title: Plasmodium falciparum M1-aminopeptidase: a promising target for the development of antimalarials.
abstract: Malaria is a devastating human parasitic disease that receives enhanced attention due to the emergence of resistance to traditional drugs. Thus, the search for new molecular targets is a major goal. PfAM1 is an aminopeptidase from Plasmodium falciparum, William H. Welch 1897, belonging to the M1 family of metalloproteases, which is a promising target of inhibitors to block the intra-erythrocytic stages of the parasite. Since its identification in 1998, many efforts have been done to validate PfAM1 as an appropriate target of antimalarials. The present work is a critical review of the main structural, functional and kinetic characteristics of PfAM1, as well as a summary of the effects of key inhibitors at molecular and cellular levels. The systematization of experimental results should contribute to a better understanding of the properties of PfAM1 as a target of antimalarials and promote research projects focused on the development of PfAM1 inhibitors.
authors.forename: Jorge
authors.initials: J
authors.lastname: González-Bacerio
authors.forename: Rafael
authors.initials: R
authors.lastname: Fando
authors.forename: Alberto
authors.initials: A
authors.lastname: del Monte-Martínez
authors.forename: Jean-Louis
authors.initials: JL
authors.lastname: Charli
authors.affiliation: Centro de Estudio de Proteínas, Facultad de Biología, Universidad de La Habana, 25 y J, 10400, La Habana, Cuba. jogoba@fbio.uh.cu.
authors.forename: María de los Á
authors.initials: Mde L
authors.lastname: Chávez
mesh_terms: D000626:Aminopeptidases / Q000037:antagonists & inhibitors / Q000737:chemistry; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008288:Malaria / Q000188:drug therapy / Q000469:parasitology; D058990:Molecular Targeted Therapy; D010963:Plasmodium falciparum / Q000187:drug effects / Q000201:enzymology*; D015800:Protozoan Proteins / Q000037:antagonists & inhibitors / Q000737:chemistry
chemical_list: D000962:Antimalarials; D004791:Enzyme Inhibitors; D015800:Protozoan Proteins; D000626:Aminopeptidases