protac erα degrader 1

PROTAC ERα Degrader-1 is a chemical compound. It consists of a ubiquitin E3 ligase binding group, a linker, and a protein binding group. This compound serves as a degrader of estrogen receptor-alpha (ERα).

PROTAC ERα Y537S degrader-1 consists of a ubiquitin E3 ligase binding group, a linker, and a protein binding group, functioning as an estrogen receptor-alpha (ERα) Y537S degrader [1].

PROTA CER Degrader-11 (Example 26-1) is an effective degrader of PROTA CER with an IC50 of 0.66 nM. It plays a crucial role in cancer research.

PROTAC ER Degrader-14 (compound 86) is a PROTAC-type estrogen receptor/ERR degrader. It comprises an E3 ubiquitin ligase ligand (blue part) (S)-Deoxy-thalidomide, a PROTAC linker (black part) N-Boc-piperazine, and a target protein ligand (red part) ER ligand-6. The combination of the E3 ligase and linker forms tert-Butyl (S)-4-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)piperazine-1-carboxylate.

PROTAC ER Degrader-15 (Compound 40) is an orally active estrogen receptor (ER) degrader with anticancer properties, suitable for breast cancer research.

PROTACER Degrader-12 (Compound 70) is an estrogen receptor PROTAC degrader with a degradation concentration (DC50) of less than 10 nM. It inhibits the proliferation of MCF-7 cells at a DC50 of under 10 nM and exhibits anticancer properties.

PROTAC ERα Degrader-2 is composed of a cIAP1 ligand binding group, a linker, and an estrogen receptor α (ERα) binding group, serving as an ERα degrader. It achieves maximal ERα degradation in human mammary tumor MCF7 cells at a concentration of 30 μM. Degradation inducers that utilize cIAP1 are referred to as specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].

PROTAC ER Degrader-2 serves as a synthesis intermediate for the production of PAC, a compound that incorporates the ADCs linker and PROTACs, which are subsequently conjugated to an antibody. PAC, exhibits a greater capability to degrade estrogen receptor-alpha (ERα) compared to PROTAC (without the presence of an antibody)[1].

PROTAC ER Degrader-3, an intermediate for the synthesis of PAC, specifically compound LP2. PAC serves as the linker for ADCs and PROTACs that are conjugated to an antibody. Notably, when PAC is conjugated to an antibody, it exhibits enhanced degradation of estrogen receptor-alpha (ERα) compared to PROTAC alone [1].

XIAPligand-Linker Conjugate 1 is an E3 ubiquitin ligase ligand-linker conjugate that comprises the XIAPBIR2 ligand XB2M54 and a linker. XIAPligand-Linker Conjugate 1 is applicable in the synthesis of PROTAC ERα Degrader-1.

ERD-3111 (Compound 44), an orally active PROTAC ERα degrader (DC50: 0.5 nM), exhibits efficacy in inhibiting tumor growth in both the parental MCF-7 xenograft model harboring wild-type ER and two ESR1-mutated mouse models. This compound has utility in the investigation of ER+ breast cancer [1].

PROTAC ERα Degrader-7 (Compound i-320) is a powerful PROTAC degrader targeting the estrogen receptor alpha (ERα), exhibiting a DC50 of 0.000006 µM. This compound consists of a cereblon-binding segment, LBM, connected to ERBM, an ERα-binding ligand that includes a benzofused partially saturated 6-membered carbocyclic or heterocyclic ring [1].

PROTAC ERα Degrader-8 (compound ii-56), a highly potent degrader of Erα, achieves a DC50 of just 0.000006 μM in MCF7 cells [1].