Covalent Hydrogen Bond Mimetics of Helical Peptide Hormones

已经确定肽激素在与其受体结合时采用螺旋形状。该项目将通过使用直接结合的化学连接物来代替相对较弱的螺旋氢键来生产这些激素的新版本。由此产生的激素模拟物将比天然激素更稳定，分子量更低，更具选择性，使其更适合作为药物。我们的新化学技术使我们第一次能够充分研究这种方法，如果成功，将适用于许多其他螺旋肽，因此可能是一种重要的药物开发技术。

Peptide hormones have been identified that adopt a helical shape when bound to their receptor. The project will produce new versions of these hormones by the use of directly bonded chemical linkers in place of the relatively weak helix hydrogen bonds. The resulting hormone mimics will be more stable, have lower molecular weight and be more selective than the natural hormones making them more suitable as drugs. Our new chemical techniques allow us for the first time to fully investigate this approach which if successful will be applicable to many other helical peptides and therefore could be an important drug development technique.