7BG0
Fusion of MBP and the backbone of the long-acting amylin analog AM833.
Summary for 7BG0
Entry DOI | 10.2210/pdb7bg0/pdb |
Related PRD ID | PRD_900001 |
Descriptor | Maltose/maltodextrin-binding periplasmic protein,Islet amyloid polypeptide, alpha-D-glucopyranose-(1-4)-alpha-D-glucopyranose (2 entities in total) |
Functional Keywords | amylin, am833, cagrilintide, hormone |
Biological source | Escherichia coli (strain K12) More |
Total number of polymer chains | 4 |
Total formula weight | 178665.78 |
Authors | Johansson, E. (deposition date: 2021-01-05, release date: 2021-08-04, Last modification date: 2024-10-09) |
Primary citation | 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 Cited by 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: 34288673DOI: 10.1021/acs.jmedchem.1c00565 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.89 Å) |
Structure validation
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