Fmoc-L-Lys[Ste(OtBu)-γ-Glu(OtBu)-AEEA-AEEA]-OH
Noi noiʻi:
ʻO kēia pūhui he lysine derivative i hoʻololi ʻia i hoʻohana ʻia i ka peptide synthesis, ʻoi loa no ke kūkulu ʻana i nā conjugates peptide i manaʻo ʻia a multifunctional. Hiki i ka pūʻulu Fmoc ke hana stepwise ma o Fmoc solid-phase peptide synthesis (SPPS). Hoʻololi ʻia ke kaulahao ʻaoʻao me ka stearic acid derivative (Ste), γ-glutamic acid (γ-Glu), a me ʻelua AEEA (aminoethoxyethoxyacetate) linkers, e hāʻawi ana i ka hydrophobicity, nā waiwai uku, a me ka spacing maʻalahi. Hoʻomaʻamaʻa maʻamau ia no kāna kuleana i nā ʻōnaehana hoʻopuka lāʻau, me ka antibody-drug conjugates (ADCs) a me nā peptides e komo ana i ke kelepona.
Hana:
Hana ʻo Fmoc-L-Lys[Ste(OtBu)-γ-Glu(OtBu)-AEEA-AEEA]-OH ma ke ʻano he hale kūkulu hale no ka hoʻomohala ʻana i nā peptides lipidated kaulahao lōʻihi a i ʻole nā mea pili lāʻau. Hoʻonui ka stearic acid i ka pili o ka membrane, hoʻomaikaʻi ʻo γ-Glu i ke kūpaʻa a me ke kūpaʻa enzymatic, a hāʻawi nā mea hoʻopili AEEA i ka solubility a me ka hoʻololi ʻana i ka hana. Hoʻohui pū ʻia kēia mau hiʻohiʻona i ka mea waiwai i ka hoʻolālā ʻana i nā peptides no ka hoʻomaikaʻi ʻana i ka bioavailability, ka hoʻokuʻu ʻia ʻana, a me nā noi hāʻawi ʻia.