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Ribosomal protein S6 kinase A1 (RPS6KA1)
- Target
- RPS6KA1
- Molecular classification
- Enzyme, Serine/threonine protein kinase, Kinase (RSK subfamily: ribosomal protein S6 kinase A1)
01
Overview
Ribosomal protein S6 kinase A1 is a member of the RSK family of serine/threonine kinases, encoded by the RPS6KA1 gene in humans. This kinase contains two nonidentical catalytic domains and phosphorylates various intracellular substrates, including components of the MAPK/ERK signaling pathway, ribosomal proteins, and key transcription factors such as CREB, ERα, and c-Fos. RPS6KA1 plays a central role in regulating cellular processes like growth, differentiation, proliferation, and survival. Its dysregulation has been linked to cancer and drug resistance, making it an important therapeutic target for small molecule kinase inhibitors and a biomarker for response/resistance in oncology and other pathologies.
- Other names
- Ribosomal protein S6 kinase alpha-1p90RSKRSK1Ribosomal protein S6 kinase, 90kDa
02
Mechanism of action
Inhibition of kinase activity: Small molecule inhibitors like BI-D1870 inhibit RPS6KA1/p90RSK by blocking serine/threonine phosphorylation activity. Modulation of cell survival and growth signaling: Resistance mechanisms involve targeting downstream signaling, such as with venetoclax/azacitidine in leukemia.
03
Biological functions
Signal transduction (especially in the MAPK/ERK pathway)Cell growthCell differentiationRegulation of transcription factorsControl of cell cyclePhosphorylation of multiple substrates (e.g., ribosomal protein S6, CREB, ERα, c-Fos, and others)
04
Disease associations
Cancer (including roles in acute myeloid leukemia resistance)Neurodevelopmental disorders (e.g., related to mutations in related family members)Other: Cell proliferation linked to various diseases
05
Safety considerations
Potential challenges include off-target effects and resistance to kinase inhibitorsInhibition of RPS6KA1 may affect essential signaling pathways, impacting cell proliferation and survival
06
Interacting drugs
BI-D1870
1 more in the full profile.
07
Biomarkers
RPS6KA1 overexpression or phosphorylation status may indicate aberrant cell growth or treatment resistance (e.g., in AML)
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