Qhov sib txawv tseem ceeb ntawm nucleoside thiab nucleotide thim rov qab transcriptase inhibitors yog tias nucleoside thim rov qab transcriptase inhibitors yuav tsum tau phosphorylated los ntawm tus tswv tsev cellular kinases thaum nucleotide thim rov qab transcriptase inhibitors tsis tas yuav tsum tau pib phosphorylation.
Reverse transcriptase yog ib qho enzyme uas hloov RNA molecule rau ssDNA. HIV thiab retroviruses muaj cov enzyme no los tsim ssDNA los ntawm lawv cov RNA genome nyob rau hauv lub xov tooj ntawm tes. Yog li, nws muaj peev xwm tiv thaiv tau tus kab mob HIV thiab lwm yam retroviruses los ntawm inhibiting qhov kev ua ntawm cov reverse transcriptase enzyme, yog li tiv thaiv cov synthesis ntawm viral genomes thiab viral multiplication. Rov qab transcriptase inhibitors yog ib chav kawm ntawm cov tshuaj tiv thaiv kab mob uas siv los kho cov kab mob zoo li no. Cov tshuaj no tsom rau qhov rov qab transcriptase enzyme thiab tiv thaiv nws qhov kev ua haujlwm catalytic, thaiv cov synthesis ntawm DNA los ntawm tus kab mob RNA. Nucleoside thiab nucleotide thim rov qab transcriptase inhibitors yog ob hom tshuaj. Cov inhibitors no tseem ceeb heev, tshwj xeeb tshaj yog nyob rau hauv kev kho mob ntawm AIDS.
Nucleoside Reverse Transcriptase Inhibitors yog dab tsi?
A nucleoside yog nucleotide tsis muaj phosphate pawg. Lawv yog lub tsev blocks ntawm nucleic acids: DNA thiab RNA. Yog li, nucleosides yog cov khoom tseem ceeb thaum ua ke DNA strands. Tsis tas li ntawd, thim rov qab transcriptase ntxiv nucleosides ib qho los ntawm ib qho thiab ua ke cov DNA tshiab strand. Txhua nucleoside muaj 3'hydroxyl pawg los khi nrog cov nucleotide tom ntej ntawm phosphodiester daim ntawv cog lus. Nucleoside thim rov qab transcriptase inhibitors yog analogues ntawm ntuj nucleosides. Txawm li cas los xij, lawv tsis muaj 3 'OH pawg los tsim 5'-3' phosphodiester daim ntawv cog lus kom txuas ntxiv txoj hlua tshiab. Yog li ntawd, thaum lawv tau txuas mus rau synthesizing viral DNA saw, cov synthesis raug txiav thiab txuas ntxiv ntawm cov hlua tshiab tau tso tseg. Yog li, cov synthesis ntawm tus kab mob DNA cuam tshuam, h alting tus kab mob replication thiab multiplication txheej txheem. Thaum kawg, tus kab mob kis tsis kis hauv tus tswv tsev.
Daim duab 01: Nucleoside Reverse Transcriptase Inhibitors - Zidovudine
Ntxiv mus, nucleoside thim rov qab transcriptase inhibitors yuav tsum tau qhib los ntawm phosphorylation siv tus tswv tsev cellular kinases. Thaum ua haujlwm, lawv ua tiav nrog cov kab mob ntuj tsim nucleotides thiab khi rau qhov loj hlob strand thiab txiav qhov txuas ntxiv ntawm tus kab mob DNA. Qhov tseeb, nucleoside thim rov qab transcriptase inhibitors yog analogues ntawm ntuj purines thiab pyrimidines. Zidovudine, didanosine, stavudine, zalcitabine, lamivudine thiab abacavir yog ntau yam tshuaj uas yog nucleoside thim rov qab transcriptase inhibitors.
Nucleotide Reverse Transcriptase Inhibitors yog dab tsi?
Nucleotide thim rov qab transcriptase inhibitors yog hom thib ob ntawm cov tshuaj tiv thaiv kab mob uas siv rau hauv kev kho mob HIV thiab lwm yam kab mob retroviral. Lawv ua haujlwm raws li kev sib tw substrate inhibitors zoo ib yam li nucleoside thim rov qab transcriptase inhibitors. Ntxiv mus, tus thawj coj ntawm kev ua haujlwm tawm tsam cov kab mob kuj zoo ib yam nrog nucleoside thim rov qab transcriptase inhibitors.
Daim duab 02: Nucleotide Reverse Transcriptase Inhibitor - Adefovir
Txawm li cas los xij, ib qho sib txawv loj yog qhov nucleotide thim rov qab transcriptase inhibitors zam qhov pib phosphorylation hauv tus tswv tsev. Tab sis, lawv xav tau phosphorylation ntawm phosphonate nucleotide analogues rau hauv lub xeev phosphonate-diphosphate rau kev tiv thaiv kab mob. Tenofovir thiab Adefovir yog ob hom tshuaj uas yog nucleotide reverse transcriptase inhibitors.
Dab tsi zoo sib xws ntawm Nucleoside thiab Nucleotide Reverse Transcriptase Inhibitors?
- Nucleoside thiab nucleotide thim rov qab transcriptase inhibitors yog ob hom tshuaj tseem ceeb hauv kev kho kab mob HIV thiab kab mob rov qab.
- Ob leeg yog tshuaj tiv thaiv kab mob.
- Lawv yog cov analogues ntawm qhov tshwm sim deoxynucleotides xws li cytidine, guanosine, thymidine thiab adenosine.
- Lawv cov txheej txheem ntawm kev ua yog tib yam.
- Lawv ua haujlwm raws li kev sib tw substrate inhibitors.
- Ntxiv mus, lawv ua haujlwm raws li cov saw terminators.
- Ob hom inhibitors tsis muaj 3'OH pawg.
- Cov tshuaj no yuav ua rau muaj kev phiv xws li mob taub hau, xeev siab, ntuav, raws plab thiab teeb meem plab
Qhov txawv ntawm Nucleoside thiab Nucleotide Reverse Transcriptase Inhibitors yog dab tsi?
Qhov sib txawv tseem ceeb ntawm nucleoside thiab nucleotide thim rov qab transcriptase inhibitors yog tias cov nucleoside thim rov qab transcriptase inhibitors yuav tsum tau ua peb-kauj ruam phosphorylation los ua kom muaj kev tiv thaiv kab mob, thaum cov nucleotide thim rov qab transcriptase inhibitors tsis tas yuav tsum tau pib phosphorylation kauj ruam los qhib. lawv cov haujlwm antiviral. Tsis tas li ntawd qhov sib txawv no, ob hom tshuaj qhia zoo sib xws hauv lub hauv paus ntsiab lus ntawm kev ua, kev mob tshwm sim, qauv, thiab lwm yam.
Summary – Nucleoside vs Nucleotide Reverse Transcriptase Inhibitors
Nucleoside thiab nucleotide thim rov qab transcriptase inhibitors yog ob hom tshuaj tiv thaiv kab mob uas pab kho AIDS thiab lwm yam kab mob retroviral. Lawv inhibit lub catalytic muaj nuj nqi ntawm tus kab mob rov qab transcriptase enzyme los ntawm kev ua raws li kev sib tw substrate inhibitors. Ob leeg tso tseg cov synthesis ntawm cov kab mob DNA loj hlob. Tsis tas li ntawd, lawv yog cov analogues ntawm ib txwm tshwm sim deoxyribonucleotides. Tab sis lawv tsis muaj 3 'OH pawg los tsim phosphodiester daim ntawv cog lus nrog cov nucleotide tom ntej. Qhov sib txawv tseem ceeb ntawm nucleoside thiab nucleotide thim rov qab transcriptase inhibitors yog thawj phosphorylation los ua kom muaj kev tiv thaiv kab mob. Hauv qhov no, nucleoside thim rov qab transcriptase yuav tsum tau ua peb kauj ruam phosphorylation thaum nucleotide thim rov qab transcriptase inhibitors bypass thawj phosphorylation.
