6yau | pdb_00006yau
CRYSTAL STRUCTURE OF ASGPR 1 IN COMPLEX WITH GN-A.
Structural highlights
FunctionASGR1_HUMAN Mediates the endocytosis of plasma glycoproteins to which the terminal sialic acid residue on their complex carbohydrate moieties has been removed. The receptor recognizes terminal galactose and N-acetylgalactosamine units. After ligand binding to the receptor, the resulting complex is internalized and transported to a sorting organelle, where receptor and ligand are disassociated. The receptor then returns to the cell membrane surface. Publication Abstract from PubMedNonalcoholic steatohepatitis (NASH) is a progressive form of nonalcoholic fatty liver disease that can lead to irreversible liver cirrhosis and cancer. Early diagnosis of NASH is vital to detect disease before it becomes life-threatening, yet noninvasively differentiating NASH from simple steatosis is challenging. Herein, bifunctional probes have been developed that target the hepatocyte-specific asialoglycoprotein receptor (ASGPR), the expression of which decreases during NASH progression. The results show that the probes allow longitudinal, noninvasive monitoring of ASGPR levels by positron emission tomography in the newly developed rat model of NASH. The probes open new possibilities for research into early diagnosis of NASH and development of drugs to slow or reverse its progression. Triantennary GalNAc Molecular Imaging Probes for Monitoring Hepatocyte Function in a Rat Model of Nonalcoholic Steatohepatitis.,Mishra A, Castaneda TR, Bader E, Elshorst B, Cummings S, Scherer P, Bangari DS, Loewe C, Schreuder H, Poverlein C, Helms M, Jones S, Zech G, Licher T, Wagner M, Schudok M, de Hoop M, Plowright AT, Atzrodt J, Kannt A, Laitinen I, Derdau V Adv Sci (Weinh). 2020 Nov 9;7(24):2002997. doi: 10.1002/advs.202002997., eCollection 2020 Dec. PMID:33344141[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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