MCT1 transporters expressed in blood brain barrier cells

A method of screening an agent, conjugate or conjugate moiety for capacity to be transported through the blood brain barrier, comprising:

• (a) providing a cell expressing the MCT1 transporter, wherein:
• a nucleic acid molecule encoding the MCT1 transporter has been transfected or injected into the cell;
• and
• the MCT1 transporter is the protein encoded by SEQ ID NO:
• 1 or has at least 90% sequence identity to the protein encoded by SEQ ID NO:1, and the MCT1 transporter can transport lactic acid, the MCT1 transporter being situated in the plasma membrane of the cell;
• (b) contacting the cell with an agent, conjugate or conjugate moiety in vitro;
• and
• (c) determining whether the agent, conjugate or conjugate moiety passes through the plasma membrane via the MCT1 transporter, passage through the plasma membrane via the MCT1 transporter indicating the agent, conjugate or conjugate moiety has capacity to be transported through the blood brain barrier;
• wherein:
• if step (b) comprises contacting the cell with the agent, the agent is a neuropharmaceutical agent or an imaging component;
• if step (b) comprises contacting the cell with the conjugate, the conjugate comprises an agent that is a neuropharmaceutical agent or an imaging component;
• or
• if step (b) comprises contacting the cell with the conjugate moiety, the method further comprises linking the conjugate moiety to an agent that is a neuropharmaceutical agent or an imaging component, and
• provided if the agent is a cytotoxic agent or an imaging component, the method further comprises:
• (i) administering the agent, conjugate, or conjugate moiety to a peripheral tissue of an animal and measuring the amount of agent, conjugate, or conjugate moiety that passes through the blood brain barrier into the brain of the animal;
• or
• (ii) contacting the agent to one side of a polarized monolayer of brain microvessel endothelial cells;
• and determining whether the agent is transported across the polarized monolayer, wherein if the agent is transported across the polarized monolayer it has the capacity to be transported through the blood brain barrier.