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Poly-lysine peptidomimetics having potent antimicrobial activity without hemolytic activity
Ahn, Mija,Jacob, Binu,Gunasekaran, Pethaiah,Murugan, Ravichandran N.,Ryu, Eun Kyoung,Lee, Ga-hyang,Hyun, Jae-Kyung,Cheong, Chaejoon,Kim, Nam-Hyung,Shin, Song Yub,Bang, Jeong Kyu Springer-Verlag 2014 Amino acids Vol.46 No.9
Mija Ahn,Ravichandran N. Murugan,신송엽,Eunjung Kim,Jun Hyuck Lee,김학준,Jeong-Kyu Bang 대한화학회 2012 Bulletin of the Korean Chemical Society Vol.33 No.11
Until now, few groups reported the antifreeze activity of cyclic glycopeptides; however, the tedious synthetic procedure is not amenable to study the intensive structure activity relationship. A series of N-linked cyclic glycopeptoids and glycopeptide have been prepared to evaluate antifreeze activity as a function of peptide backbone cyclization and methyl stereochemical effect on the rigid Thr position. This study has combined the cyclization protocol with solid phase peptide synthesis and obtained significant quantities of homogeneous cyclic glycopeptide and glycopeptoids. Analysis of antifreeze activity revealed that our cyclic peptide demonstrated RI activity while cyclic glycopeptoids showed no RI activity. These results suggest that the subtle changes in conformation and Thr orientation dramatically influence RI activity of N-linked glycopeptoids
Ahn, Mija,Murugan, Ravichandran N.,Shin, Song Yub,Kim, Eunjung,Lee, Jun Hyuck,Kim, Hak Jun,Bang, Jeong Kyu Korean Chemical Society 2012 Bulletin of the Korean Chemical Society Vol.33 No.11
Until now, few groups reported the antifreeze activity of cyclic glycopeptides; however, the tedious synthetic procedure is not amenable to study the intensive structure activity relationship. A series of N-linked cyclic glycopeptoids and glycopeptide have been prepared to evaluate antifreeze activity as a function of peptide backbone cyclization and methyl stereochemical effect on the rigid Thr position. This study has combined the cyclization protocol with solid phase peptide synthesis and obtained significant quantities of homogeneous cyclic glycopeptide and glycopeptoids. Analysis of antifreeze activity revealed that our cyclic peptide demonstrated RI activity while cyclic glycopeptoids showed no RI activity. These results suggest that the subtle changes in conformation and Thr orientation dramatically influence RI activity of N-linked glycopeptoids.
Ahn, Mija,Rajasekaran, Ganesan,Gunasekaran, P.,Ryu, Eun Kyoung,Lee, Ga-Hyang,Hyun, Jae-Kyung,Cheong, Chaejoon,Kim, Nam-Hyung,Shin, Song Yub,Bang, Jeong-Kyu Korean Chemical Society 2014 Bulletin of the Korean Chemical Society Vol.35 No.9
Trp residue is considered as one of the important constituents in antimicrobial peptides (AMPs) as it presence secured good activities in many cases. However, it is preferable to be changed because of their sensitivity towards light. We have synthesized the short Trp-rich AMP Pac-525 and its analogues to investigate the possibility of His(chx) as possible replacement analogue for Trp in AMPs. Based on the assay result of the antibacterial activity including anti-MRSA activity, His(chx) is considered as good candidate for the Trp replacement. Through these study, we found that His(chx) had several merits to design therapeutic antimicrobial agents compare to Trp in terms of i) increasing antibacterial activity without hemolytic activity, ii) successful in designing the short peptide (only four residues), iii) having anti-MRSA activity, iv) overcoming the light sensitivity. Furthermore, transmission electron microscopy (TEM) and dye leakage experiments suggested that P11 and P16 containing His(chx) kill bacteria via forming pore/ion channels on bacterial cell membranes.
안재경,송미자 서울産業大學校 2005 논문집 Vol.54 No.4
인터넷을 기반으로 하는 IT의 눈무신 발전과 더불어 언제, 어디서나, 시간과 장소에 구애받지 않고 인터넷을 사용할 수 있도록 하는 사회적 요구가 구체화 되고 있다. 이러한 요구에 부응하고자 국내에서는 200km 이상의 빠른 속도로 이동 중에 있더라도 초고속인터넷이나 방송 서비스를 제공할 수 있는 위성/무선통신 연동 초코속인터넷 시스템기술을 개발하고 있다. 본 연구에서는 위와 같이 개발된 연동시스템을 국내 고속철도(KTX)에 적용하여 서비스를 제공할 때, 관련 시설투자에 대한 경제적 타당성을 검토하고자 한다. 경제성 분석을 위해 현재 유럽에서 이미 제공되고 있는 고속철도 인처넷서비스를 조사하였고, 국내 고속철의 특성을 감안하여 필요시설과 장비의 항목별 비용분석을 수행하였다. 해외 사례와 비행기 등의 다른 운송수단에서 예상되는 수요 및 요금 수준에 근거하여 고속철도 인터넷서비스 매출을 시나리오별 산정하여으며, 각각에 대한 순현재가와 수익률을 도출하였다. 본 연구의 결과를 토대로 하여 위성/무선통신 연동 시스템 기술 개발에 대한 경제적 타당성을 도출할 수 있으며, 서비스 제공 시 마케팅자료로 활용할 수 있을 것이다.
Structure-Dependent Antimicrobial Theranostic Functions of Self-Assembled Short Peptide Nanoagents
Kim, Inhye,Jin, Seon-Mi,Han, Eun Hee,Ko, Eunhee,Ahn, MiJa,Bang, Woo-Young,Bang, Jeong-Kyu,Lee, Eunji American Chemical Society 2017 Biomacromolecules Vol.18 No.11
<P>Gadolinium (Gd[III])-based nanoaggregates are potential noninvasive magnetic resonance imaging (MRI) probes with excellent spatial and temporal resolution for cancer diagnosis. Peptides conjugated with Gd<SUP>3+</SUP> can aid in supramolecular scaffolding for MRI nanoagents because of their inherent biocompatibility and degradability. We report here a strategy to tune the MR relaxivity of tumor cell-targeted nanoagents and enhance the antimicrobial and anticancer activities of nanoagents based on rationally designed antimicrobial peptide (AMP) assembly. A tripeptide with glycyl-<SMALL>l</SMALL>-histidyl-<SMALL>l</SMALL>-lysine (GHK) capable of Gd<SUP>3+</SUP> chelation was attached to short AMPs containing pyrazole amino acids that spontaneously assembled as a function of the number of hydrophobic amino acid residues and the peptide length of AMPs. Aqueous coassembly of GHK with tumor-targeting, cyclic arginine-glycine-aspartic acid (cRGD)-tagged AMPs resulted in the formation of micelles, fibrils, vesicles, sheets, and planar networks. Interestingly, the two-dimensional planar network nanostructure showed less antibacterial activity and tumor cell cytotoxicity but greater drug loading/delivery and magnetic resonance signaling than micelles because of its intrinsic structural characteristics. This study can provide a rational approach for the design and fabrication of clinically useful nanoagents.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/bomaf6/2017/bomaf6.2017.18.issue-11/acs.biomac.7b00951/production/images/medium/bm-2017-00951h_0007.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/bm7b00951'>ACS Electronic Supporting Info</A></P>
Pyrrole-Based Macrocyclic Small-Molecule Inhibitors That Target Oocyte Maturation
Gunasekaran, Pethaiah,Lee, So-Rim,Jeong, Seung-Min,Kwon, Jeong-Woo,Takei, Toshiki,Asahina, Yuya,Bang, Geul,Kim, Seongnyeon,Ahn, Mija,Ryu, Eun Kyung,Kim, Hak Nam,Nam, Ki-Yub,Shin, Song Yub,Hojo, Hirono Wiley - V C H Verlag GmbH & Co. KGaA 2017 CHEMMEDCHEM Vol.12 No.8
<P>Polo-like kinase1 (PLK1) plays crucial roles in various stages of oocyte maturation. Recently, we reported that the peptidomimetic compound AB103-8, which targets the polo box domain (PBD) of PLK1, affects oocyte meiotic maturation and the resumption of meiosis. However, to overcome the drawbacks of peptidic compounds, we designed and synthesized a series of pyrrole-based small-molecule inhibitors and tested them for their effects on the rates of porcine oocyte maturation. Among them, the macrocyclic compound (E/Z)-3-(2,16-dioxo-19-(4-phenylbutyl)-3,19-diazabicyclo[15.2.1]icosa-1(20),6,17-trien-3-yl)propyl dihydrogen phosphate (4) showed the highest inhibitory activity with enhanced inhibition against embryonic blastocyst formation. Furthermore, the addition of this compound to culture media efficiently blocked the maturation of porcine and mouse oocytes, indicating its ability to penetrate the zona pellucida and cell membrane. We investigated mouse oocytes treated with compound 4, and the resulting impairment of spindle formation confirmed PLK1 inhibition. Finally, molecular modeling studies with PLK1 PBD also confirmed the presence of significant interactions between compound 4 and PLK1 PBD binding pocket residues, including those in the phosphate, tyrosine-rich, and pyrrolidine binding pockets. Collectively, these results suggest that the macrocyclic compound 4 may serve as a promising template for the development of novel contraceptive agents.</P>