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Items: 9

1.

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.

ACS Med Chem Lett. 2014 Jul 6;5(8):947-50. doi: 10.1021/ml500244m. eCollection 2014 Aug 14.

2.

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.

Antimicrob Agents Chemother. 2014 Sep;58(9):5060-7. doi: 10.1128/AAC.02727-13. Epub 2014 Jun 9.

3.

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.

Antimicrob Agents Chemother. 2014;58(3):1586-95. doi: 10.1128/AAC.01927-13. Epub 2013 Dec 23.

4.

Imidazolopiperazines: lead optimization of the second-generation antimalarial agents.

Nagle A, Wu T, Kuhen K, Gagaring K, Borboa R, Francek C, Chen Z, Plouffe D, Lin X, Caldwell C, Ek J, Skolnik S, Liu F, Wang J, Chang J, Li C, Liu B, Hollenbeck T, Tuntland T, Isbell J, Chuan T, Alper PB, Fischli C, Brun R, Lakshminarayana SB, Rottmann M, Diagana TT, Winzeler EA, Glynne R, Tully DC, Chatterjee AK.

J Med Chem. 2012 May 10;55(9):4244-73. doi: 10.1021/jm300041e. Epub 2012 Apr 23.

5.

Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.

Meister S, Plouffe DM, Kuhen KL, Bonamy GM, Wu T, Barnes SW, Bopp SE, Borboa R, Bright AT, Che J, Cohen S, Dharia NV, Gagaring K, Gettayacamin M, Gordon P, Groessl T, Kato N, Lee MC, McNamara CW, Fidock DA, Nagle A, Nam TG, Richmond W, Roland J, Rottmann M, Zhou B, Froissard P, Glynne RJ, Mazier D, Sattabongkot J, Schultz PG, Tuntland T, Walker JR, Zhou Y, Chatterjee A, Diagana TT, Winzeler EA.

Science. 2011 Dec 9;334(6061):1372-7. doi: 10.1126/science.1211936. Epub 2011 Nov 17.

6.

Imidazolopiperazines: hit to lead optimization of new antimalarial agents.

Wu T, Nagle A, Kuhen K, Gagaring K, Borboa R, Francek C, Chen Z, Plouffe D, Goh A, Lakshminarayana SB, Wu J, Ang HQ, Zeng P, Kang ML, Tan W, Tan M, Ye N, Lin X, Caldwell C, Ek J, Skolnik S, Liu F, Wang J, Chang J, Li C, Hollenbeck T, Tuntland T, Isbell J, Fischli C, Brun R, Rottmann M, Dartois V, Keller T, Diagana T, Winzeler E, Glynne R, Tully DC, Chatterjee AK.

J Med Chem. 2011 Jul 28;54(14):5116-30. doi: 10.1021/jm2003359. Epub 2011 Jun 23.

PMID:
21644570
7.

Whole-genome sequencing and microarray analysis of ex vivo Plasmodium vivax reveal selective pressure on putative drug resistance genes.

Dharia NV, Bright AT, Westenberger SJ, Barnes SW, Batalov S, Kuhen K, Borboa R, Federe GC, McClean CM, Vinetz JM, Neyra V, Llanos-Cuentas A, Barnwell JW, Walker JR, Winzeler EA.

Proc Natl Acad Sci U S A. 2010 Nov 16;107(46):20045-50. doi: 10.1073/pnas.1003776107. Epub 2010 Oct 29.

8.

Identification of inhibitors for putative malaria drug targets among novel antimalarial compounds.

Crowther GJ, Napuli AJ, Gilligan JH, Gagaring K, Borboa R, Francek C, Chen Z, Dagostino EF, Stockmyer JB, Wang Y, Rodenbough PP, Castaneda LJ, Leibly DJ, Bhandari J, Gelb MH, Brinker A, Engels IH, Taylor J, Chatterjee AK, Fantauzzi P, Glynne RJ, Van Voorhis WC, Kuhen KL.

Mol Biochem Parasitol. 2011 Jan;175(1):21-9. doi: 10.1016/j.molbiopara.2010.08.005. Epub 2010 Sep 15.

9.

Cell-based optimization of novel benzamides as potential antimalarial leads.

Wu T, Nagle A, Sakata T, Henson K, Borboa R, Chen Z, Kuhen K, Plouffe D, Winzeler E, Adrian F, Tuntland T, Chang J, Simerson S, Howard S, Ek J, Isbell J, Deng X, Gray NS, Tully DC, Chatterjee AK.

Bioorg Med Chem Lett. 2009 Dec 15;19(24):6970-4. doi: 10.1016/j.bmcl.2009.10.050. Epub 2009 Oct 29.

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