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Conceptual Progress for the Improvements in the Selectivity and Efficacy of G Protein-Coupled Receptor Therapeutics: An Overview

Kim KM

No abstract available.
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Recent Progress in Understanding the Conformational Mechanism of Heterotrimeric G Protein Activation

Duc NM, Kim HR, Chung KY

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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Biased G Protein-Coupled Receptor Signaling: New Player in Modulating Physiology and Pathology

Bologna Z, Teoh JP, Bayoumi AS, Tang Y, Kim IM

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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Evolutionary and Comparative Genomics to Drive Rational Drug Design, with Particular Focus on Neuropeptide Seven-Transmembrane Receptors

Furlong M, Seong JY

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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Multifactorial Regulation of G Protein-Coupled Receptor Endocytosis

Zhang X, Kim KM

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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US28, a Virally-Encoded GPCR as an Antiviral Target for Human Cytomegalovirus Infection

Lee S, Chung YH, Lee C

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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β-Adrenergic Receptor and Insulin Resistance in the Heart

Mangmool S, Denkaew T, Parichatikanond W, Kurose H

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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Sphingosine 1-Phosphate Receptor Modulators and Drug Discovery

Park SJ, Im DS

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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