7BG0

Fusion of MBP and the backbone of the long-acting amylin analog AM833.

7BG0 の概要

• エントリーDOI: 10.2210/pdb7bg0/pdb
• 関連するBIRD辞書のPRD_ID: PRD_900001
• 分子名称: Maltose/maltodextrin-binding periplasmic protein,Islet amyloid polypeptide, alpha-D-glucopyranose-(1-4)-alpha-D-glucopyranose (2 entities in total)
• 機能のキーワード: amylin, am833, cagrilintide, hormone
• 由来する生物種: Escherichia coli (strain K12); 詳細
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 178665.78

構造登録者

Johansson, E. (登録日: 2021-01-05, 公開日: 2021-08-04, 最終更新日: 2024-10-09)

主引用文献

Kruse, T.,Hansen, J.L.,Dahl, K.,Schaffer, L.,Sensfuss, U.,Poulsen, C.,Schlein, M.,Hansen, A.M.K.,Jeppesen, C.B.,Dornonville de la Cour, C.,Clausen, T.R.,Johansson, E.,Fulle, S.,Skyggebjerg, R.B.,Raun, K.
Development of Cagrilintide, a Long-Acting Amylin Analogue.
J.Med.Chem., 64:11183-11194, 2021

PubMed Abstract: A hallmark of the pancreatic hormone amylin is its high propensity toward the formation of amyloid fibrils, which makes it a challenging drug design effort. The amylin analogue pramlintide is commercially available for diabetes treatment as an adjunct to insulin therapy but requires three daily injections due to its short half-life. We report here the development of the stable, lipidated long-acting amylin analogue cagrilintide () and some of the structure-activity efforts that led to the selection of this analogue for clinical development with obesity as an indication. Cagrilintide is currently in clinical trial and has induced significant weight loss when dosed alone or in combination with the GLP-1 analogue semaglutide.

PubMed: 34288673
DOI: 10.1021/acs.jmedchem.1c00565

実験手法

X-RAY DIFFRACTION (2.89 Å)