{"id":"https://openalex.org/W2162103271","doi":"https://doi.org/10.1074/jbc.m110.213736","title":"A Novel Mode of Protein Kinase Inhibition Exploiting Hydrophobic Motifs of Autoinhibited Kinases","display_name":"A Novel Mode of Protein Kinase Inhibition Exploiting Hydrophobic Motifs of Autoinhibited Kinases","publication_year":2011,"publication_date":"2011-03-25","ids":{"openalex":"https://openalex.org/W2162103271","doi":"https://doi.org/10.1074/jbc.m110.213736","mag":"2162103271","pmid":"https://pubmed.ncbi.nlm.nih.gov/21454610","pmcid":"https://www.ncbi.nlm.nih.gov/pmc/articles/3121527"},"language":"en","primary_location":{"id":"doi:10.1074/jbc.m110.213736","doi":"https://doi.org/10.1074/jbc.m110.213736","is_oa":true,"landing_page_url":"https://doi.org/10.1074/jbc.m110.213736","pdf_url":"http://www.jbc.org/article/S0021925819491333/pdf","source":{"id":"https://openalex.org/S140251998","display_name":"Journal of Biological Chemistry","issn_l":"0021-9258","issn":["0021-9258","1067-8816","1083-351X"],"is_oa":false,"is_in_doaj":true,"is_core":true,"listed_in":["anvur-scientific","cwts-core","doaj","dongbi-b","doyens","jufo-2","ki-jl-2","medline","norway-2","poland-100","vabb-shw"],"host_organization":"https://openalex.org/P4310320990","host_organization_name":"Elsevier BV","host_organization_lineage":["https://openalex.org/P4310320990"],"host_organization_lineage_names":["Elsevier BV"],"type":"journal"},"license":"cc-by","license_id":"https://openalex.org/licenses/cc-by","version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of Biological Chemistry","raw_type":"journal-article"},"volume":null,"type":"article","is_traditional":true,"indexed_in":["crossref","doaj","pubmed"],"open_access":{"is_oa":true,"oa_status":"hybrid","oa_url":"http://www.jbc.org/article/S0021925819491333/pdf","any_repository_has_fulltext":true},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5041253361","display_name":"Sudharshan Eathiraj","orcid":"https://orcid.org/0000-0002-7260-8846","observed_orcids":["https://orcid.org/0000-0002-7260-8846"]},"institutions":[{"id":"https://openalex.org/I4210121633","display_name":"Arqule (United States)","ror":"https://ror.org/02nftnt56","country_code":"US","type":"company","lineage":["https://openalex.org/I4210121633"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Sudharshan Eathiraj","raw_affiliation_strings":["ArQule, Inc, Woburn, Massachusetts 01801, USA","ArQule, Inc., Woburn, Massachusetts, 01801"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"ArQule, Inc, Woburn, Massachusetts 01801, USA","institution_ids":[]},{"raw_affiliation_string":"ArQule, Inc., Woburn, Massachusetts, 01801","institution_ids":["https://openalex.org/I4210121633"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5029374868","display_name":"Rocio Palma","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210121633","display_name":"Arqule (United States)","ror":"https://ror.org/02nftnt56","country_code":"US","type":"company","lineage":["https://openalex.org/I4210121633"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Rocio Palma","raw_affiliation_strings":["ArQule, Inc., Woburn, Massachusetts, 01801"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"ArQule, Inc., Woburn, Massachusetts, 01801","institution_ids":["https://openalex.org/I4210121633"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5065252606","display_name":"Marscha Hirschi","orcid":"https://orcid.org/0000-0002-1813-1231","observed_orcids":["https://orcid.org/0000-0002-1813-1231"]},"institutions":[{"id":"https://openalex.org/I4210121633","display_name":"Arqule (United States)","ror":"https://ror.org/02nftnt56","country_code":"US","type":"company","lineage":["https://openalex.org/I4210121633"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Marscha Hirschi","raw_affiliation_strings":["ArQule, Inc., Woburn, Massachusetts, 01801"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"ArQule, Inc., Woburn, Massachusetts, 01801","institution_ids":["https://openalex.org/I4210121633"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5007582656","display_name":"Erika Volckova","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210121633","display_name":"Arqule (United States)","ror":"https://ror.org/02nftnt56","country_code":"US","type":"company","lineage":["https://openalex.org/I4210121633"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Erika Volckova","raw_affiliation_strings":["ArQule, Inc., Woburn, Massachusetts, 01801"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"ArQule, Inc., Woburn, Massachusetts, 01801","institution_ids":["https://openalex.org/I4210121633"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5006194586","display_name":"Enkeleda Nakuci","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210121633","display_name":"Arqule (United States)","ror":"https://ror.org/02nftnt56","country_code":"US","type":"company","lineage":["https://openalex.org/I4210121633"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Enkeleda Nakuci","raw_affiliation_strings":["ArQule, Inc., Woburn, Massachusetts, 01801"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"ArQule, Inc., Woburn, Massachusetts, 01801","institution_ids":["https://openalex.org/I4210121633"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5109694340","display_name":"Jennifer Castro","orcid":"https://orcid.org/0009-0007-5718-2692","observed_orcids":["https://orcid.org/0009-0007-5718-2692"]},"institutions":[{"id":"https://openalex.org/I4210121633","display_name":"Arqule (United States)","ror":"https://ror.org/02nftnt56","country_code":"US","type":"company","lineage":["https://openalex.org/I4210121633"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Jennifer Castro","raw_affiliation_strings":["ArQule, Inc., Woburn, Massachusetts, 01801"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"ArQule, Inc., Woburn, Massachusetts, 01801","institution_ids":["https://openalex.org/I4210121633"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5013780845","display_name":"Chang-Rung Chen","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210121633","display_name":"Arqule (United States)","ror":"https://ror.org/02nftnt56","country_code":"US","type":"company","lineage":["https://openalex.org/I4210121633"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Chang-Rung Chen","raw_affiliation_strings":["ArQule, Inc., Woburn, Massachusetts, 01801"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"ArQule, Inc., Woburn, Massachusetts, 01801","institution_ids":["https://openalex.org/I4210121633"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5057399487","display_name":"Thomas Chan","orcid":"https://orcid.org/0000-0001-6025-3796","observed_orcids":["https://orcid.org/0000-0001-6025-3796"]},"institutions":[{"id":"https://openalex.org/I4210121633","display_name":"Arqule (United States)","ror":"https://ror.org/02nftnt56","country_code":"US","type":"company","lineage":["https://openalex.org/I4210121633"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Thomas C.K. Chan","raw_affiliation_strings":["ArQule, Inc., Woburn, Massachusetts, 01801"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"ArQule, Inc., Woburn, Massachusetts, 01801","institution_ids":["https://openalex.org/I4210121633"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5112045320","display_name":"Dennis S. France","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210121633","display_name":"Arqule (United States)","ror":"https://ror.org/02nftnt56","country_code":"US","type":"company","lineage":["https://openalex.org/I4210121633"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Dennis S. France","raw_affiliation_strings":["ArQule, Inc., Woburn, Massachusetts, 01801"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"ArQule, Inc., Woburn, Massachusetts, 01801","institution_ids":["https://openalex.org/I4210121633"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5053232883","display_name":"Mark A. Ashwell","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210121633","display_name":"Arqule (United States)","ror":"https://ror.org/02nftnt56","country_code":"US","type":"company","lineage":["https://openalex.org/I4210121633"]}],"countries":["US"],"is_corresponding":true,"raw_author_name":"Mark A. Ashwell","raw_affiliation_strings":["ArQule, Inc., Woburn, Massachusetts, 01801"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"ArQule, Inc., Woburn, Massachusetts, 01801","institution_ids":["https://openalex.org/I4210121633"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":1,"corresponding_author_ids":["https://openalex.org/A5053232883"],"corresponding_institution_ids":["https://openalex.org/I4210121633"],"apc_list":{"value":3430,"currency":"USD","value_usd":3430},"apc_paid":{"value":3430,"currency":"USD","value_usd":3430},"fwci":1.9259,"has_fulltext":true,"cited_by_count":67,"citation_normalized_percentile":{"value":0.86595738,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":88,"max":99},"biblio":{"volume":"286","issue":"23","first_page":"20677","last_page":"20687"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10169","display_name":"Protein Kinase Regulation and GTPase Signaling","score":0.5464000105857849,"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/T10169","display_name":"Protein Kinase Regulation and GTPase Signaling","score":0.5464000105857849,"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/T12287","display_name":"Fibroblast Growth Factor Research","score":0.2856000065803528,"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/T10211","display_name":"Computational Drug Discovery Methods","score":0.10819999873638153,"subfield":{"id":"https://openalex.org/subfields/3002","display_name":"Drug Discovery"},"field":{"id":"https://openalex.org/fields/30","display_name":"Pharmacology, Toxicology and Pharmaceutics"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}}],"keywords":[{"id":"https://openalex.org/keywords/protein-kinase-inhibitors","display_name":"protein kinase inhibitors","score":0.9850000143051147},{"id":"https://openalex.org/keywords/inactive-kinase-conformation","display_name":"inactive kinase conformation","score":0.7059999704360962},{"id":"https://openalex.org/keywords/hydrophobic-motif","display_name":"hydrophobic motif","score":0.7459999918937683},{"id":"https://openalex.org/keywords/fgfr2-inhibitor","display_name":"FGFR2 inhibitor","score":0.9309999942779541},{"id":"https://openalex.org/keywords/kinase-inhibitor-selectivity","display_name":"kinase selectivity","score":0.6859999895095825},{"id":"https://openalex.org/keywords/atp-competitive-inhibition","display_name":"ATP-competitive inhibition","score":0.6399999856948853},{"id":"https://openalex.org/keywords/kinase-activation","display_name":"kinase activation","score":0.4339999854564667},{"id":"https://openalex.org/keywords/tumor-cell-inhibition","display_name":"cancer cell inhibition","score":0.625}],"concepts":[{"id":"https://openalex.org/C184235292","wikidata":"https://www.wikidata.org/wiki/Q421851","display_name":"Kinase","level":2,"score":0.7967076897621155},{"id":"https://openalex.org/C166342909","wikidata":"https://www.wikidata.org/wiki/Q845326","display_name":"Allosteric regulation","level":3,"score":0.7204001545906067},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.602875828742981},{"id":"https://openalex.org/C107824862","wikidata":"https://www.wikidata.org/wiki/Q616005","display_name":"Binding site","level":2,"score":0.5178537964820862},{"id":"https://openalex.org/C97029542","wikidata":"https://www.wikidata.org/wiki/Q281417","display_name":"Protein kinase A","level":3,"score":0.4680860638618469},{"id":"https://openalex.org/C42362537","wikidata":"https://www.wikidata.org/wiki/Q87099740","display_name":"Tyrosine kinase","level":3,"score":0.46046990156173706},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.45603975653648376},{"id":"https://openalex.org/C101544691","wikidata":"https://www.wikidata.org/wiki/Q420511","display_name":"Receptor tyrosine kinase","level":3,"score":0.42747724056243896},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.37772560119628906},{"id":"https://openalex.org/C181199279","wikidata":"https://www.wikidata.org/wiki/Q8047","display_name":"Enzyme","level":2,"score":0.3554344177246094},{"id":"https://openalex.org/C95444343","wikidata":"https://www.wikidata.org/wiki/Q7141","display_name":"Cell biology","level":1,"score":0.3484206199645996},{"id":"https://openalex.org/C62478195","wikidata":"https://www.wikidata.org/wiki/Q828130","display_name":"Signal transduction","level":2,"score":0.29432788491249084}],"mesh":[{"descriptor_ui":"D000255","descriptor_name":"Adenosine Triphosphate","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D006801","descriptor_name":"Humans","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D008958","descriptor_name":"Models, Molecular","qualifier_ui":null,"qualifier_name":null,"is_major_topic":true},{"descriptor_ui":"D018360","descriptor_name":"Crystallography, X-Ray","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D020816","descriptor_name":"Amino Acid Motifs","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D047428","descriptor_name":"Protein Kinase Inhibitors","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":true},{"descriptor_ui":"D051496","descriptor_name":"Receptor, Fibroblast Growth Factor, Type 1","qualifier_ui":"Q000037","qualifier_name":"antagonists & inhibitors","is_major_topic":true},{"descriptor_ui":"D051496","descriptor_name":"Receptor, Fibroblast Growth Factor, Type 1","qualifier_ui":"Q000235","qualifier_name":"genetics","is_major_topic":false},{"descriptor_ui":"D051496","descriptor_name":"Receptor, Fibroblast Growth Factor, Type 1","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":true},{"descriptor_ui":"D051497","descriptor_name":"Receptor, Fibroblast Growth Factor, Type 2","qualifier_ui":"Q000037","qualifier_name":"antagonists & inhibitors","is_major_topic":true},{"descriptor_ui":"D051497","descriptor_name":"Receptor, Fibroblast Growth Factor, Type 2","qualifier_ui":"Q000235","qualifier_name":"genetics","is_major_topic":false},{"descriptor_ui":"D051497","descriptor_name":"Receptor, Fibroblast Growth Factor, Type 2","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":true},{"descriptor_ui":"D055808","descriptor_name":"Drug Discovery","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D057927","descriptor_name":"Hydrophobic and Hydrophilic Interactions","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false}],"locations_count":4,"locations":[{"id":"doi:10.1074/jbc.m110.213736","doi":"https://doi.org/10.1074/jbc.m110.213736","is_oa":true,"landing_page_url":"https://doi.org/10.1074/jbc.m110.213736","pdf_url":"http://www.jbc.org/article/S0021925819491333/pdf","source":{"id":"https://openalex.org/S140251998","display_name":"Journal of Biological Chemistry","issn_l":"0021-9258","issn":["0021-9258","1067-8816","1083-351X"],"is_oa":false,"is_in_doaj":true,"is_core":true,"listed_in":["anvur-scientific","cwts-core","doaj","dongbi-b","doyens","jufo-2","ki-jl-2","medline","norway-2","poland-100","vabb-shw"],"host_organization":"https://openalex.org/P4310320990","host_organization_name":"Elsevier BV","host_organization_lineage":["https://openalex.org/P4310320990"],"host_organization_lineage_names":["Elsevier BV"],"type":"journal"},"license":"cc-by","license_id":"https://openalex.org/licenses/cc-by","version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of Biological Chemistry","raw_type":"journal-article"},{"id":"pmh:oai:europepmc.org:2377417","doi":null,"is_oa":true,"landing_page_url":"https://www.ncbi.nlm.nih.gov/pmc/articles/3121527","pdf_url":null,"source":{"id":"https://openalex.org/S4306400806","display_name":"Europe PMC (PubMed Central)","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I1303153112","host_organization_name":"European Bioinformatics Institute","host_organization_lineage":["https://openalex.org/I1303153112"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":null,"raw_type":"Text"},{"id":"pmh:oai:pubmedcentral.nih.gov:3121527","doi":null,"is_oa":true,"landing_page_url":"https://www.ncbi.nlm.nih.gov/pmc/articles/3121527","pdf_url":null,"source":{"id":"https://openalex.org/S2764455111","display_name":"PubMed Central","issn_l":null,"issn":null,"is_oa":true,"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":"J Biol Chem","raw_type":"Text"},{"id":"pmid:21454610","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/21454610","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":"The Journal of biological chemistry","raw_type":"Journal Article"}],"best_oa_location":{"id":"doi:10.1074/jbc.m110.213736","doi":"https://doi.org/10.1074/jbc.m110.213736","is_oa":true,"landing_page_url":"https://doi.org/10.1074/jbc.m110.213736","pdf_url":"http://www.jbc.org/article/S0021925819491333/pdf","source":{"id":"https://openalex.org/S140251998","display_name":"Journal of Biological Chemistry","issn_l":"0021-9258","issn":["0021-9258","1067-8816","1083-351X"],"is_oa":false,"is_in_doaj":true,"is_core":true,"listed_in":["anvur-scientific","cwts-core","doaj","dongbi-b","doyens","jufo-2","ki-jl-2","medline","norway-2","poland-100","vabb-shw"],"host_organization":"https://openalex.org/P4310320990","host_organization_name":"Elsevier BV","host_organization_lineage":["https://openalex.org/P4310320990"],"host_organization_lineage_names":["Elsevier BV"],"type":"journal"},"license":"cc-by","license_id":"https://openalex.org/licenses/cc-by","version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of Biological Chemistry","raw_type":"journal-article"},"sustainable_development_goals":[{"id":"https://metadata.un.org/sdg/3","score":0.5683000087738037,"display_name":"Good health and well-being"}],"study_designs":[],"awards":[{"id":"https://openalex.org/G7217644330","display_name":"Case Center for Synchrotron Bioscience","funder_award_id":"P30EB009998","funder_id":"https://openalex.org/F4320337363","funder_display_name":"National Institute of Biomedical Imaging and Bioengineering"}],"funders":[{"id":"https://openalex.org/F4320337363","display_name":"National Institute of Biomedical Imaging and Bioengineering","ror":"https://ror.org/00372qc85"}],"has_content":{"pdf":true,"grobid_xml":true},"content_urls":{"pdf":"https://content.openalex.org/works/W2162103271.pdf","grobid_xml":"https://content.openalex.org/works/W2162103271.grobid-xml"},"referenced_works_count":44,"referenced_works":["https://openalex.org/W256532953","https://openalex.org/W1973207799","https://openalex.org/W1977926787","https://openalex.org/W1988476050","https://openalex.org/W1992388470","https://openalex.org/W1992945955","https://openalex.org/W1994105285","https://openalex.org/W2000390423","https://openalex.org/W2001641653","https://openalex.org/W2001974855","https://openalex.org/W2007466764","https://openalex.org/W2012169430","https://openalex.org/W2018078143","https://openalex.org/W2036579888","https://openalex.org/W2047132220","https://openalex.org/W2050372166","https://openalex.org/W2052092007","https://openalex.org/W2052639986","https://openalex.org/W2055523288","https://openalex.org/W2056983875","https://openalex.org/W2066059461","https://openalex.org/W2070869831","https://openalex.org/W2071500926","https://openalex.org/W2074325221","https://openalex.org/W2074697882","https://openalex.org/W2079029484","https://openalex.org/W2079398727","https://openalex.org/W2082594472","https://openalex.org/W2085550501","https://openalex.org/W2098411183","https://openalex.org/W2101306957","https://openalex.org/W2106986615","https://openalex.org/W2107448187","https://openalex.org/W2116978122","https://openalex.org/W2117022661","https://openalex.org/W2118460316","https://openalex.org/W2132437319","https://openalex.org/W2133824400","https://openalex.org/W2134164143","https://openalex.org/W2134195121","https://openalex.org/W2139073495","https://openalex.org/W2156232082","https://openalex.org/W2168571726","https://openalex.org/W2171944348"],"related_works":["https://openalex.org/W2328092448","https://openalex.org/W2079398727","https://openalex.org/W2156972915","https://openalex.org/W2284698574","https://openalex.org/W1966522861","https://openalex.org/W2050372166","https://openalex.org/W3143672795","https://openalex.org/W2009222632","https://openalex.org/W2034617810","https://openalex.org/W2023701447"],"abstract_inverted_index":{"Protein":[0],"kinase":[1,116],"inhibitors":[2,20,174,222],"with":[3,13,27],"enhanced":[4],"selectivity":[5],"can":[6],"be":[7,22,34],"designed":[8],"by":[9,37,207,223],"optimizing":[10],"binding":[11,30,161],"interactions":[12],"less":[14,23,35],"conserved":[15],"inactive":[16,52,97,225],"conformations":[17,226],"because":[18],"such":[19],"will":[21],"likely":[24],"to":[25,61],"compete":[26],"ATP":[28],"for":[29,102,218],"and":[31,154,157,193],"therefore":[32],"may":[33],"impacted":[36],"high":[38],"intracellular":[39],"concentrations":[40,190],"of":[41,44,51,64,96,124,132,148,177,188,191,205,221,227],"ATP.":[42],"Analysis":[43],"the":[45,57,62,80,90,103,109,141,145,160,178,186,202,210,219],"ATP-binding":[46],"cleft":[47],"in":[48,56,70,151,185,198],"a":[49,65,119,125,130,215],"number":[50],"protein":[53,228],"kinases,":[54],"particularly":[55],"autoinhibited":[58,179],"conformation,":[59,180],"led":[60],"identification":[63],"previously":[66,81],"undisclosed":[67],"non-polar":[68],"region":[69,76],"this":[71,149],"cleft.":[72],"This":[73],"ATP-incompatible":[74],"hydrophobic":[75,83],"is":[77],"distinct":[78],"from":[79,129,140],"characterized":[82,159],"allosteric":[84],"back":[85],"pocket,":[86],"as":[87,89,118,170],"well":[88],"main":[91],"pocket.":[92],"Generalized":[93],"hypothetical":[94],"models":[95],"kinases":[98,206],"were":[99],"constructed":[100],"and,":[101],"work":[104],"described":[105,212],"here,":[106],"we":[107],"selected":[108],"fibroblast":[110],"growth":[111],"factor":[112],"receptor":[113],"(FGFR)":[114],"tyrosine":[115],"family":[117],"case":[120],"study.":[121],"Initial":[122],"optimization":[123],"FGFR2":[126],"inhibitor":[127],"identified":[128],"library":[131],"commercial":[133],"compounds":[134],"was":[135],"guided":[136],"using":[137,163],"structural":[138],"information":[139],"model.":[142],"We":[143],"describe":[144],"inhibitory":[146,183,196],"characteristics":[147],"compound":[150],"biophysical,":[152],"biochemical,":[153],"cell-based":[155],"assays,":[156],"have":[158,194],"mode":[162],"x-ray":[164],"crystallographic":[165],"studies.":[166],"The":[167],"results":[168],"demonstrate,":[169],"expected,":[171],"that":[172],"these":[173],"prevent":[175],"activation":[176],"retain":[181],"full":[182],"potency":[184],"presence":[187],"physiological":[189],"ATP,":[192],"favorable":[195],"activity":[197],"cancer":[199],"cells.":[200],"Given":[201],"widespread":[203],"regulation":[204],"autoinhibitory":[208],"mechanisms,":[209],"approach":[211],"herein":[213],"provides":[214],"new":[216],"paradigm":[217],"discovery":[220],"targeting":[224],"kinases.":[229]},"counts_by_year":[{"year":2026,"cited_by_count":6},{"year":2025,"cited_by_count":3},{"year":2024,"cited_by_count":7},{"year":2023,"cited_by_count":6},{"year":2022,"cited_by_count":1},{"year":2021,"cited_by_count":2},{"year":2020,"cited_by_count":2},{"year":2019,"cited_by_count":2},{"year":2018,"cited_by_count":2},{"year":2017,"cited_by_count":7},{"year":2016,"cited_by_count":8},{"year":2015,"cited_by_count":3},{"year":2014,"cited_by_count":4},{"year":2013,"cited_by_count":4},{"year":2012,"cited_by_count":5}],"updated_date":"2026-11-07T11:25:07.637180","created_date":"2016-06-24T00:00:00"}
