Ontology type: schema:ScholarlyArticle Open Access: True
2010-08-16
AUTHORSLi Lin, Stephanie Deangelis, Elizabeth Foust, James Fuchs, Chenglong Li, Pui-Kai Li, Eric B Schwartz, Gregory B Lesinski, Don Benson, Jiagao Lü, Dale Hoyt, Jiayuh Lin
ABSTRACTBackgroundTargeting Signal Transducer and Activator of Transcription 3 (STAT3) signaling is an attractive therapeutic approach for most types of human cancers with constitutively activated STAT3. A novel small molecular STAT3 inhibitor, FLLL32 was specifically designed from dietary agent, curcumin to inhibit constitutive STAT3 signaling in multiple myeloma, glioblastoma, liver cancer, and colorectal cancer cells.ResultsFLLL32 was found to be a potent inhibitor of STAT3 phosphorylation, STAT3 DNA binding activity, and the expression of STAT3 downstream target genes in vitro, leading to the inhibition of cell proliferation as well as the induction of Caspase-3 and PARP cleavages in human multiple myeloma, glioblastoma, liver cancer, and colorectal cancer cell lines. However, FLLL32 exhibited little inhibition on some tyrosine kinases containing SH2 or both SH2 and SH3 domains, and other protein and lipid kinases using a kinase profile assay. FLLL32 was also more potent than four previously reported JAK2 and STAT3 inhibitors as well as curcumin to inhibit cell viability in these cancer cells. Furthermore, FLLL32 selectively inhibited the induction of STAT3 phosphorylation by Interleukin-6 but not STAT1 phosphorylation by IFN-γ.ConclusionOur findings indicate that FLLL32 exhibits potent inhibitory activity to STAT3 and has potential for targeting multiple myeloma, glioblastoma, liver cancer, and colorectal cancer cells expressing constitutive STAT3 signaling. More... »
PAGES217
http://scigraph.springernature.com/pub.10.1186/1476-4598-9-217
DOIhttp://dx.doi.org/10.1186/1476-4598-9-217
DIMENSIONShttps://app.dimensions.ai/details/publication/pub.1052907373
PUBMEDhttps://www.ncbi.nlm.nih.gov/pubmed/20712901
JSON-LD is the canonical representation for SciGraph data.
TIP: You can open this SciGraph record using an external JSON-LD service: JSON-LD Playground Google SDTT
[
{
"@context": "https://springernature.github.io/scigraph/jsonld/sgcontext.json",
"about": [
{
"id": "http://purl.org/au-research/vocabulary/anzsrc-for/2008/11",
"inDefinedTermSet": "http://purl.org/au-research/vocabulary/anzsrc-for/2008/",
"name": "Medical and Health Sciences",
"type": "DefinedTerm"
},
{
"id": "http://purl.org/au-research/vocabulary/anzsrc-for/2008/1112",
"inDefinedTermSet": "http://purl.org/au-research/vocabulary/anzsrc-for/2008/",
"name": "Oncology and Carcinogenesis",
"type": "DefinedTerm"
},
{
"inDefinedTermSet": "https://www.nlm.nih.gov/mesh/",
"name": "Cell Division",
"type": "DefinedTerm"
},
{
"inDefinedTermSet": "https://www.nlm.nih.gov/mesh/",
"name": "Cell Line, Tumor",
"type": "DefinedTerm"
},
{
"inDefinedTermSet": "https://www.nlm.nih.gov/mesh/",
"name": "Curcumin",
"type": "DefinedTerm"
},
{
"inDefinedTermSet": "https://www.nlm.nih.gov/mesh/",
"name": "DNA",
"type": "DefinedTerm"
},
{
"inDefinedTermSet": "https://www.nlm.nih.gov/mesh/",
"name": "Humans",
"type": "DefinedTerm"
},
{
"inDefinedTermSet": "https://www.nlm.nih.gov/mesh/",
"name": "Phosphorylation",
"type": "DefinedTerm"
},
{
"inDefinedTermSet": "https://www.nlm.nih.gov/mesh/",
"name": "STAT3 Transcription Factor",
"type": "DefinedTerm"
}
],
"author": [
{
"affiliation": {
"alternateName": "Division of Cardiology, Department of Internal Medicine, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, 430030, Wuhan, China",
"id": "http://www.grid.ac/institutes/grid.33199.31",
"name": [
"Department of Pediatrics, College of Medicine, The Ohio State University, 43205, Columbus, Ohio, USA",
"Division of Cardiology, Department of Internal Medicine, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, 430030, Wuhan, China"
],
"type": "Organization"
},
"familyName": "Lin",
"givenName": "Li",
"id": "sg:person.01213131071.92",
"sameAs": [
"https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.01213131071.92"
],
"type": "Person"
},
{
"affiliation": {
"alternateName": "Department of Pediatrics, College of Medicine, The Ohio State University, 43205, Columbus, Ohio, USA",
"id": "http://www.grid.ac/institutes/grid.261331.4",
"name": [
"Department of Pediatrics, College of Medicine, The Ohio State University, 43205, Columbus, Ohio, USA"
],
"type": "Organization"
},
"familyName": "Deangelis",
"givenName": "Stephanie",
"id": "sg:person.0746071710.09",
"sameAs": [
"https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.0746071710.09"
],
"type": "Person"
},
{
"affiliation": {
"alternateName": "Department of Pediatrics, College of Medicine, The Ohio State University, 43205, Columbus, Ohio, USA",
"id": "http://www.grid.ac/institutes/grid.261331.4",
"name": [
"Department of Pediatrics, College of Medicine, The Ohio State University, 43205, Columbus, Ohio, USA"
],
"type": "Organization"
},
"familyName": "Foust",
"givenName": "Elizabeth",
"id": "sg:person.01005654416.33",
"sameAs": [
"https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.01005654416.33"
],
"type": "Person"
},
{
"affiliation": {
"alternateName": "Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 43210, Columbus, Ohio, USA",
"id": "http://www.grid.ac/institutes/grid.261331.4",
"name": [
"Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 43210, Columbus, Ohio, USA"
],
"type": "Organization"
},
"familyName": "Fuchs",
"givenName": "James",
"id": "sg:person.013262657617.12",
"sameAs": [
"https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.013262657617.12"
],
"type": "Person"
},
{
"affiliation": {
"alternateName": "Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 43210, Columbus, Ohio, USA",
"id": "http://www.grid.ac/institutes/grid.261331.4",
"name": [
"Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 43210, Columbus, Ohio, USA"
],
"type": "Organization"
},
"familyName": "Li",
"givenName": "Chenglong",
"id": "sg:person.07466226257.36",
"sameAs": [
"https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.07466226257.36"
],
"type": "Person"
},
{
"affiliation": {
"alternateName": "Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 43210, Columbus, Ohio, USA",
"id": "http://www.grid.ac/institutes/grid.261331.4",
"name": [
"Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 43210, Columbus, Ohio, USA"
],
"type": "Organization"
},
"familyName": "Li",
"givenName": "Pui-Kai",
"id": "sg:person.01233435521.07",
"sameAs": [
"https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.01233435521.07"
],
"type": "Person"
},
{
"affiliation": {
"alternateName": "Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 43210, Columbus, Ohio, USA",
"id": "http://www.grid.ac/institutes/grid.261331.4",
"name": [
"Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 43210, Columbus, Ohio, USA"
],
"type": "Organization"
},
"familyName": "Schwartz",
"givenName": "Eric B",
"id": "sg:person.01134016213.25",
"sameAs": [
"https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.01134016213.25"
],
"type": "Person"
},
{
"affiliation": {
"alternateName": "Department of Internal Medicine, The Ohio State University, 43210, Columbus, Ohio, USA",
"id": "http://www.grid.ac/institutes/grid.261331.4",
"name": [
"Department of Internal Medicine, The Ohio State University, 43210, Columbus, Ohio, USA"
],
"type": "Organization"
},
"familyName": "Lesinski",
"givenName": "Gregory B",
"id": "sg:person.0642400237.44",
"sameAs": [
"https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.0642400237.44"
],
"type": "Person"
},
{
"affiliation": {
"alternateName": "Department of Internal Medicine, The Ohio State University, 43210, Columbus, Ohio, USA",
"id": "http://www.grid.ac/institutes/grid.261331.4",
"name": [
"Department of Internal Medicine, The Ohio State University, 43210, Columbus, Ohio, USA"
],
"type": "Organization"
},
"familyName": "Benson",
"givenName": "Don",
"id": "sg:person.011746564122.47",
"sameAs": [
"https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.011746564122.47"
],
"type": "Person"
},
{
"affiliation": {
"alternateName": "Division of Cardiology, Department of Internal Medicine, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, 430030, Wuhan, China",
"id": "http://www.grid.ac/institutes/grid.33199.31",
"name": [
"Division of Cardiology, Department of Internal Medicine, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, 430030, Wuhan, China"
],
"type": "Organization"
},
"familyName": "L\u00fc",
"givenName": "Jiagao",
"id": "sg:person.01260311107.54",
"sameAs": [
"https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.01260311107.54"
],
"type": "Person"
},
{
"affiliation": {
"alternateName": "Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 43210, Columbus, Ohio, USA",
"id": "http://www.grid.ac/institutes/grid.261331.4",
"name": [
"Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, 43210, Columbus, Ohio, USA"
],
"type": "Organization"
},
"familyName": "Hoyt",
"givenName": "Dale",
"id": "sg:person.01242743756.91",
"sameAs": [
"https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.01242743756.91"
],
"type": "Person"
},
{
"affiliation": {
"alternateName": "Experimental Therapeutics Program, The Ohio State University Comprehensive Cancer Center, The Ohio State University, 43210, Columbus, Ohio, USA",
"id": "http://www.grid.ac/institutes/grid.261331.4",
"name": [
"Department of Pediatrics, College of Medicine, The Ohio State University, 43205, Columbus, Ohio, USA",
"Experimental Therapeutics Program, The Ohio State University Comprehensive Cancer Center, The Ohio State University, 43210, Columbus, Ohio, USA"
],
"type": "Organization"
},
"familyName": "Lin",
"givenName": "Jiayuh",
"id": "sg:person.01105454620.89",
"sameAs": [
"https://app.dimensions.ai/discover/publication?and_facet_researcher=ur.01105454620.89"
],
"type": "Person"
}
],
"citation": [
{
"id": "sg:pub.10.1038/379645a0",
"sameAs": [
"https://app.dimensions.ai/details/publication/pub.1027170927",
"https://doi.org/10.1038/379645a0"
],
"type": "CreativeWork"
},
{
"id": "sg:pub.10.1007/s00018-008-7452-4",
"sameAs": [
"https://app.dimensions.ai/details/publication/pub.1017783394",
"https://doi.org/10.1007/s00018-008-7452-4"
],
"type": "CreativeWork"
},
{
"id": "sg:pub.10.1038/sj.onc.1206047",
"sameAs": [
"https://app.dimensions.ai/details/publication/pub.1007790572",
"https://doi.org/10.1038/sj.onc.1206047"
],
"type": "CreativeWork"
},
{
"id": "sg:pub.10.1038/sj.onc.1207455",
"sameAs": [
"https://app.dimensions.ai/details/publication/pub.1034766609",
"https://doi.org/10.1038/sj.onc.1207455"
],
"type": "CreativeWork"
},
{
"id": "sg:pub.10.1038/ng0501-29",
"sameAs": [
"https://app.dimensions.ai/details/publication/pub.1003632653",
"https://doi.org/10.1038/ng0501-29"
],
"type": "CreativeWork"
},
{
"id": "sg:pub.10.1038/sj.onc.1210031",
"sameAs": [
"https://app.dimensions.ai/details/publication/pub.1031711164",
"https://doi.org/10.1038/sj.onc.1210031"
],
"type": "CreativeWork"
},
{
"id": "sg:pub.10.1038/sj.onc.1208788",
"sameAs": [
"https://app.dimensions.ai/details/publication/pub.1041084218",
"https://doi.org/10.1038/sj.onc.1208788"
],
"type": "CreativeWork"
}
],
"datePublished": "2010-08-16",
"datePublishedReg": "2010-08-16",
"description": "BackgroundTargeting Signal Transducer and Activator of Transcription 3 (STAT3) signaling is an attractive therapeutic approach for most types of human cancers with constitutively activated STAT3. A novel small molecular STAT3 inhibitor, FLLL32 was specifically designed from dietary agent, curcumin to inhibit constitutive STAT3 signaling in multiple myeloma, glioblastoma, liver cancer, and colorectal cancer cells.ResultsFLLL32 was found to be a potent inhibitor of STAT3 phosphorylation, STAT3 DNA binding activity, and the expression of STAT3 downstream target genes in vitro, leading to the inhibition of cell proliferation as well as the induction of Caspase-3 and PARP cleavages in human multiple myeloma, glioblastoma, liver cancer, and colorectal cancer cell lines. However, FLLL32 exhibited little inhibition on some tyrosine kinases containing SH2 or both SH2 and SH3 domains, and other protein and lipid kinases using a kinase profile assay. FLLL32 was also more potent than four previously reported JAK2 and STAT3 inhibitors as well as curcumin to inhibit cell viability in these cancer cells. Furthermore, FLLL32 selectively inhibited the induction of STAT3 phosphorylation by Interleukin-6 but not STAT1 phosphorylation by IFN-\u03b3.ConclusionOur findings indicate that FLLL32 exhibits potent inhibitory activity to STAT3 and has potential for targeting multiple myeloma, glioblastoma, liver cancer, and colorectal cancer cells expressing constitutive STAT3 signaling.",
"genre": "article",
"id": "sg:pub.10.1186/1476-4598-9-217",
"isAccessibleForFree": true,
"isPartOf": [
{
"id": "sg:journal.1031030",
"issn": [
"1476-4598"
],
"name": "Molecular Cancer",
"publisher": "Springer Nature",
"type": "Periodical"
},
{
"issueNumber": "1",
"type": "PublicationIssue"
},
{
"type": "PublicationVolume",
"volumeNumber": "9"
}
],
"keywords": [
"STAT3 phosphorylation",
"STAT3 downstream target genes",
"cancer cells",
"constitutive STAT3",
"colorectal cancer cells",
"STAT3 inhibitor",
"multiple myeloma",
"inhibits STAT3 phosphorylation",
"liver cancer",
"downstream target genes",
"transcription 3 (STAT3) signaling",
"growth-suppressive activity",
"potent growth suppressive activity",
"human cancer cells",
"STAT3 DNA",
"lipid kinases",
"SH3 domain",
"target genes",
"signal transducer",
"colorectal cancer cell lines",
"tyrosine kinase",
"human multiple myeloma",
"PARP cleavage",
"attractive therapeutic approach",
"phosphorylation",
"STAT1 phosphorylation",
"human cancers",
"cancer cell lines",
"STAT3",
"caspase-3",
"cell proliferation",
"SH2",
"cell lines",
"dietary agents",
"interleukin-6",
"therapeutic approaches",
"kinase",
"suppressive activity",
"ConclusionOur findings",
"potent inhibitory activity",
"cell viability",
"myeloma",
"cancer",
"DNA",
"potent inhibitor",
"cells",
"glioblastoma",
"inhibitors",
"little inhibition",
"inhibitory activity",
"induction",
"FLLL32",
"genes",
"signaling",
"inhibition",
"curcumin",
"protein",
"JAK2",
"activity",
"activator",
"most types",
"IFN",
"expression",
"proliferation",
"cleavage",
"assays",
"viability",
"domain",
"agents",
"lines",
"findings",
"transducer",
"types",
"approach"
],
"name": "A novel small molecule inhibits STAT3 phosphorylation and DNA binding activity and exhibits potent growth suppressive activity in human cancer cells",
"pagination": "217",
"productId": [
{
"name": "dimensions_id",
"type": "PropertyValue",
"value": [
"pub.1052907373"
]
},
{
"name": "doi",
"type": "PropertyValue",
"value": [
"10.1186/1476-4598-9-217"
]
},
{
"name": "pubmed_id",
"type": "PropertyValue",
"value": [
"20712901"
]
}
],
"sameAs": [
"https://doi.org/10.1186/1476-4598-9-217",
"https://app.dimensions.ai/details/publication/pub.1052907373"
],
"sdDataset": "articles",
"sdDatePublished": "2022-08-04T16:59",
"sdLicense": "https://scigraph.springernature.com/explorer/license/",
"sdPublisher": {
"name": "Springer Nature - SN SciGraph project",
"type": "Organization"
},
"sdSource": "s3://com-springernature-scigraph/baseset/20220804/entities/gbq_results/article/article_527.jsonl",
"type": "ScholarlyArticle",
"url": "https://doi.org/10.1186/1476-4598-9-217"
}
]Download the RDF metadata as: json-ld nt turtle xml License info
JSON-LD is a popular format for linked data which is fully compatible with JSON.
curl -H 'Accept: application/ld+json' 'https://scigraph.springernature.com/pub.10.1186/1476-4598-9-217'
N-Triples is a line-based linked data format ideal for batch operations.
curl -H 'Accept: application/n-triples' 'https://scigraph.springernature.com/pub.10.1186/1476-4598-9-217'
Turtle is a human-readable linked data format.
curl -H 'Accept: text/turtle' 'https://scigraph.springernature.com/pub.10.1186/1476-4598-9-217'
RDF/XML is a standard XML format for linked data.
curl -H 'Accept: application/rdf+xml' 'https://scigraph.springernature.com/pub.10.1186/1476-4598-9-217'
This table displays all metadata directly associated to this object as RDF triples.
277 TRIPLES
21 PREDICATES
113 URIs
98 LITERALS
14 BLANK NODES