MLchartDataset catalogue

TGF-beta receptor 1 kinase inhibitor SH3051

Term · Oncology and biomedicine · MLC-T-ONC-017101

An orally bioavailable, small molecule inhibitor of the serine/threonine kinase transforming growth factor-beta (TGF-beta) receptor 1 (TGFbR1; activin receptor-like kinase 5; ALK5), with potential antineoplastic and immunomodulating activities. Upon administration, TGFbR1 inhibitor SH3051 specifically targets and binds to TGFbR1, which prevents TGFbR1-mediated signal transduction. This abrogates TGFbR1-mediated immunosuppression, enhances anti-tumor immunity in the tumor microenvironment (TME) and promotes a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells leading to tumor cell death. This may lead to a reduction in TGFbR1-dependent proliferation of tumor cells. The TGF-beta signaling pathway is often deregulated in tumors and plays a key role in the regulation of cell growth, differentiation, apoptosis, motility, invasion, and angiogenesis. It plays a key role in immunosuppression in the TME and cancer cell progression.

Table 1. Record
IdentifierMLC-T-ONC-017101
FieldOncology and biomedicine
SynonymsTGFbR1 inhibitor SH3051
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-017101",
  "term": "TGF-beta receptor 1 kinase inhibitor SH3051",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable, small molecule inhibitor of the serine/threonine kinase transforming growth factor-beta (TGF-beta) receptor 1 (TGFbR1; activin receptor-like kinase 5; ALK5), with potential antineoplastic and immunomodulating activities. Upon administration, TGFbR1 inhibitor SH3051 specifically targets and binds to TGFbR1, which prevents TGFbR1-mediated signal transduction. This abrogates TGFbR1-mediated immunosuppression, enhances anti-tumor immunity in the tumor microenvironment (TME) and promotes a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells leading to tumor cell death. This may lead to a reduction in TGFbR1-dependent proliferation of tumor cells. The TGF-beta signaling pathway is often deregulated in tumors and plays a key role in the regulation of cell growth, differentiation, apoptosis, motility, invasion, and angiogenesis. It plays a key role in immunosuppression in the TME and cancer cell progression.",
  "synonyms": [
    "TGFbR1 inhibitor SH3051"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/tgf-beta-receptor-1-kinase-inhibitor-sh3051/"
}

Record 16,219 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.