BTR2000 TFA, a specifically KLHL20 ligand, is capable of binding to the KLHL20 Kelch domain with high affinity. BTR2000 TFA can be used as a ligand for E3 ligase for the synthesis of BTR2004 [1] [2].
References:
[1]. Farrell BM, et, al. A synthetic KLHL20 ligand to validate CUL3KLHL20 as a potent E3 ligase for targeted protein degradation. Genes Dev. 2022 Sep 1;36(17-18):1031-1042.
[2]. Fechtmeyer PH, et, al. Temporal and Spatial Characterization of CUL3KLHL20-driven Targeted Degradation of BET family, BRD Proteins by the Macrocycle-based Degrader BTR2004. bioRxiv. 2024 Dec 7:2024.12.07.627262.
References:
[1]. Farrell BM, et, al. A synthetic KLHL20 ligand to validate CUL3KLHL20 as a potent E3 ligase for targeted protein degradation. Genes Dev. 2022 Sep 1;36(17-18):1031-1042.
[2]. Fechtmeyer PH, et, al. Temporal and Spatial Characterization of CUL3KLHL20-driven Targeted Degradation of BET family, BRD Proteins by the Macrocycle-based Degrader BTR2004. bioRxiv. 2024 Dec 7:2024.12.07.627262.
















