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Role of Helix 8 in Dopamine Receptor Signaling

Yang HS, Sun N, Zhao X, Kim HR, Park HJ, Kim KM, Chung KY

G protein-coupled receptors (GPCRs) are membrane receptors whose agonist-induced dynamic conformational changes trigger heterotrimeric G protein activation, followed by GRK-mediated phosphorylation and arrestin-mediated desensitization. Cytosolic regions of GPCRs have been...
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LGR5 and Downstream Intracellular Signaling Proteins Play Critical Roles in the Cell Proliferation of Neuroblastoma, Meningioma and Pituitary Adenoma

Hwang M, Han MH, Park HH, Choi H, Lee KY, Lee YJ, Kim JM, Cheong JH, Ryu JI, Min KW, Oh YH, Ko Y, Koh SH

Leucine-rich repeat-containing G-protein coupled receptor 5 (LGR5) has been reported to play critical roles in the proliferation of various cancer cells. However, the roles of LGR5 in brain tumors and...
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The role of the exocyst in renal ciliogenesis, cystogenesis, tubulogenesis, and development

Lipschutz

The exocyst is a highly conserved eight-subunit protein complex (EXOC1–8) involved in the targeting and docking of exocytic vesicles translocating from the trans-Golgi network to various sites in renal cells....
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Identification of phospholipase C β downstream effect on transient receptor potential canonical 1/4, transient receptor potential canonical 1/5 channels

Ko J, Myeong J, Kwak M, Jeon JH, So I

Gα(q)-coupled receptor stimulation was implied in the activation process of transient receptor potential canonical (TRPC)1/4 and TRPC1/5 heterotetrameric channels. The inactivation occurs due to phosphatidylinositol 4,5-biphosphate (PI(4,5)P₂) depletion. When PI(4,5)P₂...
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Rab GTPases as Physiological Substrates of LRRK2 Kinase

Seol W, Nam D, Son I

LRRK2 (Leucine-Rich Repeat Kinase 2) is a gene whose specific mutations cause Parkinson's disease (PD), the most common neurodegenerative movement disorder. LRRK2 harbors GTPase and kinase activities, two enzyme activities...
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Vaccine containing G protein fragment and recombinant baculovirus expressing M2 protein induces protective immunity to respiratory syncytial virus

Jo YM, Kim J, Chang J

PURPOSE: Respiratory syncytial virus (RSV) can cause serious respiratory illnesses such as pneumonia, asthma, and bronchiolitis in infants and elderly or immunocompromised individuals. An RSV vaccine has yet to be...
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Characterization of the distinct mechanism of agonist-induced canine platelet activation

Chaudhary , Kim S

Platelet activation has a major role in hemostasis and thrombosis. Various agonists including adenosine diphosphate (ADP) and thrombin interact with G protein-coupled receptors (GPCRs) which transduce signals through various G...
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Differential Transcriptome Profile and Exercise Capacity in Cardiac Remodeling by Pressure Overload versus Volume Overload

Kim KH, Kim HM, Park JS, Kim YJ

BACKGROUND: We compared the gene expression profiles in the hypertrophied myocardium of rats subjected to pressure overload (PO) and volume overload (VO) using DNA chip technology, and compared the effects...
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Fasiglifam (TAK-875), a G Protein-Coupled Receptor 40 (GPR40) Agonist, May Induce Hepatotoxicity through Reactive Oxygen Species Generation in a GPR40-Dependent Manner

Kim M, Gu GJ, Koh YS, Lee SH, Na YR, Seok SH, Lim KM

Fasiglifam (TAK-875) a G-protein coupled receptor 40 (GPR40) agonist, significantly improves hyperglycemia without hypoglycemia and weight gain, the major side effects of conventional anti-diabetics. Unfortunately, during multi-center Phase 3 clinical...
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Depolarizing Effectors of Bradykinin Signaling in Nociceptor Excitation in Pain Perception

Choi SI, Hwang SW

Inflammation is one of the main causes of pathologic pain. Knowledge of the molecular links between inflammatory signals and pain-mediating neuronal signals is essential for understanding the mechanisms behind pain...
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Increased store-operated Ca²⁺ entry mediated by GNB5 and STIM1

Kang N, Kang JY, Park S, Shin DM

Recent human genetic studies have shown that Gβ5 is related to various clinical symptoms, such as sinus bradycardia, cognitive disability, and attention deficit hyperactivity disorder. Although the calcium signaling cascade...
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Can oliceridine (TRV130), an ideal novel µ receptor G protein pathway selective (µ-GPS) modulator, provide analgesia without opioid-related adverse reactions?

Ok HG, Kim SY, Lee SJ, Kim TK, Huh BK, Kim KH

All drugs have both favorable therapeutic and untoward adverse effects. Conventional opioid analgesics possess both analgesia and adverse reactions, such as nausea, vomiting, and respiratory depression. The opioid ligand binds...
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β-arrestin2 Affects Cardiac Progenitor Cell Survival through Cell Mobility and Tube Formation in Severe Hypoxia

Seo SK, Kim N, Lee JH, Kim SM, Lee SY, Bae JW, Hwang KK, Kim DW, Koch WJ, Cho MC

BACKGROUND AND OBJECTIVES: β-arrestin2 (β-arr2) basically regulates multiple signaling pathways in mammalian cells by desensitization and internalization of G-protein coupled receptors (GPCRs). We investigated impacts of β-arr2 on survival, mobility,...
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YH18968, a Novel 1,2,4-Triazolone G-Protein Coupled Receptor 119 Agonist for the Treatment of Type 2 Diabetes Mellitus

Han T, Lee BM, Park YH, Lee DH, Choi HH, Lee T, Kim H

G protein-coupled receptor 119 (GPR119) is expressed in the pancreas and gastrointestinal tract, and its activation promotes insulin secretion in the beta cells of the pancreatic islets as well as...
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System-Wide Expression and Function of Olfactory Receptors in Mammals

Oh SJ

Olfactory receptors (ORs) in mammals are generally considered to function as chemosensors in the olfactory organs of animals. They are membrane proteins that traverse the cytoplasmic membrane seven times and...
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Association of G-Protein β3 Subunit C825T Polymorphism with Seasonal Variations in Mood and Behavior

Nam YJ, Cho CH, Kim L, Lee HJ

OBJECTIVE: Seasonal affective disorder and seasonal changes in mood and behavior are associated with several genes that regulate circadian rhythms. In this study, we investigated the relationship between the C825T...
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Rab25 augments cancer cell invasiveness through a β1 integrin/EGFR/VEGF-A/Snail signaling axis and expression of fascin

Jeong BY, Cho KH, Jeong KJ, Park YY, Kim JM, Rha SY, Park CG, Mills GB, Cheong JH, Lee HY

The small GTP-binding protein Rab25 is associated with tumor formation and progression. However, recent studies have shown discordant effects of Rab25 on cancer cell progression depending on cell lineage. In...
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Leu72Met and Other Intronic Polymorphisms in the GHRL and GHSR Genes Are Not Associated with Type 2 Diabetes Mellitus, Insulin Resistance, or Serum Ghrelin Levels in a Saudi Population

Joatar FE, Al Qarni A, Ali ME, Al Masaud , Shire AM, Das N, Gumaa K, Giha HA

BACKGROUND: Ghrelin (GHRL), a gastric peptide encoded by the GHRL gene, is known to be involved in energy homeostasis via its G protein receptor, encoded by the growth hormone secretagogue...
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The activation of α₂-adrenergic receptor in the spinal cord lowers sepsis-induced mortality

Kim SS, Park SH, Lee JR, Jung JS, Suh HW

The effect of clonidine administered intrathecally (i.t.) on the mortality and the blood glucose level induced by sepsis was examined in mice. To produce sepsis, the mixture of D-galactosamine (GaLN;...
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p21-activated kinase 1 is allostericallyInhibited by naphthoquinone (NQ) derivatives

Oh SW, Lee KI, Choi JK, Kim KA, Kim EG, Shin EY

The p21-activated kinases (PAKs) are a family of serine/threonine protein kinases and activated by binding with activated Rho GTPases such as Rac or Cdc42. PAKs regulate actin cytoskeletal remodeling, cell...
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