• Title/Summary/Keyword: Receptor complex

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Beryllium(II) Recognition by Allosteric Effects in 1,2-Ethylenedioxybenzene Based Ditopic Receptors

  • Kim, Dong-Wan;Kim, Jung-Hwan;Hwang, Jae-Young;Choi, Myong-Yong;Kim, Jae-Sang
    • Bulletin of the Korean Chemical Society
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    • v.32 no.8
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    • pp.2643-2647
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    • 2011
  • Efficient ditopic receptor, uranyl(II) N,N'-(ethylenedioxy)benzenebis(salicylideneimine) (3) for beryllium ion has been obtained upon functionalization of 1,2-ethylenedioxybenzene (1) with a uranyl-salphen (salphen = N,N'-phenylenebis(salicylideneimine)) unit. Binding affinities of the receptor, 3 in AN-DMSO (v/v 95:5) solution have been measured for alkali and alkaline earth metal ions by conductometry comparing 1. The results showed that both monotopic 1 and ditopic receptor 3 were selective for $Be^{2+}$ ions over other cations, while especially 3 that can complex both with cations (coordinated to basic oxygen of ethylenedioxybenzene) and anions (coordinated to the Lewis acidic uranyl center) results in an increase of the stability constants by a factor of $10^{2.42}$ with respect to 1. Furthermore, the $Be^{2+}$-3 interactions are demonstrated by $^1H$ NMR experiments in highly polar solvent medium, DMSO-$d_6$. Higher selectivities were also observed for $Be^{2+}$ when the ditopic receptor, 3 was incorporated into PVC membranes and tested as ion selective electrodes at neutral pH.

SNP Analysis of the Human LDL Receptor and CETP Gene in Korean Subjects with Hypertension

  • Shin, Jae-Hyun;Kang, Byung-Yong;Lee, Kang-Oh;Eo, Hyun-Shun;Bae, Joon-Seol;Kim, Ki-Tae;Kim, Hyun-Sup;Lee, Chung-Choo
    • Environmental Mutagens and Carcinogens
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    • v.22 no.1
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    • pp.47-53
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    • 2002
  • Essential hypertension is complex disorder influenced by multiple genetic and environmental factors. Alterations of lipid metabolism in plasma have been reported to be related to an increased risk of essential hypertension. The aim of this study was to investigate the relationship between two SNPs of the human LDL receptor and CETP gene and hypertension in Korean population. There were no significant differences in allele and genotype frequencies of two SNPs in normotensives and hypertensives. With respect to Hinc II RFLP in the LDL receptor gene, pooled odds ratio value indicated the significant heterogeneity among populations studied by meta-analysis (Breslow-Day test df = 2, P<0.05). In the case of Bam HI RFLP in the CETP gene,. our study is the first report of an association between the SNP of the CETP gene and hypertension, although our result failed to demonstrate the significant association between the Bam HI RFLP of the CETP gene and hypertension in Korean population. Further work, using larger sample sizes and various ethnic groups, is required to establish the precise role of these two candidate gene polymorphisms on hypertension.

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Genetic Variations of Eight Candidate Genes in Korean Obese Group

  • Kang, Byung-Youn;Lee, Kang-Oh;Bae, Joon-Seol;Kim, Ki-Tae;Yoon, Moon-Young;Lim, Seok-Rhin;Seo, Sang-Beom;Shin, Jung-Hee;Lee, Chung-Choo
    • Environmental Mutagens and Carcinogens
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    • v.22 no.1
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    • pp.39-46
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    • 2002
  • Obesity is a complex metabolic disorder with a strong genetic component. There are many candidate genes for obesity and its related phenotypes. We studied genetic variations between Korean obese and lean groups. Polymorphisms investigated were the Msp I polymorphism of the $\alpha$$_{2A}$-adrenergic receptor ($\alpha$$_{2A}$-AR) gene, the Mnl I polymorphism of the $\alpha$$_2$-adrenergic receptor ($\alpha$$_2$-AR) gene, the BstO I polymorphism of the $\beta$$_3$-adrenergic receptor ($\beta$$_3$-AR) gene, the Pml I polymorphism of the lamin A/C (LMNA) gene, the Hga I polymorphism of the clearance receptor (NPRC) gene, the Msp I polymorphism of the leptin gene, BclI polymorphism of the uncoupling protein 1 (UCPI) gene and the Hha I polymorphism of the fatty acid binding protein 2 (FABP2) gene. Among these genetic markers, Pml I polymorphism at the LMNA gene and Bcl I polymorphism at the UCP1 gene were significantly associated with obesity. However, further studies are required whether thease findings are reproduced in large population, although two polymorphisms might be useful as genetic markers in the ethiology of obesity in Korean population.ion.

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The transfer of diacylglycerol from lipophor in to fat body in larval Manduca sexta (유충 Manduca sexta 리포포린에 의한 지방체로의 디아실글리세리드 운반)

  • Yun, Hwa-Kyung
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.12 no.4
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    • pp.1770-1774
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    • 2011
  • This paper was to characterize the transfer of diacylglycerol(DAG) from lipophorin to Manduca sexta larval fat bodies. $[^3H]$-DAG-labeled Lp($[^3H]$-DAG-Lp) was incubated with the larval fat bodies under different times and the time of DAG transfer was determined. Incubation of fat bodies with $[^3H]$-DAG-Lp resulted in accumulation of DAG and TAG in the tissue. The transfer of $[^3H]$-DAG was inhibited in the presence of suramin and unlabeled lipophorin, which would be consistent with a lipophorin receptor. The effects of suramin may be complex because it can change membrane properties when bound to the lipophorin receptor and affect the rate of DAG transfer. To investigate the lipid uptake via receptor-mediated endocytosis, we treated with endocytosis inhibitors, ammonium chloride and chloroquine. The results show that the transfer process of lipid by lipophorin and fat bodies is receptor-mediated endocytosis.

In-silico and structure-based assessment to evaluate pathogenicity of missense mutations associated with non-small cell lung cancer identified in the Eph-ephrin class of proteins

  • Shubhashish Chakraborty;Reshita Baruah;Neha Mishra;Ashok K Varma
    • Genomics & Informatics
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    • v.21 no.3
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    • pp.30.1-30.13
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    • 2023
  • Ephs belong to the largest family of receptor tyrosine kinase and are highly conserved both sequentially and structurally. The structural organization of Eph is similar to other receptor tyrosine kinases; constituting the extracellular ligand binding domain, a fibronectin domain followed by intracellular juxtamembrane kinase, and SAM domain. Eph binds to respective ephrin ligand, through the ligand binding domain and forms a tetrameric complex to activate the kinase domain. Eph-ephrin regulates many downstream pathways that lead to physiological events such as cell migration, proliferation, and growth. Therefore, considering the importance of Eph-ephrin class of protein in tumorigenesis, 7,620 clinically reported missense mutations belonging to the class of variables of unknown significance were retrieved from cBioPortal and evaluated for pathogenicity. Thirty-two mutations predicted to be pathogenic using SIFT, Polyphen-2, PROVEAN, SNPs&GO, PMut, iSTABLE, and PremPS in-silico tools were found located either in critical functional regions or encompassing interactions at the binding interface of Eph-ephrin. However, seven were reported in nonsmall cell lung cancer (NSCLC). Considering the relevance of receptor tyrosine kinases and Eph in NSCLC, these seven mutations were assessed for change in the folding pattern using molecular dynamic simulation. Structural alterations, stability, flexibility, compactness, and solvent-exposed area was observed in EphA3 Trp790Cys, EphA7 Leu749Phe, EphB1 Gly685Cys, EphB4 Val748Ala, and Ephrin A2 Trp112Cys. Hence, it can be concluded that the evaluated mutations have potential to alter the folding pattern and thus can be further validated by in-vitro, structural and in-vivo studies for clinical management.

The GABAB receptor associates with regulators of G-protein signaling 4 protein in the mouse prefrontal cortex and hypothalamus

  • Kim, Gyeongwha;Jung, Soonwoong;Son, Hyeonwi;Kim, Sujeong;Choi, Jungil;Lee, Dong Hoon;Roh, Gu Seob;Kang, Sang Soo;Cho, Gyeong Jae;Choi, Wan Sung;Kim, Hyun Joon
    • BMB Reports
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    • v.47 no.6
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    • pp.324-329
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    • 2014
  • Regulators of G-protein signaling (RGS) proteins regulate certain G-protein-coupled receptor (GPCR)-mediated signaling pathways. The GABAB receptor ($GABA_BR$) is a GPCR that plays a role in the stress response. Previous studies indicate that acute immobilization stress (AIS) decreases RGS4 in the prefrontal cortex (PFC) and hypothalamus (HY) and suggest the possibility of a signal complex composed of RGS4 and $GABA_BR$. Therefore, in the present study, we tested whether RGS4 associates with $GABA_BR$ in these brain regions. We found the co-localization of RGS4 and $GABA_BR$ subtypes in the PFC and HY using double immunohistochemistry and confirmed a direct association between $GABA_{B2}R$ and RGS4 proteins using co-immunoprecipitation. Furthermore, we found that AIS decreased the amount of RGS4 bound to $GABA_{B2}R$ and the number of double-positive cells. These results indicate that $GABA_BR$ forms a signal complex with RGS4 and suggests that RGS4 is a regulator of $GABA_BR$.

Structural and Functional Roles of Caspase-8 in Extrinsic Apoptosis (Apoptosis의 외인성 경로에서 caspase-8의 구조적 및 기능적 역할)

  • Ha, Min Seon;Jeong, Mi Suk;Jang, Se Bok
    • Journal of Life Science
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    • v.31 no.10
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    • pp.954-959
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    • 2021
  • Apoptosis is an important mechanism that regulates cellular populations to maintain homeostasis, and the caspases, a family of cysteine proteases, are key mediators of the apoptosis pathway. Caspase-8 is an initiator caspase of the extrinsic apoptotic pathway, which is initiated by extracellular stimuli. Caspase-8 have two conserved domains, N-terminal tandem death effector domains (DED) and C-terminal two catalytic domain, which are important for this extrinsic apoptosis pathway. In extrinsic apoptosis pathway, death receptors which members of TNF superfamily are activated by binding of death receptor specific ligands from cell outside. After the activated death receptors recruit adaptor protein Fas-associated death domain protein (FADD), death domains (DD) of death receptor and FADD bind to each other and FADD combined with death receptor recruits procaspase-8, a precursor form of caspase-8. The DED of FADD and procaspase-8 bind to one another and FADD-bound procaspase-8 is activated by cleavage of the prodomain. This death receptor-FADD-caspase-8 complex called death inducing signaling complex (DISC). Cellular FLICE-inhibitory proteins (c-FLIPs) regulate caspase-8 activation by acting both anti- and pro-apoptotically, and caspase-8 activation initiates the activation of executioner caspases such as caspase-3. Finally activated executioner caspases complete the apoptosis by acting critically DNA degradation, nuclear condensation, plasma membrane blebbing, and the proteolysis of certain caspase substrates.

Inhibitory effect of Quercetin 3-O-$\beta$-(2"-galloyl)-rhamnopyranoside and its building moiety on the production of oxygen radicals in activated murine macrophages Raw264.7

  • Kim, Byung-Hak;Min, Kyung-Rak;Kim, Young-Soo
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.214.2-215
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    • 2003
  • Reactive oxygen species play an important role in aging. carcinogenesis, and certain neurological disorders of human beings in addition to the host-defensive mechanism of inflammatory response. Murine macrophages Raw264.7 released superoxide anions via NADPH oxidase complex and nitric oxide (NO) via iNOS synthase when the cells were stimulated with unopsonized zymosan binding to complement receptor. (omitted)

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Control of Platelet Rolling and Adhesion

  • Moskowitz, Samuel E.
    • 제어로봇시스템학회:학술대회논문집
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    • 2002.10a
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    • pp.77.1-77
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    • 2002
  • Platelets arrest bleeding and repair damaged blood vessels. The purpose of this paper is to formulate a mathematical model for the control of platelet adhesion within the vasculature consistent with experimental findings, particularly those of Frenette, Ruggeri , Savage, Yuan, Lawrence and Springer. In addition to providing some, albeit rudimentary, insight into the behavior of platelets, a numerical simulation of this theoretical model may be useful in a systematic study of pathological cases. Glycoprotein receptor complex (GPIb/V/IX), found on the platelet surface membrane, binds to the adhesive protein and ligand von Willebrand factor (vWf), located within the sub-endothelium. The binding...

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Bending of DNA by cAMP Receptor Protein(CRP)

  • 정수열
    • Journal of Life Science
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    • v.4 no.3
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    • pp.119-123
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    • 1994
  • CRP에 의한 DNA bending의 첫 실험은 cAMP, CRP, DNA complex의 gelelectrophoresis에 의해 확인되었다. Bent DNA fragment의 이동은 같은 크기의 linear fragment보다 느리며, EH cAMP, CRP, DNA 결합위치에 따라서 상이한 이동 pattern을 나타낸다. 즉, DNA 단편의 중앙에 CRP binding site가 있을 때는 말단부분에 있을 때보다 이동도가 느리다. benting각의 크기는 일반적으로 안정한 복합체의 형성에 관계하며, 큰 각을 갖는 것이 보다 더 안정된 구조를 형성하여 전사가 촉진되는 것으로 밝혀져 있다. 본고에서는 CRP에 의한 bending과 CRP에 의한 전사조절 관계와 bending의 관계에 대하여 알아보았다.

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