dual IRAK1/4 inhibitor R906289 monosodium
Term · Oncology and biomedicine · MLC-T-ONC-013176
An orally bioavailable, monosodium salt form of R906289, a prodrug of R835, a small molecule inhibitor of interleukin-1 receptor-associated kinases 1 (IRAK1) and 4 (IRAK4), with potential immunomodulating and anti-inflammatory activities. Upon oral administration, R906289 is converted to its active metabolite R835. R835 targets, binds to, and inhibits the activity of IRAK1 and IRAK4. This inhibits lipopolysaccharide (LPS)/Toll-like receptor 4 (TLR4) signaling and LPS/TLR4-induced proinflammatory cytokine production. This may inhibit inflammation and immune-mediated cell destruction in inflammatory and auto-immune diseases where TLR or interleukin 1 receptor (IL-1R) signaling is overactivated. IRAK1 and IRAK4, serine/threonine-protein kinases, play key roles in signaling downstream of TLR and IL-1R, and TLR/IL-1R-induced production of proinflammatory cytokines.
| Identifier | MLC-T-ONC-013176 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | IRAK1/4 inhibitor R289 Na; R289 Na; R906289 monosodium |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-013176",
"term": "dual IRAK1/4 inhibitor R906289 monosodium",
"field": "Oncology and biomedicine",
"definition": "An orally bioavailable, monosodium salt form of R906289, a prodrug of R835, a small molecule inhibitor of interleukin-1 receptor-associated kinases 1 (IRAK1) and 4 (IRAK4), with potential immunomodulating and anti-inflammatory activities. Upon oral administration, R906289 is converted to its active metabolite R835. R835 targets, binds to, and inhibits the activity of IRAK1 and IRAK4. This inhibits lipopolysaccharide (LPS)/Toll-like receptor 4 (TLR4) signaling and LPS/TLR4-induced proinflammatory cytokine production. This may inhibit inflammation and immune-mediated cell destruction in inflammatory and auto-immune diseases where TLR or interleukin 1 receptor (IL-1R) signaling is overactivated. IRAK1 and IRAK4, serine/threonine-protein kinases, play key roles in signaling downstream of TLR and IL-1R, and TLR/IL-1R-induced production of proinflammatory cytokines.",
"synonyms": [
"IRAK1/4 inhibitor R289 Na",
"R289 Na",
"R906289 monosodium"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/dual-irak1-4-inhibitor-r906289-monosodium/"
}
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