This paper is particularly interesting to me. I worked on telomerase earlier in my career, and had actually discovered a novel series of inhibitors using pharmacophore modeling. They eventually proved to have PK issues, but hey, this was before all the physical property/PK-PD relations was well understood. Knowing structural information would have been very useful. I used nucleotide binding site HIV molecules to construct a pharmacophore and searched the ACD (for you youngsters, that was a product MDL sold with ISIS that contained available chemicals) and ordered a few dozen molecules. And by gum! we got about a 30% hit rate from that. As I mentioned, the telomerase project went no where, but such is life on the mean streets of drug discovery.
One other fact is the Julie Feigon, the principle author was a young new faculty member at UCLA when I was getting my Ph.D. She was pioneering protein NMR and I thought she was quite exceptional. I am quite impressed with this feather in her cap, and I can say I knew her back when...
One other fact is the Julie Feigon, the principle author was a young new faculty member at UCLA when I was getting my Ph.D. She was pioneering protein NMR and I thought she was quite exceptional. I am quite impressed with this feather in her cap, and I can say I knew her back when...
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