Fmoc-NH-PEG2-CH2CH2COOH is a PEG linker compound commonly used in peptide synthesis and molecular linking. Fmoc-NH-PEG2-CH2CH2COOH consists of two ethoxy repeating units forming PEG2, with an amino group protected by Fmoc at one end and a carboxyl group at the other, allowing for amide coupling reactions. Fmoc-NH-PEG2-CH2CH2COOH binds to the amino group on the protein ligand at the carboxyl group and couples to the E3 ligase ligand at the other end via deamination, becoming the linker wall in the PROTAC molecule that connects the target protein ligand and the E3 ligase ligand[1]. Fmoc-NH-PEG2-CH2CH2COOH is also used in the synthesis of antibody-drug conjugates (ADCs)[2].
References:
[1] Hales LT, Thompson PE. Solid-Phase Synthesis of PROTACs and SNIPERs on Backbone Amide Linked (BAL) Resin. Chemistry. 2023;29(56):e202301975.
[2] Fulcher JM, et al. Chemical synthesis of Shiga toxin subunit B using a next-generation traceless "helping hand" solubilizing tag. Org Biomol Chem. 2019 Dec 28;17(48):10237-10244.
Fmoc-NH-PEG2-CH2CH2COOH是一种常用于肽合成和分子连接的PEG间隔臂化合物。Fmoc-NH-PEG2-CH2CH2COOH由2个乙氧基重复单元组成PEG2，一端为Fmoc 保护的氨基，另一端为羧基，可进行酰胺键偶联反应。Fmoc-NH-PEG2-CH2CH2COOH利用羧基和蛋白配体上的氨基结合，另一端通过脱氨与E3连接酶配体偶联，成为PROTAC分子中连接靶蛋白配体和E3连接酶配体的连接臂[1]。Fmoc-NH-PEG2-CH2CH2COOH也可用于抗体药物偶联物（ADCs）合成[2]。