Pharmacopeia, Inc. (ACCL) (Prev: PCOP) Message Board

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Biotech / Medical : Pharmacopeia, Inc. (ACCL) (Prev: PCOP)

ACCL 4.028

+0.7%

3:59 PM EST

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To: tommysdad who wrote (15)	8/7/1997 2:27:00 PM
From: kinkblot	of 179

Pharmacopeia recently received an SBIR grant from NIH for their internal drug discovery program targeting the protease plasmepsin. They describe their results in the press release: Plasmepsin is a protease (enzyme) produced in the parasite that causes malaria. This protease is believed to play a key role in the pathogenesis of malaria as it digests the human host's hemoglobin. Using structure-guided drug design and its patented ECLiPS(TM) tagging technology, Pharmacopeia identified several compounds that are highly potent and selective for plasmepsin and not for closely related members of the aspartyl protease family. . . The cover story of the August 1997 Atlantic Monthly is a lengthy article about past and present efforts to fight malaria: theatlantic.com Worldwide incidence of malaria has quadrupled in the past five years as the parasite responsible for the disease has developed resistance to quinine analogues used to treat it. The article discusses attempts to develop a vaccine; success to date has been limited, possibly because the parasite does not elicit a complete immune response. Harold Varmus at NIH is quoted saying "HIV, TB, and malaria are among the most important infectious agents in the world. There are no effective vaccines against them, and all have the same property of establishing chronic infection without an effective immune response." He seems doubtful that a vaccine will be developed anytime soon, so maybe that's why PCOP is being funded. Pharmacopeia's approach is apparently based on starving the parasite. Does anyone know whether the company has any drug discovery program related to HIV-1 virus? The protease retropepsin targeted by protease inhibitors is an aspartyl protease. Human proteases pepsin, gastricsin, renin are also from the same family. Maybe these are the closely related members they refer to when discussing the high degree of selectivity achieved. Could they use what they learn on plasmepsin to reduce discovery time on similar targets, or do they start from scratch on each one? Will

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