MEK1/2 inhibitor PAS-004
Term · Oncology and biomedicine · MLC-T-ONC-015070
An orally bioavailable macrocyclic inhibitor of mitogen-activated protein kinase kinase (MAP2K, MAPK/ERK kinase, or MEK) 1 and 2, with potential antineoplastic activity. Upon oral administration, MEK1/2 inhibitor PAS-004 selectively and allosterically binds to and inhibits the activity of MEK1 and MEK2, preventing the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1/2 are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway that regulates cell growth. This pathway is often dysregulated in a variety of tumor cell types through BRAF, KRAS and NRAS mutations.
| Identifier | MLC-T-ONC-015070 |
|---|---|
| Field | Oncology and biomedicine |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-015070",
"term": "MEK1/2 inhibitor PAS-004",
"field": "Oncology and biomedicine",
"definition": "An orally bioavailable macrocyclic inhibitor of mitogen-activated protein kinase kinase (MAP2K, MAPK/ERK kinase, or MEK) 1 and 2, with potential antineoplastic activity. Upon oral administration, MEK1/2 inhibitor PAS-004 selectively and allosterically binds to and inhibits the activity of MEK1 and MEK2, preventing the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK1/2 are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway that regulates cell growth. This pathway is often dysregulated in a variety of tumor cell types through BRAF, KRAS and NRAS mutations.",
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/mek1-2-inhibitor-pas-004/"
}
Record 10,779 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.