مشخصات پژوهش

عنوان	Branched montbretin A mimics allow derivatisation and potent amylase inhibition†
نوع پژوهش	مقاله چاپ‌شده در مجلات علمی
کلیدواژه‌ها	glycoside montbretin A.fluorophores.
چکیده	Mimics of the complex flavonol glycoside montbretin A in which a flavonol moiety is coupled to a caffeic acid via partially peptidic linkers have proved to be potent inhibitors of human pancreatic alpha-amylase with potential as therapeutics for control of blood glucose levels. After exploring optimal linker length, a synthetic route to a version with a branched linker was devised based on the structure of the enzyme/ inhibitor complex. The resultant branched inhibitors were shown to retain nanomolar potency even when decorated with polymers as a means of modifying solubility. Similar improvements, along with nanomolar affinity, could also be achieved through conjugation to cyclodextrins which have the potential to bind to starch binding sites found on the surface of human amylase. Incorporation of a conjugatable branch into this unusual pharmacophore thereby affords considerable flexibility for further modifications to improve pharmacokinetic behaviour or as a site for attachment of capture tags or fluorophores
پژوهشگران	متیو کلور (نفر اول)، ریان اسیینی (نفر دوم)، هانگ مینگ چین (نفر سوم)، هاربیر باجوا (نفر چهارم)، سعید ناصری (نفر پنجم)، استفان ویترس (نفر ششم به بعد)، داود حبیبی (نفر ششم به بعد)