SNIPERs

SNIPER(TACC3)-2 hydrochloride 是一个基于IAPE3配体的小分子化合物，其作用机制为通过泛素－蛋白酶体系统靶向降解TACC3蛋白，从而诱导癌细胞死亡。

SNIPER(ABL)-015, conjugating GNF5 (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 5 μM [1].

PROTACAR Degrader-4 包含IAP 配体结合基团，linker 和雄激素受体 (AR) 配体结合基团。基于cIAP1的降解剂也被称为SNIPER。

PROTAC CRABP-II Degrader-2 is a potent cIAp1-based degrader of cellular retinoic acid binding protein (CRABP-II).

PROTAC ERα Degrader-2 comprises a cIAP1 ligand binding group, a linker and an estrogen receptor α (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader. Maximal ERα degradation at 30 μM concentration in human mammary tumor MCF7 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].

SNIPER(ABL)-047, conjugating HG-7-85-01 (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 2 μM[1].

SNIPER(ABL)-013, conjugating GNF5 (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 20 μM[1].

SNIPER(ABL)-024, conjugating GNF5 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 5μM[1].

SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 nM. IC50s are 0.54 nM, 10 nM, 12 nM, and 50 nM for ABL, cIAP1, cIAP2, XIAP, respectively[1].

SNIPER(ABL)-019, conjugating Dasatinib (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 0.3 μM[1].

SNIPER(ER)-110 comprises a cIAP1 ligand and an estrogen ligand connected by a linker. SNIPER(ER)-51 induces estrogen receptor (ER) protein degradation with DC50s of <3 nM and 7.7 nM after 4 h and 48 h, respectively [1].

SNIPER(ABL)-058, conjugating Imatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 μM[1].

SNIPER(ABL)-033, conjugating HG-7-85-01 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 0.3 μM[1].

SNIPER(ABL)-050 is a chemical compound that combines Imatinib, an ABL inhibitor, with MV-1, an IAP ligand, using a linker. This conjugation results in the reduction of BCR-ABL protein[1].

SNIPER(TACC3)-11是一种针对FGFR3-TACC3的有效抑制剂，能够降低FGFR3-TACC3蛋白水平，并抑制FGFR3-TACC3阳性癌细胞增殖。

SNIPERTACC3-1 hydrochloride 是一种基于IAPE3连接酶的化合物，其机制是针对泛素-蛋白酶体系统，靶向性地降解TACC3蛋白，从而诱导癌细胞死亡。

BzNH-BS is a chemical compound comprising two distinct ligands: methyl-bestatin (MeBS) for cIAP1 and benzoyl-amide. The ligands are interconnected through linkers. MeBS functions as a ligand for cIAP1, a ubiquitin ligase involved in cellular inhibition of apoptosis processes [1].

PROTAC RAR Degrader-1 comprises a cIAP1 ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader. Maximal RAR degradation at 30 μM concentration in HT1080 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].

SNIPER(ABL)-044, conjugating HG-7-85-01 (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 μM[1].

SNIPER(ABL)-049, conjugating Imatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 100 μM[1].

SNIPER(TACC3)-1 targets TACC3 protein degradation via the ubiquitin-proteasome pathway.It induces cancer cell death.

SNIPER(TACC3)-2 targets TACC3 protein degradation via the ubiquitin-proteasome pathway. It induces cancer cell death.

PROTAC CRABP-II Degrader-3 is a potent degrader of cellular retinoic acid binding protein (CRABP-II) based on [cIAp1].

PROTAC CRABP-II Degrader-1 is a potent degrader of cellular retinoic acid binding protein (CRABP-II) based on cIAp1.