I-Fmoc-L-Lys[Ste(OtBu)-γ-Glu-(OtBu)-AEEA-AEEA]-OH

I-Fmoc-L-Lys[Ste(OtBu)-γ-Glu(OtBu)-AEEA-AEEA]-OH

Isicelo socwaningo:
Le nhlanganisela iwukuphuma kwe-lysine eguquliwe esetshenziswa ku-peptide synthesis, ikakhulukazi ekwakheni ama-conjugates e-peptide ahlosiwe noma asebenzayo. Iqembu le-Fmoc livumela ukuhlanganiswa kwesinyathelo ngesinyathelo nge-Fmoc solid-phase peptide synthesis (SPPS). Iketango elisemaceleni lilungiswa ngokuphuma kwe-stearic acid (Ste), γ-glutamic acid (γ-Glu), nezixhumi ezimbili ze-AEEA (aminoethoxyethoxyacetate), ezihlinzeka nge-hydrophobicity, izakhiwo zokushaja, nesikhala esivumelana nezimo. Ivamise ukufundelwa indima yayo ezinhlelweni zokulethwa kwezidakamizwa, okuhlanganisa ama-antibody-drug conjugates (ADCs) kanye nama-peptide angena kumaseli.

Umsebenzi:
I-Fmoc-L-Lys[Ste(OtBu)-γ-Glu(OtBu)-AEEA-AEEA]-OH isebenza njengebhlokhi yokwakha yokwakhiwa kwama-peptide ane-lipidated anochungechunge olude noma ama-drug-linker complexes. I-stearic acid ithuthukisa ukuhlangana kwe-membrane, i-γ-Glu ithuthukisa ukuzinza nokumelana ne-enzymatic, futhi izixhumanisi ze-AEEA zinikeza ukunyibilika nokuguquguquka kwesakhiwo. Ndawonye, ​​lezi zici zenza inhlanganisela ibe yigugu ekuklameni ama-peptide ukuze kuthuthukiswe i-bioavailability, ukukhululwa okulawulwayo, nezinhlelo zokusebenza zokulethwa okuhlosiwe.