It is an antisense oligonucleotide (ASO) targeting clusterin expression. (wikipedia.org)
Custirsen (OGX-011) is a second-generation, 2′-methoxyethyl-modified phosphorothioate antisense oligonucleotide that inhibits clusterin expression. (medscape.com)
Prostate cancer1
[ 76 ] In prostate cancer, clusterin overexpression is associated with a high Gleason score and has been detected in patients with mCRPC after neoadjuvant hormone therapy. (medscape.com)
Gene2
Custirsen acts as an anti-cancer drug by binding to the mRNA initiation site of the clusterin gene, reducing clusterin protein plasma concentrations. (wikipedia.org)
The synthetic addition of a 2'-methoxyethyl on each nucleotide bookending the phosphorothioate backbone causes: An increased affinity for the RNA54 targeted gene sequence An increased resistance to digestive nucleases Decreased toxicity Increased tissue half-life by approximately seven days Decrease adverse side effects, enabling more potent concentrations Clusterin is upregulation in many tumours including prostate, breast, non-small cell lung, ovary and colorectal. (wikipedia.org)
Decrease1
The results found that the recommended dose of Custirsen was 640 mg, with maximum decrease of clusterin blood plasma occurring at this dose. (wikipedia.org)
Expression1
3. Clusterin promotes growth and invasion of clear cell renal carcinoma cell by upregulation of S100A4 expression. (nih.gov)
Protein3
The anti-apoptotic activity of clusterin in aiding tumour growth is due to interactions with protein complexes. (wikipedia.org)
Clusterin is an ATP-independent cytoprotective and antiapoptotic chaperone protein that inhibits protein precipitation and aggregation in order to preserve protein function during cellular stress. (medscape.com)
Proteomic analysis showed significant upregulation of six 14-3-3 protein isoforms in hypertrophied cardiomyocytes compared to those in control cells. (bmbreports.org)
Interactions1
BACKGROUND: Clusterin and transient receptor potential melastatin 2 (TRPM2) play significant roles in acute myocardial infarction (AMI), but their interactions in AMI are unclear. (bvsalud.org)
Significant1
Our CR diet elicits significant prevention of oxidative damages with the upregulation of antioxidant defenses (levels of glutathione [GSH], mRNAs of clusterin and of three key antioxidant enzymes) as compared to age-matched AL controls, in a strikingly region-specific pattern. (hal.science)