| Identification | Back Directory | [Name]
clitocine | [CAS]
105798-74-1 | [Synonyms]
clitocine
N-(6-Amino-5-nitro-4-pyrimidinyl)-β-D-ribofuranosylamine
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 | [Molecular Formula]
C9H13N5O6 | [MDL Number]
MFCD00875657 | [MOL File]
105798-74-1.mol | [Molecular Weight]
287.23 |
| Hazard Information | Back Directory | [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. div> | [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. < td class="col1 fwb"> Animal 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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