Pub. Date : 2014 Aug 15
PMID : 25071018
12 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | SHP-1 is a target of regorafenib in colorectal cancer. | regorafenib | protein tyrosine phosphatase non-receptor type 6 | Homo sapiens |
| 2 | However, little is known about the mechanism regarding regorafenib affects SHP-1 tyrosine phosphatase activity and leads to apoptosis and tumor suppression in CRC. | regorafenib | protein tyrosine phosphatase non-receptor type 6 | Homo sapiens |
| 3 | Here, we found that regorafenib triggered apoptotic cell death and significantly enhanced SHP-1 activity, which dramatically decreased the phosphorylated form of STAT3 at Tyr705 (p-STAT3(Tyr705)). | regorafenib | protein tyrosine phosphatase non-receptor type 6 | Homo sapiens |
| 4 | Importantly, regorafenib augmented SHP-1 activity by direct disruption of the association between N-SH2 and catalytic PTP domain of SHP-1. | regorafenib | protein tyrosine phosphatase non-receptor type 6 | Homo sapiens |
| 5 | Importantly, regorafenib augmented SHP-1 activity by direct disruption of the association between N-SH2 and catalytic PTP domain of SHP-1. | regorafenib | protein tyrosine phosphatase non-receptor type 6 | Homo sapiens |
| 6 | Deletion of the N-SH2 domain (dN1) or point mutation (D61A) of SHP-1 blocked the effect of regorafenib-induced SHP-1 activity, growth inhibition and a decrease of p-STAT3(Tyr705) expression, suggesting that regorafenib triggers a conformational change in SHP-1 by relieving its autoinhibition. | regorafenib | protein tyrosine phosphatase non-receptor type 6 | Homo sapiens |
| 7 | Deletion of the N-SH2 domain (dN1) or point mutation (D61A) of SHP-1 blocked the effect of regorafenib-induced SHP-1 activity, growth inhibition and a decrease of p-STAT3(Tyr705) expression, suggesting that regorafenib triggers a conformational change in SHP-1 by relieving its autoinhibition. | regorafenib | protein tyrosine phosphatase non-receptor type 6 | Homo sapiens |
| 8 | Deletion of the N-SH2 domain (dN1) or point mutation (D61A) of SHP-1 blocked the effect of regorafenib-induced SHP-1 activity, growth inhibition and a decrease of p-STAT3(Tyr705) expression, suggesting that regorafenib triggers a conformational change in SHP-1 by relieving its autoinhibition. | regorafenib | protein tyrosine phosphatase non-receptor type 6 | Homo sapiens |
| 9 | Deletion of the N-SH2 domain (dN1) or point mutation (D61A) of SHP-1 blocked the effect of regorafenib-induced SHP-1 activity, growth inhibition and a decrease of p-STAT3(Tyr705) expression, suggesting that regorafenib triggers a conformational change in SHP-1 by relieving its autoinhibition. | regorafenib | protein tyrosine phosphatase non-receptor type 6 | Homo sapiens |
| 10 | In vivo assay showed that regorafenib significantly inhibited xenograft growth and decreased p-STAT3(Tyr705) expression but induced higher SHP-1 activity. | regorafenib | protein tyrosine phosphatase non-receptor type 6 | Homo sapiens |
| 11 | Collectively, regorafenib is a novel SHP-1 agonist exerts superior anti-tumor effects by enhancing SHP-1 activity that directly targets p-STAT3(Tyr705). | regorafenib | protein tyrosine phosphatase non-receptor type 6 | Homo sapiens |
| 12 | Collectively, regorafenib is a novel SHP-1 agonist exerts superior anti-tumor effects by enhancing SHP-1 activity that directly targets p-STAT3(Tyr705). | regorafenib | protein tyrosine phosphatase non-receptor type 6 | Homo sapiens |