If antisense compounds can be designed to block the synthesisof testosterone receptors, they may become the new drugs forpreventing or treating hair loss in men.

This could be the ultimate outcome of a collaborative researchagreement announced Monday between Genta Inc.(NASDAQ:GNTA) and researcher Michael McPhaul of theUniversity of Texas Southwestern Medical Center at Dallas (UTSouthwestern).

The research will focus on testing the ability of Genta'sAnticode oligonucleotide constructs (which include bothantisense and triplex configurations) to modulate androgenreceptor levels in human cell lines.

Androgen receptors bind specific types of the hormonetestosterone, explained McPhaul, and they are X-chromosome-linked. Thus androgen receptors not only figure in male-pattern baldness, but they play a role in a "huge number ofbiological processes required for maleness," McPhaul explained.

In fact, if there's a mutation in a genotypic male thatinactivates the receptor, the male is phenotypically female,McPhaul explained. And in laboratory experiments on selectedbiopsied tissues from such individuals, "it's quite clear inpatients with androgen resistance that when the receptor isn'tthere, the ability of the cells to respond to the hormone is notpossible."

Previous experiments aimed at understanding androgen-receptor interactions have attempted to antagonize theinteraction by occupying the receptor sites with some othercompound. In the antisense approach envisioned by McPhauland his corporate collaborators, however, "instead ofinterfering with the action of the receptor, we'll be interferingwith its presence."

The initial agreement between San Diego-based Genta and UTSouthwestern is for one year, by which time "there should bean indication as to whether Anticode technology will bebeneficial," said Kenneth Brown, Genta's director of businessdevelopment. "Hopefully this collaboration will lead to productcandidates that will go into the clinic," Brown added.

-- Jennifer Van Brunt Senior Editor

(c) 1997 American Health Consultants. All rights reserved.

No Comments