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Home >>Protein Engineering, Immunotoxins and Drug Designing - Engineering of Macromolecules >> Drug Designing Through Blocking Hormone Receptors
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Drug Designing Through Blocking Hormone Receptors - Drugs have also been produced through a study of receptor molecules that are responsible for the disease, followed by identification of chemicals that will block such receptors.

Utilizing this strategy, atleast two drugs were developed by Dr. James Black (of UK), who shared with Drs. G. Elion and G. Hitchings (of USA), the 1988 Nobel Prize for Physiology and Medicine.These two medicines are briefly described in the following text.

Propranolol. This drug is widely used for treating heart disease and high blood pressure. Heart diseases result due to the presence (in excess) of hormones 'norepinephrine' and 'epinephrine', due to their role in contraction and relaxation of cardiac muscles. These hormones act through two receptors a and p.

 

The drug 'propranolol' is a 'blocker' and relaxes the heart muscles. It has been shown that the drug not only cures the heart diseases but reduces the death rate of heart disease survivors by 25%. The drug is also used for treatments of 'angina pectoris' and 'high blood pressure. Obviously by blocking the receptor 'P', the drug inhibits the activity of hormones which act through a receptor molecule.

Cimetidine. This drug is antiulcer and is used for treatment of ulcers. Ulcers result from acid production due to histamine release in the stomach and therefore attempts were made to treat these ulcers through antihis tamines that were earlier used to combat respiratory allergies.

These antihistamines proved ineffective for ulcer treatment and James Black attributed this to use of receptors that were different in stomach lining and respiratory tract.

He was able to characterize histamine receptor of stomach lining and called it H2 acceptor, which is blocked by the drug 'cimetidine', thus leading to healing of ulcers by preventing acid production due to nonavailability of histamine. Therefore 'cimetidine' marked the beginning of a new era in ulcer treatment, since earlier ulcers, that did not heal, had to be removed surgically.

 
 

 
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