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

D Chirnomas, KR Hornberger, CM Crews - Nature Reviews Clinical …, 2023 - nature.com
therapies. Herein, we review advances in protein degrader development, the preclinical
research that supported their entry into clinical studies, the available data for protein degraders

Advancing targeted protein degradation for cancer therapy

B Dale, M Cheng, KS Park, HÜ Kaniskan… - … Reviews Cancer, 2021 - nature.com
… opportunities to develop degraders that target … protein degradation. We then offer a
comprehensive account of the most promising degraders in development as cancer therapies to …

[HTML][HTML] Targeted protein degrader development for cancer: advances, challenges, and opportunities

Y Fang, S Wang, S Han, Y Zhao, C Yu, H Liu… - Trends in pharmacological …, 2023 - cell.com
Protein degraders for cancer treatment A range of new targeted drugs have been developed
for cancer therapy … of precisely targeted protein degraders as cancer therapeutics, and …

PROTAC: an effective targeted protein degradation strategy for cancer therapy

SM Qi, J Dong, ZY Xu, XD Cheng, WD Zhang… - Frontiers in …, 2021 - frontiersin.org
… the desired degradation results. In this paper, we classify PROTACs according to E3 ligase
and summarize the PROTAC degradation strategies for different target proteins (Table 1). …

Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy

X Li, Y Song - Journal of hematology & oncology, 2020 - Springer
… To date, PROTACs targeting ~ 50 proteins, many of which are clinically validated … cancer
therapy. This article reviews PROTAC-mediated degradation of critical oncoproteins in cancer, …

PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy

JM Kelm, DS Pandey, E Malin, H Kansou, S Arora… - Molecular Cancer, 2023 - Springer
protein by hijacking the cellular protein destruction machinery. Degraders offer several
advantages for cancer therapy including resiliency to acquired mutations in the target protein, …

Cancer therapies based on targeted protein degradation—lessons learned with lenalidomide

M Jan, AS Sperling, BL Ebert - Nature Reviews Clinical Oncology, 2021 - nature.com
… of extended target suppression until protein re-synthesis 65 (Fig. 2), … of protein degradation
and contribute to the efficacy of the counterintuitive combination of targeted protein degraders

Targeting Brd4 for cancer therapy: inhibitors and degraders

Y Duan, Y Guan, W Qin, X Zhai, B Yu, H Liu - Medchemcomm, 2018 - pubs.rsc.org
… Recently, selective degradation of target proteins by small bifunctional molecules (… Brd4
degraders have been reported and showed more efficient anticancer activities than just protein

Targeted protein degraders from an oncologist point of view: The Holy Grail of cancer therapy?

M Ambrosini, G Fucà, M Duca, S Damian… - Critical Reviews in …, 2022 - Elsevier
… In conclusion, protein degradation seems a promising approach to expand a synthetic
lethality approach in cancer therapy and to hit specific molecular vulnerabilities in solid tumors. …

Targeted protein degradation: an emerging therapeutic strategy in cancer

SH Barghout - … Current Medicinal Chemistry-Anti-Cancer …, 2021 - ingentaconnect.com
Drug discovery in the scope of cancer therapy has been focused on conventional agents …
molecules without affecting their protein levels. An emerging therapeutic strategy that garnered …