• 식품기술
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• 제22권4호
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• pp.721-730
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• 2009

• 통합자연과학논문집
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• 제9권2호
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• pp.121-127
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• 2016

CXC chemokine receptor 2 (CXCR2) is a prominent chemokine receptor on neutrophils. The neutrophilic inflammation in the lung diseases is found to be largely regulated through CXCR2 receptor. Antagonist of CXCR2 may reduce the neutrophil chemotaxis and alter the inflammatory response. Hence, in the present study, ligand based Comparative molecular field analysis (CoMFA) was performed on a series of CXCR2 antagonist named pyrimidine-5-carbonitrile-6-alkyl derivatives. The optimum CoMFA model was obtained with statistically significant cross-validated coefficients ($q^2$) of 0.568 and conventional coefficients ($r^2$) of 0.975. The contour maps suggest the important structural modifications and this study can be used to guide the development of potent CXCR2 antagonist.

• Bulletin of the Korean Chemical Society
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• 제31권7호
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• pp.1827-1828
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• 2010

• 한국어병학회지
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• 제20권3호
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• pp.299-306
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• 2007

Cysteine-cysteine chemokine receptor 9 (CCR9) homologue cDNA was isolated from olive flounder leukocyte cDNA library. Olive flounder CCR9 homologue consisted of 1709 bp encoding 367amino acid residues. When compared with other known CCR peptide sequences, the most conserved region of the olive flounder CCR9 peptide is the seven transmembranes. A phylogenetic analysis based on the deduced amino acid sequence showed the homologous relationship between the olive flounder CCR9 sequence and that of Mouse CCR9. The olive flounder CCR9 gene was predominantly expressed in the Peripheral blood leukocytes (PBLs), kidney, spleen, and gills.

• 통합자연과학논문집
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• 제10권4호
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• pp.209-215
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• 2017

CXC chemokine receptor 2 (CXCR2) is a prominent chemokine receptor on neutrophils. CXCR2 antagonist may reduce the neutrophil chemotaxis and alter the inflammatory response because the neutrophilic inflammation in the lung diseases is found to be largely regulated through CXCR2 receptor. Hence, in the present study, Topomer based Comparative Molecular Field Analysis (Topomer CoMFA) was performed on a series of CXCR2 antagonist named pyrimidine-5-carbonitrile-6-alkyl derivatives. The best Topomer COMFA model was obtained with significant cross-validated correlation coefficient ($q^2$ = 0.487) and non cross-validated correlation coefficients ($r^2$ = 0.980). The model was evaluated with six external test compounds and its $r^2{_{pred}}$ was found to be 0.616. The steric and electrostatic contribution map show that presence of bulkier and electropositive group around cyclopropyl ring may contribute more for improving the biological activities of these compounds. The generated Topomer CoMFA model could be helpful for future design of novel and structurally related CXCR2 antagonists.

• 대한의생명과학회지
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• 제18권4호
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• pp.435-437
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• 2012

House dust mite (HDM) is important in the pathogenesis of allergic diseases including asthma and atopic dermatitis. Dermatophagoides pteronissinus (Dp) is one of major HDM allergens. In this study, we investigated that Dp extract (DpE) affects on the chemotactic activity of monocytes isolated from the peripheral blood. DpE inhibited the migration of human monocytes in response to CC chemokines such as MIP-$1{\alpha}$, RANTES, HCC-4, MCP-1, and TARC. DpE did not alter the expression of CC chemokine receptors (CCRs) such as CCR1, CCR2, CCR3, CCR4, and CCR5. These results indicate that DpE blocks the chemotaxis of human monocytes and its mechanism is not involved in alteration of CCR expression. Better understanding of the effect of DpE on monocytes will enable elucidation of the role of Dp in the development of allergic diseases.

• 통합자연과학논문집
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• 제9권3호
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• pp.177-184
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• 2016

CXC chemokine receptor 2 (CXCR2) is a prominent chemokine receptor on neutrophils and it regulates the neutrophilic inflammation in the lung diseases. CXCR2 antagonist may reduce the neutrophil chemotaxis and alter the inflammatory response. Hence, in the present study, ligand based Comparative Molecular Similar Indices Analysis (CoMSIA) was performed on a series of CXCR2 antagonist named pyrimidine-5-carbonitrile-6-alkyl derivatives. The optimum CoMSIA model was obtained with statistically significant cross-validated coefficients ($q^2$) of 0.582 and conventional coefficients ($r^2$) of 0.987 with steric, electrostatic, hydrophobic, donor and acceptor fields. The contour maps suggest the important structural modifications and this study can be used to guide the development of potent CXCR2 antagonist.

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.382.1-382.1
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• 2002

Blood monocytes are the precursors for the lipid-laden foam cells of early atherosclerotic lesions. Monocyte chemoattractant protein-1 (MCP-1), a CC chemokine. and chemokine receptor 2 (CCR2) playa crucial role in the recruitment of monocytes to the vascular lesion. Using the human monocyte THP-1 cell line. we investigated the inhibitory effects of methanol extracts of 127 medicinal herbs on MCP-1-induced chemotaxis. (omitted)

• 대한흉부심장혈관외과학회:학술대회논문집
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• 대한흉부외과학회 1998년도 제30차 추계학술대회 대한흉부외과학회
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• pp.17-17
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• 1998

• BMB Reports
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• 제51권8호
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• pp.394-399
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• 2018

Human immunodeficiency virus-1 (HIV-1) transactivator of transcription (Tat) is an important viral factor in neuro-inflammation. Hindsiipropane B, present in Celastrus hindsii, possesses various biological mechanisms including anti-inflammatory activity. In this report, we explored the regulatory activity of hindsiipropane B on HIV-1 Tat-mediated chemokine production and its mode of action in astrocytes. Hindsiipropane B significantly alleviated HIV-1 Tat-mediated production of inflammatory chemokines, CCL2, CXCL8, and CXCL10. Hindsiipropane B inhibited expression of HDAC6, which is important regulator in HIV-1 Tat-mediated chemokine production. Hindsiipropane B diminished HIV-1 Tat-mediated reactive oxygen species (ROS) generation and NADPH oxidase activation/expression. Furthermore, hindsiipropane B inhibited HIV-1 Tat-mediated signaling cascades including MAPK, $NF-{\kappa}B$, and AP-1. These data suggest that hindsiipropane B exerts its inhibitory effects on HIV-1 Tat-mediated chemokine production via down-regulating the HDAC6-NADPH oxidaseMAPK-$NF-{\kappa}B$/AP-1 signaling axis, and could serve as a therapeutic lead compound against HIV-1 Tat-associated neuro-inflammation.