PROTAC-Linker Conjugates for PAC

PROTAC BRD4 degrader for PAC-1 (compound 5) is a chimeric BET degrader GNE-987 conjugated with a disulfide-containing linker[1]. This PROTAC-linker conjugate specifically targets and degrades BRD4, enabling selective proteolysis of PAC-1.

PROTAC BRD4 Degrader-13 (compound 9d) is a bioactive compound that functions as a proteolysis targeting chimera (PROTAC), linking ligands for von Hippel-Lindau and BRD4 proteins. In the context of PC3 prostate cancer cells, this compound effectively degrades the BRD4 protein through conjugation with STEAP1 and CLL1 antibodies. The degradation of BRD4 protein is achieved with remarkable potency, exhibiting a DC 50 of 0.025 nM and 6.0 nM when combined with STEAP1 and CLL1 antibodies, respectively.

PROTACBRD4Degrader-12 (compound 9c) 是一种由 von Hippel-Lindau 配体和 BRD4配体相连的 PROTAC。PROTACBRD4Degrader-12 可与 STEAP1 和 CLL1 抗体偶联从而降解 PC3 前列腺癌细胞中的 BRD4蛋白，DC50值分别为 0.39 nM 和 0.24 nM。

PAC is a chemical conjugate consisting of an ADCs linker and PROTACs linked to an antibody. When PAC is conjugated to an antibody, it exhibits enhanced degradation of estrogen receptor-alpha (ERα) in comparison to PROTAC alone.

Comp Ie (MC-(β-Ala)-PABC-(β-D-GlcUA)-amide-PEG1-CH2-CC-885) 为一种新型抗体新降解剂偶联活性分子 (AnDC) 的合成降解剂偶联物。

PROTACBTK Degrader-8 (compound 3) 是一种高效的 PROTACBTK 降解剂，配备接头，可与 ADC 抗体结合形成 PAC。

cBu-Cit-PROTAC BRD4 Degrader-5，一种与cBu-Cit偶联的PROTAC降解剂，能够有效地降解HER2阳性及阴性乳腺癌细胞系中的BRD4。

PROTACBRD4Degrader-11 (compound 9a) 是一种有效的由von Hippel-Lindau 配体和BRD4配体相连的PROTAC。PROTACBRD4Degrader-11 可与 STEAP1 和 CLL1 抗体偶联从而降解 PC3 前列腺癌细胞中的BRD4蛋白，DC50值分别为 0.23 nM 和 0.38 nM。