Ngwaahịa

Beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) bụ ihe mgbochi siri ike nke nje ịba ọcha n'anya C (HCV) RNA njikọ na mkpụrụ ndụ Huh-7.Iji gbochie HCV NS5B RNA polymerase, PSI-6130 ga-abụrịrị phosphorylate na ụdị 5'-triphosphate.Achọpụtara phosphorylation nke PSI-6130 na mgbochi nke HCV NS5B.A tụrụ phosphorylation nke PSI-6130 site na recombinant mmadụ 2'-deoxycytidine kinase (dCK) na uridine-cytidine kinase 1 (UCK-1) site na iji mmeghachi omume spectrophotometric jikọtara ọnụ.E gosiputara PSI-6130 ka ọ bụrụ mkpụrụ maka dCK dị ọcha, nwere km nke 81 microM na kcat nke 0.007 s-1, mana ọ bụghị mkpụrụ maka UCK-1.PSI-6130 monophosphate (PSI-6130-MP) bụ nke ọma phosphorylated na diphosphate na emesia na triphosphate site recombinant mmadụ UMP-CMP kinase na nucleoside diphosphate kinase, n'otu n'otu.A mụrụ ihe mgbochi nke ụdị anụ ọhịa na mutated (S282T) HCV NS5B RNA polymerases.Mgbochi steeti na-adịgide adịgide (Ki) maka PSI-61 30 triphosphate (PSI-6130-TP) nwere ụdị enzyme anụ ọhịa bụ 4.3 microM.E nwetara nsonaazụ ndị yiri ya na 2'-C-methyladenosine triphosphate (Ki=1.5 microM) na 2'-C-methylcytidine triphosphate (Ki=1.6 microM).NS5B nwere ngbanwe S282T, nke amara na ọ na-enye iguzogide 2'-C-methyladenosine, nke PSI-6130-TP gbochiri ya nke ọma dị ka ụdị anụ ọhịa.Ntinye nke PSI-6130-MP n'ime RNA nke NS5B RNA polymerase sachara emechara butere nkwụsị agbụ.