CRYSTAL STRUCTURE OF PFA-MI AND THE PFA-MI CO4 COMPLEX

WIPO Patent Application WO/2009/100489

A8

The invention relates to the X-ray crystal structure of PfA-M1 aminopeptidase alone, and in complex with the phosphinate dipeptide analogue hPheP[CH2]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.

WO/2007/089851	COMPOSITIONS AND METHODS FOR TREATING COLLAGEN-MEDIATED DISEASES
WO/1997/015588	PROTECTIVE PROTEIN/CATHEPSIN A AND PRECURSOR: CRYSTALLIZATION, X-RAY DIFFRACTION, THREE-DIMENSIONAL STRUCTURE DETERMINATION AND RATIONAL DRUG DESIGN
WO/2009/132575	NATTOKINASE POWDERS WITH SUPER HIGH ACTIVITY AND PRODUCING METHOD THEREOF

WHISSTOCK JAMES CHARLES (AU)
BUCKLE ASHLEY MAURICE (AU)
MCGOWAN SHEENA (AU)
PORTER CORRINE JOY (AU)
DALTON JOHN P (AU)
LOWTHER JONATHON (GB)
STACK COLIN MARTIN (AU)
DONNELLY SHEILA MARY (AU)

PCT/AU2009/000161

October 06, 2011

February 12, 2009

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UNIV MONASH (US)
UNIV SYDNEY TECH (AU)
WHISSTOCK JAMES CHARLES (AU)
BUCKLE ASHLEY MAURICE (AU)
MCGOWAN SHEENA (AU)
PORTER CORRINE JOY (AU)
DALTON JOHN P (AU)
LOWTHER JONATHON (GB)
STACK COLIN MARTIN (AU)
DONNELLY SHEILA MARY (AU)

C12N9/48; A61P33/06; C07K14/445; C12Q1/37

SMOORENBURG PINI PATENT & TRADE MARK ATTORNEYS (Ringwood, VIC 3134, AU)

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