NEW TECHNOLOGY FOR DRUG DISCOVERY BASED UPON INSERTION OF LIGANDS INTO GENE SEQUENCES BY NUCLEAR RECEPTOR PROTEINS.

Autor: Mahesh, Virendra B., Ewing, Douglas E., Sidell, Neil, Bransome, Edwin D., Hendry, Lawrence B.
Zdroj: Medicinal Chemistry Research; Jul2004, Vol. 13 Issue 6/7, p497-508, 12p
Abstrakt: A gene regulatory mechanism has been proposed in which steroid hormones and certain other drugs bind to nuclear receptor proteins followed by transfer to DNA where they are inserted between base pairs. Here, we report using the estrogen receptor that the location of drugs in x-ray crystal structures of the receptors matches closely their predicted spatial locations in the DNA. These findings provide compelling evidence that DNA is the ultimate target of these drugs that act on the human genome. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index