SHP-1 agonist SC-43
Term · Oncology and biomedicine · MLC-T-ONC-016712
An orally available, small molecule agonist of Src homology region 2 domain-containing phosphatase-1 (SHP-1; tyrosine-protein phosphatase non-receptor type 6; PTPN6) with potential antineoplastic activity. Upon administration, SHP-1 agonist SC-43 enhances SHP-1 activity by impairing the association between the N-terminal Src homology 2 (N-SH2) domain and the protein tyrosine phosphatase (PTP) domain of SHP-1, triggering a conformational change of SHP-1 and relieving its autoinhibition. Activation of SHP-1 represses signal transducer and activator of transcription 3 (STAT3) signaling by inhibiting constitutive and interleukin-6 (IL-6)-induced STAT3 phosphorylation. The STAT3 pathway is overly active in many cancer types and is implicated in cancer stem cell-mediated growth, recurrence, stemness, and resistance to conventional chemotherapies.
| Identifier | MLC-T-ONC-016712 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | SC-43 oral solution |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-016712",
"term": "SHP-1 agonist SC-43",
"field": "Oncology and biomedicine",
"definition": "An orally available, small molecule agonist of Src homology region 2 domain-containing phosphatase-1 (SHP-1; tyrosine-protein phosphatase non-receptor type 6; PTPN6) with potential antineoplastic activity. Upon administration, SHP-1 agonist SC-43 enhances SHP-1 activity by impairing the association between the N-terminal Src homology 2 (N-SH2) domain and the protein tyrosine phosphatase (PTP) domain of SHP-1, triggering a conformational change of SHP-1 and relieving its autoinhibition. Activation of SHP-1 represses signal transducer and activator of transcription 3 (STAT3) signaling by inhibiting constitutive and interleukin-6 (IL-6)-induced STAT3 phosphorylation. The STAT3 pathway is overly active in many cancer types and is implicated in cancer stem cell-mediated growth, recurrence, stemness, and resistance to conventional chemotherapies.",
"synonyms": [
"SC-43 oral solution"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/shp-1-agonist-sc-43/"
}
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