TY - JOUR
T1 - Plasmodium falciparum neutral aminopeptidases
T2 - new targets for anti-malarials
AU - Skinner-Adams, Tina S.
AU - Stack, Colin M.
AU - Trenholme, Katharine R.
AU - Brown, Chris L.
AU - Grembecka, Jolanta
AU - Lowther, Jonathan
AU - Mucha, Artur
AU - Drag, Marcin
AU - Kafarski, Pawel
AU - McGowan, Sheena
AU - Whisstock, James C.
AU - Gardiner, Donald L.
AU - Dalton, John P.
PY - 2010/1
Y1 - 2010/1
N2 - The neutral aminopeptidases M1 alanyl aminopeptidase (PfM1AAP) and M17 leucine aminopeptidase (PfM17LAP) of the human malaria parasite Plasmodium falciparum are targets for the development of novel anti-malarial drugs. Although the functions of these enzymes remain unknown, they are believed to act in the terminal stages of haemoglobin degradation, generating amino acids essential for parasite growth and development. Inhibitors of both enzymes are lethal to P. falciparum in culture and kill the murine malaria P. chabaudi in vivo. Recent biochemical, structural and functional studies provide the substrate specificity and mechanistic binding data needed to guide the development of more potent anti-malarial drugs. Together with biological studies, these data form the rationale for choosing PfM1AAP and PfM17LAP as targets for anti-malarial development.
AB - The neutral aminopeptidases M1 alanyl aminopeptidase (PfM1AAP) and M17 leucine aminopeptidase (PfM17LAP) of the human malaria parasite Plasmodium falciparum are targets for the development of novel anti-malarial drugs. Although the functions of these enzymes remain unknown, they are believed to act in the terminal stages of haemoglobin degradation, generating amino acids essential for parasite growth and development. Inhibitors of both enzymes are lethal to P. falciparum in culture and kill the murine malaria P. chabaudi in vivo. Recent biochemical, structural and functional studies provide the substrate specificity and mechanistic binding data needed to guide the development of more potent anti-malarial drugs. Together with biological studies, these data form the rationale for choosing PfM1AAP and PfM17LAP as targets for anti-malarial development.
UR - https://www.scopus.com/pages/publications/74049107406
U2 - 10.1016/j.tibs.2009.08.004
DO - 10.1016/j.tibs.2009.08.004
M3 - Review article
C2 - 19796954
AN - SCOPUS:74049107406
SN - 0968-0004
VL - 35
SP - 53
EP - 61
JO - Trends in Biochemical Sciences
JF - Trends in Biochemical Sciences
IS - 1
ER -