ABT-888

Veliparib yog dab tsi

ABT-888, tseem hu ua Veliparib, yog hmoov dawb. Veliparib yog ib qho muaj zog PARP1 thiab PARP2 inhibitor nrog Ki ntawm 5.2 nM thiab 2.9 nM, raws li, uas inhibits SIRT2. Theem 3. Veliparib zoo inhibits PARP, nrog rau Ki qhov tseem ceeb ntawm 5.2 thiab 2.9 nM rau PARP-1 thiab PARP{13}}, raws li. Veliparib txo cov ciaj sia ntawm cloned noob thiab inhibits DNA kho hauv lub ntsws H460 hlwb. Veliparib inhibits C41 hlwb nrog EC50 ntawm 2nM. Kev sib xyaw ntawm Veliparib thiab hluav taws xob txo cov qog angiogenesis. Xi'an Sonwnu muab ntau Veliparib, thiab yog tias koj xav yuav lawv, koj tuaj yeem tiv tauj Xi'an Sonwnu yam tsis muaj kev cuam tshuam.

COA

Qhov twg yuav Veliparib

Xi'an Sonwu Biotech Co. ltd, cov khoom tsim tau nruj me ntsis tswj nyob rau hauv zoo txij thaum pib ntawm cov khoom raw hmoov. Hauv kev tsim cov khoom lag luam, peb ua txhua yam kom zoo thiab pab peb cov neeg siv khoom kom tau txais cov khoom lag luam zoo. Ntau tus neeg siv khoom tau muab cov lus pom zoo rau peb cov khoom tom qab tau txais cov khoom.

Txhawm rau kom ntseeg tau cov khoom zoo, peb tuaj yeem muab cov qauv rau kev kuaj. Ntawm no yog qhov ntau.

Cov neeg siv khoom zoo lus

Dab tsi yog PARP Inhibitors
1. Cov txheej txheem tseem ceeb ntawm DNA kev puas tsuaj kho
DNA yog cov khoom siv tseem ceeb tshaj plaws rau kev ua haujlwm ntawm tes, thiab tswj kev ncaj ncees thiab kev ruaj ntseg ntawm nws cov qauv molecular yog qhov tseem ceeb tshaj plaws rau kev ciaj sia ntawm tes thiab kev ua haujlwm ntawm lub cev. Cov DNA ntawm cov hlwb hauv tib neeg lub cev muaj ntau hom kev puas tsuaj txhua hnub, yog li cov kev puas tsuaj no yuav tsum tau kho kom haum rau lub sijhawm kom ntseeg tau tias kev ua haujlwm tsis tu ncua ntawm tib neeg lub cev. Yog li ntawd, cov hlwb tau tsim cov txheej txheem ntawm cov txheej txheem nyuaj thiab meej los daws cov kev puas tsuaj no, feem ntau suav nrog kev sib tsoo ib leeg, kev tsis sib haum xeeb, lub hauv paus puas, ob-strand so, inter-strand cross-links, intra-strand cross-links. , thiab lwm yam kev puas tsuaj.

Thaum DNA muaj cov kev puas tsuaj saum toj no, lub xov tooj ntawm tes tuaj yeem pib rau 6 txoj hauv kev kho kom zoo nrog ntau hom kev puas tsuaj:

(1) Txoj kev kho ncaj qha (DR) kho qhov kev puas tsuaj los ntawm O6-alkylguanine

(2) Base excision kho (BER) txoj hauv kev, phiaj xwm kev puas tsuaj los ntawm redox lossis alkylation

(3) Nucleotide excision kho (NER) txoj hauv kev, uas kho qhov kev puas tsuaj ntawm qib nucleotide tshwm sim los ntawm hluav taws xob, tshuaj siv tshuaj, lossis protein-DNA cross-linking

(4) Kev kho lub hauv paus tsis sib haum (kev kho tsis haum, MMR) txoj hauv kev, kho cov hauv paus tsis sib haum

(5) Homologous recombination kho (HR)

(6) Non-homologous end joining (NHEJ)

2. DNA puas kho thiab tumorigenesis
①. DNA puas kho tsis xws luag tsav tumorigenesis
Piv nrog rau cov ntaub so ntswg ib txwm muaj, hyperplasia, dysplasia, thiab qog cov ntaub so ntswg muaj kev puas tsuaj DNA ntau dua, ntau dua kev loj hlob, inactivation ntawm apoptosis gene P53, thiab ua kom cov noob tsav tsheb, ua rau muaj zog DNA replication siab thiab DNA puas, tshwj xeeb tshaj yog ob chav DNA puas tsub kom. . Ntawm ib sab, DNA kev puas tsuaj kho mechanism yog qhib los ntawm kev puas tsuaj xws li ATM thiab ATR, thiab cov qog suppressor noob P53 yog qhib kom induce apoptosis; Ntawm qhov tod tes, qhov sib sau ntawm DNA puas ua rau genome tsis ruaj khov thiab ua rau cov qog nqaij hlav tshiab Gene hloov, uas nws thiaj li tsim los ntawm cov nqaij mos mus rau mob qog noj ntshav.

②.Drug-targeted therapy ntawm DNA puas receptor protein
DDR yog qhov tseem ceeb rau kev ua kom txoj hauv kev kho thiab kev muaj sia nyob ntawm tes. DDR sensor protein uas teb rau ntau yam DNA puas tsuaj yog tus yuam sij rau kev pib kho, thiab PARP-1 yog qhov tseem ceeb DNA puas sensor protein.
③. Kev siv tshuaj kho mob rau DNA kev puas tsuaj rau cov proteins
DDR signaling proteins ua rau muaj ntau yam kev hloov pauv tom qab kev hloov pauv thiab sib sau ua ke ntawm cov protein ntau uas nthuav dav thiab nthuav tawm cov cim DNA puas tsuaj kom cov lus teb tsim nyog tuaj yeem pib thiab tuaj yeem suav nrog: kev hloov pauv hloov pauv, ua kom lub voj voog ntawm tes, lwm qhov sib txuas, kev koom tes ntawm DNA Kho cov txheej txheem, los yog cov ntsiab lus ntawm kev puas tsuaj loj, qhib cellular senescence thiab apoptotic txoj kev. Cov proteins tseem ceeb ntawm cov tshuaj tshiab tsom rau txoj hauv kev no yog DNA-PK, ATM, ATR, CHK1, thiab WEE1.

④. DNA kev puas tsuaj teb (DDR) sib koom ua ke zoo
Hauv ntau hom kab mob, qhov twg muaj peev xwm los teb tau zoo rau DNA kev puas tsuaj feem ntau ploj, DDR inhibitors tuaj yeem siv ua ke nrog cov tshuaj uas tsom mus rau lwm yam DDR cov proteins lossis cov kev taw qhia sib txawv los thaiv txoj hauv kev uas cov kab mob muaj sia nyob. Ntau txoj kev.

Dab tsi yog PARP Inhibitors siv rau

1. Synthetic lethal therapy

Feem ntau muaj ob hom DNA molecular puas tsuaj, ib qho yog DNA ib leeg-strand so, thiab lwm yam yog DNA ob-strand so. Thaum tib txoj hlua ntawm DNA molecule puas lawm, nws tsuas yog kho los ntawm poly ADP-ribose polymerase (PARP), XCCR1, thiab DNA ligase IIIa.

Lub mechanism ntawm kev txiav txim ntawm PARP:Yog tias PARP noob raug txwv, BRCA noob hloov pauv hauv tus neeg mob lub cev yuav tiv thaiv homologous recombination kho los ntawm kev ua haujlwm ib txwm ua thiab nws thiaj li ua rau cell apoptosis. Yog li ntawd, BRCA thiab PARP ua tau raws li lub ntsiab lus ntawm hluavtaws lethality. Thaum BRCA noob hloov pauv, txoj hauv kev kho DNA yuav nyob ntawm PARP-1 enzyme, thiab PARP inhibitors yuav tiv thaiv DNA kho thiab, thaum kawg, apoptosis. Cov neeg mob siv PARP inhibitors yuav tsum tua lub luag haujlwm ntawm cov qog. Txawm li cas los xij, nyob rau hauv lub xub ntiag ntawm BRCA nyob rau hauv ib txwm hlwb, DNA tseem tuaj yeem kho kom cov hlwb muaj sia nyob, yog li PARP inhibitors tuaj yeem siv los ua cov tshuaj tsom mus tua BRCA mutant hlwb xaiv.

2. Lub peev xwm ntawm PARP-1 inhibitors los ntes PARP-1 muaj txiaj ntsig zoo nrog nws cov haujlwm hauv inhibiting qog hlwb

Lub mechanism ntawm kev txiav txim ntawm PARP:PARP inhibitors yog nicotinamide adenine dinucleotide (NAD plus) analogs, thiab lawv cov txheej txheem molecular ntawm kev ua haujlwm yog inhibit qhov kev ua ntawm PARP enzymes los ntawm kev khi rau qhov chaw nquag ntawm catalytic domain ntawm PARP enzymes los ntawm kev sib tw nrog NAD ntxiv.

(1) PARP-1 inhibitors khi rau CAT (catalytic domain, C-terminal catalytic domain) ntawm PARP-1 kev sib tw, inhibit nws txoj haujlwm catalytic, thiab tiv thaiv SSB (ib leeg-strand so, ib leeg-strand so) los ntawm kev kho nyob rau lub sijhawm, Tsim DSB (ob-strand so, ob-strand so);

(2) PARP-1 inhibitors tuaj yeem cuam tshuam PARP-1's PAR (poly ADP ribosylation, poly-ADP ribosylation) hloov kho, ua ke nrog CAT ua rau PARP-1 allosteric, thiab txhim khu kev khi lub zog ntawm PARP-1 kom puas DNA, "capturing" PARP-1 ntawm cov DNA puas, ua rau nws nyuaj rau lwm yam PARP-1 nyob rau hauv lub nucleus los ua ke nrog cov DNA puas, ntxiv thaiv cov ua tau kho txoj kev ntawm DSB, thiab txhawb cell apoptosis.

Ua liABT-888Muaj kev nyab xeeb thiab ua tau zoo

Thaum Lub Xya Hli 2021, "Lung Cancer" tau tshaj tawm qhov kev ntsuam xyuas ntawm kev ua tau zoo ntawm veliparib ua ke nrog platinum-based radiotherapy thiab chemotherapy hauv kev kho cov neeg mob nrog theem III uas tsis yog mob qog noj ntshav me me. Cov kev kho mob rau theem III NSCLC suav nrog kev phais, kws khomob, thiab kev kho hluav taws xob. Tus 3- xyoo PFS tus nqi thiab OS tus nqi ntawm cov neeg mob tom qab tus qauv siv hluav taws xob kho mob thiab kws khomob tsuas yog 16 feem pua ​​thiab 24 feem pua ​​; Raws li RTOG0617 txoj kev tshawb fawb, kev siv hluav taws xob sib txuas thiab kev siv tshuaj khomob tuaj yeem ua tiav cov txiaj ntsig zoo, tab sis tsuas yog 12 lub hlis ntawm PFS. Yog li, cov neeg mob uas muaj theem III NSCLC sai sai xav tau tus qauv kho kom zoo dua.

Ntau qhov kev tshawb fawb soj ntsuam tau lees paub tias veliparib ua ke nrog cov tshuaj khomob muaj kev nyab xeeb tshwj xeeb thiab ua haujlwm zoo hauv kev kho mob qog noj ntshav, mob qog noj ntshav, mob qog noj ntshav mis, melanoma, thiab lwm yam qog nqaij hlav. Ib theem II randomized txoj kev tshawb fawb ntawm qib siab NSCLC pom tias veliparib ua ke nrog CP (carboplatin plus paclitaxel) tuaj yeem txhim kho txoj sia nyob ntawm cov neeg mob; Hauv kev tshawb fawb yooj yim, veliparib tuaj yeem ua rau kom cov ionizing hluav taws xob-induced DNA ob-strand lov ua rau kev loj hlob qeeb hauv xenografts hauv nas.

Ib qho ntawm cov qauv kev kho mob tam sim no rau kev kho tsis tau theem III NSCLC yog ib qho kev kho mob chemoradiotherapy ua ke nrog kev sib koom ua ke chemotherapy (chemotherapy feem ntau xaiv CP regimen). Platinum tuaj yeem ua rau muaj kev puas tsuaj DNA, thiab veliparib tuaj yeem cuam tshuam DNA kev puas tsuaj. Yog li ntawd, peb speculate. Kev sib xyaw ua ke ntawm veliparib nrog tus qauv chemoradiotherapy ua raws li kev siv tshuaj khomob sib sau ua ke tuaj yeem txhim kho kev ciaj sia nyob rau theem III uas tsis tuaj yeem kho tau NSCLC. Yog li, kev nyab xeeb thiab kev ua tau zoo ntawm veliparib ua ke nrog chemoradiotherapy raug soj ntsuam nyob rau theem no kuv kawm hauv cov neeg mob uas tsis tuaj yeem kho tau theem III NSCLC. Veliparib ua ke nrog cov txheej txheem sib xyaw ua ke chemoradiotherapy ua raws li kev siv tshuaj khomob sib koom ua ke hauv cov neeg mob uas muaj theem III tsis tuaj yeem kho NSCLC muaj kev mob toxicity thiab ua haujlwm tau zoo, nrog mPFS txog 19.6m.

Hoobkas ib puag ncig

1. Xi'an Sonwu Biotech Co., Ltd muaj lub Hoobkas nrog txaus Tshuag. Tsis tas li ntawd, lub tuam tsev tsim khoom ntawm Xi'an Matsuya yog huv si thiab huv si. Siv cov khoom siv ntau lawm, cov kws tshawb fawb txuas ntxiv tsim cov khoom tshiab kom tau raws li cov neeg siv khoom xav tau.

2. Xi'an Sonwu Biotech Co., Ltd muaj cov cuab yeej ntsuas qib siab thiab cov neeg ua haujlwm kuaj, uas tau tsim lub hauv paus ruaj khov rau kev muab cov neeg siv khoom nrog cov ntaub ntawv raug thiab siv tau.

Daim ntawv pov thawj

Ntim

Tsis ntev los no Logistics

Tsuas yog lav cov khoom lag luam, lwm qhov tseem ceeb tshaj plaws yog cov neeg siv khoom tuaj yeem tau txais cov khoom zoo. Yog li, Xi'an Sonwu muab txhua yam kev xa khoom raws li qhov xav tau sib txawv.

FAQ

Yuav ntim thiab khaws cia li casABT-888?

Ntim: export qib ntim nruas, lub tshuab nqus tsev ntim aluminium foil ntim, kuj tuaj yeem ntim raws li cov neeg siv khoom xav tau.

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Yog tias koj xav yuav Veliparib, thov hu rau Xi'an Sonwu.

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