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  • 09월 23일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제126회 대한화학회 학술발표회 및 총회 Small molecules can function like antibodies: Discovery of small molecule TNF-α inhibitors

2020년 9월 7일 20시 40분 30초
MEDI-2 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
화 13시 : 40분
Medicinal Chemistry - The Cutting Edge of Medicinal Chemistry
저자 및
Kye jung Shin
College of Pharmacy, The Catholic University of Korea, Korea
Cytokines (ILs, TNFα, etc.) and corresponding receptor protein bindings that are part of the stimulatory or inhibitory signaling are critical for cell response and are important therapeutic targets for immunomodulation. Antibody biologics targeting cytokines and their receptors have revolutionized treatment of cytokine-related diseases such as rheumatoid arthritis and Crohn’s disease due to their specificity, efficacy, and speed of onset. However, although antibodies have achieved considerable clinical and pharmaceutical success, unmet medical needs are existed in the antibody treatment on the points of cost, non-oral administration, and immunogenicity. To overcome these drawbacks of antibody biologics, many efforts have been carried out to find small molecule drugs that play a same role of antibody. In the last several years, we have focused on finding small molecules that bind directly to TNFα, inhibit the binding of TNFα to its receptors, and modulate its signal transduction pathways in consequence. To date, none of small molecule TNFα inhibitors have made it in vivo testing, even though there are some known small molecule scaffolds that have binding affinity to TNFα in vitro. In this presentation, we demonstrate that small molecule compounds that bind directly to TNFα could function like TNFα antibodies including in vitro and in vivo animal experiments.