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Protease-activated receptor 2 attenuates doxorubicin-induced apoptosis in colon cancer cells
Drug resistance represents a major problem in cancer treatment. Doxorubicin (adriamycin) is an injectable DNA intercalating drug that halts cancer...
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Blockade of protease-activated receptor 2 attenuates allergen-mediated acute lung inflammation and leukocyte recruitment in mice
Protease-activated receptor (PAR)2 has been implicated in mediating allergic airway inflammation. We investigate the role of PAR2 in lung...
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Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition
Protease-activated receptor-2 (PAR2) has been implicated in multiple pathophysiologies but drug discovery is challenging due to low small molecule...
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Serine protease PRSS56, a novel cancer-testis antigen activated by DNA hypomethylation, promotes colorectal and gastric cancer progression via PI3K/AKT axis
BackgroundCancer/testis (CT) antigens/genes are usually overexpressed in cancers and exhibit high immunogenicity, making them promising targets for...
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Cytosolic Calcium Distribution and Thrombin Receptor Activation
Since, receptor plays significant role in calcium signalling and to understand the mechanism of signalling in detail; an essential component is the...
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Neurokinin-2 receptor negatively modulates substance P responses by forming complex with Neurokinin-1 receptor
BackgroundTachykinins and their cognate receptors, neurokinin receptors (NKs) including NK1, NK2, and NK3 play vital roles in regulating various...
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Diversification of PAR signaling through receptor crosstalk
Protease activated receptors (PARs) are among the first receptors shown to transactivate other receptors: noticeably, these interactions are not...
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SARS-CoV-2: Receptor and Co-receptor Tropism Probability
The recent pandemic which arose from China, is caused by a pathogenic virus named “severe acute respiratory syndrome-related coronavirus-2...
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Inhibition of Toll-like receptor 4 and Interleukin-1 receptor prevent SARS-CoV-2 mediated kidney injury
Acute kidney injury (AKI) is a common and severe complication of the coronavirus disease 2019 (COVID-19). Severe acute respiratory syndrome...
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Methods for Investigating Transient Receptor Potential Melastatin-2 (TRPM2): A Cation Channel Activated by ADP-Ribose and Involved in Cell Death
Transient receptor potential melastatin-2 (TRPM2) is an emerging chemotherapeutic target due to its involvement in poly(ADP-ribose) metabolism and...
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AXL receptor tyrosine kinase modulates gonadotropin-releasing hormone receptor signaling
BackgroundGonadotropin-releasing hormone (GnRH) receptors are essential for reproduction and are expressed in numerous urogenital, reproductive, and...
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Structural basis of signaling regulation of the human melanocortin-2 receptor by MRAP1
G protein-coupled receptors (GPCRs) are regulated by various downstream proteins, of which the melanocortin receptor accessory protein 1 (MRAP1) is...
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Thrombin induces morphological and inflammatory astrocytic responses via activation of PAR1 receptor
Spinal cord injury (SCI) will result in the significant elevation of thrombin production at lesion site via either breakage of blood-spinal cord...
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Discovery of small molecule agonists of the Relaxin Family Peptide Receptor 2
The relaxin/insulin-like family peptide receptor 2 (RXFP2) belongs to the family of class A G-protein coupled receptors (GPCRs) and it is the only...
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Modulating effect of Eunkyo-san on expression of inflammatory cytokines and angiotensin-converting enzyme 2 in human mast cells
Eunkyo-san is widely used in the treatment of severe respiratory infections. Mast cells not only serve as host cells for the severe acute respiratory...
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Crosstalk between KDEL receptor and EGF receptor mediates cell proliferation and migration via STAT3 signaling
Hostile microenvironment of cancer cells provoke a stressful condition for endoplasmic reticulum (ER) and stimulate the expression and secretion of...
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The aryl hydrocarbon receptor controls mesenchymal stromal cell-mediated immunomodulation via ubiquitination of eukaryotic elongation factor-2 kinase
Mesenchymal stem cells (MSCs) have great therapeutic advantages due to their immunosuppressive properties. The aryl hydrocarbon receptor (AHR) is a...
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Regulators of G-protein signaling, RGS2 and RGS4, inhibit protease-activated receptor 4-mediated signaling by forming a complex with the receptor and Gα in live cells
BackgroundProtease-activated receptor 4 (PAR4) is a seven transmembrane G-protein coupled receptor (GPCR) activated by endogenous proteases, such as...
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Nuclear receptor corepressors non-canonically drive glucocorticoid receptor-dependent activation of hepatic gluconeogenesis
Nuclear receptor corepressors (NCoRs) function in multiprotein complexes containing histone deacetylase 3 (HDAC3) to alter transcriptional output...
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Angiotensin-(1–9) attenuates adriamycin-induced cardiomyopathy in rats via the angiotensin type 2 receptor
Adriamycin (ADR) causes irreversible damage to the heart, leading to ADR-induced cardiomyopathy (ACM). Angiotensin-(1–9) [Ang-(1–9)] is a peptide...
