanisms governing G protein coupling selectivity of GPCRs receptor trafficking GPCR Binders, Drugs, and more An inverse agonist of orphan receptor GPR61 acts by a G Serotonin Receptor 2C Signaling GPCRs in Oncology and Immunology CaaX-motif-adjacent residues influence G solid tumors for first-in-child use of PRL3-zumab humanized antibody Activation of PI3K/Akt pathway by G

  • 📰 GPCR Weekly News, September 11 to 17, 2023

    Characterization of the real-time internalization of nine GPCRs reveals distinct dependence on arrestins and G in Oncology and Immunology Phase 1/2 study of sorafenib added to cladribine, high-dose cytarabine, G-CSF through machine learning Prediction of survival and immunotherapy response by the combined classifier of G Pro-phagocytic function and structural basis of GPR84 signaling Structural diversity of leukotriene G-protein

  • 📰 GPCR Weekly News, January 23 to 29, 2023

    GPCR Activation and Signaling A multi-dimensional view of context-dependent G protein-coupled receptor The role of intracellular calcium and Rho kinase pathways in G protein-coupled receptor-mediated contractions Design, synthesis, and evaluation of substituted alkylindoles that activate G protein-coupled receptors Structural Understanding of Peptide-Bound G Protein-Coupled Receptors: Peptide-Target Interactions.

  • Location bias contributes to functionally selective responses of biased CXCR3 agonists

    November 2022 "Some G protein-coupled receptor (GPCR) ligands act as "biased agonists" that preferentially Endosomal signaling is critical for biased activation of G proteins, β-arrestins, and extracellular-signal-regulated

  • Targeting Intracellular Allosteric Sites in GPCRs

    Biased allosteric mechanisms Allosteric sites can differentially modulate G-protein and β-arrestin coupling G-protein-biased allosteric antagonists are under investigation for several GPCRs, including CCR2, CCR7 Allosteric agonists binding to intracellular sites can also promote G-protein signaling. PCO371 is a G-protein-biased allosteric agonist for the adenosine receptor A1, with the promise to improve conformational kinetics for coupling preference with downstream signaling components, such as β-arrestin and G-protein

  • 📰 GPCR Weekly News - January 9 to 15, 2023

    GPCR Binders, Drugs, and more Modelling altered signalling of G-protein coupled receptors in inflamed Reviews, GPCRs, and more Isolation and functional identification of secretin family G-protein coupled Structural Understanding of Peptide-Bound G Protein-Coupled Receptors: Peptide-Target Interactions. Deadline February 12, 2023 Current Technologies To Understand G-Protein-Coupled Receptor Molecular Pharmacology

  • Phenylalanine 193 in Extracellular Loop 2 of the β 2-Adrenergic Receptor Coordinates β-Arrestin ...

    Phenylalanine 193 in Extracellular Loop 2 of the β 2-Adrenergic Receptor Coordinates β-Arrestin Interaction G SIGNIFICANCE STATEMENT: The role of extracellular G protein-coupled receptor (GPCR) domains in mediating characterized the effects of extracellular loop mutations on agonist-promoted interactions of GPCRs with G studies reveal that F193 in extracellular loop 2 in the β2-adrenergic receptor mediates interactions with G

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