Quinoline-Carboxylic acids are potent inhibitors that inhibit the binding of insulin-Like growth factor (IGF) to IGF-Binding proteins
2003; Elsevier BV; Volume: 13; Issue: 11 Linguagem: Inglês
10.1016/s0960-894x(03)00322-6
ISSN1464-3405
AutoresYunfei Zhu, Xiaochuan Wang, Patrick J. Connors, Keith Wilcoxen, Yinghong Gao, Raymond S. Gross, Nathalie Strack, Timothy D. Gross, James McCarthy, Qiu Xie, Nicholas Ling, Chen Chen,
Tópico(s)Lipid metabolism and disorders
Resumo4-benzylquinolines 5, based on a series of isoquinolines 1, were prepared and tested as inhibitors of the IGF/IGFBP-3 complex based on their ability to displace IGF-I from its binding to IGF-binding protein-3. SAR studies on the 6,7-dihydroxy moiety of the quinoline 5a showed that the catecol moiety could be replaced with other functional groups. Computational modeling of the 5a/mini-IGFBP-5 complex revealed the possible binding site of 5a on IGFBP-5.
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