Page 77 - 81_02

A brief updated report on the battle against malaria
based on the mechanism of action of artemisinin. Pure
Appl Chem 2001; 73: 1173-88.
35. O'Neill PM, Barton VE, Ward, SA. The molecular
mechanism of action of artemisinin. The debate
continues. Molecules 2010; 15: 1705-21.
36. Takala-Harrison S, Jacob CG, Arze C, et al.
Independent emergence of Plasmodium falciparum
artemisinin resistance mutations in Southeast Asia. J
Infect Dis 2015; 211: 670-79.
37. Arley F, Witkowski B, Amaratunga Ch, et al. A
molecular marker of artemisinin- resistant
Plasmodium falciparum malaria. Nature 2014; 505:
50-5.
38. Bhattacharjee S, Stahelin RV, Speicher KD, Speicher
DW, Haldar K. Endoplasmic reticulum PI3P lipid
binding targets malaria proteins to the host cell. Cell
2012; 148: 201-12.
39. Mbengue A, Bhattacharjee S, Pandharkar T, et al. A
molecular mechanism of artemisinin resistance in
Plasmodium falciparum malaria. Nature 2015; 520:
683-7.
40. Wells TNC, Alonso PL, Gutteridge WE. New
medicines to improve control and contribute to the
eradication of malaria. Nature Reviews Drug
Discovery 2009, 8: 879-91.
41. Para una revisión de los progresos más relevantes
realizados entre 2010 y 2012 ver: Biamonte MA,
Wanner J, Le Roch KG. Recent advances in malaria
drug discovery. Bioorg Med Chem Letters 2013; 23:
2829-43.
42. Heidebrecht R, Mulrooney C, Austin ChP, et al.
Diversity-Oriented Synthesis Yields a Novel Lead for
Treatment of Malaria, ACS Med Chem Lett 2012; 3:
112-7. Ver el comentario de esta noticia en: Avendaño
C. Anal Real Acad Nac Farm 2012; 78: 418-24.
43. Lukens AK, Heidebrecht RW, Mulrooney C, et al.
Diversity-Oriented Synthesis Probe Targets
Plasmodium falciparum Cytochrome b Ubiquinone
Reduction Site and Synergizes With Oxidation Site
Inhibitors. J Infect Dis 2015; 211: 1097-103.
44. Painter HJ, Morrisey JM, Mather MW, Vaidya AB.
Specific role of mitochondrial electron transport in
blood-stage Plasmodium falciparum. Nature 2007;
446: 88-91.
45. a) Fisher N, Meunier B. Molecular basis of resistance
to cytochrome bc1 inhibitors. FEMS Yeast Res 2008;
8: 183-92. b) Dong CK, Urgaonkar S, Cortese JF, et
al. Identification and validation of tetracyclic
benzothiazepines as Plasmodium falciparum
Cytochrome bc1 Inhibitors. Chem Biol 2011; 18:
1602-10. c) Nam T-G, McNamara CW, Bopp S, et al.
A chemical genomic analysis of decoquinate, a
Plasmodium falciparum cytochrome b inhibitor. ACS
Chem Biol 2011; 6: 1214-22.
46. Jiménez-Díaz MB, Ebert D, Salinas Y, et al. (+)-
SJ733, a clinical candidate for malaria that acts
through ATP4 to induce rapid host-mediated clearance
@Real Academia Nacional de Farmacia. Spain
of Plasmodium. Proc Natl Acad Sci U S A 2014; 111:
E5455-62.
47. Ralph SA, D’Ombrain MC, McFadden GI. The
apicoplast as an antimalarial drug target. Drug Resist
Updat 2001; 4: 145-51.
48. a) Kim S, Lee SW, Choi EC, Choi SY. Aminoacyl-
tRNA synthetases and their inhibitors as a novel
family of antibiotics. Appl Microbiol Biotechnol
2003; 61:278-88. b) Pohlmann J, Brotz-Oesterhelt H.
New aminoacyl-tRNA synthetase inhibitors as
antibacterial agents. Curr Drug Targets Infect Disord
2004; 4: 261-72. c) Hurdle JC, O'Neill AJ, Chopra I.
Prospects for Aminoacyl-tRNA Synthetase Inhibitors
as New Antimicrobial Agents. Antimicrob Agents
Chemother 2005; 49: 4821-33.
49. Connell SR, Tracz DM, Nierhaus KH, Taylor DE.
Ribosomal Protection Proteins and Their Mechanism
of Tetracycline Resistance. Antimicrob Agents
Chemother 2003; 47: 3675-81.
50. Nakama T, Nureki O, Yokohama S. Structural basis
for the recognition of isoleucyl-adenylate and an
antibiotic, mupirocin, by isoleucyl-tRNA synthetase. J
Biol Chem 2001; 276: 47387-93.
51. Hoen R, Novoa EM, López A, et al. Selective
inhibition of an apicoplastic aminoacyl-tRNA
synthetase from Plasmodium falciparum.
ChemBioChem 2013; 14: 499-509.
52. Bhatt TK, Khan S, Dwivedi VP, et al. Malaria parasite
tyrosyl-tRNA synthetase secretion triggers pro-
inflammatory responses. Nat Commun 2011; 2: 530.
doi: 10.1038/ ncomms1522.
53. Hoepfner D, McNamara C, Lim CS, et al. Selective
and specific inhibition of the Plasmodium falciparum
lysyl-tRNA synthetase by the fungal secondary
metabolite cladosporin. Cell Host Microbe 2012; 11:
654-63.
54. Istvan ES, Dharia NV, Bopp SE, et al. Validation of
isoleucine utilization targets in Plasmodium
falciparum. Proc Natl Acad Sci USA 2011; 108: 1627-
32.
55. Azcárate IG, Marín-García P, Camacho N, et al.
Insights into the preclinical treatment of blood-stage
malaria by the antibiotic borrelidin. Br J Pharmacol
2013, 169: 645-58.
56. Ruan B, Bovee ML, Sacher M, et al. A unique
hydrophobic cluster near the active site contributes to
differences in borrelidin inhibition among threonyl-
tRNA synthetases. J Biol Chem 2005; 280:571-77.
57. Novoa EA, Camacho N, Tor A, et al. Analogs of
natural aminoacyl-tRNA synthetase inhibitors clear
malaria in vivo. Proc Natl Acad Sci USA 2014; 111:
E5508-17.
157