{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,2]],"date-time":"2026-10-02T10:32:33Z","timestamp":1790937153360,"version":"4.1.0"},"update-to":[{"DOI":"10.1371\/journal.ppat.1012429","type":"new_version","label":"New version","source":"publisher","updated":{"date-parts":[[2024,12,26]],"date-time":"2024-12-26T00:00:00Z","timestamp":1735171200000}}],"reference-count":59,"publisher":"Public Library of Science (PLoS)","issue":"12","license":[{"start":{"date-parts":[[2024,12,9]],"date-time":"2024-12-09T00:00:00Z","timestamp":1733702400000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100013996","name":"Global Health Innovative Technology Fund","doi-asserted-by":"publisher","award":["H2019-104"],"award-info":[{"award-number":["H2019-104"]}],"id":[{"id":"10.13039\/501100013996","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100000925","name":"National Health and Medical Research Council","doi-asserted-by":"publisher","award":["APP2022075"],"award-info":[{"award-number":["APP2022075"]}],"id":[{"id":"10.13039\/501100000925","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100000923","name":"Australian Research Council","doi-asserted-by":"publisher","award":["DE230101173"],"award-info":[{"award-number":["DE230101173"]}],"id":[{"id":"10.13039\/501100000923","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100004167","name":"Medicines for Malaria Venture","doi-asserted-by":"publisher","award":["RD-19-001"],"award-info":[{"award-number":["RD-19-001"]}],"id":[{"id":"10.13039\/501100004167","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100004167","name":"Medicines for Malaria Venture","doi-asserted-by":"publisher","award":["RD-08-0015"],"award-info":[{"award-number":["RD-08-0015"]}],"id":[{"id":"10.13039\/501100004167","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100004167","name":"Medicines for Malaria Venture","doi-asserted-by":"publisher","award":["RD-21-1003"],"award-info":[{"award-number":["RD-21-1003"]}],"id":[{"id":"10.13039\/501100004167","id-type":"DOI","asserted-by":"publisher"}]},{"name":"The Foundation for Research Support of the State of S\u00e3o Paulo","award":["2019\/19708-0"],"award-info":[{"award-number":["2019\/19708-0"]}]},{"name":"The Foundation for Research Support of the State of S\u00e3o Paulo","award":["2013\/07600-3"],"award-info":[{"award-number":["2013\/07600-3"]}]},{"DOI":"10.13039\/501100001321","name":"National Research Foundation","doi-asserted-by":"crossref","award":["UID 84627"],"award-info":[{"award-number":["UID 84627"]}],"id":[{"id":"10.13039\/501100001321","id-type":"DOI","asserted-by":"crossref"}]},{"DOI":"10.13039\/501100000265","name":"Medical Research Council","doi-asserted-by":"publisher","award":["MR\/V010034\/1"],"award-info":[{"award-number":["MR\/V010034\/1"]}],"id":[{"id":"10.13039\/501100000265","id-type":"DOI","asserted-by":"publisher"}]},{"name":"Millennium Pharmaceuticals"}],"content-domain":{"domain":["www.plospathogens.org"],"crossmark-restriction":false},"short-container-title":["PLoS Pathog"],"abstract":"<jats:p>The <jats:italic>Plasmodium falciparum<\/jats:italic> cytoplasmic tyrosine tRNA synthetase (<jats:italic>Pf<\/jats:italic>TyrRS) is an attractive drug target that is susceptible to reaction-hijacking by AMP-mimicking nucleoside sulfamates. We previously identified an exemplar pyrazolopyrimidine ribose sulfamate, ML901, as a potent reaction hijacking inhibitor of <jats:italic>Pf<\/jats:italic>TyrRS. Here we examined the stage specificity of action of ML901, showing very good activity against the schizont stage, but lower trophozoite stage activity. We explored a series of ML901 analogues and identified ML471, which exhibits improved potency against trophozoites and enhanced selectivity against a human cell line. Additionally, it has no inhibitory activity against human ubiquitin-activating enzyme (UAE) <jats:italic>in vitro<\/jats:italic>. ML471 exhibits low nanomolar activity against asexual blood stage <jats:italic>P<\/jats:italic>. <jats:italic>falciparum<\/jats:italic> and potent activity against liver stage parasites, gametocytes and transmissible gametes. It is fast-acting and exhibits a long <jats:italic>in vivo<\/jats:italic> half-life. ML471 is well-tolerated and shows single dose oral efficacy in the SCID mouse model of <jats:italic>P<\/jats:italic>. <jats:italic>falciparum<\/jats:italic> malaria. We confirm that ML471 is a reaction hijacking inhibitor that is converted into a tight binding Tyr-ML471 conjugate by the <jats:italic>Pf<\/jats:italic>TyrRS enzyme. A crystal structure of the <jats:italic>Pf<\/jats:italic>TyrRS\/ Tyr-ML471 complex offers insights into improved potency, while molecular docking into UAE provides a rationale for improved selectivity.<\/jats:p>","DOI":"10.1371\/journal.ppat.1012429","type":"journal-article","created":{"date-parts":[[2024,12,9]],"date-time":"2024-12-09T18:41:42Z","timestamp":1733769702000},"page":"e1012429","update-policy":"https:\/\/doi.org\/10.1371\/journal.ppat.corrections_policy","source":"Crossref","is-referenced-by-count":5,"title":["A potent and selective reaction hijacking inhibitor of Plasmodium falciparum tyrosine tRNA synthetase exhibits single dose oral efficacy in vivo"],"prefix":"10.1371","volume":"20","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-7003-4677","authenticated-orcid":true,"given":"Stanley C.","family":"Xie","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Chia-Wei","family":"Tai","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Craig J.","family":"Morton","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Liting","family":"Ma","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shih-Chung","family":"Huang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sergio","family":"Wittlin","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yawei","family":"Du","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yongbo","family":"Hu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Con","family":"Dogovski","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mina","family":"Salimimarand","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Robert","family":"Griffin","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dylan","family":"England","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Elisa","family":"de la Cruz","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ioanna","family":"Deni","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Tomas","family":"Yeo","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Anna Y.","family":"Burkhard","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Josefine","family":"Striepen","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kyra A.","family":"Schindler","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Benigno","family":"Crespo","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Francisco J.","family":"Gamo","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yogesh","family":"Khandokar","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Craig A.","family":"Hutton","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Tayla","family":"Rabie","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lyn-Mari\u00e9","family":"Birkholtz","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mufuliat T.","family":"Famodimu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Michael J.","family":"Delves","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Judith","family":"Bolsher","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Karin M. J.","family":"Koolen","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Rianne","family":"van der Laak","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Anna C. C.","family":"Aguiar","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dhelio B.","family":"Pereira","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Rafael V. C.","family":"Guido","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Darren J.","family":"Creek","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"David A.","family":"Fidock","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lawrence R.","family":"Dick","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Stephen L.","family":"Brand","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Alexandra E.","family":"Gould","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Steven","family":"Langston","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Michael D. W.","family":"Griffin","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9910-0199","authenticated-orcid":true,"given":"Leann","family":"Tilley","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"340","published-online":{"date-parts":[[2024,12,9]]},"reference":[{"key":"ppat.1012429.ref001","volume-title":"WHO World Malaria Report 2023","author":"World_Health_Organisation","year":"2023"},{"issue":"1","key":"ppat.1012429.ref002","doi-asserted-by":"crossref","first-page":"239","DOI":"10.1186\/s12916-020-01710-x","article-title":"Identifying and combating the impacts of COVID-19 on malaria","volume":"18","author":"SJ Rogerson","year":"2020","journal-title":"BMC Medicine"},{"issue":"9","key":"ppat.1012429.ref003","doi-asserted-by":"crossref","first-page":"952","DOI":"10.1016\/S1473-3099(19)30391-3","article-title":"Determinants of dihydroartemisinin-piperaquine treatment failure in Plasmodium falciparum malaria in Cambodia, Thailand, and Vietnam: a prospective clinical, pharmacological, and genetic study","volume":"19","author":"RW van der Pluijm","year":"2019","journal-title":"Lancet Infect Dis"},{"issue":"12","key":"ppat.1012429.ref004","doi-asserted-by":"crossref","first-page":"1470","DOI":"10.1016\/S1473-3099(20)30228-0","article-title":"Molecular epidemiology of resistance to antimalarial drugs in the Greater Mekong subregion: an observational study","volume":"20","author":"M Imwong","year":"2020","journal-title":"Lancet Infect Dis"},{"issue":"8","key":"ppat.1012429.ref005","doi-asserted-by":"crossref","first-page":"1411","DOI":"10.1093\/infdis\/jiab352","article-title":"High prevalence of Plasmodium falciparum K13 mutations in Rwanda is associated with slow parasite clearance after treatment with artemether-lumefantrine","volume":"225","author":"J Straimer","year":"2021","journal-title":"The Journal of infectious diseases"},{"issue":"13","key":"ppat.1012429.ref006","doi-asserted-by":"crossref","first-page":"1163","DOI":"10.1056\/NEJMoa2101746","article-title":"Evidence of artemisinin-resistant malaria in Africa","volume":"385","author":"B Balikagala","year":"2021","journal-title":"New England Journal of Medicine"},{"issue":"13","key":"ppat.1012429.ref007","doi-asserted-by":"crossref","first-page":"1191","DOI":"10.1056\/NEJMoa2210956","article-title":"Increasing prevalence of artemisinin-resistant HRP2-negative malaria in Eritrea","volume":"389","author":"S Mihreteab","year":"2023","journal-title":"N Engl J Med"},{"issue":"1","key":"ppat.1012429.ref008","doi-asserted-by":"crossref","first-page":"26","DOI":"10.1186\/s12936-016-1675-x","article-title":"New developments in anti-malarial target candidate and product profiles","volume":"16","author":"JN Burrows","year":"2017","journal-title":"Malaria Journal"},{"issue":"7239","key":"ppat.1012429.ref009","doi-asserted-by":"crossref","first-page":"732","DOI":"10.1038\/nature07884","article-title":"An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer","volume":"458","author":"TA Soucy","year":"2009","journal-title":"Nature"},{"issue":"1","key":"ppat.1012429.ref010","doi-asserted-by":"crossref","first-page":"102","DOI":"10.1016\/j.molcel.2009.12.024","article-title":"Substrate-assisted inhibition of ubiquitin-like protein-activating enzymes: the NEDD8 E1 inhibitor MLN4924 forms a NEDD8-AMP mimetic in situ","volume":"37","author":"JE Brownell","year":"2010","journal-title":"Mol Cell"},{"issue":"2","key":"ppat.1012429.ref011","doi-asserted-by":"crossref","first-page":"186","DOI":"10.1038\/nm.4474","article-title":"A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment","volume":"24","author":"ML Hyer","year":"2018","journal-title":"Nat Med"},{"issue":"19","key":"ppat.1012429.ref012","doi-asserted-by":"crossref","first-page":"115681","DOI":"10.1016\/j.bmc.2020.115681","article-title":"Discovery and optimization of pyrazolopyrimidine sulfamates as ATG7 inhibitors","volume":"28","author":"S-C Huang","year":"2020","journal-title":"Bioorganic & medicinal chemistry"},{"issue":"3","key":"ppat.1012429.ref013","doi-asserted-by":"crossref","first-page":"388","DOI":"10.1016\/j.ccr.2012.02.009","article-title":"Treatment-emergent mutations in NAE\u03b2 confer resistance to the NEDD8-activating enzyme inhibitor MLN4924","volume":"21","author":"MA Milhollen","year":"2012","journal-title":"Cancer Cell"},{"issue":"1","key":"ppat.1012429.ref014","doi-asserted-by":"crossref","first-page":"61","DOI":"10.1038\/s41420-020-00296-w","article-title":"Pevonedistat (MLN4924): mechanism of cell death induction and therapeutic potential in colorectal cancer","volume":"6","author":"J Ferris","year":"2020","journal-title":"Cell Death Discovery"},{"issue":"1","key":"ppat.1012429.ref015","doi-asserted-by":"crossref","first-page":"87","DOI":"10.1186\/s13045-023-01485-7","article-title":"Targeting NEDD8-activating enzyme for cancer therapy: developments, clinical trials, challenges and future research directions","volume":"16","author":"D-J Fu","year":"2023","journal-title":"Journal of Hematology & Oncology"},{"issue":"6597","key":"ppat.1012429.ref016","doi-asserted-by":"crossref","first-page":"1074","DOI":"10.1126\/science.abn0611","article-title":"Reaction hijacking of tyrosine tRNA synthetase as a new whole-of-life-cycle antimalarial strategy","volume":"376","author":"SC Xie","year":"2022","journal-title":"Science"},{"issue":"1","key":"ppat.1012429.ref017","doi-asserted-by":"crossref","first-page":"937","DOI":"10.1038\/s41467-024-45224-z","article-title":"Reaction hijacking inhibition of Plasmodium falciparum asparagine tRNA synthetase","volume":"15","author":"SC Xie","year":"2024","journal-title":"Nat Commun"},{"issue":"4","key":"ppat.1012429.ref018","doi-asserted-by":"crossref","first-page":"e1002132","DOI":"10.1371\/journal.pbio.1002132","article-title":"Targeting the cell stress response of Plasmodium falciparum to overcome artemisinin resistance","volume":"13","author":"C Dogovski","year":"2015","journal-title":"PLoS Biol"},{"issue":"3","key":"ppat.1012429.ref019","doi-asserted-by":"crossref","first-page":"253","DOI":"10.1002\/cyto.a.20856","article-title":"Dual labeling with a far red probe permits analysis of growth and oxidative stress in P. falciparum-infected erythrocytes","volume":"77","author":"Y Fu","year":"2010","journal-title":"Cytometry A"},{"issue":"24","key":"ppat.1012429.ref020","doi-asserted-by":"crossref","first-page":"4395","DOI":"10.1021\/bi00800a007","article-title":"Inhibition of protein synthesis by 5\u2019-sulfamoyladenosine","volume":"10","author":"A Bloch","year":"1971","journal-title":"Biochemistry"},{"issue":"5","key":"ppat.1012429.ref021","doi-asserted-by":"crossref","first-page":"1091","DOI":"10.1016\/S0021-9258(18)96807-9","article-title":"Inhibition of protein synthesis in vitro and in vivo by nucleocidin, an antitrypanosomal antibiotic","volume":"241","author":"JR Florini","year":"1966","journal-title":"J Biol Chem"},{"key":"ppat.1012429.ref022","volume-title":"Atg7 inhibitors and the uses thereof","author":"S Adhikari","year":"2017"},{"key":"ppat.1012429.ref023","doi-asserted-by":"crossref","first-page":"0","DOI":"10.1080\/15548627.2015.1056966","article-title":"Identification of a lung cancer cell line deficient in atg7-dependent autophagy","author":"J Mandelbaum","year":"2015","journal-title":"Autophagy"},{"issue":"5","key":"ppat.1012429.ref024","doi-asserted-by":"crossref","first-page":"319","DOI":"10.1038\/nrm2673","article-title":"Ubiquitin-like protein activation by E1 enzymes: the apex for downstream signalling pathways","volume":"10","author":"BA Schulman","year":"2009","journal-title":"Nat Rev Mol Cell Biol"},{"issue":"47","key":"ppat.1012429.ref025","doi-asserted-by":"crossref","first-page":"40867","DOI":"10.1074\/jbc.M111.279984","article-title":"Mechanistic studies of substrate-assisted inhibition of ubiquitin-activating enzyme by adenosine sulfamate analogues","volume":"286","author":"JJ Chen","year":"2011","journal-title":"J Biol Chem"},{"issue":"7556","key":"ppat.1012429.ref026","doi-asserted-by":"crossref","first-page":"315","DOI":"10.1038\/nature14451","article-title":"A novel multiple-stage antimalarial agent that inhibits protein synthesis","volume":"522","author":"B Baraga\u00f1a","year":"2015","journal-title":"Nature"},{"issue":"2","key":"ppat.1012429.ref027","doi-asserted-by":"crossref","first-page":"e30949","DOI":"10.1371\/journal.pone.0030949","article-title":"P. falciparum in vitro killing rates allow to discriminate between different antimalarial mode-of-action","volume":"7","author":"LM Sanz","year":"2012","journal-title":"PloS one"},{"issue":"12","key":"ppat.1012429.ref028","doi-asserted-by":"crossref","first-page":"3467","DOI":"10.1016\/j.bmcl.2010.05.009","article-title":"Carbonic anhydrase inhibitors","volume":"20","author":"CT Supuran","year":"2010","journal-title":"Bioorg Med Chem Lett"},{"issue":"3","key":"ppat.1012429.ref029","doi-asserted-by":"crossref","first-page":"203","DOI":"10.1023\/A:1015957315462","article-title":"Binding of sulfonamides to carbonic anhydrase: influence on distribution within blood and on pharmacokinetics","volume":"6","author":"A Boddy","year":"1989","journal-title":"Pharm Res"},{"issue":"5","key":"ppat.1012429.ref030","doi-asserted-by":"crossref","first-page":"e2252","DOI":"10.1371\/journal.pone.0002252","article-title":"A murine model of falciparum-malaria by in vivo selection of competent strains in non-myelodepleted mice engrafted with human erythrocytes","volume":"3","author":"I Angulo-Barturen","year":"2008","journal-title":"PloS one"},{"issue":"3","key":"ppat.1012429.ref031","doi-asserted-by":"crossref","first-page":"225","DOI":"10.1002\/cyto.a.20647","article-title":"Quantitative measurement of Plasmodium-infected erythrocytes in murine models of malaria by flow cytometry using bidimensional assessment of SYTO-16 fluorescence","volume":"75","author":"MB Jimenez-Diaz","year":"2009","journal-title":"Cytometry A"},{"issue":"6372","key":"ppat.1012429.ref032","doi-asserted-by":"crossref","first-page":"191","DOI":"10.1126\/science.aan4472","article-title":"Mapping the malaria parasite druggable genome by using in vitro evolution and chemogenomics","volume":"359","author":"AN Cowell","year":"2018","journal-title":"Science"},{"issue":"3","key":"ppat.1012429.ref033","doi-asserted-by":"crossref","first-page":"301","DOI":"10.1021\/acsinfecdis.7b00276","article-title":"Using in vitro evolution and whole genome analysis to discover next generation targets for antimalarial drug discovery","volume":"4","author":"MR Luth","year":"2018","journal-title":"ACS Infect Dis"},{"issue":"8","key":"ppat.1012429.ref034","doi-asserted-by":"crossref","first-page":"709","DOI":"10.1016\/j.pt.2021.04.006","article-title":"Assessing risks of Plasmodium falciparum resistance to select next-generation antimalarials","volume":"37","author":"M Duffey","year":"2021","journal-title":"Trends in Parasitology"},{"issue":"14","key":"ppat.1012429.ref035","doi-asserted-by":"crossref","first-page":"e133","DOI":"10.1093\/nar\/gkx514","article-title":"Determination of tRNA aminoacylation levels by high-throughput sequencing","volume":"45","author":"ME Evans","year":"2017","journal-title":"Nucleic Acids Res"},{"issue":"47","key":"ppat.1012429.ref036","doi-asserted-by":"crossref","first-page":"18337","DOI":"10.1074\/jbc.RA118.003975","article-title":"Crystal structure of a human ubiquitin E1-ubiquitin complex reveals conserved functional elements essential for activity","volume":"293","author":"Z Lv","year":"2018","journal-title":"J Biol Chem"},{"issue":"11","key":"ppat.1012429.ref037","doi-asserted-by":"crossref","first-page":"3246","DOI":"10.1093\/nar\/gkl441","article-title":"Structure of human tryptophanyl-tRNA synthetase in complex with tRNATrp reveals the molecular basis of tRNA recognition and specificity","volume":"34","author":"N Shen","year":"2006","journal-title":"Nucleic Acids Res"},{"issue":"7296","key":"ppat.1012429.ref038","doi-asserted-by":"crossref","first-page":"305","DOI":"10.1038\/nature09107","article-title":"Thousands of chemical starting points for antimalarial lead identification","volume":"465","author":"FJ Gamo","year":"2010","journal-title":"Nature"},{"issue":"13","key":"ppat.1012429.ref039","doi-asserted-by":"crossref","first-page":"5157","DOI":"10.1073\/pnas.1217452110","article-title":"Altered temporal response of malaria parasites determines differential sensitivity to artemisinin","volume":"110","author":"N Klonis","year":"2013","journal-title":"Proc Natl Acad Sci U S A"},{"issue":"6220","key":"ppat.1012429.ref040","doi-asserted-by":"crossref","first-page":"428","DOI":"10.1126\/science.1260867","article-title":"Drug resistance. K13-propeller mutations confer artemisinin resistance in Plasmodium falciparum clinical isolates","volume":"347","author":"J Straimer","year":"2015","journal-title":"Science"},{"issue":"28","key":"ppat.1012429.ref041","doi-asserted-by":"crossref","first-page":"11405","DOI":"10.1073\/pnas.1104063108","article-title":"Artemisinin activity against Plasmodium falciparum requires hemoglobin uptake and digestion","volume":"108","author":"N Klonis","year":"2011","journal-title":"Proc Natl Acad Sci U S A"},{"issue":"6","key":"ppat.1012429.ref042","doi-asserted-by":"crossref","first-page":"1926","DOI":"10.1128\/AAC.01607-06","article-title":"Assessment and continued validation of the malaria SYBR green I-based fluorescence assay for use in malaria drug screening","volume":"51","author":"JD Johnson","year":"2007","journal-title":"Antimicrob Agents Chemother"},{"key":"ppat.1012429.ref043","doi-asserted-by":"crossref","first-page":"73","DOI":"10.1186\/1475-2875-13-73","article-title":"Plasmodium vivax and Plasmodium falciparum ex vivo susceptibility to anti-malarials and gene characterization in Rondonia, West Amazon, Brazil","volume":"13","author":"AC Aguiar","year":"2014","journal-title":"Malar J"},{"key":"ppat.1012429.ref044","doi-asserted-by":"crossref","first-page":"213","DOI":"10.1186\/s12936-015-0718-z","article-title":"Nowhere to hide: interrogating different metabolic parameters of Plasmodium falciparum gametocytes in a transmission blocking drug discovery pipeline towards malaria elimination","volume":"14","author":"J Reader","year":"2015","journal-title":"Malar J"},{"key":"ppat.1012429.ref045","doi-asserted-by":"crossref","first-page":"926460","DOI":"10.3389\/fcimb.2022.926460","article-title":"Streamlined and robust stage-specific profiling of gametocytocidal compounds against Plasmodium falciparum","volume":"12","author":"J Reader","year":"2022","journal-title":"Front Cell Infect Microbiol"},{"issue":"9","key":"ppat.1012429.ref046","doi-asserted-by":"crossref","first-page":"1668","DOI":"10.1038\/nprot.2016.096","article-title":"Routine in vitro culture of P. falciparum gametocytes to evaluate novel transmission-blocking interventions","volume":"11","author":"MJ Delves","year":"2016","journal-title":"Nat Protoc"},{"issue":"1","key":"ppat.1012429.ref047","doi-asserted-by":"crossref","first-page":"216","DOI":"10.1038\/s42003-023-04599-3","article-title":"Assessment of the drugability of initial malaria infection through miniaturized sporozoite assays and high-throughput screening","volume":"6","author":"M Miglianico","year":"2023","journal-title":"Commun Biol"},{"issue":"6","key":"ppat.1012429.ref048","doi-asserted-by":"crossref","first-page":"e106583","DOI":"10.15252\/embj.2020106583","article-title":"Zonal human hepatocytes are differentially permissive to Plasmodium falciparum malaria parasites","volume":"40","author":"ASP Yang","year":"2021","journal-title":"Embo J"},{"issue":"4","key":"ppat.1012429.ref049","first-page":"201","article-title":"P-glycoprotein and breast cancer resistance protein affect disposition of tandutinib, a tyrosine kinase inhibitor.","volume":"4","author":"JJ Yang","year":"2010","journal-title":"Drug Metab Lett"},{"issue":"10","key":"ppat.1012429.ref050","doi-asserted-by":"crossref","first-page":"4533","DOI":"10.1128\/AAC.00519-09","article-title":"Improved murine model of malaria using Plasmodium falciparum competent strains and non-myelodepleted NOD-scid IL2Rgammanull mice engrafted with human erythrocytes","volume":"53","author":"MB Jimenez-Diaz","year":"2009","journal-title":"Antimicrob Agents Chemother"},{"issue":"Pt 3","key":"ppat.1012429.ref051","doi-asserted-by":"crossref","first-page":"885","DOI":"10.1107\/S1600577518003120","article-title":"MX2: a high-flux undulator microfocus beamline serving both the chemical and macromolecular crystallography communities at the Australian Synchrotron","volume":"25","author":"D Arag\u00e3o","year":"2018","journal-title":"J Synchrotron Radiat"},{"key":"ppat.1012429.ref052","doi-asserted-by":"crossref","first-page":"1204","DOI":"10.1107\/S0907444913000061","article-title":"How good are my data and what is the resolution?","volume":"69","author":"PR Evans","year":"2013","journal-title":"Acta Crystallogr D"},{"key":"ppat.1012429.ref053","doi-asserted-by":"crossref","first-page":"235","DOI":"10.1107\/S0907444910045749","article-title":"Overview of the CCP4 suite and current developments","volume":"67","author":"MD Winn","year":"2011","journal-title":"Acta Crystallogr D"},{"key":"ppat.1012429.ref054","doi-asserted-by":"crossref","first-page":"658","DOI":"10.1107\/S0021889807021206","article-title":"Phaser crystallographic software","volume":"40","author":"AJ Mccoy","year":"2007","journal-title":"Journal of Applied Crystallography"},{"key":"ppat.1012429.ref055","doi-asserted-by":"crossref","first-page":"213","DOI":"10.1107\/S0907444909052925","article-title":"PHENIX: a comprehensive Python-based system for macromolecular structure solution","volume":"66","author":"PD Adams","year":"2010","journal-title":"Acta Crystallogr D"},{"key":"ppat.1012429.ref056","doi-asserted-by":"crossref","first-page":"486","DOI":"10.1107\/S0907444910007493","article-title":"Features and development of Coot","volume":"66","author":"P Emsley","year":"2010","journal-title":"Acta Crystallographica Section D-Biological Crystallography"},{"key":"ppat.1012429.ref057","doi-asserted-by":"crossref","first-page":"1074","DOI":"10.1107\/S0907444909029436","article-title":"Electronic ligand builder and optimization workbench (eLBOW): A tool for ligand coordinate and restraint generation","volume":"65","author":"NW Moriarty","year":"2009","journal-title":"Acta Crystallographica Section D: Biological Crystallography"},{"issue":"17","key":"ppat.1012429.ref058","doi-asserted-by":"crossref","first-page":"3009","DOI":"10.1016\/j.bmcl.2018.04.038","article-title":"Synthesis, structure and bioactivity of primary sulfamate-containing natural products","volume":"28","author":"P Mujumdar","year":"2018","journal-title":"Bioorg Med Chem Lett"},{"issue":"10","key":"ppat.1012429.ref059","doi-asserted-by":"crossref","first-page":"1880","DOI":"10.1002\/pro.3701","article-title":"A simple model for determining affinity from irreversible thermal shifts","volume":"28","author":"J. Hall","year":"2019","journal-title":"Protein Sci"}],"updated-by":[{"DOI":"10.1371\/journal.ppat.1012429","type":"new_version","label":"New version","source":"publisher","updated":{"date-parts":[[2024,12,26]],"date-time":"2024-12-26T00:00:00Z","timestamp":1735171200000}}],"container-title":["PLOS Pathogens"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/dx.plos.org\/10.1371\/journal.ppat.1012429","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2024,12,26]],"date-time":"2024-12-26T18:47:04Z","timestamp":1735238824000},"score":1,"resource":{"primary":{"URL":"https:\/\/dx.plos.org\/10.1371\/journal.ppat.1012429"}},"subtitle":[],"editor":[{"given":"Audrey Ragan","family":"John","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"editor"}]}],"short-title":[],"issued":{"date-parts":[[2024,12,9]]},"references-count":59,"journal-issue":{"issue":"12","published-online":{"date-parts":[[2024,12,9]]}},"URL":"https:\/\/doi.org\/10.1371\/journal.ppat.1012429","relation":{"new_version":[{"id-type":"doi","id":"10.1371\/journal.ppat.1012429","asserted-by":"object"}]},"ISSN":["1553-7374"],"issn-type":[{"value":"1553-7374","type":"electronic"}],"subject":[],"published":{"date-parts":[[2024,12,9]]}}}