Protein degraders enter the clinic—a new approach to cancer therapy

D Chirnomas, KR Hornberger, CM Crews - Nature Reviews Clinical …, 2023 - nature.com
… , they have flexibility to robustly degrade a wide variety of … of systemic degradation to be
achieved. However, exploitable … PROTAC AR degrader bavdegalutamide, the PROTAC ER …

Discovery of a PROTAC targeting ALK with in vivo activity

G Yan, X Zhong, L Yue, C Pu, H Shan, S Lan… - European Journal of …, 2021 - Elsevier
… LDK378 and the antiproliferative activity to xenograft tumor … ALK degrader B3 with in vitro
and in vivo anti-cancer activities … of PROTAC BCL-XL degraders as potent anticancer agents …

Discovery of SHP2-D26 as a first, potent, and effective PROTAC degrader of SHP2 protein

M Wang, J Lu, M Wang, CY Yang… - Journal of medicinal …, 2020 - ACS Publications
… -targeting chimera (PROTAC) concept. This work has led to the discovery of potent and
effective SHP2 degraders, exemplified by SHP2-D26. SHP2-D26 achieves DC 50 values of 6.0 …

A selective Fibroblast Growth Factor Receptor 1/2 PROTAC degrader with antitumor activity

Y Kong, X Zhao, Z Wang, S Yuan, S Chen, S Lou… - Molecular Cancer …, 2024 - AACR
… for degrading various protein targets (24). For example, our group has 104 developed a
tissue-selective PROTAC for degrading BCL-XL … that PROTAC degrader may achieve 577 long-…

[HTML][HTML] Degradation of proteins by PROTACs and other strategies

Y Wang, X Jiang, F Feng, W Liu, H Sun - Acta Pharmaceutica Sinica B, 2020 - Elsevier
… to selectively degrade target proteins. Recent progress in the … protein degradation are mostly
achieved via biomacromolecules. … and risks of this emerging PROTAC technology in clinical …

Sulfatase-Induced In Situ Formulation of Antineoplastic Supra-PROTACs

N Chen, Z Zhang, X Liu, H Wang, RC Guo… - Journal of the …, 2024 - ACS Publications
… the prevented Bcl-xL degradation … the Bcl-xL degradation caused by the pro-Supra-PROTAC.
In addition, to confirm the capability of the pro-Supra-PROTAC to selectively degrade Bcl-xL

[HTML][HTML] Targeting BCL-XL in fibrolamellar hepatocellular carcinoma

B Shebl, D Ng, G Lalazar, C Rosemore… - JCI insight, 2022 - ncbi.nlm.nih.gov
… (PROTAC) that can selectively degrade BCL-XL via the VHL ubiquitin E3 ligase (20). Our lead
BCL-XL PROTAC, … Second, this particular PROTAC was effective at engaging BCL-XL but …

[HTML][HTML] Peptide-based PROTAC degrader of FOXM1 suppresses cancer and decreases GLUT1 and PD-L1 expression

K Wang, X Dai, A Yu, C Feng, K Liu… - Journal of Experimental & …, 2022 - Springer
… Here, we develop a peptide-based PROTAC, which achieves the purpose of degrading
FOXM1 by facilitating the recruitment of E3 ubiquitin to FOXM1. Phage display technology was …

Optimization of PROTAC ternary complex using DNA encoded library approach

Q Chen, C Liu, W Wang, X Meng, X Cheng… - ACS Chemical …, 2023 - ACS Publications
… In the PROTAC process, a heterobifunctional degrader forms a … The majority of PROTAC
discovery and development … molecule to achieve the required degradation potency, selectivity, …

Design, synthesis, and evaluation of potent, selective, and bioavailable AKT kinase degraders

X Yu, J Xu, L Xie, L Wang, Y Shen… - Journal of medicinal …, 2021 - ACS Publications
potent AKT proteolysis targeting chimera (PROTAC) degraders: von Hippel–Lindau (VHL)-recruiting
degrader … substantially at 100 nM and achieved near-complete depletion of T-AKT at …