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7BG0

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

Summary for 7BG0
Entry DOI10.2210/pdb7bg0/pdb
Related PRD IDPRD_900001
DescriptorMaltose/maltodextrin-binding periplasmic protein,Islet amyloid polypeptide, alpha-D-glucopyranose-(1-4)-alpha-D-glucopyranose (2 entities in total)
Functional Keywordsamylin, am833, cagrilintide, hormone
Biological sourceEscherichia coli (strain K12)
More
Total number of polymer chains4
Total formula weight178665.78
Authors
Johansson, E. (deposition date: 2021-01-05, release date: 2021-08-04, Last modification date: 2024-10-09)
Primary citationKruse, 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: 34288673
DOI: 10.1021/acs.jmedchem.1c00565
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (2.89 Å)
Structure validation

227111

數據於2024-11-06公開中

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