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Biotech / Medical : AMLN (DIABETES DRUGS)
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To: D.Right who wrote (932)11/9/1997 12:29:00 PM
From: Henry Niman  Read Replies (2) of 2173
 
I think there is a fundamental misunderstanding of non-polypetide hormones in general and Rezulin in particular, so it might be useful to review a few basic concepts on hormones and analogs.

Polypeptide hormones are the target of Biotechs. These gene products are injected, find an appropiate receptor on the surface of the cell and cause the receptor to change shape which then transmits the signal inside the cell and eventually affects which genes are expressed in the cell. Non-polypeptide hormones are much smaller, so the can be cheaply synthesized in the lab, they are taken orally, and they diffuse into cells and find appropriate receptors which then change shape and eventually affect which genes are expressed in the cell.

Analogs of these hormones can have two general effects. If the analog mimics the hormone, then it is an agonist. If it blocks the hormone, then it is an antagonist. The classification is somewhat of an oversimplification, because the same drug can act as an agonist in one cell type, but an antagonist in another (because the ultimate controllers of gene expression are complexes made of different combinations in different cell types).

Drugs that are agonists can be referrred to as "hormone replacements" because they mimic the hormone. Many, if not most hormone analogs, are agonists. Pramlintide is an agonist of the polypeptide hormone amylin. Rezulin is an agonist of non-polypeptide hormone prostaglandin J12?. Targretin is an agonist of the non-polypeptide hormone 9-cis-retinoic acid. Each analog mimics a natural hormone. An "add on" drug is a term that is an agonist for a misconception.
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