Ontology highlight
ABSTRACT:
SUBMITTER: Sanhueza CA
PROVIDER: S-EPMC6991140 | biostudies-literature | 2017 Mar
REPOSITORIES: biostudies-literature
Sanhueza Carlos A CA Baksh Michael M MM Thuma Benjamin B Roy Marc D MD Dutta Sanjay S Préville Cathy C Chrunyk Boris A BA Beaumont Kevin K Dullea Robert R Ammirati Mark M Liu Shenping S Gebhard David D Finley James E JE Salatto Christopher T CT King-Ahmad Amanda A Stock Ingrid I Atkinson Karen K Reidich Benjamin B Lin Wen W Kumar Rajesh R Tu Meihua M Menhaji-Klotz Elnaz E Price David A DA Liras Spiros S Finn M G MG Mascitti Vincent V
Journal of the American Chemical Society 20170223 9
A compact and stable bicyclic bridged ketal was developed as a ligand for the asialoglycoprotein receptor (ASGPR). This compound showed excellent ligand efficiency, and the molecular details of binding were revealed by the first X-ray crystal structures of ligand-bound ASGPR. This analogue was used to make potent di- and trivalent binders of ASGPR. Extensive characterization of the function of these compounds showed rapid ASGPR-dependent cellular uptake in vitro and high levels of liver/plasma s ...[more]