Inhibition of vertebrate telomerases by the triphosphate derivatives of carbocyclic oxetanocin analogs | Zendy

Hazuki Takahashi | Zendy; Ryosuke Amano | Zendy; M Saneyoshi | Zendy; Tsubasa Maruyama | Zendy; Toshiaki Yamaguchi | Zendy

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Inhibition of vertebrate telomerases by the triphosphate derivatives of carbocyclic oxetanocin analogs

Author(s) -

Hazuki Takahashi,

Ryosuke Amano,

M Saneyoshi,

Tsubasa Maruyama,

Toshiaki Yamaguchi

Publication year - 2003

Publication title -

nucleic acids symposium series

Language(s) - English

Resource type - Journals

eISSN - 1746-8272

pISSN - 0261-3166

DOI - 10.1093/nass/3.1.285

Subject(s) - vertebrate , chemistry , stereochemistry , biology , combinatorial chemistry , biochemistry , gene

Telomerase is a cellular endogenous reverse transcriptase that uses its internal RNA as a template for extension of the telomere repeat, thus maintaining telomere length. In order to clarify the susceptibility of telomerase to triphosphate derivatives of carbocyclic oxetanocins, inhibition by 9-[trans-trans-2,3-bis(hydroxymethyl)cyclobutyl]guanine triphosphate (C.OXT-GTP) and its methylene analog, 9-(cis-3-hydroxymethyl-2-methylenecyclobutyl)guanine triphosphate (m-C.OXT-GTP) was investigated. Both compounds showed potent inhibitory activity. Lineweaver-Burk plot analyses showed that the inhibition mode of these compounds was competitive with dGTP, the Ki values for C.OXT-GTP and m-C.OXT-GTP being 2.0 microM and 4.9 microM, respectively, and thus smaller than the Km of dGTP (11 microM).

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