[Drug conjugation in the brain]

Several drugs and environmental pollutants can cross the blood-brain barrier and reach the brain. This organ possesses an enzymatic equipment able to metabolize xenobiotics, therefore facilitating their elimination and maintaining brain homeostasis. This metabolism may result in the formation of toxic metabolites, which endanger neuronal integrity and may result in neurological disturbances. The main function of the conjugation enzymes present in the brain parenchyma and blood-brain or blood-cerebrospinal fluid interfaces is the detoxification of these reactive molecules, thus protecting the central nervous system. This review presents the main cerebral conjugating enzymes, and shows the interest for the design of new drugs of the knowledge of their activities.