Transporter proteins comprise 5% of all human drug targets. This category encompasses the ATP-binding cassette (ABC) transporter family, ATPases, and the solute carrier (SLC) family. SLC6 is the most exploited family among all transporters (55%), with approximately 42 drugs currently approved by the US Food and Drug Administration (FDA) (Figure 4.9a)76. Currently, around 60 clinical trials are in progress for drugs that specifically target SLC6 family members, mainly for analgesia, psychiatric disorders and Attention deficit hyperactivity disorder (ADHD) (Figure 4.9 b). New indications are also undergoing development e.g. for migraines and cognitive dysfunction in multiple sclerosis patients. The specific targeting of SLC6 family transporters has led to vast improvements in the treatment of psychiatric disorders such as depression, anxiety and obsessive-compulsive disorder77. Tricyclic antidepressants are less selective and thus patients suffered more side effects. The improved therapeutic effect of
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They are widely exploited by loop and thiazide diuretics to treat hypertension78. SLC12A3 is currently a target for eight approved and marketed molecular agents, while SLC12A1 is targeted by ten76. SLC12 have also been discussed as possible targets for the treatment of neurological disorders such as seizures and neuropathic pain79.
The gastric H+/K+-ATPase, which makes up 12% of all transporter targets, is the molecular target for the class of antisecretory drugs knows as proton-pump inhibitors (PPIs). Examples of PPIs include esomeprazole, lansoprazole, omeprazole, and pantoprazole. The effectiveness of these drugs is due to the fact that H+/K+-ATPase is the enzyme responsible for gastric acid secretion and their mechanism of action involves covalent binding of the activated drug to the enzyme80. Na+/K+-ATPase is the target for the cardiac glycoside
They are widely exploited by loop and thiazide diuretics to treat hypertension78. SLC12A3 is currently a target for eight approved and marketed molecular agents, while SLC12A1 is targeted by ten76. SLC12 have also been discussed as possible targets for the treatment of neurological disorders such as seizures and neuropathic pain79.
The gastric H+/K+-ATPase, which makes up 12% of all transporter targets, is the molecular target for the class of antisecretory drugs knows as proton-pump inhibitors (PPIs). Examples of PPIs include esomeprazole, lansoprazole, omeprazole, and pantoprazole. The effectiveness of these drugs is due to the fact that H+/K+-ATPase is the enzyme responsible for gastric acid secretion and their mechanism of action involves covalent binding of the activated drug to the enzyme80. Na+/K+-ATPase is the target for the cardiac glycoside