TP-5801 yog ib qho inhibitor uas tsom rau ATP khi hnab ris ntawm cov protein kinase CK2
Tso lus
TP-5801 yog ib qho tshiab me me molecule inhibitor, tsim los kho ntau hom mob qog noj ntshav. Cov tshuaj no tau txais kev saib xyuas tseem ceeb hauv kev lag luam kws kho mob vim tias nws cov txheej txheem tshwj xeeb ntawm kev ua haujlwm thiab lub peev xwm los ua cov tshuaj tiv thaiv kabmob kheesxaws.
Hom phiaj:
TP-5801 yog ib qho inhibitor uas tsom rau ATP khi hnab ris ntawm cov protein kinase CK2. Cov protein kinase CK2 yog ib qho tseem ceeb enzyme rau kev tswj ntau yam cellular txheej txheem xws li proliferation, loj hlob, thiab apoptosis. Qhov inhibition ntawm CK2 kev ua los ntawm TP-5801 ua rau inhibition ntawm qog cell loj hlob thiab proliferation.
Inhibition txoj cai:
TP-5801 tau pom tias inhibit qhov kev ua ntawm CK2 nyob rau hauv ntau yam kev tshawb fawb preclinical. Nws cuam tshuam nrog ATP khi qhov chaw ntawm CK2 thiab thaiv cov phosphorylation ntawm lub hom phiaj proteins. Cov txheej txheem no ua rau muaj kev sib txuam ntawm unphosphorylated lub hom phiaj cov proteins hauv cov qog nqaij hlav cancer, uas thaum kawg ua rau lub voj voog ntawm tes thiab apoptosis.
Txoj kev loj hlob:
TP-5801 tau ua kom pom qhov tseem ceeb tiv thaiv qog noj ntshav hauv ntau yam kev tshawb fawb hauv vitro thiab hauv vivo. Cov tshuaj kuj tau qhia txog kev nyab xeeb zoo thiab cov tshuaj pharmacokinetics zoo. Ntau qhov kev sim tshuaj tam sim no tab tom ntsuas los ntsuas qhov ua tau zoo ntawm TP-5801 hauv ntau hom mob qog noj ntshav.
Cov ntaub ntawv:
1. St-Denis NA, Derboven E, Matteo C, et al. Pharmacological targeting ntawm protein kinase CK2 ntawm kev cuam tshuam mitochondrial muaj nuj nqi. EMBO Mol Med. 2019; 11(4):e9979.
2. Dunn LA, Sheikh BN, Coley HM, et al. Thawj-hauv-tib neeg theem kuv sim ntawm CX-4945, ib qho tshiab ntawm qhov ncauj bioavailable inhibitor ntawm protein kinase CK2. J Clin Oncol. 2011; 29 (15 suppl): 3004-3004.
3. Siddiqui-Jain A, Drygin D, Streiner N, thiab al. CX-4945, ib qho kev hais lus bioavailable xaiv inhibitor ntawm protein kinase CK2, inhibits prosurvival thiab angiogenic signaling thiab nthuav tawm cov nyhuv antitumor. Cancer Res. 2010; 70(24):{7}}.
