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  • 09월 04일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제114회 대한화학회 학술발표회, 총회 및 기기전시회 안내 SPECIFIC INTRODUCTION OF A GLUTAMINE RESIDUE OF AN ALPHA-HELICAL ANTIMICROBIAL PEPTIDE CONVERTS ITS MEMBRANE DISRUPTING TO CELL PENETRATING ABILITY ELUCIDATED BY METHOTREXATED-CONJUGATED HEMOLYTIC ACTIVITY

등록일
2014년 8월 28일 16시 07분 57초
접수번호
1193
발표코드
BIO.P-641 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
10월 15일 (수요일) 16:00~19:00
발표형식
포스터
발표분야
생명화학
저자 및
공동저자
김서연, 유재훈*
서울대학교 화학교육과, Korea
Antimicrobial peptides (AMPs) are results of innate immune response of most of all living creatures against pathogens. Membrane disruption by the AMPs is a major mode of action for pathogen death, but translocation of AMPs followed by modulation of internal targets might be other causes for the pathogen death. While those cell disrupting and cell penetrating characters might exist simultaneously in natural AMPs, we tried to convert cell disrupting to the cell penetrating character by systematic mutations of a model LK peptide that possesses antimicrobial activity. For this purpose, methotrexate (MTX) was conjugated to the N-terminus of the mutant peptides and hemolytic toxicity of the resulting MTX-conjugated peptides were observed and compared with non-conjugated peptides in human red blood cells. Indeed, a specific MTX-conjugated Gln mutation (MTX-L8Q) gave 16-fold improved hemolytic toxicity relative to non-conjugated mutant. It was verified the cell penetrating ability of L8Q accompanies with no observable membrane disruption. Encouraged by these results, we applied this approach to naturally occurring amphipathic AMPs and confirmed the possibility that Gln mutation could be one of strategies for converting cell disrupting to cell penetrating character.

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