Crystal Structure of PfA-M1 and the Pfa-mi Co4 Complex

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.

Attached files:


Patents:
EP 2,250,261   [MORE INFO]

Inventor(s): WHISSTOCK JAMES CHARLES [AU]; BUCKLE ASHLEY MAURICE [AU]; MCGOWAN SHEENA [AU]; PORTER CORRINE JOY [AU]; DALTON JOHN P [AU]; LOWT

Type of Offer: Sale



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