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  • 09월 05일 13시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

Inhibitors of TACE as anti-inflammatory drugs

등록일
2007년 8월 16일 14시 36분 18초
접수번호
1170
발표코드
목20G4심 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
목 15시 : 30분
발표형식
심포지엄
발표분야
의약화학 - Recent Overview for Overcoming Immune and Inflammatory Diseases
저자 및
공동저자
김명화
제일약품(주) 신약연구실,
TNF-α converting enzyme (TACE) is a major metalloproteinase for the processing of TNF-α, a key inflammatory cytokine. A novel series of Chromen-based hydroxamate compounds was designed, synthesized, and evaluated for enzyme inhibition. These compounds exhibited activities in nanomolar range in TACE enzyme assay and inhibited LPS-induced TNF-α secretion in cell-based assay with an IC50 value of 0.10 μM for the most potent one. The most potent highly water-soluble TACE inhibitor has good selectivity over MMP-1, MMP-3 and MMP-9 and oral activity in a model of TNF-α production and a collagen-induced arthritis model. Pharmacokinetic study in rat reveled that this potent compound is orally bioavailable with oral bioavailability of 41.6%.

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