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US 7,610,156 B2Granted
Methods for rational pegylation of proteins
AssigneeXencor, Inc.
InventorsJohn R. Desjarlais, Jonathan Zalevsky, Gregory L. Moore
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Abstract
The present invention relates to the use of simulation technology to rationally optimize the locations and sizes of attached polymeric moieties for modification of therapeutic proteins and the proteins generated from this method.
Claims16
A method of identifying at least one favorable attachment site for a polymeric moiety on a target protein comprising:
- a) inputting a set of coordinates into a computer for said target protein;
- b) inputting a set of coordinates for said polymeric moiety;
- c) selecting a criteria for said favorable attachment site based upon at least one desired characteristic,
- d) using a simulation module comprising the steps of:
- i) computationally attaching conformers of said polymeric moiety to a plurality of amino acids in said target protein;
- and
- ii) disallowing conformers at each of said amino acids on the basis of a distance cutoff;
- e) selecting based upon said criteria one of said amino acids for attachment of said polymeric moiety;
- and
- f) physically making and screening for said at least one desired characteristic at least one target protein with a polymeric moiety attached at said favorable attachment site amino acid position.
7 more elements
Dependencies are inferred from the claim text.