Cov khoom

Kev cuam tshuam ntawm cov tshuaj detergents ntawm P-glycoprotein atpase kev ua haujlwm: qhov sib txawv ntawm kev cuam tshuam ntawm basal thiab verapamil-dependent kev ua ub no.

P-glycoprotein (P-gp), plasma membrane glycoprotein cuam tshuam nrog ntau hom tshuaj tiv thaiv phenotype, yog lub luag haujlwm rau ATP-dependent efflux ntawm ntau yam tshuaj amphiphilic.Siv daim nyias nyias vesicles npaj los ntawm multidrug resistant cell kab DC-3F / ADX, peb kawm cov perturbation ntawm lub basal (piv txwv li nyob rau hauv tsis muaj tshuaj) thiab verapamil-dependent P-gp ATPase cov dej num induced los ntawm ntau yam detergents, ntawm tsis-solubilizing, Raws li nyob rau hauv solubilizing, concentrations.Qhov kev loj hlob ntawm daim nyias nyias solubilization nrog nce detergent concentration tau soj ntsuam los ntawm lub teeb tawg thiab centrifugation thwmsim.Rau cov tsis-solubilizing detergent concentrations, tag nrho cov soj ntsuam detergents tshwj tsis yog DOC induced ib feem inhibition ntawm P-gp ATPase kev ua, uas tsis correlated nrog ntau npaum li cas detergents nyob rau hauv daim nyias nyias.Kev tshuaj xyuas ntawm verapamil-induced P-gp activation qhia tau hais tias P-gp ATPase kev ua ub no yog txawv modulated los ntawm ntau yam detergents ntawm non-solubilizing concentrations.Yog li, kev sib cuam tshuam tshwj xeeb ntawm P-gp thiab cov tshuaj ntxuav tes muaj feem yuav tshwm sim ntau dua li lub ntiaj teb membrane perturbation.Tom qab solubilization los ntawm ntau yam tshuaj detergents, basal P-gp ATPase kev ua tau zoo tag nrho inhibited, tshwj tsis yog nyob rau hauv lub xub ntiag ntawm CHAPS uas muaj peev xwm khaws cia cov dej num no nyob rau theem piv rau qhov ntsuas nyob rau hauv ib txwm daim nyias nyias.Txawm li cas los xij, verapamil-induced P-gp ATPase activation tau ploj thaum P-gp solubilization los ntawm CHAPS, tab sis zoo li qub tom qab dilution ntawm CHAPS hauv qab nws qhov tseem ceeb micellar concentration.Cov kev soj ntsuam no qhia txog kev sib cuam tshuam ntawm P-gp thiab CHAPS molecules hauv cov micelles sib xyaw.Ntawm qhov tod tes, peb cov ntaub ntawv pov thawj kev cuam tshuam tshwj xeeb P-gp / tshuaj ntxuav tes yog ua raws li qhov chaw ntawm cov chaw thauj tshuaj ntawm P-gp transmembrane domains.