{"id":"https://openalex.org/W2953284201","doi":"https://doi.org/10.1021/ol034212n","title":"Synthesis and Characterization of an N-Acylsulfonamide Inhibitor of Human Asparagine Synthetase","display_name":"Synthesis and Characterization of an N-Acylsulfonamide Inhibitor of Human Asparagine Synthetase","publication_year":2003,"publication_date":"2003-05-09","ids":{"openalex":"https://openalex.org/W2953284201","doi":"https://doi.org/10.1021/ol034212n","mag":"2953284201","pmid":"https://pubmed.ncbi.nlm.nih.gov/12790521"},"language":"en","primary_location":{"id":"doi:10.1021/ol034212n","doi":"https://doi.org/10.1021/ol034212n","is_oa":false,"landing_page_url":"https://doi.org/10.1021/ol034212n","pdf_url":null,"source":{"id":"https://openalex.org/S201989124","display_name":"Organic Letters","issn_l":"1523-7052","issn":["1523-7052","1523-7060"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["cwts-core","dongbi-a","jufo-2","ki-jl-2","medline","norway-2","poland-140","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320006","host_organization_name":"American Chemical Society","host_organization_lineage":["https://openalex.org/P4310320006"],"host_organization_lineage_names":["American Chemical Society"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Organic Letters","raw_type":"journal-article"},"volume":null,"type":"article","indexed_in":["crossref","pubmed"],"open_access":{"is_oa":false,"oa_status":"closed","oa_url":null,"any_repository_has_fulltext":false},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5051286606","display_name":"\u0141ukasz Koroniak","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I33213144","display_name":"University of Florida","ror":"https://ror.org/02y3ad647","country_code":"US","type":"education","lineage":["https://openalex.org/I33213144"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Lukasz Koroniak","raw_affiliation_strings":["Department of Chemistry, University of Florida, Gainesville, Florida 32611"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Chemistry, University of Florida, Gainesville, Florida 32611","institution_ids":["https://openalex.org/I33213144"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5087220087","display_name":"Mihai Ciustea","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I33213144","display_name":"University of Florida","ror":"https://ror.org/02y3ad647","country_code":"US","type":"education","lineage":["https://openalex.org/I33213144"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Mihai Ciustea","raw_affiliation_strings":["Department of Chemistry, University of Florida, Gainesville, Florida 32611"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Chemistry, University of Florida, Gainesville, Florida 32611","institution_ids":["https://openalex.org/I33213144"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5047853402","display_name":"Jemy A. Gutierrez","orcid":"https://orcid.org/0000-0002-5882-0955","observed_orcids":["https://orcid.org/0000-0002-5882-0955"]},"institutions":[{"id":"https://openalex.org/I33213144","display_name":"University of Florida","ror":"https://ror.org/02y3ad647","country_code":"US","type":"education","lineage":["https://openalex.org/I33213144"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Jemy A. Gutierrez","raw_affiliation_strings":["Department of Chemistry, University of Florida, Gainesville, Florida 32611"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Chemistry, University of Florida, Gainesville, Florida 32611","institution_ids":["https://openalex.org/I33213144"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5033047262","display_name":"Nigel G. J. Richards","orcid":"https://orcid.org/0000-0002-0375-0881","observed_orcids":["https://orcid.org/0000-0002-0375-0881"]},"institutions":[{"id":"https://openalex.org/I33213144","display_name":"University of Florida","ror":"https://ror.org/02y3ad647","country_code":"US","type":"education","lineage":["https://openalex.org/I33213144"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Nigel G. J. Richards","raw_affiliation_strings":["Department of Chemistry, University of Florida, Gainesville, Florida 32611"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Department of Chemistry, University of Florida, Gainesville, Florida 32611","institution_ids":["https://openalex.org/I33213144"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":1,"corresponding_author_ids":[],"corresponding_institution_ids":["https://openalex.org/I33213144"],"apc_list":{"value":4500,"currency":"USD","value_usd":4500},"apc_paid":null,"fwci":1.427,"has_fulltext":false,"cited_by_count":48,"citation_normalized_percentile":{"value":0.77388019,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":88,"max":98},"biblio":{"volume":"5","issue":"12","first_page":"2033","last_page":"2036"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T12770","display_name":"Amino Acid Enzymes and Metabolism","score":0.49900001287460327,"subfield":{"id":"https://openalex.org/subfields/1303","display_name":"Biochemistry"},"field":{"id":"https://openalex.org/fields/13","display_name":"Biochemistry, Genetics and Molecular Biology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},"topics":[{"id":"https://openalex.org/T12770","display_name":"Amino Acid Enzymes and Metabolism","score":0.49900001287460327,"subfield":{"id":"https://openalex.org/subfields/1303","display_name":"Biochemistry"},"field":{"id":"https://openalex.org/fields/13","display_name":"Biochemistry, Genetics and Molecular Biology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},{"id":"https://openalex.org/T12827","display_name":"Biochemical and Molecular Research","score":0.4235999882221222,"subfield":{"id":"https://openalex.org/subfields/1312","display_name":"Molecular Biology"},"field":{"id":"https://openalex.org/fields/13","display_name":"Biochemistry, Genetics and Molecular Biology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},{"id":"https://openalex.org/T10274","display_name":"Synthesis and biological activity","score":0.025100000202655792,"subfield":{"id":"https://openalex.org/subfields/1605","display_name":"Organic Chemistry"},"field":{"id":"https://openalex.org/fields/16","display_name":"Chemistry"},"domain":{"id":"https://openalex.org/domains/3","display_name":"Physical Sciences"}}],"keywords":[{"id":"https://openalex.org/keywords/n-acylsulfonamides","display_name":"N-acylsulfonamides","score":0.9100000262260437},{"id":"https://openalex.org/keywords/asparagine-synthetase","display_name":"asparagine synthetase","score":0.9459999799728394},{"id":"https://openalex.org/keywords/enzyme-inhibitors","display_name":"enzyme inhibitors","score":0.8799999952316284},{"id":"https://openalex.org/keywords/hydrogen-bonding","display_name":"hydrogen bonding","score":0.9089999794960022},{"id":"https://openalex.org/keywords/drug-resistant-leukemia","display_name":"drug-resistant leukemia","score":0.7720000147819519},{"id":"https://openalex.org/keywords/asparagine-biosynthesis","display_name":"asparagine biosynthesis","score":0.46799999475479126}],"concepts":[{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.8359723091125488},{"id":"https://openalex.org/C2775895851","wikidata":"https://www.wikidata.org/wiki/Q185906","display_name":"Asparagine","level":3,"score":0.757283091545105},{"id":"https://openalex.org/C2780240386","wikidata":"https://www.wikidata.org/wiki/Q21131459","display_name":"Asparagine synthetase","level":4,"score":0.5948165059089661},{"id":"https://openalex.org/C181199279","wikidata":"https://www.wikidata.org/wiki/Q8047","display_name":"Enzyme","level":2,"score":0.5114644765853882},{"id":"https://openalex.org/C71240020","wikidata":"https://www.wikidata.org/wiki/Q186011","display_name":"Stereochemistry","level":1,"score":0.5074552893638611},{"id":"https://openalex.org/C148898269","wikidata":"https://www.wikidata.org/wiki/Q1108792","display_name":"Kinetics","level":2,"score":0.47753942012786865},{"id":"https://openalex.org/C112887158","wikidata":"https://www.wikidata.org/wiki/Q169324","display_name":"Hydrogen bond","level":3,"score":0.4297240376472473},{"id":"https://openalex.org/C56856141","wikidata":"https://www.wikidata.org/wiki/Q883112","display_name":"Enzyme kinetics","level":4,"score":0.4220890998840332},{"id":"https://openalex.org/C21951064","wikidata":"https://www.wikidata.org/wiki/Q899212","display_name":"Combinatorial chemistry","level":1,"score":0.3789830505847931},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.3611365556716919},{"id":"https://openalex.org/C32909587","wikidata":"https://www.wikidata.org/wiki/Q11369","display_name":"Molecule","level":2,"score":0.22178491950035095},{"id":"https://openalex.org/C41183919","wikidata":"https://www.wikidata.org/wiki/Q423026","display_name":"Active site","level":3,"score":0.21740812063217163},{"id":"https://openalex.org/C178790620","wikidata":"https://www.wikidata.org/wiki/Q11351","display_name":"Organic chemistry","level":1,"score":0.09781280159950256},{"id":"https://openalex.org/C62520636","wikidata":"https://www.wikidata.org/wiki/Q944","display_name":"Quantum mechanics","level":1,"score":0.0},{"id":"https://openalex.org/C121332964","wikidata":"https://www.wikidata.org/wiki/Q413","display_name":"Physics","level":0,"score":0.0}],"mesh":[{"descriptor_ui":"D001217","descriptor_name":"Aspartate-Ammonia Ligase","qualifier_ui":"Q000037","qualifier_name":"antagonists & inhibitors","is_major_topic":true},{"descriptor_ui":"D001217","descriptor_name":"Aspartate-Ammonia Ligase","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D004791","descriptor_name":"Enzyme Inhibitors","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D004791","descriptor_name":"Enzyme Inhibitors","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":true},{"descriptor_ui":"D006801","descriptor_name":"Humans","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D007700","descriptor_name":"Kinetics","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D009943","descriptor_name":"Organophosphorus Compounds","qualifier_ui":"Q000032","qualifier_name":"analysis","is_major_topic":false},{"descriptor_ui":"D009943","descriptor_name":"Organophosphorus Compounds","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D011994","descriptor_name":"Recombinant Proteins","qualifier_ui":"Q000037","qualifier_name":"antagonists & inhibitors","is_major_topic":false},{"descriptor_ui":"D011994","descriptor_name":"Recombinant Proteins","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D013449","descriptor_name":"Sulfonamides","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D013449","descriptor_name":"Sulfonamides","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":true},{"descriptor_ui":"D013449","descriptor_name":"Sulfonamides","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false}],"locations_count":2,"locations":[{"id":"doi:10.1021/ol034212n","doi":"https://doi.org/10.1021/ol034212n","is_oa":false,"landing_page_url":"https://doi.org/10.1021/ol034212n","pdf_url":null,"source":{"id":"https://openalex.org/S201989124","display_name":"Organic Letters","issn_l":"1523-7052","issn":["1523-7052","1523-7060"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["cwts-core","dongbi-a","jufo-2","ki-jl-2","medline","norway-2","poland-140","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320006","host_organization_name":"American Chemical Society","host_organization_lineage":["https://openalex.org/P4310320006"],"host_organization_lineage_names":["American Chemical Society"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Organic Letters","raw_type":"journal-article"},{"id":"pmid:12790521","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/12790521","pdf_url":null,"source":{"id":"https://openalex.org/S4306525036","display_name":"PubMed","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I1299303238","host_organization_name":"National Institutes of Health","host_organization_lineage":["https://openalex.org/I1299303238"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Organic letters","raw_type":"Journal Article"}],"best_oa_location":null,"sustainable_development_goals":[{"score":0.4043000042438507,"display_name":"Good health and well-being","id":"https://metadata.un.org/sdg/3"}],"study_designs":[],"awards":[],"funders":[{"id":"https://openalex.org/F4320307773","display_name":"GlaxoSmithKline","ror":"https://ror.org/01xsqw823"}],"has_content":{"grobid_xml":false,"pdf":false},"content_urls":null,"referenced_works_count":16,"referenced_works":["https://openalex.org/W1976375282","https://openalex.org/W1997966635","https://openalex.org/W2006546058","https://openalex.org/W2012713167","https://openalex.org/W2017572765","https://openalex.org/W2017770922","https://openalex.org/W2029657967","https://openalex.org/W2034703012","https://openalex.org/W2042338355","https://openalex.org/W2046292937","https://openalex.org/W2049817920","https://openalex.org/W2060350094","https://openalex.org/W2069302342","https://openalex.org/W2081604308","https://openalex.org/W2227208022","https://openalex.org/W4248107770"],"related_works":["https://openalex.org/W2011758691","https://openalex.org/W169514160","https://openalex.org/W2074899677","https://openalex.org/W2041683509","https://openalex.org/W2051177012","https://openalex.org/W2029834368","https://openalex.org/W2311774495","https://openalex.org/W2091198719","https://openalex.org/W2076090859","https://openalex.org/W2034703012"],"abstract_inverted_index":{"[structure:":[0],"see":[1],"text]":[2],"The":[3,37],"synthesis":[4],"of":[5,12,27,47,53,63,69,84,92],"N-acylsulfonamide":[6,38,56],"6,":[7],"which":[8],"is":[9,14],"an":[10],"analogue":[11],"beta-aspartyl-AMP,":[13],"described.":[15],"This":[16],"compound":[17],"appears":[18],"to":[19,35],"be":[20],"the":[21,61,67,70,74,79,82,90],"first":[22],"and":[23,51],"only":[24],"potent":[25],"inhibitor":[26,72],"human":[28],"asparagine":[29],"synthetase":[30],"that":[31],"has":[32,58],"been":[33],"described":[34],"date.":[36],"6":[39],"exhibits":[40],"slow-onset":[41],"inhibition":[42],"kinetics,":[43],"with":[44,73,87],"a":[45],"K(i)":[46],"728":[48],"nM.":[49],"Preparation":[50],"characterization":[52],"two":[54],"additional":[55],"analogues":[57],"also":[59],"demonstrated":[60],"importance":[62],"hydrogen-bonding":[64],"interactions":[65],"in":[66,89],"recognition":[68],"AS":[71],"enzyme.":[75],"These":[76],"observations":[77],"provide":[78],"basis":[80],"for":[81],"discovery":[83],"new":[85],"compounds":[86],"application":[88],"treatment":[91],"drug-resistant":[93],"leukemia.":[94]},"counts_by_year":[{"year":2026,"cited_by_count":1},{"year":2025,"cited_by_count":3},{"year":2024,"cited_by_count":1},{"year":2023,"cited_by_count":1},{"year":2022,"cited_by_count":3},{"year":2021,"cited_by_count":1},{"year":2020,"cited_by_count":2},{"year":2019,"cited_by_count":6},{"year":2018,"cited_by_count":3},{"year":2017,"cited_by_count":3},{"year":2016,"cited_by_count":1},{"year":2013,"cited_by_count":3},{"year":2012,"cited_by_count":1}],"updated_date":"2026-10-31T12:09:11.096373","created_date":"2019-06-27T00:00:00"}