Mowery Brendan P, Prasad Vidya, Kenesky Craig S, Angeles Angie R, Taylor Laurie L, Feng Jin-Jye, Chen Wen-Long, Lin Atsui, Cheng Fong-Chi, Smith Amos B, Hirschmann Ralph
Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA.
Org Lett. 2006 Sep 28;8(20):4397-400. doi: 10.1021/ol061488x.
The design, synthesis, and evaluation of a series of catechol-based non-peptide peptidomimetics of the peptide hormone somatostatin have been achieved. These ligands comprise the simplest known non-peptide mimetics of the i + 1 and i + 2 positions of the somatostatin beta-turn. Incorporation of an additional side chain to include the i position of the beta-turn induces a selective 9-fold affinity enhancement at the sst2 receptor.
已完成一系列基于儿茶酚的肽激素生长抑素非肽类拟肽的设计、合成及评估。这些配体构成了生长抑素β-转角处i + 1和i + 2位置已知最简单的非肽类模拟物。引入额外侧链以包含β-转角的i位置会在sst2受体处诱导选择性9倍的亲和力增强。
