School of Biomolecular and Biomedical Science, Conway Institute, University College Dublin, Belfield, Dublin 4, Ireland.
ChemMedChem. 2013 Apr;8(4):560-7. doi: 10.1002/cmdc.201200445. Epub 2013 Jan 4.
Gut hormones represent a niche subset of pharmacologically active agents that are rapidly gaining importance in medicine. Due to their exceptional specificity for their receptors, these hormones along with their analogues have attracted considerable pharmaceutical interest for the treatment of human disorders including type 2 diabetes. With the recent advances in the structural biology, a significant amount of structural information for these hormones is now available. This Minireview presents an overview of the structural aspects of these hormones, which have roles in physiological processes such as insulin secretion, as well as a discussion on the relevant structural modifications used to improve these hormones for the treatment of type 2 diabetes.
肠激素是一类具有药理活性的特殊物质,它们在医学领域的重要性日益凸显。由于其与受体的高度特异性,这些激素及其类似物已引起制药界的广泛关注,有望用于治疗包括 2 型糖尿病在内的多种人类疾病。随着结构生物学的最新进展,这些激素的大量结构信息现已可得。本文综述了这些激素在胰岛素分泌等生理过程中的结构特征,并讨论了相关的结构修饰,这些修饰旨在改善这些激素用于 2 型糖尿病的治疗效果。