{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,31]],"date-time":"2026-10-31T01:23:55Z","timestamp":1793409835758,"version":"4.5.0"},"reference-count":71,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2025,7,1]],"date-time":"2025-07-01T00:00:00Z","timestamp":1751328000000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2025,7,1]],"date-time":"2025-07-01T00:00:00Z","timestamp":1751328000000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2025,7,1]],"date-time":"2025-07-01T00:00:00Z","timestamp":1751328000000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-017"},{"start":{"date-parts":[[2025,7,1]],"date-time":"2025-07-01T00:00:00Z","timestamp":1751328000000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-037"},{"start":{"date-parts":[[2025,7,1]],"date-time":"2025-07-01T00:00:00Z","timestamp":1751328000000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-012"},{"start":{"date-parts":[[2025,7,1]],"date-time":"2025-07-01T00:00:00Z","timestamp":1751328000000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-029"},{"start":{"date-parts":[[2025,7,1]],"date-time":"2025-07-01T00:00:00Z","timestamp":1751328000000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-004"}],"funder":[{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["22177140"],"award-info":[{"award-number":["22177140"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["22207133"],"award-info":[{"award-number":["22207133"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100012165","name":"Key Technologies Research and Development Program","doi-asserted-by":"publisher","award":["2023YFF1204902"],"award-info":[{"award-number":["2023YFF1204902"]}],"id":[{"id":"10.13039\/501100012165","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100009659","name":"Guangzhou Medical University","doi-asserted-by":"publisher","award":["202301-303"],"award-info":[{"award-number":["202301-303"]}],"id":[{"id":"10.13039\/100009659","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100017688","name":"Guangdong Provincial Key Laboratory of Construction Foundation","doi-asserted-by":"publisher","award":["2023B1212060022"],"award-info":[{"award-number":["2023B1212060022"]}],"id":[{"id":"10.13039\/501100017688","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100021171","name":"Basic and Applied Basic Research Foundation of Guangdong Province","doi-asserted-by":"publisher","award":["2022B1515130008"],"award-info":[{"award-number":["2022B1515130008"]}],"id":[{"id":"10.13039\/501100021171","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100021171","name":"Basic and Applied Basic Research Foundation of Guangdong Province","doi-asserted-by":"publisher","award":["2023A1515012453"],"award-info":[{"award-number":["2023A1515012453"]}],"id":[{"id":"10.13039\/501100021171","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100021171","name":"Basic and Applied Basic Research Foundation of Guangdong Province","doi-asserted-by":"publisher","award":["2023A1515012936"],"award-info":[{"award-number":["2023A1515012936"]}],"id":[{"id":"10.13039\/501100021171","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100021171","name":"Basic and Applied Basic Research Foundation of Guangdong Province","doi-asserted-by":"publisher","award":["2023B1515040006"],"award-info":[{"award-number":["2023B1515040006"]}],"id":[{"id":"10.13039\/501100021171","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100009666","name":"Salt Science Research Foundation","doi-asserted-by":"publisher","id":[{"id":"10.13039\/100009666","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100012166","name":"National Key Research and Development Program of China","doi-asserted-by":"publisher","id":[{"id":"10.13039\/501100012166","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["European Journal of Medicinal Chemistry"],"published-print":{"date-parts":[[2025,7]]},"DOI":"10.1016\/j.ejmech.2025.117647","type":"journal-article","created":{"date-parts":[[2025,4,17]],"date-time":"2025-04-17T06:22:52Z","timestamp":1744870972000},"page":"117647","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":8,"special_numbering":"C","title":["Development of potent inhibitors targeting bacterial prolyl-tRNA synthetase through fluorine scanning-directed activity tuning"],"prefix":"10.1016","volume":"291","author":[{"given":"Zhiteng","family":"Luo","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Haipeng","family":"Qiu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xiaoying","family":"Peng","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Qingyun","family":"Tan","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Bingyi","family":"Chen","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Qiong","family":"Gu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hongwei","family":"Liu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9675-5007","authenticated-orcid":false,"given":"Huihao","family":"Zhou","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"key":"10.1016\/j.ejmech.2025.117647_bib1","doi-asserted-by":"crossref","first-page":"629","DOI":"10.1038\/s41573-019-0026-3","article-title":"Aminoacyl-tRNA synthetases as therapeutic targets","volume":"18","author":"Kwon","year":"2019","journal-title":"Nat. Rev. Drug Discov."},{"key":"10.1016\/j.ejmech.2025.117647_bib2","doi-asserted-by":"crossref","first-page":"111","DOI":"10.1146\/annurev-micro-032421-121210","article-title":"Targeting aminoacyl tRNA synthetases for antimalarial drug development","volume":"77","author":"Xie","year":"2023","journal-title":"Annu. Rev. Microbiol."},{"key":"10.1016\/j.ejmech.2025.117647_bib3","doi-asserted-by":"crossref","first-page":"4447","DOI":"10.1021\/jm0603724","article-title":"Discovery of a new boron-containing antifungal agent, 5-Fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2690), for the potential treatment of onychomycosis","volume":"49","author":"Baker","year":"2006","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib4","doi-asserted-by":"crossref","first-page":"1671","DOI":"10.1517\/13543784.17.11.1671","article-title":"New agents for clostridium difficile-associated disease","volume":"17","author":"Guiles","year":"2008","journal-title":"Expet Opin. Invest. Drugs"},{"key":"10.1016\/j.ejmech.2025.117647_bib5","doi-asserted-by":"crossref","first-page":"8011","DOI":"10.1021\/acs.jmedchem.7b00631","article-title":"Discovery of a potent and specific M. tuberculosis leucyl-tRNA synthetase inhibitor: (S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H)-ol (GSK656)","volume":"60","author":"Li","year":"2017","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib6","doi-asserted-by":"crossref","first-page":"8346","DOI":"10.1016\/S0140-6736(83)90358-6","article-title":"Pseudomonic acid: a new topical antimicrobial agent","volume":"322","author":"Wuite","year":"1983","journal-title":"Lancet"},{"key":"10.1016\/j.ejmech.2025.117647_bib7","doi-asserted-by":"crossref","first-page":"1511","DOI":"10.1016\/j.str.2006.08.007","article-title":"Structures of two bacterial prolyl-tRNA synthetases with and without a cis-editing domain","volume":"14","author":"Crepin","year":"2006","journal-title":"Structure"},{"key":"10.1016\/j.ejmech.2025.117647_bib8","doi-asserted-by":"crossref","first-page":"121","DOI":"10.1038\/nature11774","article-title":"ATP-directed capture of bioactive herbal-based medicine on human tRNA synthetase","volume":"494","author":"Zhou","year":"2013","journal-title":"Nature"},{"key":"10.1016\/j.ejmech.2025.117647_bib9","doi-asserted-by":"crossref","first-page":"34","DOI":"10.1021\/acsinfecdis.6b00078","article-title":"Biochemical and structural characterization of selective allosteric inhibitors of the plasmodium falciparum drug target, prolyl-tRNA-synthetase","volume":"3","author":"Hewitt","year":"2017","journal-title":"ACS Infect. Dis."},{"key":"10.1016\/j.ejmech.2025.117647_bib10","doi-asserted-by":"crossref","DOI":"10.1126\/scitranslmed.aaa3575","article-title":"The cytoplasmic prolyl-tRNA synthetase of the malaria parasite is a dual-stage target of febrifugine and its analogs","volume":"7","author":"Herman","year":"2015","journal-title":"Sci. Transl. Med."},{"key":"10.1016\/j.ejmech.2025.117647_bib11","doi-asserted-by":"crossref","first-page":"4976","DOI":"10.1038\/s41467-022-32630-4","article-title":"Elucidating the path to plasmodium prolyl-tRNA synthetase inhibitors that overcome halofuginone resistance","volume":"13","author":"Tye","year":"2022","journal-title":"Nat. Commun."},{"key":"10.1016\/j.ejmech.2025.117647_bib12","article-title":"Quinazolinone alkaloid febrifugine and its analogues to control phytopathogenic diseases caused by oomycete fungi","volume":"13","author":"Fehr","year":"2022","journal-title":"Eur. J. Org. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib13","doi-asserted-by":"crossref","first-page":"15840","DOI":"10.1021\/acs.jmedchem.2c01496","article-title":"Structure-guided design of halofuginone derivatives as ATP-aided inhibitors against bacterial prolyl-tRNA synthetase","volume":"65","author":"Cheng","year":"2022","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib14","doi-asserted-by":"crossref","first-page":"648","DOI":"10.1016\/j.bbrc.2017.01.045","article-title":"Prolyl-tRNA synthetase inhibition promotes cell death in SK-MEL-2 cells through GCN2-ATF4 pathway activation","volume":"488","author":"Arita","year":"2017","journal-title":"Biochem. Biophys. Res. Commun."},{"key":"10.1016\/j.ejmech.2025.117647_bib15","doi-asserted-by":"crossref","DOI":"10.15252\/emmm.202216940","article-title":"Control of fibrosis with enhanced safety via asymmetric inhibition of prolyl-tRNA synthetase 1","volume":"15","author":"Yoon","year":"2023","journal-title":"EMBO Mol. Med."},{"key":"10.1016\/j.ejmech.2025.117647_bib16","doi-asserted-by":"crossref","first-page":"3907","DOI":"10.1038\/s41467-021-24156-y","article-title":"A high-throughput screen for TMPRSS2 expression identifies FDA-approved compounds that can limit SARS-CoV-2 entry","volume":"12","author":"Chen","year":"2021","journal-title":"Nat. Commun."},{"key":"10.1016\/j.ejmech.2025.117647_bib17","doi-asserted-by":"crossref","first-page":"393","DOI":"10.1016\/j.bbrc.2017.05.064","article-title":"Discovery of a novel prolyl-tRNA synthetase inhibitor and elucidation of its binding mode to the ATP site in complex with l-proline","volume":"488","author":"Adachi","year":"2017","journal-title":"Biochem. Biophys. Res. Commun."},{"key":"10.1016\/j.ejmech.2025.117647_bib18","doi-asserted-by":"crossref","first-page":"1680","DOI":"10.1021\/acsinfecdis.1c00020","article-title":"Repositioning and characterization of 1-(pyridin-4-yl)pyrrolidin-2-one derivatives as plasmodium cytoplasmic prolyl-tRNA synthetase inhibitors","volume":"7","author":"Okaniwa","year":"2021","journal-title":"ACS Infect. Dis."},{"key":"10.1016\/j.ejmech.2025.117647_bib19","doi-asserted-by":"crossref","first-page":"3803","DOI":"10.3390\/ijms21113803","article-title":"Identification of selective novel hits against plasmodium falciparum prolyl tRNA synthetase active site and a predicted allosteric site using in silico approaches","volume":"27","author":"Nyamai","year":"2020","journal-title":"Int. J. Mol. Sci."},{"key":"10.1016\/j.ejmech.2025.117647_bib20","doi-asserted-by":"crossref","first-page":"3020","DOI":"10.1021\/jm8000746","article-title":"Aminoacyl-tRNA synthetase inhibitors as potent and synergistic immunosuppressants","volume":"51","author":"Van de Vijver","year":"2008","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib21","doi-asserted-by":"crossref","first-page":"273","DOI":"10.1006\/bioo.1996.0025","article-title":"Synthesis and aminoacyl-tRNA synthetase inhibitory activity of prolyl adenylate analogs","volume":"24","author":"Heacock","year":"1996","journal-title":"Bioorg. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib22","doi-asserted-by":"crossref","first-page":"4821","DOI":"10.1128\/AAC.49.12.4821-4833.2005","article-title":"Prospects for aminoacyl-tRNA synthetase inhibitors as new antimicrobial agents","volume":"49","author":"Hurdle","year":"2005","journal-title":"Antimicrob. Agents Chemother."},{"key":"10.1016\/j.ejmech.2025.117647_bib23","doi-asserted-by":"crossref","DOI":"10.1126\/sciadv.adf1027","article-title":"The binding mode of orphan glycyl-tRNA synthetase with tRNA supports the synthetase classification and reveals large domain movements","volume":"9","author":"Han","year":"2023","journal-title":"Sci. Adv."},{"key":"10.1016\/j.ejmech.2025.117647_bib24","doi-asserted-by":"crossref","first-page":"10106","DOI":"10.1093\/nar\/gkab707","article-title":"X-shaped structure of bacterial heterotetrameric tRNA synthetase suggests cryptic prokaryote functions and a rationale for synthetase classifications","volume":"49","author":"Ju","year":"2021","journal-title":"Nucleic Acids Res."},{"key":"10.1016\/j.ejmech.2025.117647_bib25","doi-asserted-by":"crossref","first-page":"689","DOI":"10.1101\/gr.9.8.689","article-title":"Evolution of aminoacyl-tRNA synthetases--analysis of unique domain architectures and phylogenetic trees reveals a complex history of horizontal gene transfer events","volume":"9","author":"Wolf","year":"1999","journal-title":"Genome Res."},{"key":"10.1016\/j.ejmech.2025.117647_bib26","doi-asserted-by":"crossref","first-page":"12256","DOI":"10.1002\/anie.201303207","article-title":"Profound methyl effects in drug discovery and a call for new C-H methylation reactions","volume":"52","author":"Sch\u00f6nherr","year":"2013","journal-title":"Angew Chem. Int. Ed. Engl."},{"key":"10.1016\/j.ejmech.2025.117647_bib27","doi-asserted-by":"crossref","first-page":"5305","DOI":"10.1021\/acs.jmedchem.2c02015","article-title":"\"Magic chloro\": profound effects of the chlorine atom in drug discovery","volume":"66","author":"Chiodi","year":"2023","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib28","doi-asserted-by":"crossref","first-page":"5822","DOI":"10.1021\/acs.jmedchem.7b01788","article-title":"Fluorine and fluorinated motifs in the design and application of bioisosteres for drug design","volume":"61","author":"Meanwell","year":"2018","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib29","doi-asserted-by":"crossref","first-page":"4359","DOI":"10.1021\/jm800219f","article-title":"The many roles for fluorine in medicinal chemistry","volume":"51","author":"K Hagmann","year":"2008","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib30","doi-asserted-by":"crossref","first-page":"8315","DOI":"10.1021\/acs.jmedchem.5b00258","article-title":"Applications of fluorine in medicinal chemistry","volume":"58","author":"Gillis","year":"2015","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib31","doi-asserted-by":"crossref","first-page":"23068","DOI":"10.1002\/anie.202103211","article-title":"Modulating the efficacy of carbonic anhydrase inhibitors through fluorine substitution","volume":"60","author":"Berrino","year":"2021","journal-title":"Angew. Chem. Int. In Engl."},{"key":"10.1016\/j.ejmech.2025.117647_bib32","doi-asserted-by":"crossref","first-page":"6315","DOI":"10.1021\/acs.jmedchem.9b01877","article-title":"Metabolic and pharmaceutical aspects of fluorinated compounds","volume":"63","author":"Johnson","year":"2020","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib33","doi-asserted-by":"crossref","first-page":"1261","DOI":"10.1080\/17460441.2021.1933427","article-title":"Applications of fluorine to the construction of bioisosteric elements for the purposes of novel drug discovery","volume":"16","author":"Richardson","year":"2021","journal-title":"Expet Opin. Drug Discov."},{"key":"10.1016\/j.ejmech.2025.117647_bib34","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2023.115476","article-title":"Highlights on U.S. FDA-approved fluorinated drugs over the past five years (2018-2022)","volume":"256","author":"Ali","year":"2023","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib35","doi-asserted-by":"crossref","DOI":"10.1016\/j.ejmech.2024.116446","article-title":"Fluorine in the pharmaceutical industry: synthetic approaches and application of clinically approved fluorine-enriched anti-infectious medications","volume":"271","author":"Niu","year":"2024","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib36","doi-asserted-by":"crossref","first-page":"777","DOI":"10.4155\/fmc.09.65","article-title":"Fluorine in medicinal chemistry: a century of progress and a 60-year retrospective of selected highlights","volume":"1","author":"Filler","year":"2009","journal-title":"Future Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib37","doi-asserted-by":"crossref","first-page":"473","DOI":"10.1016\/j.ejmech.2017.11.055","article-title":"A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: design, synthesis, molecular modelling, and biological evaluation","volume":"143","author":"Naret","year":"2018","journal-title":"Eur. J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib38","doi-asserted-by":"crossref","first-page":"2507","DOI":"10.1002\/anie.200351268","article-title":"A fluorine scan of thrombin inhibitors to map the fluorophilicity\/fluorophobicity of an enzyme active site: evidence for C-F\u2026C=O interactions","volume":"42","author":"A Olsen","year":"2003","journal-title":"Angew Chem. Int. Ed. Engl."},{"key":"10.1016\/j.ejmech.2025.117647_bib39","doi-asserted-by":"crossref","first-page":"1205","DOI":"10.1002\/cmdc.200600124","article-title":"Mapping the fluorophilicity of a hydrophobic pocket: synthesis and biological evaluation of tricyclic thrombin inhibitors directing fluorinated alkyl groups into the p pocket","volume":"1","author":"Hoffmann-R\u00f6der","year":"2006","journal-title":"ChemMedChem"},{"key":"10.1016\/j.ejmech.2025.117647_bib40","doi-asserted-by":"crossref","first-page":"3980","DOI":"10.1021\/jm400225m","article-title":"\u03b2-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease","volume":"56","author":"Hilpert","year":"2013","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib41","doi-asserted-by":"crossref","first-page":"1059","DOI":"10.1021\/ml4002419","article-title":"Fluorine scanning by nonselective fluorination: enhancing Raf\/MEK inhibition while keeping physicochemical properties","volume":"4","author":"Hyohdoh","year":"2013","journal-title":"ACS Med. Chem. Lett."},{"key":"10.1016\/j.ejmech.2025.117647_bib42","doi-asserted-by":"crossref","first-page":"367","DOI":"10.1016\/j.bmcl.2014.11.030","article-title":"Finding the perfect spot for fluorine: improving potency up to 40-fold during a rational fluorine scan of a Bruton's Tyrosine Kinase (BTK) inhibitor scaffold","volume":"25","author":"Lou","year":"2015","journal-title":"Bioorg. Med. Chem. Lett."},{"key":"10.1016\/j.ejmech.2025.117647_bib43","doi-asserted-by":"crossref","first-page":"1748","DOI":"10.1021\/jm301756m","article-title":"Identification of bacteria-selective threonyl-tRNA synthetase substrate inhibitors by structure-based design","volume":"56","author":"Teng","year":"2013","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib44","doi-asserted-by":"crossref","first-page":"5800","DOI":"10.1021\/acs.jmedchem.2c00134","article-title":"Design, synthesis, and proof-of-concept of triple-site inhibitors against aminoacyl-tRNA synthetases","volume":"65","author":"Cai","year":"2022","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib45","doi-asserted-by":"crossref","first-page":"5310","DOI":"10.1039\/c3ob40236c","article-title":"Discovery of N-(4-sulfamoylphenyl)thioureas as Trypanosoma brucei leucyl-tRNA synthetase inhibitors","volume":"11","author":"Zhang","year":"2013","journal-title":"Org. Biomol. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib46","doi-asserted-by":"crossref","first-page":"84","DOI":"10.1021\/acsmedchemlett.7b00374","article-title":"N-leucinyl benzenesulfonamides as structurally simplified leucyl-tRNA synthetase inhibitors","volume":"9","author":"H Charlton","year":"2018","journal-title":"ACS Med. Chem. Lett."},{"key":"10.1016\/j.ejmech.2025.117647_bib47","doi-asserted-by":"crossref","DOI":"10.3390\/ijms232315095","article-title":"Structural basis of cysteine ligase mshC inhibition by cysteinyl-sulfonamides","volume":"23","author":"Pang","year":"2022","journal-title":"Int. J. Mol. Sci."},{"key":"10.1016\/j.ejmech.2025.117647_bib48","doi-asserted-by":"crossref","first-page":"73","DOI":"10.1007\/s00239-021-10043-z","article-title":"Amino acid specificity of ancestral aminoacyl-tRNA synthetase prior to the last universal common ancestor","volume":"90","author":"Furukawa","year":"2022","journal-title":"J. Mol. Evol."},{"key":"10.1016\/j.ejmech.2025.117647_bib49","doi-asserted-by":"crossref","first-page":"9703","DOI":"10.1021\/acs.jmedchem.9b01131","article-title":"Structure-guided enhancement of selectivity of chemical probe inhibitors targeting bacterial seryl-tRNA synthetase","volume":"62","author":"Cain","year":"2019","journal-title":"J. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib50","doi-asserted-by":"crossref","first-page":"669","DOI":"10.1039\/c1md00093d","article-title":"Intramolecular hydrogen bonding to improve membrane permeability and absorption in beyond rule of five chemical space","volume":"2","author":"Alex","year":"2011","journal-title":"Med. Chem. Commun."},{"key":"10.1016\/j.ejmech.2025.117647_bib51","doi-asserted-by":"crossref","first-page":"38","DOI":"10.3762\/bjoc.6.38","article-title":"The C-F bond as a conformational tool in organic and biological chemistry","volume":"6","author":"Hunter","year":"2010","journal-title":"Beilstein J. Org. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib52","doi-asserted-by":"crossref","first-page":"777","DOI":"10.1021\/ja005542v","article-title":"Conformational stability of collagen relies on a stereoelectronic effect","volume":"123","author":"Bretscher","year":"2001","journal-title":"J. Am. Chem. Soc."},{"key":"10.1016\/j.ejmech.2025.117647_bib53","doi-asserted-by":"crossref","first-page":"559","DOI":"10.1073\/pnas.0909592107","article-title":"Stereoelectronic and steric effects in side chains preorganize a protein main chain","volume":"107","author":"Shoulders","year":"2010","journal-title":"Proc. Natl. Acad. Sci. U. S. A"},{"key":"10.1016\/j.ejmech.2025.117647_bib54","doi-asserted-by":"crossref","first-page":"8831","DOI":"10.1021\/acs.joc.7b00803","article-title":"Peptidyl-prolyl model study: how does the electronic effect influence the amide bond conformation?","volume":"82","author":"Mykhailiuk","year":"2017","journal-title":"J. Org. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib55","doi-asserted-by":"crossref","first-page":"6540","DOI":"10.1016\/j.bmc.2009.08.010","article-title":"Synthesis and biological evaluation of 4-fluoroproline and 4-fluoropyrrolidine-2-acetic acid derivatives as new GABA uptake inhibitors","volume":"17","author":"Zhuang","year":"2009","journal-title":"Bioorg. Med. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib56","doi-asserted-by":"crossref","first-page":"186","DOI":"10.1038\/nprot.2006.28","article-title":"Isothermal titration calorimetry to determine association constants for high-affinity ligands","volume":"1","author":"Velazquez-Campoy","year":"2006","journal-title":"Nat. Protoc."},{"key":"10.1016\/j.ejmech.2025.117647_bib57","doi-asserted-by":"crossref","first-page":"260","DOI":"10.1006\/abio.1999.4402","article-title":"Exact analysis of competition ligand binding by displacement isothermal titration calorimetry","volume":"277","author":"Sigurskjold","year":"2000","journal-title":"Anal. Biochem."},{"key":"10.1016\/j.ejmech.2025.117647_bib58","doi-asserted-by":"crossref","first-page":"311","DOI":"10.1038\/nchembio.790","article-title":"Halofuginone and other febrifugine derivatives inhibit prolyl-tRNA synthetase","volume":"8","author":"Keller","year":"2012","journal-title":"Nat. Chem. Biol."},{"key":"10.1016\/j.ejmech.2025.117647_bib59","doi-asserted-by":"crossref","first-page":"511","DOI":"10.1186\/s13059-014-0511-2","article-title":"A genomic and evolutionary approach reveals non-genetic drug resistance in malaria","volume":"15","author":"Herman","year":"2014","journal-title":"Genome Biol."},{"key":"10.1016\/j.ejmech.2025.117647_bib60","doi-asserted-by":"crossref","first-page":"515","DOI":"10.1021\/acsinfecdis.8b00363","article-title":"The adaptive proline response in P. falciparum is independent of PfeIK1 and eIF2\u03b1 signaling","volume":"5","author":"Fagbami","year":"2019","journal-title":"ACS Infect. Dis."},{"key":"10.1016\/j.ejmech.2025.117647_bib61","doi-asserted-by":"crossref","first-page":"4755","DOI":"10.1093\/nar\/gkac285","article-title":"Fragment screening and structural analyses highlight the ATP-assisted ligand binding for inhibitor discovery against type 1 methionyl-tRNA synthetase","volume":"50","author":"Yi","year":"2022","journal-title":"Nucleic Acids Res."},{"key":"10.1016\/j.ejmech.2025.117647_bib62","doi-asserted-by":"crossref","first-page":"27862","DOI":"10.1074\/jbc.M605856200","article-title":"Pre-transfer editing by class II prolyl-tRNA synthetase: role of aminoacylation active site in \"selective release\" of noncognate amino acids","volume":"281","author":"Hati","year":"2006","journal-title":"J. Biol. Chem."},{"key":"10.1016\/j.ejmech.2025.117647_bib63","doi-asserted-by":"crossref","first-page":"307","DOI":"10.1016\/S0076-6879(97)76066-X","article-title":"Processing of X-ray diffraction data collected in oscillation mode","volume":"276","author":"Otwinowski","year":"1997","journal-title":"Methods Enzymol."},{"key":"10.1016\/j.ejmech.2025.117647_bib64","doi-asserted-by":"crossref","first-page":"859","DOI":"10.1107\/S0907444906019949","article-title":"HKL-3000: the integration of data reduction and structure solution--from diffraction images to an initial model in minute","volume":"62","author":"Minor","year":"2006","journal-title":"Acta. Crystallogr. D. Biol. Crystallogr."},{"key":"10.1016\/j.ejmech.2025.117647_bib65","doi-asserted-by":"crossref","first-page":"293","DOI":"10.1107\/S0907444911007773","article-title":"Data processing and analysis with the autoPROC toolbox","volume":"67","author":"Vonrhein","year":"2011","journal-title":"Acta. Crystallogr. D. Biol. Crystallogr."},{"key":"10.1016\/j.ejmech.2025.117647_bib66","doi-asserted-by":"crossref","first-page":"727","DOI":"10.1002\/pro.3579","article-title":"Characterization and structure determination of prolyl-tRNA synthetase from Pseudomonas aeruginosa and development as a screening platform","volume":"28","author":"Pena","year":"2019","journal-title":"Protein Sci."},{"key":"10.1016\/j.ejmech.2025.117647_bib67","doi-asserted-by":"crossref","first-page":"2281","DOI":"10.1038\/s41467-017-02201-z","article-title":"Double mimicry evades tRNA synthetase editing by toxic vegetable-sourced non-proteinogenic amino acid","volume":"8","author":"Song","year":"2017","journal-title":"Nat. Commun."},{"key":"10.1016\/j.ejmech.2025.117647_bib68","doi-asserted-by":"crossref","first-page":"22","DOI":"10.1107\/S0907444909042589","article-title":"Acta. Crystallogr. Molecular replacement with MOLREP","volume":"66","author":"Vagin","year":"2010","journal-title":"Acta. Crystallogr. D. Biol. Crystallogr."},{"key":"10.1016\/j.ejmech.2025.117647_bib69","doi-asserted-by":"crossref","first-page":"486","DOI":"10.1107\/S0907444910007493","article-title":"Features and development of coot","volume":"66","author":"Emsley","year":"2010","journal-title":"Acta. Crystallogr. D. Biol. Crystallogr."},{"key":"10.1016\/j.ejmech.2025.117647_bib70","doi-asserted-by":"crossref","first-page":"355","DOI":"10.1107\/S0907444911001314","article-title":"REFMAC5 for the refinement of macromolecular crystal structures","volume":"67","author":"Murshudov","year":"2011","journal-title":"Acta. Crystallogr. D. Biol. Crystallogr."},{"key":"10.1016\/j.ejmech.2025.117647_bib71","doi-asserted-by":"crossref","first-page":"293","DOI":"10.1002\/pro.3330","article-title":"MolProbity: more and better reference data for improved all-atom structure validation","volume":"27","author":"Williams","year":"2018","journal-title":"Protein Sci."}],"container-title":["European Journal of Medicinal Chemistry"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S022352342500412X?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S022352342500412X?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2026,5,6]],"date-time":"2026-05-06T04:51:09Z","timestamp":1778043069000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S022352342500412X"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2025,7]]},"references-count":71,"alternative-id":["S022352342500412X"],"URL":"https:\/\/doi.org\/10.1016\/j.ejmech.2025.117647","relation":{},"ISSN":["0223-5234"],"issn-type":[{"value":"0223-5234","type":"print"}],"subject":[],"published":{"date-parts":[[2025,7]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Development of potent inhibitors targeting bacterial prolyl-tRNA synthetase through fluorine scanning-directed activity tuning","name":"articletitle","label":"Article Title"},{"value":"European Journal of Medicinal Chemistry","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.ejmech.2025.117647","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2025 Elsevier Masson SAS. All rights are reserved, including those for text and data mining, AI training, and similar technologies.","name":"copyright","label":"Copyright"}],"article-number":"117647"}}