CRYSTAL STRUCTURE OF PfA-M1 AND THE PfA-M1 Co4 COMPLEX
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United States of America Patent
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Issued Date -
Dec 22, 2011
app pub date -
Feb 12, 2009
filing date -
Feb 14, 2008
priority date (Note) -
Abandoned
status (Latency Note)
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Abstract
The invention relates to the X-ray crystal structure of PfA-M1 aminopeptidase alone, and in complex with the phosphinate dipeptide analogue hPheP[CH.sub.2]Phe. More specifically the present invention provides the structure coordinates of PfA-M1 and PfA-M1 in complex with Co4. The invention also includes the use of the X-ray crystal structures as drug target models for anti-malarial drug design and a method for identifying or designing novel anti-malarial drugs, for example using high-throughput chemical screening and medicinal chemistry methods. The invention further provides anti-malarial drugs identified or designed according to the aforementioned method and their use for obstructing protein metabolism and synthesis in a parasite by blocking the entrance of Hb-derived peptides and/or blocking the exit of released amino acids at the active site of PfA-M1 protease.
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International Classification(s)
- A61K:PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOS....
- C12Q:MEASURING OR TESTING PROCESSES INVOLVING ENZYMES O....
- C12N:MICRO-ORGANISMS OR ENZYMES; COMPOSITIONS THEREOF
- G06F:ELECTRIC DIGITAL DATA PROCESSING
- A61P:THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDI....
- G06G:ANALOGUE COMPUTERS
- C40B:COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL ....
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