err

Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM. It can reduce the expression of classically regulated ER target genes and inhibit the growth of ER-dependent cell lines (including those expressing ESR1 variants, such as Y537S and D538G) by degrading ER.

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 ERRα ligand 1 is an estrogen-related receptor α (ERRα) antagonist with IC50 values of 0.04 μM for ERRα and 2.8 μM for ERRγ.

PROTAC ERRα ligand 2 is an inverse agonist for the estrogen-related receptor α (ERRα) with an IC50 of 5.67 nM.

PROTAC ERRα Degrader-2 is a compound consisting of an MDM2 ligand binding group, a linker, and an estrogen-related receptor alpha (ERRα) binding group. This compound is designed to specifically degrade estrogen-related receptor alpha (ERRα), acting as an ERRα degrader[1].

ERRα Ligand-Linker Conjugates 1 refers to a chemical compound that consists of a ligand targeting estrogen-related receptor alpha (ERRα), and a PROTAC linker that facilitates the recruitment of E3 ligases MDM2. It finds utility in the synthesis of a range of PROTACs, including one known as PROTAC ERRalpha Degrader-1. With its capability to induce degradation of ERRα, PROTAC ERRalpha Degrader-1 functions as an ERRα degrader[1].

PROTAC ERRα Degrader-3 is a highly effective and selective von Hippel-Lindau-based ligand that efficiently degrades the ERRα protein, reducing its levels by >80% at a concentration of 30 nM. Notably, this compound shows no activity against the ERRβ and ERRγ proteins.

(rel)-PROTAC ERRα Degrader-1, a relative configuration of PROTAC ERRα Degrader-1, is an estrogen-related receptor alpha (ERRα) degrader comprising an MDM2 ligand binding moiety, a linker, and an ERRα binding moiety [1].

Aberrant tau degrader 2 (Compound 4-12) acts as a degrader of tau protein and serves as a target protein ligand for the synthesis of PROTAC degrader C004019.

PROTAC_ERRalpha is a proteolysis targeting chimeras (PROTAC) which provides broad tissue distribution and knockdown of the targeted ERRalpha protein in tumor xenografts.

PROTAC ERα Degrader-4, a highly potent and selective agent (K i: 5.08 μM), contains OBHSAs, a linker, and E3 ligase ligands. This compound demonstrates superb inhibitory effects and ERα degradation activity in both Tamoxifen-sensitive and -resistant ER+ breast cancer (BC) cells, as well as in ERα-mutated BC cells. Additionally, PROTAC ERα Degrader-4 can induce apoptosis, making it valuable for cancer research.

ER ligand-9 is a conjugate of an estrogen receptor (Estrogen Receptor ERR) ligand and a linker, utilized in the synthesis of PROTACs ERD-1233.

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.

ER ligand-8 is a ligand of the estrogen receptor (Estrogen Receptor ERR) and can be used for the synthesis of the PROTAC molecule ERD-1233.