| http://purl.uniprot.org/citations/26543230 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/26543230 | http://www.w3.org/2000/01/rdf-schema#comment | "The hepatocyte growth factor receptor (HGFR or c-Met) is a driver of multiple cancer subtypes. While there are several c-Met inhibitors in development, few have been approved for clinical use, warranting the need for continued research and development of c-Met targeting therapeutic modalities. The research presented here demonstrates a particular class of compounds known as isothiocyanatostilbenes can act as c-Met inhibitors in multiple cancer cell lines. Specifically, we found that 4,4'-Diisothiocyanatostilbene-2,2'-disulfonic acid (DIDS) and 4,4'-Diisothiocyanatodihydrostilbene-2,2'-disulfonic acid (H2DIDS) had c-Met inhibitory effective doses in the low micromolar range while 4-acetamido-4'-isothiocyanatostilbene-2,2'-disulfonic acid (SITS) and 4,4'-dinitrostilbene-2, 2'-disulfonic acid (DNDS) exhibited IC50s 100 to 1000 fold higher. These compounds displayed much greater selectivity for inhibiting c-Met activation compared to similar receptor tyrosine kinases. In addition, DIDS and H2DIDS reduced hepatocyte growth factor (HGF)-induced, but not epidermal growth factor (EGF)-induced, cell scattering, wound healing, and 3-dimensional (3D) proliferation of tumor cell spheroids. In-cell and cell-free assays suggested that DIDS and H2DIDS can inhibit and reverse c-Met phosphorylation, similar to SU11274. Additional data demonstrated that DIDS is tolerable in vivo. These data provide preliminary support for future studies examining DIDS, H2DIDS, and derivatives as potential c-Met therapeutics."xsd:string |
| http://purl.uniprot.org/citations/26543230 | http://purl.org/dc/terms/identifier | "doi:10.18632/oncotarget.5748"xsd:string |
| http://purl.uniprot.org/citations/26543230 | http://purl.uniprot.org/core/author | "Cardelli J.A."xsd:string |
| http://purl.uniprot.org/citations/26543230 | http://purl.uniprot.org/core/author | "El Sayed K.A."xsd:string |
| http://purl.uniprot.org/citations/26543230 | http://purl.uniprot.org/core/author | "Mohyeldin M.M."xsd:string |
| http://purl.uniprot.org/citations/26543230 | http://purl.uniprot.org/core/author | "Gray A.L."xsd:string |
| http://purl.uniprot.org/citations/26543230 | http://purl.uniprot.org/core/author | "Coleman D.T."xsd:string |
| http://purl.uniprot.org/citations/26543230 | http://purl.uniprot.org/core/author | "Castore R.F."xsd:string |
| http://purl.uniprot.org/citations/26543230 | http://purl.uniprot.org/core/date | "2015"xsd:gYear |
| http://purl.uniprot.org/citations/26543230 | http://purl.uniprot.org/core/name | "Oncotarget"xsd:string |
| http://purl.uniprot.org/citations/26543230 | http://purl.uniprot.org/core/pages | "41180-41193"xsd:string |
| http://purl.uniprot.org/citations/26543230 | http://purl.uniprot.org/core/title | "Isothiocyanatostilbenes as novel c-Met inhibitors."xsd:string |
| http://purl.uniprot.org/citations/26543230 | http://purl.uniprot.org/core/volume | "6"xsd:string |
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