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Structural Refinement of Glucagon for Therapeutic Use.
Journal of Medicinal Chemistry ( IF 7.3 ) Pub Date : 2019-12-18 , DOI: 10.1021/acs.jmedchem.9b01493 Joseph R Chabenne 1 , Piotr A Mroz 2 , John P Mayer 3 , Richard D DiMarchi 1, 2
Journal of Medicinal Chemistry ( IF 7.3 ) Pub Date : 2019-12-18 , DOI: 10.1021/acs.jmedchem.9b01493 Joseph R Chabenne 1 , Piotr A Mroz 2 , John P Mayer 3 , Richard D DiMarchi 1, 2
Affiliation
Glucagon counters insulin's effects on glucose metabolism and serves as a rescue medicine in the treatment of hypoglycemia. Acute hypoglycemia, a common occurrence in insulin-dependent diabetes, is the central obstacle to correcting high blood glucose, a primary cause of long-term microvascular complications. As a result, there has been a resurgence of interest in improved glucagon therapy, including nonconventional liquid formulations, alternative routes of administration, and novel analogs with optimized biophysical properties. These options collectively minimize the complexity of glucagon delivery and enable its application in ways not feasible with conventional emergency rescue kits. These advances have indirectly promoted the integrated use of glucagon agonism with other hormones in a manner that runs counter to the long-standing pursuit of glucagon antagonism. This review summarizes novel approaches to glucagon optimization, methods with potential application to the broader family of therapeutic peptides, where biophysical challenges may be encountered.
中文翻译:
用于治疗用途的胰高血糖素的结构精制。
胰高血糖素抵抗胰岛素对葡萄糖代谢的影响,并作为低血糖治疗中的急救药物。急性低血糖症(胰岛素依赖型糖尿病中常见)是纠正高血糖的主要障碍,高血糖是长期微血管并发症的主要原因。结果,人们对改良的胰高血糖素疗法重新产生了兴趣,包括非常规液体制剂,替代给药途径以及具有优化的生物物理特性的新型类似物。这些选择共同降低了胰高血糖素递送的复杂性,并使其能够以常规应急救援工具包不可行的方式进行应用。这些进展间接促进了胰高血糖素激动剂与其他激素的综合使用,其方式与长期追求的胰高血糖素拮抗作用背道而驰。这篇综述总结了胰高血糖素优化的新方法,这些方法有可能应用于可能遇到生物物理挑战的更广泛的治疗性肽家族。
更新日期:2019-12-19
中文翻译:
用于治疗用途的胰高血糖素的结构精制。
胰高血糖素抵抗胰岛素对葡萄糖代谢的影响,并作为低血糖治疗中的急救药物。急性低血糖症(胰岛素依赖型糖尿病中常见)是纠正高血糖的主要障碍,高血糖是长期微血管并发症的主要原因。结果,人们对改良的胰高血糖素疗法重新产生了兴趣,包括非常规液体制剂,替代给药途径以及具有优化的生物物理特性的新型类似物。这些选择共同降低了胰高血糖素递送的复杂性,并使其能够以常规应急救援工具包不可行的方式进行应用。这些进展间接促进了胰高血糖素激动剂与其他激素的综合使用,其方式与长期追求的胰高血糖素拮抗作用背道而驰。这篇综述总结了胰高血糖素优化的新方法,这些方法有可能应用于可能遇到生物物理挑战的更广泛的治疗性肽家族。