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Biotech / Medical : ARRIS - Another partner -- Ignore unavailable to you. Want to Upgrade?

To: John Dwyer who wrote (285)	12/5/1997 1:27:00 AM
From: Miljenko Zuanic	Read Replies (1) \| Respond to of 353

John: Can you clarify this two point: >> There are two points where I think Delta offers a great advantage over traditional drug design. First, it allows a means by which to target something away from the active site. << The active site for serine type proteases are composed of the catalytic site (Ser-OH...N=His), oxyonium hole (stabilizing the tetrahedral intermediate), substrate site and specificity pocket(which is very close to oxyanion hole). I agree that catalytic site and oxyanion hole are standard and this is probably site for primary metal complex (assume that it is octahedral). Because the ARRS PI inhibitors are small molecules, they will have to recognize environment around substrate site and specificity pocket in compact 3D structure. My understanding is that they use small peptide fragment to mask part of the substrate site in rational drug designee process. By this I will not agree that they target something away from active site. Actually, they make, by introducing metal ion in complex, active site more visible to specific inhibitor by eliminating part of the molecule (inhibitor) which will have to bind to catalytic site and oxyanion hole. Any idea, from your training and experience, which metal ion will be appropriate for this complex type? Thanks. mz