ADC Forms: Cov Ntsiab Lus ntawm Linker Cleavage thiab PayDload tso tawm

Linker Cleavage thiab PayDload tso tawm hauv ADC cov tshuaj

Tshuaj tiv thaiv - Cov tshuaj sib txuas (ADCS) cia siab rau cov txuas tshwj xeeb uas txuas cov tshuaj tiv thaiv kom me - molecule toxin payloads. Cov kab ntawv txuas no tau faib ua ke li cleavable lossis tsis - tsuas yog -

Cleavable Linkers

Cleavable Linkers yog tsim los siv tshuaj tsis khov, siv kom zoo dua ntawm cov sib txawv ntawm cov khoom sib txawv xws li pH theem thiab cov peev xwm redeb. Lawv kuj tseem tuaj yeem ua rau muaj kev cuam tshuam tsis raws li Lysosomes.

Tshuaj chructically cleavable Lillers feem ntau nrog rau acid - refillers (xws li cov ntawv sib txawv lossis cov txhab nyiaj rov qab (xws li kev cuam tshuam nrog kev cuam tshuam). Acid - Lub neej ua ke tawg hauv cov acidic ib puag ncig, tshwj xeeb nyob rau endosomes (PH 5.5-5.0), ua rau cov nyiaj tso tawm.

Lwm qhov tseem ceeb tshaj plaws txuas yog lub enzyme - rhiab linker, uas tau tawg los ntawm inracellular hydolytic enzymes. Ntawm cov no, peptide - Raws Linters pab txhawb ADC cov tshuaj sab hauv ntawm Endocytosis thiab cia rau ntawm Lysosomal Cathepsins rau Cleavage. Cov enzyme - Rhiab txuas nrog nrog GGFG (Gly - Gly - Phe - Gly) thiab VC (VIT - CAPPERS. Lub GGFG Linker yog tshwj xeeb tshwj xeeb rau Cathlsin L, uas ua rau qhov kev tso tawm ntawm DXD los ntawm 72 teev, thaum Catchepsin B cov khoom ua haujlwm tsawg kawg ntawm cov txheej txheem no. Txawm li cas los xij, ob qho tib si ggfg thiab VC cov ntsiab lus dhau los ntawm cathepsin b hauv lysosomsin b hauv Lysosomes lossis endosomes ntawm cov qog nqaij hlav.

Piv rau acid - cerveavable thiab glutathione (GHSE) (GGFG Linkers muaj kev ruaj khov ntau dua nyob rau hauv cov ntshav, txo cov kev nyab xeeb thiab siv tshuaj yeeb. Ib yam li ntawd, VC cov neeg txuas tseem ruaj khov hauv ntshav thiab cov tshuaj tau zoo tshaj plaws hauv cov tshuaj qog cov khoom xa tuaj.

Txij li cov kab sib txawv ntawm cov kab sib txawv ntawm kev ua tshuab, xaiv txoj cai cleavage system yog qhov tseem ceeb rau kev ntsuas tshuaj kom zoo. Feem ntau hauv cov tshuab kev ntsuas vitro rau cov nyiaj tso tawm siv tau muaj acidsins b, m, thiab l, gluacuronidase, gsh), thiab legumain. Qhov kev xaiv ntawm cov kab ke yog nyob ntawm hom kev sib txuas ua kev ntsuas

Tsis - Cleavable Liners

Tsis yog - cleavable Lillers yog nyob ntawm cov kev tiv thaiv tiav ntawm Cytopasmic by Cytopodasmic thiab lysosomal tiv thaiv, thaum kawg tso cov payload uas txuas rau cov khoom tiv thaiv antibdodation. Txawm li cas los xij, lawv cov txiaj ntsig kev cia siab rau ntau cov antigen qhia nyob rau hauv cov qog nqaij hlav uas muaj peev xwm sib txuam ntawm cov tshuaj sib piv los ua kom muaj txiaj ntsig zoo.

Rau hauv kev tshawb fawb veno, sim cov qauv xws li acidifify homogenate, Acidosomes lub siab s antibodation, facilitating appload. Cov kab ntawv no yog qhov tseem ceeb rau kev ntsuas cov khoom siv tshuaj ntawm adcs uas tsis siv cov peev txheej -

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