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Allosteric Gating Mechanism Regulates Odorant Selectivity and Antagonism in Odorant Receptors.

Journal article bioRxiv · July 10, 2026 Odorant receptors (ORs) belong to class A G protein coupled receptors that detect diverse small molecules, yet the steps that link odorant association to receptor mediated selectivity remains incompletely defined. Here we combined 1.26 milliseconds of all- ... Full text Link to item Cite

Rapid odorant metabolism organizes identity- and timing-based odor representations by olfactory bulb inputs and outputs.

Journal article bioRxiv · July 7, 2026 Sensory neurons encode information about external stimuli in the form of stimulus-specific patterns of activity across their population. In the mammalian olfactory system, olfactory sensory neurons (OSNs) encode odor identity with odorant-specific combinat ... Full text Link to item Cite

Evolutionary diversity and function of odorant receptors in birds.

Journal article bioRxiv · November 21, 2025 Odorant receptors (ORs) form one of the largest gene families in vertebrates; most mammals have hundreds of intact OR genes. Although birds display diverse breeding and foraging behaviors, they were long assumed to rely minimally on olfaction. Here we show ... Full text Link to item Cite

The GPR4 antagonist NE-52-QQ57 increases survival, mitigates the hyperinflammatory response and reduces viral load in SARS-CoV-2-infected K18-hACE2 transgenic mice

Journal article Frontiers in Pharmacology · January 1, 2025 COVID-19 (Coronavirus disease 19) is caused by infection with SARS-CoV-2 (severe acute respiratory syndrome coronavirus 2) in the respiratory system and other organ systems. Tissue injuries resulting from viral infection and host hyperinflammatory response ... Full text Cite

The Roles of Proton-Sensing G-Protein-Coupled Receptors in Inflammation and Cancer.

Journal article Genes · September 2024 The precise regulation of pH homeostasis is crucial for normal physiology. However, in tissue microenvironments, it can be impacted by pathological conditions such as inflammation and cancer. Due to the overproduction and accumulation of acids (protons), t ... Full text Cite

Increased interleukin-6/C-reactive protein levels are associated with the upregulation of the adenosine pathway and serve as potential markers of therapeutic resistance to immune checkpoint inhibitor-based therapies in non-small cell lung cancer.

Journal article Journal for immunotherapy of cancer · October 2023 BackgroundSystemic immune activation, hallmarked by C-reactive protein (CRP) and interleukin-6 (IL-6), can modulate antitumor immune responses. In this study, we evaluated the role of IL-6 and CRP in the stratification of patients with non-small c ... Full text Cite

GPR4 Knockout Attenuates Intestinal Inflammation and Forestalls the Development of Colitis-Associated Colorectal Cancer in Murine Models.

Journal article Cancers · October 2023 GPR4 is a proton-sensing G protein-coupled receptor highly expressed in vascular endothelial cells and has been shown to potentiate intestinal inflammation in murine colitis models. Herein, we evaluated the proinflammatory role of GPR4 in the development o ... Full text Cite

Transwell In Vitro Cell Migration and Invasion Assays.

Book section · January 2023 Cell migration and invasion have essential roles in both normal physiology and disease. As such, methodologies to assess cell migratory and invasive capacities are necessary to elucidate normal cell processes and underlying mechanisms of disease. Here, we ... Full text Cite

GPR4 knockout attenuates intestinal inflammation and forestalls the development of colitis-associated colorectal cancer in murine models

Preprint · 2023 GPR4 is a proton-sensing G protein-coupled receptor highly expressed in vascular endothelial cells and has been shown to potentiate intestinal inflammation in murine colitis models. Herein, we evaluated the proinflammatory role of GPR4 in the development o ... Full text Cite

GPR65 (TDAG8) inhibits intestinal inflammation and colitis-associated colorectal cancer development in experimental mouse models.

Journal article Biochimica et biophysica acta. Molecular basis of disease · January 2022 GPR65 (TDAG8) is a proton-sensing G protein-coupled receptor predominantly expressed in immune cells. Genome-wide association studies (GWAS) have identified GPR65 gene polymorphisms as an emerging risk factor for the development of inflammatory bowel disea ... Full text Cite

Case Report: Peripheral blood T cells and inflammatory molecules in lung cancer patients with immune checkpoint inhibitor-induced thyroid dysfunction: Case studies and literature review.

Journal article Frontiers in oncology · January 2022 Immunotherapy has changed the paradigm of cancer treatment, yet immune checkpoint inhibitors (ICIs) such as PD-1/PD-L1 monoclonal antibodies may cause immune-related adverse events (irAEs) in some patients. In this report, two non-small cell lung cancer (N ... Full text Cite

The Proton-Sensing GPR4 Receptor Regulates Paracellular Gap Formation and Permeability of Vascular Endothelial Cells.

Journal article iScience · February 2020 GPR4 is a pH-sensing G protein-coupled receptor highly expressed in vascular endothelial cells and can be activated by protons in the inflamed tissue microenvironment. Herein, we report that acidosis-induced GPR4 activation increases paracellular gap forma ... Full text Cite

Heme-Dependent ER Stress Apoptosis: A Mechanism for the Selective Toxicity of the Dihydroartemisinin, NSC735847, in Colorectal Cancer Cells.

Journal article Frontiers in oncology · January 2020 Colorectal cancer (CRC) is a leading cause of cancer death in the United States. Artemisinin derivatives, including the dihydroartemisinin (DHA) monomers, are widely used as clinical agents for the treatment of malaria. Numerous studies demonstrate that th ... Full text Cite

Can GPR4 Be a Potential Therapeutic Target for COVID-19?

Journal article Frontiers in medicine · January 2020 Coronavirus disease 19 (COVID-19), caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), first emerged in late 2019 and has since rapidly become a global pandemic. SARS-CoV-2 infection causes damages to the lung and other organs. The clin ... Full text Cite

Isolated neutropenia as a rare but serious adverse event secondary to immune checkpoint inhibition.

Journal article Journal for immunotherapy of cancer · July 2019 BackgroundCompared to conventional chemotherapy, Immune checkpoint inhibitors (ICI) are known to have a distinct toxicity profile commonly identified as immune-related adverse events (irAEs). These irAEs that are believed to be related to immune d ... Full text Cite

Abstract 1206: Inhibition of GPR4 attenuates intestinal inflammation in a mouse colitis model

Conference Cancer Research · July 1, 2019 AbstractInflammatory bowel disease (IBD), a chronic inflammatory disorder of the digestive tract, is associated with a higher risk of colorectal cancer development. Current therapeutic approaches for IBD ... Full text Cite

Pharmacological inhibition of GPR4 remediates intestinal inflammation in a mouse colitis model.

Journal article European journal of pharmacology · June 2019 Inflammatory bowel disease (IBD) is characterized by chronic, recurring inflammation of the digestive tract. Current therapeutic approaches are limited and include biologics and steroids such as anti-TNFα monoclonal antibodies and corticosteroids, respecti ... Full text Cite

Pharmacological inhibition of GPR4 remediates intestinal inflammation in a mouse colitis model

Preprint · 2019 Inflammatory bowel disease (IBD) is characterized by chronic, recurring inflammation of the digestive tract. Current therapeutic approaches are limited and include biologics and steroids such as anti-TNFα monoclonal antibodies and corticosteroids, respecti ... Full text Cite

The proton-sensing GPR4 receptor regulates paracellular gap formation and permeability of vascular endothelial cells

Preprint · 2019 Tissue acidosis can be a consequence of numerous disease states including stroke, myocardial infarction, limb ischemia, and inflammation. Blood vessels existing in the affected tissues are associated with the progression of acidosis-related diseases. Howev ... Full text Cite

Novel mechanism of cannabidiol-induced apoptosis in breast cancer cell lines.

Journal article Breast (Edinburgh, Scotland) · October 2018 Studies have emphasized an antineoplastic effect of the non-psychoactive, phyto-cannabinoid, Cannabidiol (CBD). However, the molecular mechanism underlying its antitumor activity is not fully elucidated. Herein, we have examined the effect of CBD on two di ... Full text Cite

TDAG8 (GPR65) Inhibits Intestinal Inflammation in the DSS-Induced Experimental Colitis Mouse Model

Preprint · 2018 T cell death-associated gene 8 (TDAG8, also known as GPR65) is a proton-sensing G protein-coupled receptor (GPCR) predominantly expressed in immune cells. Genome-wide association studies identify TDAG8 as a susceptibility candidate gene linked to several h ... Full text Cite