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2013 3
2014 8
2017 1
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Page 1
A Cryptosporidium PI(4)K inhibitor is a drug candidate for cryptosporidiosis.
Manjunatha UH, Vinayak S, Zambriski JA, Chao AT, Sy T, Noble CG, Bonamy GMC, Kondreddi RR, Zou B, Gedeck P, Brooks CF, Herbert GT, Sateriale A, Tandel J, Noh S, Lakshminarayana SB, Lim SH, Goodman LB, Bodenreider C, Feng G, Zhang L, Blasco F, Wagner J, Leong FJ, Striepen B, Diagana TT. Manjunatha UH, et al. Nature. 2017 Jun 15;546(7658):376-380. doi: 10.1038/nature22337. Epub 2017 May 31. Nature. 2017. PMID: 28562588 Free PMC article.
Lead optimization of imidazopyrazines: a new class of antimalarial with activity on Plasmodium liver stages.
Zou B, Nagle A, Chatterjee AK, Leong SY, Tan LJ, Sim WL, Mishra P, Guntapalli P, Tully DC, Lakshminarayana SB, Lim CS, Tan YC, Abas SN, Bodenreider C, Kuhen KL, Gagaring K, Borboa R, Chang J, Li C, Hollenbeck T, Tuntland T, Zeeman AM, Kocken CH, McNamara C, Kato N, Winzeler EA, Yeung BK, Diagana TT, Smith PW, Roland J. Zou B, et al. ACS Med Chem Lett. 2014 Jul 6;5(8):947-50. doi: 10.1021/ml500244m. eCollection 2014 Aug 14. ACS Med Chem Lett. 2014. PMID: 25147620 Free PMC article.
A first-in-human randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study of novel Imidazolopiperazine KAF156 to assess its safety, tolerability, and pharmacokinetics in healthy adult volunteers.
Leong FJ, Zhao R, Zeng S, Magnusson B, Diagana TT, Pertel P. Leong FJ, et al. Antimicrob Agents Chemother. 2014 Nov;58(11):6437-43. doi: 10.1128/AAC.03478-14. Epub 2014 Aug 18. Antimicrob Agents Chemother. 2014. PMID: 25136017 Free PMC article. Clinical Trial.
A first-in-human randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study of novel antimalarial Spiroindolone KAE609 (Cipargamin) to assess its safety, tolerability, and pharmacokinetics in healthy adult volunteers.
Leong FJ, Li R, Jain JP, Lefèvre G, Magnusson B, Diagana TT, Pertel P. Leong FJ, et al. Antimicrob Agents Chemother. 2014 Oct;58(10):6209-14. doi: 10.1128/AAC.03393-14. Epub 2014 Aug 11. Antimicrob Agents Chemother. 2014. PMID: 25114127 Free PMC article. Clinical Trial.
Spiroindolone KAE609 for falciparum and vivax malaria.
White NJ, Pukrittayakamee S, Phyo AP, Rueangweerayut R, Nosten F, Jittamala P, Jeeyapant A, Jain JP, Lefèvre G, Li R, Magnusson B, Diagana TT, Leong FJ. White NJ, et al. N Engl J Med. 2014 Jul 31;371(5):403-10. doi: 10.1056/NEJMoa1315860. N Engl J Med. 2014. PMID: 25075833 Free PMC article. Clinical Trial.
KAF156 is an antimalarial clinical candidate with potential for use in prophylaxis, treatment, and prevention of disease transmission.
Kuhen KL, Chatterjee AK, Rottmann M, Gagaring K, Borboa R, Buenviaje J, Chen Z, Francek C, Wu T, Nagle A, Barnes SW, Plouffe D, Lee MC, Fidock DA, Graumans W, van de Vegte-Bolmer M, van Gemert GJ, Wirjanata G, Sebayang B, Marfurt J, Russell B, Suwanarusk R, Price RN, Nosten F, Tungtaeng A, Gettayacamin M, Sattabongkot J, Taylor J, Walker JR, Tully D, Patra KP, Flannery EL, Vinetz JM, Renia L, Sauerwein RW, Winzeler EA, Glynne RJ, Diagana TT. Kuhen KL, et al. Antimicrob Agents Chemother. 2014 Sep;58(9):5060-7. doi: 10.1128/AAC.02727-13. Epub 2014 Jun 9. Antimicrob Agents Chemother. 2014. PMID: 24913172 Free PMC article.
Persistence and activation of malaria hypnozoites in long-term primary hepatocyte cultures.
Dembélé L, Franetich JF, Lorthiois A, Gego A, Zeeman AM, Kocken CH, Le Grand R, Dereuddre-Bosquet N, van Gemert GJ, Sauerwein R, Vaillant JC, Hannoun L, Fuchter MJ, Diagana TT, Malmquist NA, Scherf A, Snounou G, Mazier D. Dembélé L, et al. Nat Med. 2014 Mar;20(3):307-12. doi: 10.1038/nm.3461. Epub 2014 Feb 9. Nat Med. 2014. PMID: 24509527
KAI407, a potent non-8-aminoquinoline compound that kills Plasmodium cynomolgi early dormant liver stage parasites in vitro.
Zeeman AM, van Amsterdam SM, McNamara CW, Voorberg-van der Wel A, Klooster EJ, van den Berg A, Remarque EJ, Plouffe DM, van Gemert GJ, Luty A, Sauerwein R, Gagaring K, Borboa R, Chen Z, Kuhen K, Glynne RJ, Chatterjee AK, Nagle A, Roland J, Winzeler EA, Leroy D, Campo B, Diagana TT, Yeung BK, Thomas AW, Kocken CH. Zeeman AM, et al. Antimicrob Agents Chemother. 2014;58(3):1586-95. doi: 10.1128/AAC.01927-13. Epub 2013 Dec 23. Antimicrob Agents Chemother. 2014. PMID: 24366744 Free PMC article.
Targeting Plasmodium PI(4)K to eliminate malaria.
McNamara CW, Lee MC, Lim CS, Lim SH, Roland J, Simon O, Yeung BK, Chatterjee AK, McCormack SL, Manary MJ, Zeeman AM, Dechering KJ, Kumar TS, Henrich PP, Gagaring K, Ibanez M, Kato N, Kuhen KL, Fischli C, Nagle A, Rottmann M, Plouffe DM, Bursulaya B, Meister S, Rameh L, Trappe J, Haasen D, Timmerman M, Sauerwein RW, Suwanarusk R, Russell B, Renia L, Nosten F, Tully DC, Kocken CH, Glynne RJ, Bodenreider C, Fidock DA, Diagana TT, Winzeler EA. McNamara CW, et al. Nature. 2013 Dec 12;504(7479):248-253. doi: 10.1038/nature12782. Epub 2013 Nov 27. Nature. 2013. PMID: 24284631 Free PMC article.