{"id":"https://openalex.org/W2540299541","doi":null,"title":"The biological evaluation of inhibitors of the Keap1-Nrf2 protein-protein interaction","display_name":"The biological evaluation of inhibitors of the Keap1-Nrf2 protein-protein interaction","publication_year":2015,"publication_date":"2015-01-01","ids":{"openalex":"https://openalex.org/W2540299541","mag":"2540299541"},"language":"en","primary_location":{"id":"pmh:oai:eprints.ucl.ac.uk.OAI2:1473105","doi":null,"is_oa":false,"landing_page_url":"https://discovery.ucl.ac.uk/id/eprint/1473105/","pdf_url":null,"source":{"id":"https://openalex.org/S4306400024","display_name":"UCL Discovery (University College London)","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I45129253","host_organization_name":"University College London","host_organization_lineage":["https://openalex.org/I45129253"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":"Doctoral thesis, UCL (University College London).","raw_type":"Thesis"},"volume":null,"type":"dissertation","is_traditional":true,"indexed_in":[],"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/A5040364995","display_name":"Marjolein Schaap","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":true,"raw_author_name":"Schaap","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]}],"institutions":[],"countries_distinct_count":0,"institutions_distinct_count":0,"corresponding_author_ids":["https://openalex.org/A5040364995"],"corresponding_institution_ids":[],"apc_list":null,"apc_paid":null,"fwci":null,"has_fulltext":false,"cited_by_count":0,"citation_normalized_percentile":null,"cited_by_percentile_year":null,"biblio":{"volume":null,"issue":null,"first_page":null,"last_page":null},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T11332","display_name":"Genomics, phytochemicals, and oxidative stress","score":1.0,"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"}},"topics":[{"id":"https://openalex.org/T11332","display_name":"Genomics, phytochemicals, and oxidative stress","score":1.0,"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/T12356","display_name":"Bioactive Compounds and Antitumor Agents","score":0.0,"subfield":{"id":"https://openalex.org/subfields/3005","display_name":"Toxicology"},"field":{"id":"https://openalex.org/fields/30","display_name":"Pharmacology, Toxicology and Pharmaceutics"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},{"id":"https://openalex.org/T11884","display_name":"Redox biology and oxidative stress","score":0.0,"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"}}],"keywords":[{"id":"https://openalex.org/keywords/keap1-nrf2-pathway","display_name":"Nrf2/Keap1 pathway","score":0.9620000123977661},{"id":"https://openalex.org/keywords/protein-protein-interaction-inhibitors","display_name":"protein-protein interaction inhibitors","score":0.9240000247955322},{"id":"https://openalex.org/keywords/nrf2-inducers","display_name":"Nrf2 inducers","score":0.7699999809265137},{"id":"https://openalex.org/keywords/oxidative-stress","display_name":"oxidative stress","score":0.6779999732971191},{"id":"https://openalex.org/keywords/nqo1-induction","display_name":"NQO1 induction","score":0.699999988079071},{"id":"https://openalex.org/keywords/sulforaphane","display_name":"sulforaphane","score":0.7590000033378601},{"id":"https://openalex.org/keywords/1-2-3-triazole-derivatives","display_name":"1,2,3-triazole derivatives","score":0.9779999852180481},{"id":"https://openalex.org/keywords/chemoprevention","display_name":"chemoprevention","score":0.7680000066757202},{"id":"https://openalex.org/keywords/nrf2-translocation","display_name":"Nrf2 nuclear translocation","score":0.5950000286102295}],"concepts":[{"id":"https://openalex.org/C2776529522","wikidata":"https://www.wikidata.org/wiki/Q18034700","display_name":"KEAP1","level":4,"score":0.9033832550048828},{"id":"https://openalex.org/C2780841255","wikidata":"https://www.wikidata.org/wiki/Q424489","display_name":"Sulforaphane","level":2,"score":0.7386711239814758},{"id":"https://openalex.org/C2225953","wikidata":"https://www.wikidata.org/wiki/Q1661899","display_name":"Inducer","level":3,"score":0.5793007016181946},{"id":"https://openalex.org/C11804247","wikidata":"https://www.wikidata.org/wiki/Q896177","display_name":"Protein\u2013protein interaction","level":2,"score":0.5709941983222961},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.5580381751060486},{"id":"https://openalex.org/C96305047","wikidata":"https://www.wikidata.org/wiki/Q367473","display_name":"F\u00f6rster resonance energy transfer","level":3,"score":0.5456952452659607},{"id":"https://openalex.org/C86339819","wikidata":"https://www.wikidata.org/wiki/Q407384","display_name":"Transcription factor","level":3,"score":0.5426831841468811},{"id":"https://openalex.org/C202751555","wikidata":"https://www.wikidata.org/wiki/Q221681","display_name":"In vitro","level":2,"score":0.49115487933158875},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.4781292974948883},{"id":"https://openalex.org/C161624437","wikidata":"https://www.wikidata.org/wiki/Q1988322","display_name":"Small molecule","level":2,"score":0.45045050978660583},{"id":"https://openalex.org/C183786373","wikidata":"https://www.wikidata.org/wiki/Q5964993","display_name":"Signal transducing adaptor protein","level":3,"score":0.4471118450164795},{"id":"https://openalex.org/C95444343","wikidata":"https://www.wikidata.org/wiki/Q7141","display_name":"Cell biology","level":1,"score":0.3672780394554138},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.30634525418281555},{"id":"https://openalex.org/C62478195","wikidata":"https://www.wikidata.org/wiki/Q828130","display_name":"Signal transduction","level":2,"score":0.21305370330810547},{"id":"https://openalex.org/C91881484","wikidata":"https://www.wikidata.org/wiki/Q191807","display_name":"Fluorescence","level":2,"score":0.18515914678573608},{"id":"https://openalex.org/C104317684","wikidata":"https://www.wikidata.org/wiki/Q7187","display_name":"Gene","level":2,"score":0.12418022751808167},{"id":"https://openalex.org/C121332964","wikidata":"https://www.wikidata.org/wiki/Q413","display_name":"Physics","level":0,"score":0.0},{"id":"https://openalex.org/C62520636","wikidata":"https://www.wikidata.org/wiki/Q944","display_name":"Quantum mechanics","level":1,"score":0.0}],"mesh":[],"locations_count":3,"locations":[{"id":"pmh:oai:eprints.ucl.ac.uk.OAI2:1473105","doi":null,"is_oa":false,"landing_page_url":"https://discovery.ucl.ac.uk/id/eprint/1473105/","pdf_url":null,"source":{"id":"https://openalex.org/S4306400024","display_name":"UCL Discovery (University College London)","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I45129253","host_organization_name":"University College London","host_organization_lineage":["https://openalex.org/I45129253"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":"Doctoral thesis, UCL (University College London).","raw_type":"Thesis"},{"id":"mag:2540299541","doi":null,"is_oa":false,"landing_page_url":"https://discovery.ucl.ac.uk/1473105/","pdf_url":null,"source":{"id":"https://openalex.org/S4306508231","display_name":"Doctoral thesis, UCL (University College London).","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":null,"host_organization_name":null,"host_organization_lineage":[],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":null,"is_accepted":false,"is_published":false,"raw_source_name":"Doctoral thesis, UCL (University College London).","raw_type":null},{"id":"mag:3144359741","doi":null,"is_oa":false,"landing_page_url":"https://discovery.ucl.ac.uk/id/eprint/1473105/","pdf_url":null,"source":null,"license":null,"license_id":null,"version":null,"is_accepted":false,"is_published":false,"raw_source_name":null,"raw_type":null}],"best_oa_location":null,"sustainable_development_goals":[{"score":0.8560000061988831,"display_name":"Good health and well-being","id":"https://metadata.un.org/sdg/3"}],"study_designs":[],"awards":[],"funders":[],"has_content":{"pdf":false,"grobid_xml":false},"content_urls":null,"referenced_works_count":0,"referenced_works":[],"related_works":["https://openalex.org/W2013718757","https://openalex.org/W840875033","https://openalex.org/W1767659454","https://openalex.org/W2901856770","https://openalex.org/W2591754869","https://openalex.org/W3015901374","https://openalex.org/W2620237393","https://openalex.org/W2907808098","https://openalex.org/W2166498300","https://openalex.org/W2126184403"],"abstract_inverted_index":{"The":[0,21,79,182,283],"Keap1-Nrf2":[1,109,115,233],"pathway":[2],"has":[3],"been":[4],"identified":[5,214],"as":[6,45,148,192,215],"a":[7,46,120,173,193,202,209,216,264],"key":[8],"regulator":[9],"of":[10,14,23,31,81,89,113,204,230,285],"the":[11,29,32,58,61,87,108,114,164,231,278,286],"cytoprotective":[12],"response":[13],"cells":[15],"when":[16],"exposed":[17],"to":[18,49,85,153,280],"oxidative":[19],"stress.":[20],"induction":[22,123],"detoxification":[24],"gene":[25],"products":[26],"by":[27,96,290],"increasing":[28],"activity":[30],"transcription":[33,297],"factor":[34,36,39,298],"nuclear":[35,74],"erythroid":[37],"2-related":[38],"2":[40],"(Nrf2)":[41],"can":[42,56],"be":[43],"used":[44,191],"chemopreventive":[47],"approach":[48],"cancer":[50],"treatment.":[51],"Natural":[52],"and":[53,70,77,91,125,172,185,236,256,263],"synthetic":[54],"agents":[55],"disrupt":[57],"interaction":[59,235],"between":[60],"substrate":[62],"adaptor":[63],"protein":[64,67],"Kelch-like":[65],"ECH-associated":[66],"1":[68,222],"(Keap1)":[69],"Nrf2,":[71],"which":[72],"allows":[73],"Nrf2":[75,93,176,187],"translocation":[76],"accumulation.":[78],"aim":[80],"this":[82],"project":[83],"was":[84,146,161,190,213,288],"characterize":[86],"behaviour":[88],"direct":[90,134,232],"indirect":[92],"inducer":[94,188,218],"molecules":[95,167,245],"applying":[97],"several":[98],"biological":[99,159],"methods":[100],"that":[101],"were":[102,117,227],"specifically":[103],"optimised":[104],"or":[105],"developed":[106,147],"for":[107,133,179],"pathway.":[110],"Potential":[111],"inhibitors":[112,229],"complex":[116],"screened":[118],"using":[119,168],"cellular":[121],"NQO1":[122,251,258,268],"assay":[124,132,145],"an":[126,149],"in":[127,138,277],"vitro":[128,139],"fluorescence":[129],"polarisation":[130],"(FP)":[131],"inhibitors.":[135],"A":[136],"novel":[137],"F\u00f6rster":[140],"resonance":[141],"energy":[142],"transfer":[143],"(FRET)":[144],"additional":[150],"screening":[151],"tool":[152],"identify":[154],"Keap1":[155],"binding":[156],"partners.":[157],"Further":[158],"evaluation":[160],"conducted":[162],"with":[163,273],"most":[165],"promising":[166,238],"western":[169],"blotting":[170],"analysis":[171],"new":[174],"intracellular":[175],"staining":[177],"method":[178],"flow":[180],"cytometry.":[181],"natural":[183],"product":[184],"\\nindirect":[186],"sulforaphane":[189],"reference":[194],"compound":[195,211],"(NQO1":[196,219],"CD":[197,220,252,259,269],"=":[198,221,253,260,270],"0.4":[199],"\u00b5M).":[200,223],"From":[201],"library":[203],"Michael":[205],"acceptor-containing":[206],"cyclohexadienone":[207],"\\nanalogues,":[208],"3-chlorophenyl":[210],"(6.49)":[212],"potent":[217,228],"Stearoyl-capped":[224],"Nrf2-derived":[225],"peptides":[226],"protein-protein":[234],"showed":[237],"cell":[239],"penetrating":[240],"properties.":[241],"Direct":[242],"inhibitor":[243],"small":[244],"included":[246],"two":[247],"bissulphonamide":[248],"derivatives":[249],"(7A4,":[250],"8":[254],"\u00b5M":[255],"7B1,":[257],"4":[261],"\u00b5M)":[262,272],"1,2,3-triazole":[265],"derivative":[266],"(7C55,":[267],"0.6":[271],"FP":[274],"IC50":[275],"values":[276],"nano-":[279],"micromolar":[281],"range.":[282],"selectivity":[284],"compounds":[287],"assessed":[289],"revealing":[291],"potential":[292],"aryl":[293],"hydrocarbon":[294],"receptor":[295],"(AhR)":[296],"cross-talk.":[299]},"counts_by_year":[],"updated_date":"2026-11-08T12:12:28.789561","created_date":"2016-11-04T00:00:00"}