Search Results
329 items found for "receptor binding"
- Unveiling G-protein coupled receptors as potential targets for ovarian cancer nanomedicines: from RNA sequencing data analysis to in vitro validation
< GPCR News < GPCRs in Oncology and Immunology Unveiling G-protein coupled receptors as potential targets Currently, very few G-protein coupled receptors (GPCRs) have been investigated for active targeting with GPCR Industry News Adhesion GPCRs GPCR Events, Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders
- Ep 142 with Dr Claudia Stäubert
degree in biochemistry from Leipzig University (Germany) being already fascinated by G protein-coupled receptors They also discussed the challenges of studying metabolites and their receptors, the relationship between in learning more about this topic as she realized her lack of knowledge on metabolite recognition or binding Challenges in Studying Metabolites and Receptors Claudia and Yamina discussed the challenges of studying metabolites and their receptors, particularly in relation to fermented foods.
- Ep 45 with Dr Ralf Jockers
Strosberg AD in France, where he worked on the regulation of ß-adrenergic receptors. He is the Research director at INSERM with a specific interest in G protein-coupled receptors by developing He showed the formation of melatonin receptor heteromers in vitro and in vivo and their importance in He established the concept of ligand-independent functions of orphan receptors in heterodimers with other He discovered multiple rare and loss-of-function variants of the MT2 melatonin receptors that are associated
- Ep 13 with Dr. Amynah Pradhan
Paul Clarck , where she studied opioid receptors. AstraZeneca as a postdoctoral trainee, where she studied animal models of pain and sensory neuron sensitive-receptor Brigitte Kieffer , where she studied ligand-directed signaling at the delta-opioid receptor. Amynah studied how arrestins regulate ligand-directed signaling at delta-opioid receptors, and it is Andrew Charles that who specialized in animal models of migraine and delta-opioid receptors as a therapeutic
- Distinct Activation Mechanisms of CXCR4 and ACKR3 Revealed by Single-Molecule Analysis of their Conformational Landscapes
Analysis of their Conformational Landscapes Published date June 20, 2024 Abstract "The canonical chemokine receptor CXCR4 and atypical receptor ACKR3 both respond to CXCL12 but induce different effector responses to The receptors also have distinct activation requirements. of CXCR4 and ACKR3, we employed single-molecule FRET to track discrete conformational states of the receptors This and the markedly different conformational landscapes of the receptors suggest that activation of
- Ep 152 with Dr Arthur Christopoulos
Summary Arthur's Career Journey and Allosteric Receptors Yamina and Arthur discussed Arthur's career journey and his contributions to the field of pharmacology, with a focus on allosteric receptors and He also discussed the evolution of the field, from biochemical radioligand binding assays to cell-based They also discussed their own research on chemokine receptors and the importance of understanding the They also delved into the different signaling of Class B receptors and the potential for modulation at
- Lactate receptor GPR81 drives breast cancer growth and invasiveness through regulation of ECM properties and Notch ligand DLL4
< GPCR News < GPCRs in Oncology and Immunology Lactate receptor GPR81 drives breast cancer growth and properties and Notch ligand DLL4 Published date November 22, 2023 Abstract " Background: The lactate receptor Key findings were additionally studied in other breast cancer cell lines and in mammary epithelial cells Our findings reveal a new GPR81-driven mechanism in breast cancer and substantiate GPR81 as a promising GPCR Industry News Adhesion GPCRs GPCR Events, Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders
- The landscape of cancer-rewired GPCR signaling axes
signaling axes Published date May 8, 2024 Abstract "We explored the dysregulation of G-protein-coupled receptor We derived an interaction network of receptors with ligands and their biosynthetic enzymes. The expression of both receptor-ligand (or enzymes) partners improved patient stratification, suggesting Remarkably, we identified many such axes across several cancer molecular subtypes, including many involving receptor-biosynthetic from these actionable axes, including, e.g., muscarinic, adenosine, 5-hydroxytryptamine, and chemokine receptors
- Increased protease-activated receptor 1 autoantibodies are associated with severe COVID-19
< GPCR News < GPCRs in Oncology and Immunology Increased protease-activated receptor 1 autoantibodies GPCR Industry News Adhesion GPCRs GPCR Events, Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders
- Dopamine-Mediated Motor Recovery after Ischemic Stroke
regulation of axonal transport by tricyclic antidepressants (M.Sc.) and molecular pharmacology of opioid receptors Marc Caron, where I cloned the dopamine D5 receptor gene and investigated the regulation of dopaminergic and adrenergic receptors. pursues the study of the molecular, structural, pharmacological and signaling features of dopamine (DA) receptors druggability potential of new signaling partners we identified that drive the formation of different DA receptor
- Session I | Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
Holo-Adhesion GPCR Demet Araç Heterogeneity of Tethered Agonist Signaling in Adhesion G Protein-Coupled Receptors It has been suggested that the TA can regulate receptor signaling without coming out of the GAIN domain At low force or no force conditions, aGPCR may be reversibly regulated by binding and dissociation of As an undergraduate, he studied opioid receptor trafficking and G protein conformational dynamics in We utilize several genetically modified mouse models to investigate requirements for receptor activator
- Ep 33 with Dr. David E. Gloriam
Gloriam About this episode David Gloriam is a Professor in Computational Receptor Biology at the University University in Sweden where he worked on the bioinformatic identification of 24 novel human G protein-coupled receptors He later identified physiological hormones of such under characterized ‘orphan’ receptors and functional probes for a range of receptors. Gloriam on the web LinkedIn ResearchGate Twitter Google Scholar Computation Receptor Biology- Gloriam
- Ep 82 with Dr. Lauren M. Slosky
Slosky’s research is focused on understanding how neuropeptide G protein-coupled receptors (GPCRs) regulate motivated behavior and how these receptors can be targeted for therapeutic benefit. These ligands stimulate receptor β-arrestin recruitment without activating canonical G protein signaling addiction-associated behaviors in animal models without the side effects characteristic of balanced receptor Because BAMs engage less well-conserved allosteric sites and exert pathway-specific effects on receptor
- Ep 119 with Tanishka S. Saraf
Saraf " My research focuses on evaluating and targeting serotonin 1A receptors for therapeutic outcomes During my PhD, I learnt radioligand binding assays, behavioral assays, autoradiography, stereotaxic surgeries
- Natural carboxyterminal truncation of human CXCL10 attenuates glycosaminoglycan binding, CXCR3A signaling and lymphocyte chemotaxis, while retaining angiostatic activity
Oncology and Immunology Natural carboxyterminal truncation of human CXCL10 attenuates glycosaminoglycan binding chemotaxis of activated T cells and natural killer (NK) cells via interaction with its G protein-coupled receptor (GPCR), CXC chemokine receptor 3 (CXCR3). 73) was compared to intact CXCL10(1-77) using surface plasmon resonance for glycosaminoglycan (GAG) binding Conclusion: Our study shows that the C-terminal residues Lys74-Pro77 of CXCL10 are important for GAG binding
- Activation of orphan receptor GPR132 induces cell differentiation in acute myeloid leukemia
< GPCR News < GPCRs in Oncology and Immunology Activation of orphan receptor GPR132 induces cell differentiation GPCR Industry News Adhesion GPCRs GPCR Events, Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders
- Biased agonism at the GLP-1 receptor: from structure to animal models of disease
Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Biased agonism at the GLP-1 receptor
- Session VI | Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
Antibody-drug conjugates targeting CD97 in glioblastoma Dimitris Placantonakis Adhesion G protein-coupled receptor localized in the developing and adult synapses and interact with synaptic scaffold proteins and glutamate receptors We showed that oligomeric Aβ binds to ADGRC3 on the same domain required for the interaction with Frizzled3 Several adhesion G protein-coupled receptors (aGPCRs) have recently been shown to play critical roles Dimitris Placantonakis on the web Placantonakis Lab Google Scholar LinkedIn Adhesion G protein-coupled receptor
- GPCR Retreat 2023 - Part I
With respect to GPCRs, I'm particularly interested in peptide/small protein receptors and the mechanisms With a special emphasis on G protein coupled receptors and receptor activity modifying proteins in vascular motivated behavior and how these receptors can be targeted for therapeutic benefit. These ligands stimulate receptor β-arrestin recruitment without activating canonical G protein signaling Because BAMs engage less well-conserved allosteric sites and exert pathway-specific effects on receptor
- Trainee Symposium II
Symposium II Date & Time Thursday, November 2nd / 3:00 PM - 4:00 PM Title: Linking Proteinase Activated Receptor Medicine and Dentistry, Western University, researching the molecular mechanisms of Proteinase-Activated Receptors GPCR Title: Balancing G Protein Selectivity and Efficacy in the Adenosine A2A Receptor About Louis-Philippe GPCR Title: Antibodies Expand the Scope of Angiotensin Receptor Pharmacology About Meredith Skiba "Meredith pharmacology, and structural biology to study how different types of ligands modulate angiotensin receptor
- Phase 1/2 study of sorafenib added to cladribine, high-dose cytarabine, G-CSF, and mitoxantrone in untreated AML
, G-CSF, and mitoxantrone in untreated AML Published date September 12, 2023 Abstract "CC chemokine receptor -3 (hCCR3), a G protein-coupled receptor (GPCR) expressed predominantly on eosinophils, is an important This study constructed a nanogold receptor sensor using hCCR3 as the molecular recognition element and This offers a novel approach to quantitatively evaluate chemokine-receptor activation and antagonism GPCR Industry News Adhesion GPCRs GPCR Events, Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders
- Ep 83 with Dr. Jean-Philippe Pin
Jean-Philippe Pin Jean-Philippe Pin participated in the discovery of metabotropic glutamate receptors been studying the allosteric modulation and activation mechanism of this family of G protein-coupled receptors His studies led to new concepts in the GPCR field, such as the activation of cell surface receptors by
- Ep 42 with Dr. Randy Hall
graduate school at the University of California at Irvine, studying the regulation of ionotropic glutamate receptors , Oregon, to do a post-doctoral fellowship in the laboratory of Thomas Soderling studying glutamate receptor continued his post-doctoral training at Duke University, where he studied the regulation of adrenergic receptors contributions to understanding the signaling, regulation and in vivo actions of the neuroprotective receptors Randy’s lab has a special interest in studying disease-associated mutations to human GPCRs that perturb receptor
- Emerging GPCR targets for AUD: Insights from preclinical studies
for AUD: Insights from preclinical studies Published date July 5, 2024 Abstract "G protein-coupled receptors (GPCRs) are the largest group of membrane receptors in the central nervous system and one of the key Currently, many drugs available on the market act via GPCRs and these receptors remain attractive targets GPCR Industry News Adhesion GPCRs GPCR Events, Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders
- Ep 02 with Dr. Terry Hébert
Today he and his team are working on understanding receptor signaling in specialized cellular environments to gain a better grasp of receptor function in pathophysiological settings with a special interest in His favorite GPCR is the angiotensin 1 receptor, especially for its ability to activate a large variety
- Metabolic crosstalk: Extracellular ATP and the tumor microenvironment in cancer progression and therapy
In the tumor microenvironment (TME), purinergic receptors such as ATP-gated ion channels P2X1-5 and G protein-coupled receptors (GPCR) (P2Y) interact with ATP and other nucleotides, influencing diverse explores e-ATP metabolism, its purinergic signaling, and therapeutic strategies targeting associated receptors Parameswar Dalai, Reena Agrawal-Rajput Tags Extracellular ATP (e-ATP) , Immunosuppression , Purinergic receptors GPCR Industry News Adhesion GPCRs GPCR Events, Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders
- Minireview: functional roles of tissue kallikrein, kinins, and kallikrein-related peptidases in lung cancer
One approach to treating patients suffering from lung cancer is to target surface receptors overexpressed on tumor cells, such as GPCR-family kinin receptors, and proteases that control tumor progression, such Considering the multiple functions of kinin receptors and KLKs, this review highlights their roles, even Villarroel-Espindola , Carlos D Figueroa , Pamela Ehrenfeld Tags KLKs , Kallikrein-related peptidases , Kinin receptors GPCR Industry News Adhesion GPCRs GPCR Events, Meetings, and Webinars Reviews, GPCRs, and more GPCR Binders
- Molecular characterization of breast cancer cell pools with normal or reduced ability to respond to progesterone: a study based on RNA-seq
RNA-seq Published date August 8, 2023 Abstract "Background: About one-third of patients with estrogen receptor alpha (ERα)-positive breast cancer have tumors which are progesterone receptor (PR) negative. seven significantly enriched biological processes affected by PR and associated with G protein-coupled receptor Rolf Jaggi Tags Breast cancer cell pools , progesterone response , RNA-seq , CRISPR/Cas9 , estrogen receptor alpha , gene expression , Progesterone receptor.