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Biotech / Medical : Ligand (LGND) Breakout! -- Ignore unavailable to you. Want to Upgrade?

To: squetch who wrote (19428)	4/22/1998 10:15:00 PM
From: Henry Niman	Read Replies (1) \| Respond to of 32384

Stan, As noted in one of the references (#31), LG268 is LGD268 which is LG1268. It activates the RXR part of the heterodimer (PPAR/RXR). The papers that I saw on LG100153 indicated that it was specific for RXR. I'm a bit surprised that it would also react so strongly with RAR-a. I would expect that type of binding with RXR-a.

To: squetch who wrote (19428)	4/23/1998 11:10:00 AM
From: Peter Singleton	Respond to of 32384

Henry, I'm out of my league on the science here, but the JCI article Stan posted raised an interesting issue. How LGND's products (RXR-based) compare in potency with TZD's. If I remember, the pre-clinical data showed they were equivalent, and synergistic. Take a look at the charts in the article. These would indicate a substantial, though weaker effect for LGD268, compared with WLA's troglitazone and Upjohn's pioglitazone charts showing %phosphorylation of Insulin receptor, IRS-1 (effect of drug countering TNF-a activity): LGD268 jci.org pioglitazone, troglitazone jci.org