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SETDB1 antisense oligonucleotide
- Development stage
- Preclinical
- Modality
- Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Modified DNA Oligonucleotides → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Single-strand DNA → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics
- Administration
- Intravenous, Subcutaneous, Intrathecal, Ophthalmic, Intranasal
01
Overview
SETDB1 antisense oligonucleotide is an experimental RNA-based therapeutic designed to silence the expression of the SETDB1 (SET domain bifurcated histone lysine methyltransferase 1) gene. SETDB1 is an epigenetic enzyme that is frequently overexpressed in various malignancies, including prostate cancer, where it protects phosphorylated retinoblastoma (RB) protein from TRIM28-mediated ubiquitination and proteasomal degradation. This protection is independent of SETDB1's methyltransferase activity. By utilizing an antisense mechanism to reduce SETDB1 mRNA levels, this oligonucleotide promotes the degradation of p-RB and inhibits tumor growth. Research indicates that while SETDB1 inhibition can be effective as a monotherapy, its combination with CDK4/6 inhibitors like palbociclib may provide superior anticancer efficacy by preventing the loss of RB protein and maintaining its tumor-suppressive functions.
- Other names
- SETDB1 ASOSETDB-1 ASOSETDB 1 ASO
02
Targets
SETDB1
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