Adc zvinodhaka: concepts yematehwe emhanza uye kubhadhara kubudiswa

Linker Clavage uye payload kuburitswa mune adc zvinodhaka

Antibody - Conjugates Aya matauro anokamurwa seanoshandurwa kana asiri - kuchinjika, zvichienderana nemabatirwo avanoita musero.

Clavable Linckers

Kuchinjika Linkers kwakagadzirirwa kuve nemakemikari kusasimba, kutora mukana wemisiyano pakati peiyo yekuwedzera uye intracellular mamiriro akadai sePh mazinga uye redox inogona. Ivo vanogona zvakare kuve vakasvibiswa zvine simba mukati meRsosomes.

Chemical Clavable Linkers inonyanya kusanganisira Acid - Setting Linkers (senge persylene kana carbonate zvisungo) uye kuderedza Linkera (sekudzora zvidhori). Acid - Servilly Linkers inopwanya munzvimbo dzepidic, zvakananga muEndosomes (Ph 5.5-6.2) uye Lysosomes (pH 4.5-5.0)

Rimwe rudzi rwekiyi yemhando yekuchinjika mwenga ndeye enzyme - inokatyamadzwa nemabhonzo, iyo yakaputsika neIntracellular Hydrolytic enzymes. Pakati peizvi, peptide - Yakavakirwa Linkers inofambisa Adc zvinodhaka zvemukati kuburikidza neEndocytosis uye vimba neRysosomal Cathapsins yekuchenesa. Kazhinji Iyo GGFG Lethker inonyanya kutevera kuCathepsin L, iyo inogonesa kusunungurwa kwakazara kweDXD kubva kuAdc yayo yeADC mukati memaawa makumi manomwe nenomwe Nekudaro, zvese ggfg uye VC Linkers UnderGege neCathepsin B muRysosomes kana Endosomes yemapundu masero, anoverengera kusunungurwa kwezvinodhaka.

Kuenzaniswa neAcid - Kuchinjika uye Glutatione (Gsh) - Lincable Linker inopa kugadzikana kukuru muropa, kuderedza isina kugadziriswa kubhadhara uye kusimudzira kuchengetedzwa kwezvinodhaka. Saizvozvo, iyo VC Linker inosara yakagadzikana muPlasma uye inobudirira inoburitsa mushonga mumatumba masero, kuvimba nekuvanzika kwakanangidzirwa.

Sezvo yakachinjika linkers inosiyana mumuchina, kusarudza iyo chaiyo yekuchenesa system yakakosha yekuedza kushanda kwezvinodhaka. Zvakajairika muVitro Test Systems Kuti Uburitswe Lever Lever Homogenate Sarudzo yehurongwa zvinoenderana nemhando yemhando yekuvezwa

Kwete - Kuchinjika Linkers

Kwete Nekudaro, kushanda kwavo kunovimba zvakanyanya pakurarama kwepamusoro muTumor masero embato uye kugona kwakasimba kwemukati kwemushonga wakabatanidzwa kuti uve nechokwadi chekubhadhara zvakanaka.

Nekuti muVitro Zvidzidzo, Test Systems yakadai seyakagadziriswa chiropa, acidified chiropa s9 chidimbu, uye manosomes inogona kuita zvinobudirira degrade chikamu, kufambisa kubhadhara kubhadhara. Masisitimu aya akakosha pakuongorora iyo pharmacokinetic zvivakwa zve adcs uchishandisa isiri - inochinjika Linkers.

Keywords: Adc Linker, Payload Kuburitswa, Chombo Lossome, Lysosomal Kugadzikana, Lysosome Catabolism, Cathepsin B, DS8201A, GGFG - DXD - DXD - DXD - DXD - DXD - DXD - DXD - DXD - DXD - DXD - DXD - DXD - DXD - DXD - DXD - DXD - DXD - DXD - DXD - DXD - DXD - DXD - DXD