Method for screening drug-saccharide conjugates

A method for selecting a drug-saccharide conjugate that exhibits decreased uptake by target cells that express a human mannose receptor, C type 1 (MRC1) in the presence of an inhibitor from a plurality of candidate drug-saccharide congugates, comprising:

• (a) providing the target cells that express the human MRC1;
• (b) exposing the target cells to the plurality of candidate drug-saccharide conjugates and selecting candidate drug-saccharide conjugates that are taken up into the target cells;
• (d) determining whether the uptake of the selected candidate drug-saccharide conjugate is decreased when the target cells are exposed to the selected candidate drug-saccharide conjugate and an inhibitor that binds the human MRC1;
• and
• (e) selecting at least one candidate drug-saccharide conjugate which exhibits uptake by the target cells in the absence of the inhibitor and decreased uptake in the presence of the inhibitor to select the drug-saccharide conjugate.

A method for selecting a drug-saccharide conjugate which decreases uptake of a control compound by target cells that express the human mannose receptor, C type 1 (MRC1), comprising:

• (a) providing the target cells that express the human MRC1;
• (b) exposing the target cells to a control compound that binds the human MRC1 and is internalized into the target cells and a plurality of candidate drug-saccharide conjugates;
• (c) determining whether the uptake of the control compound is decreased when the target cells are exposed to a candidate drug-saccharide conjugate;
• and
• (e) selecting the candidate drug-saccharide conjugate which inhibits uptake of the control compound by the target cells in the to provide the drug-saccharide conjugate.