• Molecules and Cells
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• v.45 no.11
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• pp.789-791
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• 2022

Targeting fibroblast growth factor receptors (FGFRs) has been slow compared to other targeted cancer therapies for receptor tyrosine kinases, such as epidermal growth factor receptors. The low efficacy and variable response have limited the growth of FGFR inhibitors in clinical use. Nevertheless, recent systematic and genomic approaches have identified the biological conditions for effectively targeting FGFRs and can accelerate the development of targeted drugs. Under clinical and preclinical trials, the inhibitors started fast growing furious races to target FGFRs. Finally, FGFRs will be more actionable and targetable with more precise and effective drugs at the end of the race, passing the finish line.

• Korean Journal of Environmental Biology
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• v.22 no.4
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• pp.479-486
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• 2004

Phytoestrogens display estrogen-like activity because of their structural similarity to human estrogens and exhibit high affinity binding for the estrogen receptors (ERs). The prevalence of phytoestrogens in our diets and the biological effects that they may cause need to be fully examined. ER is the ancestral receptor from which all other steroid receptors have evolved. Although phytoestrogens serve specific signaling functions between the plants and insects, fungi, and bacteria, many chemical signals are often misinterpreted as estrogenic signals in non-target organisms such as vertebrates. There are no ERs in plants or in their most common partners, insects. However, Rhizobium soil bacteria have NodD proteins which is an intended target of phytoestrogen signaling and share genetic homology with the ER. These two evolutionarily distant receptors both recognize and respond to a shared group of chemical signals and ligands, including both agonists and antagonists. This review briefly summarizes estrogen and estrogen receptors, kinds of important phytoestrogens, their health effects as well as some of the evolutionary aspects of mechanism by which phytoestrogen mimics the endogenous ER signaling in our body.

• Biomolecules & Therapeutics
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• v.25 no.1
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• pp.26-43
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• 2017

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 with specific binding sites for extracellular molecules internalize via vesicles. G protein-coupled receptors (GPCRs) are the largest single family of plasma-membrane receptors with more than 1000 family members. But the molecular mechanisms involved in the regulation of GPCRs are believed to be highly conserved. For example, receptor phosphorylation in collaboration with ${\beta}$-arrestins plays major roles in desensitization and endocytosis of most GPCRs. Nevertheless, a number of subsequent studies showed that GPCR regulation, such as that by endocytosis, occurs through various pathways with a multitude of cellular components and processes. This review focused on i) functional interactions between homologous and heterologous pathways, ii) methodologies applied for determining receptor endocytosis, iii) experimental tools to determine specific endocytic routes, iv) roles of small guanosine triphosphate-binding proteins in GPCR endocytosis, and v) role of post-translational modification of the receptors in endocytosis.

• Anxiety and mood
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• v.3 no.1
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• pp.8-14
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• 2007

Although treatments of anxiety symptom have been available for decades, the biological basis for anxiety disorders in humans is just beginning to emerge. Recently, there is a growing body of literature suggesting that group II metabotrpic glutamate (mGlu) receptors and group I mGlu receptors are important in the physiological and behavioral sequelae associated with stressful stimuli. Moreover, compounds selective for mGlu receptors, particularly mGlu2/3 and/or mGlu5, have proven as effective as classical anxiolytics in various animal models of anxiety without producing many of the unwanted side effects that are typical of current therapies. This article will focus on the emerging preclinical and clinical data that implicate modulation of the mGlu receptors as a potential anxiolytic strategy.

• Proceedings of the Ginseng society Conference
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• 2004.12a
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• pp.7-11
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• 2004

We previously reported that ginseng inhibited NMDA receptors in cultured hippocampal neurons. Here, we further examined the detailed mechanism of ginseng-mediated inhibition using its main active ingredient, ginsenoside Rg$_3$. Co-application of ginsenoside Rg$_3$ with increasing concentrations of NMDA did not change the EC$_{50}$ of NMDA to the receptor, suggesting ginsenoside Rg$_3$ inhibits NMDA receptors without competing with the NMDA-binding site. Ginsenoside Rg$_3$-mediated inhibition also occurred in a distinctive manner from the well-characterized NMDA receptor open channel blocker, MK-801, However, ginsenoside Rg$_3$ produced its effect in a glycine concentration-dependent manner and shifted the glycine concentration-response curve to the right without changing the maximal response, suggesting the role of ginsenoside Rg$_3$ as a competitive NMDA receptor antagonist. We also demonstrated that ginsenoside Rg$_3$ significantly protected neurons against NMDA insults. Therefore, these results suggest that ginsenoside Rg$_3$ protects NMDA-induced neuronal death via a competitive interaction with the glycine-binding site of NMDA receptors in cultured hippocampal neurons.

• Animal cells and systems
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• v.11 no.2
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• pp.93-98
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• 2007

Gonadotropin-releasing hormone (GnRH), synthesized in the hypothalamus, plays a pivotal role in the regulation of vertebrate reproduction. Since molecular isoforms of GnRH and their receptors (GnRHR) have been isolated in a broad range of vertebrate species, GnRH and GnRHR provide an excellent model for understanding the molecular co-evolution of a peptide ligand-receptor pair. Vertebrate species possess multiple forms of GnRH, which have been created through evolutionary mechanisms such as gene/chromosome duplication, gene deletion and modification. Similar to GnRHs, GnRH receptors (GnRHR) have also been diversified evolutionarily. Comparative ligand-receptor interaction studies for non-mammalian and mammalian GnRHRs combined with mutational mapping studies of GnRHRs have aided the identification of domains or motifs responsible for ligand binding and receptor activation. Here we discuss the molecular basis of GnRH-GnRHR co-evolution, particularly the structure-function relationship regarding ligand selectivity and signal transduction of mammalian and non-mammalian GnRHRs.

• Molecules and Cells
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• v.25 no.2
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• pp.149-157
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• 2008

Dopamine is a major neurotransmitter in the mammalian central nervous system (CNS) that regulates neuroendocrine functions, locomotor activity, cognition and emotion. The dopamine system has been extensively studied because dysfunction of this system is linked to various pathological conditions including Parkinson's disease, schizophrenia, Tourette's syndrome, and drug addiction. Accordingly, intense efforts to delineate the full complement of signaling pathways mediated by individual receptor subtypes have been pursued. Dopamine D1-like receptors are of particular interest because they are the most abundant dopamine receptors in CNS. Recent work suggests that dopamine signaling could be regulated via dopamine receptor interacting proteins (DRIPs). Unraveling these DRIPs involved in the dopamine system may provide a better understanding of the mechanisms underlying CNS disorders related to dopamine system dysfunction and may help identify novel therapeutic targets.

• The Korean Journal of Nuclear Medicine
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• v.34 no.3
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• pp.159-168
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• 2000

In the 1980s, techniques to image the human subjects in a three-dimensional direction were developed. Two major techniques are SPECT (Single Photon Emission Computed Tomography) and PET (Positron Emission Tomography) which allow the detector to detect a single photon or annihilation photons emitted from the subjects injected with radiopharmaceuticals. Since the latter two techniques can measure the density of receptors, enzymes and transporters in living human, it may be very important project to develop selective methods of labeling with radionuclides and to develop new radiopharmaceuticals. There has been a considerable interest in developing new compounds which specifically bind to dopamine and serotonin receptor and transporters, and it will be thus very useful to label those compounds with radionuclides in order to gain a better understanding in biochemical and pharmacological interactions in living human. This review mentions the characteristics of radioligands for the imaging of dopamine and serotonin receptors and transporters. Although significant progress has been achieved in the development of new PET and SPECT ligands for in vivo imaging of those receptors and transporters, there are continuous needs of new diagnostic radioligands.

• Journal of Physiology & Pathology in Korean Medicine
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• v.16 no.3
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• pp.490-494
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• 2002

The purpose of this study is to investigate the effect of Shudihuang water extracts on the cGMP production of medulla and cortical membranes, receptors for atrial natriuretic peptide in the kidney by in vitro autoradiography in rats for 8, 16 weeks. The cGMP production of medullary and cortical membranes of the kidney decreased after the administration of Shudihuang water extracts. The density of receptors for atrial natriuretic peptide in the kidney decreased after the administration of Shudihuang water extracts only for 16 weeks. These results suggest that the long term administration of Shudihuang water extracts has decreased plasma renin activity and plasma levels of aldosterone modulated cGMP production of medullary and cortical membranes, density of receptors for atrial natriuretic peptide in the kidney.

• IMMUNE NETWORK
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• v.11 no.4
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• pp.191-195
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• 2011

${\beta}$-Glucans are naturally occurring polysaccharides that are produced by bacteria, yeast, fungi, and many plants. Although their pharmacological activities, such as immunomodulatory, anti-infective and anti-cancer effects, have been well studied, it is still unclear how ${\beta}$-glucans exert their activities. However, recent studies on the ${\beta}$-glucans receptors shed some light on their mechanism of action. Since ${\beta}$-glucans have large molecular weights, they must bind surface receptors to activate immune cells. In this review, we summarize the immunopharmacological activities and the potential receptors of ${\beta}$-glucans in immune cells.