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12 items found for "Sun-Young Kong"

  • Adrenal G Protein-Coupled Receptors and the Failing Heart: A Long-distance, Yet Intimate Affair

    October 2022 "Systolic heart failure (HF) is a chronic clinical syndrome characterized by the reduction in cardiac function and still remains the disease with the highest mortality worldwide. Despite considerable advances in pharmacological treatment, HF represents a severe clinical and social burden. Chronic human HF is characterized by several important neurohormonal perturbations, emanating from both the autonomic nervous system and the adrenal glands. Circulating catecholamines (norepinephrine and epinephrine) and aldosterone elevations are among the salient alterations that confer significant hormonal burden on the already compromised function of the failing heart. This is why sympatholytic treatments (such as β-blockers) and renin-angiotensin system inhibitors or mineralocorticoid receptor antagonists, which block the effects of angiotensin II (AngII) and aldosterone on the failing heart, are part of the mainstay HF pharmacotherapy presently. The adrenal gland plays an important role in the modulation of cardiac neurohormonal stress because it is the source of almost all aldosterone, of all epinephrine, and of a significant amount of norepinephrine reaching the failing myocardium from the blood circulation. Synthesis and release of these hormones in the adrenals is tightly regulated by adrenal G protein-coupled receptors (GPCRs), such as adrenergic receptors and AngII receptors. In this review, we discuss important aspects of adrenal GPCR signaling and regulation, as they pertain to modulation of cardiac function in the context of chronic HF, by focusing on the 2 best studied adrenal GPCR types in that context, adrenergic receptors and AngII receptors (AT 1 Rs). Particular emphasis is given to findings from the past decade and a half that highlight the emerging roles of the GPCR-kinases and the β-arrestins in the adrenals, 2 protein families that regulate the signaling and functioning of GPCRs in all tissues, including the myocardium and the adrenal gland." Read more at the source #DrGPCR #GPCR #IndustryNews

  • Regulator of G Protein Signaling 20 Correlates with Long Intergenic Non-Coding RNA (lincRNAs)...

    September 2022 Regulator of G Protein Signaling 20 Correlates with Long Intergenic Non-Coding RNA (lincRNAs ; (d) RGS20 was found to be significantly associated with some tumor-related signaling pathways and long

  • Decoding β-Arrestins: from Structure to function

    detection, receptor activation initiates conformational changes, exposing an intracellular cavity (Kang recognized for inhibiting G protein signaling, they also influence specific pathways such as MAPK signaling (Song high-resolution protein structures, illuminating side chain orientations and overall conformational states (Kang , as well as MAPK cascade kinases which can be activated through specific β-arrestin conformations (Song , and their imbalance is linked to pathological conditions, including cancer (Gros, R. et al. 2000, Sun

  • Artificial intelligence – faster, smarter, cheaper GPCR drug discovery

    Artificial intelligence - Machine learning vs Deep Learning GPCRs have long been recognized as important predict subtype-selective ligands for dopamine receptors and adenosine receptors (He, Ben, Kuang, Wang & Kong , 2016; Kuang, Feng, Hu, Wang, He & Kong, 2016). 5. ability of a ligand to induce or inhibit a cellular response (pEC50 or pIC50, respectively), and how long

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

    Graeme Milligan for receiving the Order of British Empire from King Charles III in recognition of his Graeme Milligan was awarded the Order of British Empire by King Charles III for services to Biochemical

  • Odorant receptors – a bit of smell for drug discovery

    odorant molecules which initiate a neuronal response that drives odorant discrimination and perception (Young non-small-cell lung cancer OR2J3 activation induced apoptosis and inhibited cell proliferation and migration in long-term

  • 📰 GPCR Weekly News, December 18 to 31, 2023

    Morgan Healthcare Conference Andrew Hopkins appointed CBE by HM King Charles III Voyager Therapeutics

  • Glyco-sulfo hotspots in the chemokine receptor system

    the observed phenotype since many glycosyltransferases and the two TPSTs also carry O-glycosylation (King GSnP-6 displays nanomolar affinity and promising potential for blocking PSGL-1/P-selectin interaction (Wong

  • An overview of the compartmentalized GPCR Signaling: Relevance and Implications

    Nature communications, 8(1), 443. https://doi.org/10.1038/s41467-017-00357-2 Jong, Y.

  • Structural landscape of the Chemokine Receptor system

    interaction follows a common pattern which is generally described by the classic “two-site” model (Crump, Gong

  • Extracellular signal-regulated kinases – a potential pathway for GPCR-targeted drug discovery

    Sir William Osler Scientists have long sought to discover a “golden bullet” that would cure every disease signal-regulated kinases (ERK), a subset of the mitogen-activated protein kinase (MAPK) family, have long activation, contributing to the broader toolkit available for GPCR-related drug discovery (Eishingdrelo & Kongsamut References Eishingdrelo, H., & Kongsamut, S. (2013).

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