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Items: 29

1.

Open-source discovery of chemical leads for next-generation chemoprotective antimalarials.

Antonova-Koch Y, Meister S, Abraham M, Luth MR, Ottilie S, Lukens AK, Sakata-Kato T, Vanaerschot M, Owen E, Jado JC, Maher SP, Calla J, Plouffe D, Zhong Y, Chen K, Chaumeau V, Conway AJ, McNamara CW, Ibanez M, Gagaring K, Serrano FN, Eribez K, Taggard CM, Cheung AL, Lincoln C, Ambachew B, Rouillier M, Siegel D, Nosten F, Kyle DE, Gamo FJ, Zhou Y, Llinás M, Fidock DA, Wirth DF, Burrows J, Campo B, Winzeler EA.

Science. 2018 Dec 7;362(6419). pii: eaat9446. doi: 10.1126/science.aat9446.

PMID:
30523084
2.

Identification of Collateral Sensitivity to Dihydroorotate Dehydrogenase Inhibitors in Plasmodium falciparum.

Ross LS, Lafuente-Monasterio MJ, Sakata-Kato T, Mandt REK, Gamo FJ, Wirth DF, Lukens AK.

ACS Infect Dis. 2018 Apr 13;4(4):508-515. doi: 10.1021/acsinfecdis.7b00217. Epub 2018 Jan 22.

3.

Mapping the malaria parasite druggable genome by using in vitro evolution and chemogenomics.

Cowell AN, Istvan ES, Lukens AK, Gomez-Lorenzo MG, Vanaerschot M, Sakata-Kato T, Flannery EL, Magistrado P, Owen E, Abraham M, LaMonte G, Painter HJ, Williams RM, Franco V, Linares M, Arriaga I, Bopp S, Corey VC, Gnädig NF, Coburn-Flynn O, Reimer C, Gupta P, Murithi JM, Moura PA, Fuchs O, Sasaki E, Kim SW, Teng CH, Wang LT, Akidil A, Adjalley S, Willis PA, Siegel D, Tanaseichuk O, Zhong Y, Zhou Y, Llinás M, Ottilie S, Gamo FJ, Lee MCS, Goldberg DE, Fidock DA, Wirth DF, Winzeler EA.

Science. 2018 Jan 12;359(6372):191-199. doi: 10.1126/science.aan4472.

4.

Quantitative Proteomic Profiling Reveals Novel Plasmodium falciparum Surface Antigens and Possible Vaccine Candidates.

Nilsson Bark SK, Ahmad R, Dantzler K, Lukens AK, De Niz M, Szucs MJ, Jin X, Cotton J, Hoffmann D, Bric-Furlong E, Oomen R, Parrington M, Milner D, Neafsey DE, Carr SA, Wirth DF, Marti M.

Mol Cell Proteomics. 2018 Jan;17(1):43-60. doi: 10.1074/mcp.RA117.000076. Epub 2017 Nov 21.

5.

Genome-Wide Association Studies of Drug-Resistance Determinants.

Volkman SK, Herman J, Lukens AK, Hartl DL.

Trends Parasitol. 2017 Mar;33(3):214-230. doi: 10.1016/j.pt.2016.10.001. Epub 2016 Oct 27. Review.

PMID:
28179098
6.

Intramolecular Diaza-Diels-Alder Protocol: A New Diastereoselective and Modular One-Step Synthesis of Constrained Polycyclic Frameworks.

Srinivasulu V, Reddy A, Mazitschek R, Lukens AK, Wirth DF, Li L, Naumov P, O'Connor MJ, Al-Tel TH.

Chemistry. 2017 Mar 23;23(17):4137-4148. doi: 10.1002/chem.201605231. Epub 2017 Feb 17.

PMID:
27997727
7.

Plasmodium falciparum Cyclic Amine Resistance Locus (PfCARL), a Resistance Mechanism for Two Distinct Compound Classes.

Magistrado PA, Corey VC, Lukens AK, LaMonte G, Sasaki E, Meister S, Wree M, Winzeler E, Wirth DF.

ACS Infect Dis. 2016 Nov 11;2(11):816-826. Epub 2016 Apr 7.

8.

Diversity-oriented synthesis yields novel multistage antimalarial inhibitors.

Kato N, Comer E, Sakata-Kato T, Sharma A, Sharma M, Maetani M, Bastien J, Brancucci NM, Bittker JA, Corey V, Clarke D, Derbyshire ER, Dornan GL, Duffy S, Eckley S, Itoe MA, Koolen KM, Lewis TA, Lui PS, Lukens AK, Lund E, March S, Meibalan E, Meier BC, McPhail JA, Mitasev B, Moss EL, Sayes M, Van Gessel Y, Wawer MJ, Yoshinaga T, Zeeman AM, Avery VM, Bhatia SN, Burke JE, Catteruccia F, Clardy JC, Clemons PA, Dechering KJ, Duvall JR, Foley MA, Gusovsky F, Kocken CH, Marti M, Morningstar ML, Munoz B, Neafsey DE, Sharma A, Winzeler EA, Wirth DF, Scherer CA, Schreiber SL.

Nature. 2016 Oct 20;538(7625):344-349. doi: 10.1038/nature19804. Epub 2016 Sep 7.

9.

Probing the Azaaurone Scaffold against the Hepatic and Erythrocytic Stages of Malaria Parasites.

Carrasco MP, Machado M, Gonçalves L, Sharma M, Gut J, Lukens AK, Wirth DF, André V, Duarte MT, Guedes RC, Dos Santos DJ, Rosenthal PJ, Mazitschek R, Prudêncio M, Moreira R.

ChemMedChem. 2016 Oct 6;11(19):2194-2204. doi: 10.1002/cmdc.201600327. Epub 2016 Aug 19.

PMID:
27538856
10.

New paradigms for understanding and step changes in treating active and chronic, persistent apicomplexan infections.

McPhillie M, Zhou Y, El Bissati K, Dubey J, Lorenzi H, Capper M, Lukens AK, Hickman M, Muench S, Verma SK, Weber CR, Wheeler K, Gordon J, Sanders J, Moulton H, Wang K, Kim TK, He Y, Santos T, Woods S, Lee P, Donkin D, Kim E, Fraczek L, Lykins J, Esaa F, Alibana-Clouser F, Dovgin S, Weiss L, Brasseur G, Wirth D, Kent M, Hood L, Meunieur B, Roberts CW, Hasnain SS, Antonyuk SV, Fishwick C, McLeod R.

Sci Rep. 2016 Jul 14;6:29179. doi: 10.1038/srep29179.

11.

A broad analysis of resistance development in the malaria parasite.

Corey VC, Lukens AK, Istvan ES, Lee MC, Franco V, Magistrado P, Coburn-Flynn O, Sakata-Kato T, Fuchs O, Gnädig NF, Goldgof G, Linares M, Gomez-Lorenzo MG, De Cózar C, Lafuente-Monasterio MJ, Prats S, Meister S, Tanaseichuk O, Wree M, Zhou Y, Willis PA, Gamo FJ, Goldberg DE, Fidock DA, Wirth DF, Winzeler EA.

Nat Commun. 2016 Jun 15;7:11901. doi: 10.1038/ncomms11901.

12.

Exploring the 3-piperidin-4-yl-1H-indole scaffold as a novel antimalarial chemotype.

Santos SA, Lukens AK, Coelho L, Nogueira F, Wirth DF, Mazitschek R, Moreira R, Paulo A.

Eur J Med Chem. 2015 Sep 18;102:320-33. doi: 10.1016/j.ejmech.2015.07.047. Epub 2015 Jul 31.

PMID:
26295174
13.

Clinical Sequencing Uncovers Origins and Evolution of Lassa Virus.

Andersen KG, Shapiro BJ, Matranga CB, Sealfon R, Lin AE, Moses LM, Folarin OA, Goba A, Odia I, Ehiane PE, Momoh M, England EM, Winnicki S, Branco LM, Gire SK, Phelan E, Tariyal R, Tewhey R, Omoniwa O, Fullah M, Fonnie R, Fonnie M, Kanneh L, Jalloh S, Gbakie M, Saffa S, Karbo K, Gladden AD, Qu J, Stremlau M, Nekoui M, Finucane HK, Tabrizi S, Vitti JJ, Birren B, Fitzgerald M, McCowan C, Ireland A, Berlin AM, Bochicchio J, Tazon-Vega B, Lennon NJ, Ryan EM, Bjornson Z, Milner DA Jr, Lukens AK, Broodie N, Rowland M, Heinrich M, Akdag M, Schieffelin JS, Levy D, Akpan H, Bausch DG, Rubins K, McCormick JB, Lander ES, Günther S, Hensley L, Okogbenin S; Viral Hemorrhagic Fever Consortium, Schaffner SF, Okokhere PO, Khan SH, Grant DS, Akpede GO, Asogun DA, Gnirke A, Levin JZ, Happi CT, Garry RF, Sabeti PC.

Cell. 2015 Aug 13;162(4):738-50. doi: 10.1016/j.cell.2015.07.020.

14.

The cytoplasmic prolyl-tRNA synthetase of the malaria parasite is a dual-stage target of febrifugine and its analogs.

Herman JD, Pepper LR, Cortese JF, Estiu G, Galinsky K, Zuzarte-Luis V, Derbyshire ER, Ribacke U, Lukens AK, Santos SA, Patel V, Clish CB, Sullivan WJ Jr, Zhou H, Bopp SE, Schimmel P, Lindquist S, Clardy J, Mota MM, Keller TL, Whitman M, Wiest O, Wirth DF, Mazitschek R.

Sci Transl Med. 2015 May 20;7(288):288ra77. doi: 10.1126/scitranslmed.aaa3575.

15.

Triaminopyrimidine is a fast-killing and long-acting antimalarial clinical candidate.

Hameed P S, Solapure S, Patil V, Henrich PP, Magistrado PA, Bharath S, Murugan K, Viswanath P, Puttur J, Srivastava A, Bellale E, Panduga V, Shanbag G, Awasthy D, Landge S, Morayya S, Koushik K, Saralaya R, Raichurkar A, Rautela N, Roy Choudhury N, Ambady A, Nandishaiah R, Reddy J, Prabhakar KR, Menasinakai S, Rudrapatna S, Chatterji M, Jiménez-Díaz MB, Martínez MS, Sanz LM, Coburn-Flynn O, Fidock DA, Lukens AK, Wirth DF, Bandodkar B, Mukherjee K, McLaughlin RE, Waterson D, Rosenbrier-Ribeiro L, Hickling K, Balasubramanian V, Warner P, Hosagrahara V, Dudley A, Iyer PS, Narayanan S, Kavanagh S, Sambandamurthy VK.

Nat Commun. 2015 Mar 31;6:6715. doi: 10.1038/ncomms7715.

16.

Diversity-oriented synthesis probe targets Plasmodium falciparum cytochrome b ubiquinone reduction site and synergizes with oxidation site inhibitors.

Lukens AK, Heidebrecht RW Jr, Mulrooney C, Beaudoin JA, Comer E, Duvall JR, Fitzgerald ME, Masi D, Galinsky K, Scherer CA, Palmer M, Munoz B, Foley M, Schreiber SL, Wiegand RC, Wirth DF.

J Infect Dis. 2015 Apr 1;211(7):1097-103. doi: 10.1093/infdis/jiu565. Epub 2014 Oct 21.

17.

Diversity-oriented synthesis-facilitated medicinal chemistry: toward the development of novel antimalarial agents.

Comer E, Beaudoin JA, Kato N, Fitzgerald ME, Heidebrecht RW, Lee Md 4th, Masi D, Mercier M, Mulrooney C, Muncipinto G, Rowley A, Crespo-Llado K, Serrano AE, Lukens AK, Wiegand RC, Wirth DF, Palmer MA, Foley MA, Munoz B, Scherer CA, Duvall JR, Schreiber SL.

J Med Chem. 2014 Oct 23;57(20):8496-502. doi: 10.1021/jm500994n. Epub 2014 Oct 13.

18.

Aminoazabenzimidazoles, a novel class of orally active antimalarial agents.

Hameed P S, Chinnapattu M, Shanbag G, Manjrekar P, Koushik K, Raichurkar A, Patil V, Jatheendranath S, Rudrapatna SS, Barde SP, Rautela N, Awasthy D, Morayya S, Narayan C, Kavanagh S, Saralaya R, Bharath S, Viswanath P, Mukherjee K, Bandodkar B, Srivastava A, Panduga V, Reddy J, Prabhakar KR, Sinha A, Jiménez-Díaz MB, Martínez MS, Angulo-Barturen I, Ferrer S, Sanz LM, Gamo FJ, Duffy S, Avery VM, Magistrado PA, Lukens AK, Wirth DF, Waterson D, Balasubramanian V, Iyer PS, Narayanan S, Hosagrahara V, Sambandamurthy VK, Ramachandran S.

J Med Chem. 2014 Jul 10;57(13):5702-13. doi: 10.1021/jm500535j. Epub 2014 Jun 24.

PMID:
24914738
19.

Harnessing evolutionary fitness in Plasmodium falciparum for drug discovery and suppressing resistance.

Lukens AK, Ross LS, Heidebrecht R, Javier Gamo F, Lafuente-Monasterio MJ, Booker ML, Hartl DL, Wiegand RC, Wirth DF.

Proc Natl Acad Sci U S A. 2014 Jan 14;111(2):799-804. doi: 10.1073/pnas.1320886110. Epub 2013 Dec 31.

20.

Changes in drug sensitivity and anti-malarial drug resistance mutations over time among Plasmodium falciparum parasites in Senegal.

Van Tyne D, Dieye B, Valim C, Daniels RF, Sène PD, Lukens AK, Ndiaye M, Bei AK, Ndiaye YD, Hamilton EJ, Ndir O, Mboup S, Volkman SK, Wirth DF, Ndiaye D.

Malar J. 2013 Dec 6;12:441. doi: 10.1186/1475-2875-12-441.

21.

Genetic surveillance detects both clonal and epidemic transmission of malaria following enhanced intervention in Senegal.

Daniels R, Chang HH, Séne PD, Park DC, Neafsey DE, Schaffner SF, Hamilton EJ, Lukens AK, Van Tyne D, Mboup S, Sabeti PC, Ndiaye D, Wirth DF, Hartl DL, Volkman SK.

PLoS One. 2013 Apr 4;8(4):e60780. doi: 10.1371/journal.pone.0060780. Print 2013.

22.

ML238: An Antimalarial Small Molecule of a Unique Structural Class.

Weiwer M, Mulrooney C, Massi D, Heidebrecht R, Wiegand R, Lukens AK, Dick J, Wirth D, Ekland E, Cheng CC, Zhao J, Yuan J, Su XZ, Johnson RL, Guha R, Dandapani S, Munoz B, Palmer M, Thomas C, Austin CP, Fidock D, Schreiber SL.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Apr 14 [updated 2011 Dec 12].

23.

Sequence-based association and selection scans identify drug resistance loci in the Plasmodium falciparum malaria parasite.

Park DJ, Lukens AK, Neafsey DE, Schaffner SF, Chang HH, Valim C, Ribacke U, Van Tyne D, Galinsky K, Galligan M, Becker JS, Ndiaye D, Mboup S, Wiegand RC, Hartl DL, Sabeti PC, Wirth DF, Volkman SK.

Proc Natl Acad Sci U S A. 2012 Aug 7;109(32):13052-7. doi: 10.1073/pnas.1210585109. Epub 2012 Jul 23.

24.

SNP genotyping identifies new signatures of selection in a deep sample of West African Plasmodium falciparum malaria parasites.

Amambua-Ngwa A, Park DJ, Volkman SK, Barnes KG, Bei AK, Lukens AK, Sene P, Van Tyne D, Ndiaye D, Wirth DF, Conway DJ, Neafsey DE, Schaffner SF.

Mol Biol Evol. 2012 Nov;29(11):3249-53. doi: 10.1093/molbev/mss151. Epub 2012 Jun 11.

25.

Diversity-Oriented Synthesis Yields a Novel Lead for the Treatment of Malaria.

Heidebrecht RW Jr, Mulrooney C, Austin CP, Barker RH Jr, Beaudoin JA, Cheng KC, Comer E, Dandapani S, Dick J, Duvall JR, Ekland EH, Fidock DA, Fitzgerald ME, Foley M, Guha R, Hinkson P, Kramer M, Lukens AK, Masi D, Marcaurelle LA, Su XZ, Thomas CJ, Weïwer M, Wiegand RC, Wirth D, Xia M, Yuan J, Zhao J, Palmer M, Munoz B, Schreiber S.

ACS Med Chem Lett. 2012 Feb 9;3(2):112-117. Epub 2011 Dec 22.

26.

Human cerebral malaria and Plasmodium falciparum genotypes in Malawi.

Milner DA Jr, Vareta J, Valim C, Montgomery J, Daniels RF, Volkman SK, Neafsey DE, Park DJ, Schaffner SF, Mahesh NC, Barnes KG, Rosen DM, Lukens AK, Van Tyne D, Wiegand RC, Sabeti PC, Seydel KB, Glover SJ, Kamiza S, Molyneux ME, Taylor TE, Wirth DF.

Malar J. 2012 Feb 7;11:35. doi: 10.1186/1475-2875-11-35.

27.

Identification and functional validation of the novel antimalarial resistance locus PF10_0355 in Plasmodium falciparum.

Van Tyne D, Park DJ, Schaffner SF, Neafsey DE, Angelino E, Cortese JF, Barnes KG, Rosen DM, Lukens AK, Daniels RF, Milner DA Jr, Johnson CA, Shlyakhter I, Grossman SR, Becker JS, Yamins D, Karlsson EK, Ndiaye D, Sarr O, Mboup S, Happi C, Furlotte NA, Eskin E, Kang HM, Hartl DL, Birren BW, Wiegand RC, Lander ES, Wirth DF, Volkman SK, Sabeti PC.

PLoS Genet. 2011 Apr;7(4):e1001383. doi: 10.1371/journal.pgen.1001383. Epub 2011 Apr 21.

28.

Intrinsic susceptibility of mouse trophoblasts to natural killer cell-mediated attack in vivo.

Erlebacher A, Lukens AK, Glimcher LH.

Proc Natl Acad Sci U S A. 2002 Dec 24;99(26):16940-5. Epub 2002 Dec 16.

29.

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