A Phenotypic Cell-Binding Screen Identifies a Novel Compound Targeting Triple-Negative Breast Cancer

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dc.contributor.ORCID0000-0002-4455-3358 (Lee, J)
dc.contributor.authorChen, Luxi
dc.contributor.authorLong, Chao
dc.contributor.authorYoun, Jonghae
dc.contributor.authorLee, Jiyong
dc.contributor.utdAuthorChen, Luxi
dc.contributor.utdAuthorLong, Chao
dc.contributor.utdAuthorYoun, Jonghae
dc.contributor.utdAuthorLee, Jiyong
dc.date.accessioned2019-05-31T22:27:31Z
dc.date.available2019-05-31T22:27:31Z
dc.date.created2018-05-02
dc.descriptionFull text access from Treasures at UT Dallas is restricted to current UTD affiliates.
dc.descriptionSipplementary information is available.
dc.description.abstractWe describe a "phenotypic cell-binding screen" by which therapeutic candidate targeting cancer cells of a particular phenotype can be isolated without knowledge of drug targets. Chemical library beads are incubated with cancer cells of the phenotype of interest in the presence of cancer cells lacking the phenotype of interest, and then the beads bound to only cancer cells of the phenotype of interest are selected as hits. We have applied this screening strategy in discovering a novel compound (LC129-8) targeting triple-negative breast cancer (TNBC). LC129-8 displayed highly specific binding to TNBC in cancer cell lines and patient-derived tumor tissues. LC129-8 exerted anti-TNBC activity by inducing apoptosis, inhibiting proliferation, reversing epithelial-mesenchymal transition, downregulating cancer stem cell activity and blocking in vivo tumor growth.
dc.identifier.bibliographicCitationChen, Luxi, Chao Long, Jonghae Youn and Jiyong Lee. 2018. "A phenotypic cell-binding screen identifies a novel compound targeting triple-negative breast cancer." ACS Combinatorial Science 20(6): 330-334, doi:10.1021/acscombsci.8b00026
dc.identifier.issn1939-134X; 2045-2322
dc.identifier.issue6
dc.identifier.urihttps://hdl.handle.net/10735.1/6547
dc.identifier.volume20
dc.relation.urihttp://dx.doi.org/10.1021/acscombsci.8b00026
dc.rights©2018 American Chemical Society
dc.source.journalACS Combinatorial Science;
dc.subjectChemical libraries
dc.subjectPhenotype
dc.subjectApoptosis
dc.subjectEpithelial-Mesenchymal Transition
dc.subjectTriple Negative Breast Neoplasms
dc.subjectCancer—Treatment
dc.subjectNeoplastic Stem Cells
dc.titleA Phenotypic Cell-Binding Screen Identifies a Novel Compound Targeting Triple-Negative Breast Cancer
dc.type.genrearticle

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