Mahindroo Neeraj, Peng Yi-Hui, Lin Chia-Hui, Tan Uan-Kang, Prakash Ekambaranellore, Lien Tzu-Wen, Lu I-Lin, Lee Hong-Jen, Hsu John Tsu-An, Chen Xin, Liao Chun-Chen, Lyu Ping-Chiang, Chao Yu-Sheng, Wu Su-Ying, Hsieh Hsing-Pang
Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, 35 Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, Republic of China.
J Med Chem. 2006 Oct 19;49(21):6421-4. doi: 10.1021/jm060663c.
Type 2 diabetes has rapidly reached an epidemic proportion becoming a major threat to global public health. PPAR agonists have emerged as a leading class of oral antidiabetic drugs. We report a structure biology analysis of novel indole-based PPAR agonists to explain the structure-activity relationships and present a critical analysis of reasons for change in selectivity with change in the orientation of the same scaffolds. The results would be helpful in designing novel PPAR agonists.
2型糖尿病已迅速发展到流行程度，成为全球公共卫生的重大威胁。过氧化物酶体增殖物激活受体（PPAR）激动剂已成为一类主要的口服抗糖尿病药物。我们报告了新型吲哚基PPAR激动剂的结构生物学分析，以解释构效关系，并对同一支架方向改变时选择性变化的原因进行批判性分析。这些结果将有助于设计新型PPAR激动剂。
