clitocine
clitocine Basic information
- Product Name:
- clitocine
- Synonyms:
-
- clitocine
- b-D-RibofuranosylaMine, N-(6-aMino-5-nitro-4-pyriMidinyl)-
- β-D-Ribofuranosylamine, N-(6-amino-5-nitro-4- pyrimidinyl)-
- N-(6-Amino-5-nitro-4-pyrimidinyl)-beta-D-ribofuranosylamine
- N-(6-Amino-5-nitro-4-pyrimidinyl)-β-D-ribofuranosylamine
- N-?(6-?amino-?5-?nitro-?4-?pyrimidinyl)?-β-?D-?Ribofuranosylamine
- CAS:
- 105798-74-1
- MF:
- C9H13N5O6
- MW:
- 287.231
- Mol File:
- 105798-74-1.mol
clitocine Chemical Properties
- form
- Solid
- color
- White to off-white
clitocine Usage And Synthesis
Uses
Clitocine, an adenosine nucleoside analog isolated from mushroom, is a potent and efficacious readthrough agent. Clitocine acts as a suppressor of nonsense mutations and can induce the production of p53 protein in cells harboring p53 nonsense-mutated alleles. Clitocine can induce apoptosis in multidrug-resistant human cancer cells by targeting Mcl-1. Anticancer activity[1][2].
Definition
ChEBI: Clitocine is a N-glycosyl compound.
Biological Activity
Clitocine, an adenosine nucleoside analog derived from mushrooms, is a potent readthrough. As an inhibitor of nonsense mutations, it can induce the production of p53 protein in cells carrying p53 nonsense mutant alleles. It induces apoptosis in multidrug-resistant tumor cells by targeting Mcl-1. Has anticancer activity.
in vitro
Clitocine incorporation into mRNA is required for premature stop codon readthrough activity, and the presence of clitocine at the third position of a premature stop codon is sufficient to promote robust readthrough.
Clitocine (0-0.8 μM ; 24 hours) enhances TRAIL-lethality in in LS411N and SW620 cells. It (0.2μM; 36 hours) significantly potentiates TRAIL-mediated apoptosis.
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in vivo
Citocine (0.3-3 mg/kg; sc; five times per week)-induced p53 inhibits CAOV-33 p53-UAA136 tumor growth in a xenograft model.
| nu/nu mice (CAOV-3p53-UAA136 xenograft tumors) | |
| Dosage: | 0.3, 3 mg/kg (or 20 mg/kg once per week) |
| Administration: | Sc; five times per week |
| Result: | CAOV-33 p53-UAA136 tumor growth was inhibited. |
References
[1] Friesen WJ, et al. The nucleoside analog clitocine is a potent and efficacious readthrough agent. RNA. 2017;23(4):567-577. DOI:10.1261/rna.060236.116
[2] Sun JG, et al. Clitocine potentiates TRAIL-mediated apoptosis in human colon cancer cells by promoting Mcl-1 degradation. Apoptosis. 2016;21(10):1144-1157. DOI:10.1007/s10495-016-1273-y
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