Patent ID: 7919454
Filing Date: 2011-04-05
Classification: A61K,C07C,C07D,C07K,G01N

Abstract:
1. A method of treatment comprising: providing a conjugate comprising an agent linked to a conjugate moiety, which conjugate has a Vmax for the PEPT2 transporter of at least 1% of the Vmax of substrate Gly-Sar for PEPT2; wherein the agent has a pharmacological activity without the conjugate moiety, and the conjugate has a greater Vmax for PEPT2 than the agent without the conjugate moiety, wherein the PEPT2 transporter has the amino acid sequence of SEQ ID NO:2 or has at least 90% sequence identity to the amino acid sequence of SEQ ID NO:2, and the PEPT2 transporter can transport Gly-Sar; orally administering a pharmacologically effective amount of the conjugate to a patient, wherein the conjugate has a Vmax for the PEPT1 transporter of less than 1% of the Vmax of substrate Gly-Sar for PEPT1, wherein the PEPT1 transporter has the amino acid sequence of SEQ ID NO:1 or has at least 90% sequence identity to the amino acid sequence of SEQ ID NO:1, and the PEPT1 transporter can transport Gly-Sar.