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Deriving new drugs from thalidomide.


Thalidomide thalidomide (thəlĭd`əmĭd'), sleep-inducing drug found to produce skeletal defects in developing fetuses. The drug was marketed in Europe, especially in West Germany and Britain, from 1957 to 1961, and was thought to be so safe that , a nausea-fighting sedative synthesized during the 1950s but never approved for use in the United States because of its fetus-harming effects, is spawning a new generation of drugs that can treat inflammation and immune system disorders (SN: 12/24&31/94, p.424).

George W. Muller and David I. Stirling, chemists at Celgene Corp. in Warren, N.J., reengineered thalidomide to create a new series of therapeutic agents.

The researchers have designed the drugs, they say, to regulate the body's production of tumor necrosis factor tumor necrosis factor
n. Abbr. TNF
A protein that is produced in the presence of an endotoxin, especially by monocytes and macrophages, is able to attack and destroy tumor cells, and exacerbates chronic inflammatory diseases.
 alpha. This protein plays a key role in inflammatory and immunological disorders such as rheumatoid arthritis, lupus, inflammatory bowel disease inflammatory bowel disease
n. Abbr. IBD
Any of several incurable and debilitating diseases of the gastrointestinal tract characterized by inflammation and obstruction of parts of the intestine.
, and leprosy leprosy or Hansen's disease (hăn`sənz), chronic, mildly infectious malady capable of producing, when untreated, various deformities and disfigurements. .

Scientists at Johns Hopkins University Johns Hopkins University, mainly at Baltimore, Md. Johns Hopkins in 1867 had a group of his associates incorporated as the trustees of a university and a hospital, endowing each with $3.5 million. Daniel C.  in Baltimore are currently studying several of these new Celgene agents for treatment of graft-versus-host disease, which often follows bone marrow transplants, Muller adds.

In designing these new molecules, Muller and Stirling said, they improved the potency of the portion of thalidomide exhibiting medicinal properties and removed the segment causing birth defects.
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Copyright 1995, Gale Group. All rights reserved. Gale Group is a Thomson Corporation Company.

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Title Annotation:Chemistry; new thalidomide agents regulate body's ability to produce tumor necrosis factor alpha, a major contributor to inflammatory and immunological disorders
Author:Lipkin, Richard
Publication:Science News
Article Type:Brief Article
Date:Sep 9, 1995
Words:165
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