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Inhibition of IκB Kinase β (IKKβ) and Anti-diabetic Effect of SA51
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  • Inhibition of IκB Kinase β (IKKβ) and Anti-diabetic Effect of SA51
저자명
Bhattarai. Bharat Raj,Kafle. Bhooshan,Hwang. Ji-Sun,Han. Inn-Oc,Cho. Hyeongjin
간행물명
Bulletin of the Korean Chemical Society
권/호정보
2013년|34권 8호|pp.2487-2490 (4 pages)
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

SA51, a medium potency inhibitor of protein tyrosine phosphatase 1B (PTP1B), was identified to be a potent inhibitor of $I{kappa}B$ kinase ${eta}$ ($IKK{eta}$). Consistent with this, SA51 prevented lipopolysaccharide (LPS)-induced breakdown of $I{kappa}B{alpha}$ in macrophages. The effects of SA51 in mice were compared with those of structurally related compounds, SA18 and SA32, which were previously reported as inhibitors of both enzymes - less potent against $IKK{eta}$ but more potent against PTP1B compared to SA51. SA51 improved glucose tolerance and lipid parameters in mice, consistent with the results reported for $IKK{eta}^{+/-}$ mice. In contrast, SA18 and SA32 showed anti-obesity effects without anti-diabetic effects. Collectively, the effects of SA51 could be due largely to the inhibition of $IKK{eta}$, whereas SA18 and SA32 may be more likely to inhibit PTP1B, consistent with their relative in vitro inhibitory effects.