- DA-1241, a Novel GPR119 Agonist, Improves Hyperglycaemia by Inhibiting Hepatic Gluconeogenesis and Enhancing Insulin Secretion in Diabetic Mice
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Kim Y, Lee SW, Wang H, Kim RH, Park HK, Lee H, Kang ES
- KMID: 2527726
- Diabetes Metab J.
- 2022 Mar;46(2):337-348.
- doi: 10.4093/dmj.2021.0056
Background: We investigated the antidiabetic effects of DA-1241, a novel G protein-coupled receptor (GPR) 119 agonist, in vitro and in vivo. Methods: DA-1241 was administrated to high-fat diet (HFD)-fed C57BL/6J mice... -
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- Development of Free Fatty Acid Receptor 4 (FFA4/GPR120) Agonists in Health Science
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Son SE, Kim NJ, Im DS
- KMID: 2510121
- Biomol Ther.
- 2021 Jan;29(1):22-30.
- doi: 10.4062/biomolther.2020.213
Till the 21st century, fatty acids were considered as merely building blocks for triglycerides, phospholipids, or cholesteryl esters. However, the discovery of G protein-coupled receptors (GPCRs) for free fatty acids at... -
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- Leucine-rich G Protein-coupled Receptor-5 Is Significantly Increased in the Aqueous Humor of Human Eye with Proliferative Diabetic Retinopathy
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Hong EH, Hwang M, Shin YU, Park HH, Koh SH, Cho H
- KMID: 2416251
- Exp Neurobiol.
- 2018 Jun;27(3):238-244.
- doi: 10.5607/en.2018.27.3.238
Leucine-rich G protein-coupled receptor-5 (LGR5) is known to be a stem cell marker in many organs. LGR5 may have important roles in proliferative diabetic retinopathy (PDR) because LGR5 potentiate the... -
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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?
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Ok HG, Kim SY, Lee SJ, Kim TK, Huh BK, Kim KH
- KMID: 2410828
- Korean J Pain.
- 2018 Apr;31(2):73-79.
- doi: 10.3344/kjp.2018.31.2.73
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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- Comprehensive Analysis of Non-Synonymous Natural Variants of G Protein-Coupled Receptors
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Kim HR, Duc NM, Chung KY
- KMID: 2429048
- Biomol Ther.
- 2018 Mar;26(2):101-108.
- doi: 10.4062/biomolther.2017.073
G protein-coupled receptors (GPCRs) are the largest superfamily of transmembrane receptors and have vital signaling functions in various organs. Because of their critical roles in physiology and pathology, GPCRs are... -
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- System-Wide Expression and Function of Olfactory Receptors in Mammals
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Oh SJ
- KMID: 2413245
- Genomics Inform.
- 2018 Mar;16(1):2-9.
- doi: 10.5808/GI.2018.16.1.2
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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- G2A Attenuates Propionibacterium acnes Induction of Inflammatory Cytokines in Human Monocytes
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Park AJ, Agak GW, Qin M, Hisaw LD, Pirouz A, Kao S, Marinelli , Garbán HJ, Thiboutot , Liu PT, Kim J
- KMID: 2395175
- Ann Dermatol.
- 2017 Dec;29(6):688-698.
- doi: 10.5021/ad.2017.29.6.688
BACKGROUND: Acne vulgaris is a disease of the pilosebaceous unit characterized by increased sebum production, hyperkeratinization, and immune responses to Propionibacterium acnes (PA). Here, we explore a possible mechanism by... -
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- Sphingosine 1-Phosphate Receptor Modulators and Drug Discovery
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Park SJ, Im DS
- KMID: 2367621
- Biomol Ther.
- 2017 Jan;25(1):80-90.
- doi: 10.4062/biomolther.2016.160
Initial discovery on sphingosine 1-phosphate (S1P) as an intracellular second messenger was faced unexpectedly with roles of S1P as a first messenger, which subsequently resulted in cloning of its G... -
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- US28, a Virally-Encoded GPCR as an Antiviral Target for Human Cytomegalovirus Infection
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Lee S, Chung YH, Lee C
- KMID: 2367620
- Biomol Ther.
- 2017 Jan;25(1):69-79.
- doi: 10.4062/biomolther.2016.208
Viruses continue to evolve a new strategy to take advantage of every aspect of host cells in order to maximize their survival. Due to their central roles in transducing a... -
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- Evolutionary and Comparative Genomics to Drive Rational Drug Design, with Particular Focus on Neuropeptide Seven-Transmembrane Receptors
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Furlong M, Seong JY
- KMID: 2367619
- Biomol Ther.
- 2017 Jan;25(1):57-68.
- doi: 10.4062/biomolther.2016.199
Seven transmembrane receptors (7TMRs), also known as G protein-coupled receptors, are popular targets of drug development, particularly 7TMR systems that are activated by peptide ligands. Although many pharmaceutical drugs have... -
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- β-Adrenergic Receptor and Insulin Resistance in the Heart
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Mangmool S, Denkaew T, Parichatikanond W, Kurose H
- KMID: 2367618
- Biomol Ther.
- 2017 Jan;25(1):44-56.
- doi: 10.4062/biomolther.2016.128
Insulin resistance is characterized by the reduced ability of insulin to stimulate tissue uptake and disposal of glucose including cardiac muscle. These conditions accelerate the progression of heart failure and... -
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- Multifactorial Regulation of G Protein-Coupled Receptor Endocytosis
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Zhang X, Kim KM
- KMID: 2367617
- Biomol Ther.
- 2017 Jan;25(1):26-43.
- doi: 10.4062/biomolther.2016.186
Endocytosis is a process by which cells absorb extracellular materials via the inward budding of vesicles formed from the plasma membrane. Receptor-mediated endocytosis is a highly selective process where receptors... -
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- Biased G Protein-Coupled Receptor Signaling: New Player in Modulating Physiology and Pathology
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Bologna Z, Teoh JP, Bayoumi AS, Tang Y, Kim IM
- KMID: 2367616
- Biomol Ther.
- 2017 Jan;25(1):12-25.
- doi: 10.4062/biomolther.2016.165
G protein-coupled receptors (GPCRs) are a family of cell-surface proteins that play critical roles in regulating a variety of pathophysiological processes and thus are targeted by almost a third of... -
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- Recent Progress in Understanding the Conformational Mechanism of Heterotrimeric G Protein Activation
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Duc NM, Kim HR, Chung KY
- KMID: 2367615
- Biomol Ther.
- 2017 Jan;25(1):4-11.
- doi: 10.4062/biomolther.2016.169
Heterotrimeric G proteins are key intracellular coordinators that receive signals from cells through activation of cognate G protein-coupled receptors (GPCRs). The details of their atomic interactions and structural mechanisms have... -
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- Conceptual Progress for the Improvements in the Selectivity and Efficacy of G Protein-Coupled Receptor Therapeutics: An Overview
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Kim KM
- KMID: 2367614
- Biomol Ther.
- 2017 Jan;25(1):1-3.
- doi: 10.4062/biomolther.2016.262
No abstract available. -
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- Roles of Dopamine D₂ Receptor Subregions in Interactions with β-Arrestin2
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Zhang X, Choi BG, Kim KM
- KMID: 2351676
- Biomol Ther.
- 2016 Sep;24(5):517-522.
- doi: 10.4062/biomolther.2015.198
β-Arrestins are one of the protein families that interact with G protein-coupled receptors (GPCRs). The roles of β-arrestins are multifaceted, as they mediate different processes including receptor desensitization, endocytosis, and... -
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- Differential Gene Expression in GPR40-Overexpressing Pancreatic beta-cells Treated with Linoleic Acid
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Kim IS, Yang SY, Han JH, Jung SH, Park HS, Myung CS
- KMID: 2285566
- Korean J Physiol Pharmacol.
- 2015 Mar;19(2):141-149.
- doi: 10.4196/kjpp.2015.19.2.141
"G protein-coupled receptor 40" (GPR40), a receptor for long-chain fatty acids, mediates the stimulation of glucose-induced insulin secretion. We examined the profiles of differential gene expression in GPR40-activated cells treated... -
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- Kisspeptin/G protein-coupled receptor-54 system as an essential gatekeeper of pubertal development
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Rhie YJ
- KMID: 2047461
- Ann Pediatr Endocrinol Metab.
- 2013 Jun;18(2):55-59.
- doi: 10.6065/apem.2013.18.2.55
Puberty is the end-point of a complex series of developmental events, defined by the dynamic interaction between genetic factors and environmental cues, ultimately leading to the attainment of reproductive capacity.... -
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- Characteristics in Molecular Vibrational Frequency Patterns between Agonists and Antagonists of Histamine Receptors
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Oh SJ
- KMID: 2166496
- Genomics Inform.
- 2012 Jun;10(2):128-132.
- doi: 10.5808/GI.2012.10.2.128
To learn the differences between the structure-activity relationship and molecular vibration-activity relationship in the ligand-receptor interaction of the histamine receptor, 47 ligands of the histamine receptor were analyzed by structural... -
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- The use of intra-cellular signaling pathways in anesthesiology and pain medicine field
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Joo JD
- KMID: 2236494
- Korean J Anesthesiol.
- 2009 Sep;57(3):277-283.
- doi: 10.4097/kjae.2009.57.3.277
At the level of individual cells, signaling is crucial in cell division, differentiation, metabolic control and death. Reception of the signals depends on receptor proteins that are usually at the... -
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