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 …
research that supported their entry into clinical studies, the available data for protein degraders …
Advancing targeted protein degradation for cancer therapy
… 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 …
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 …
for cancer therapy … of precisely targeted protein degraders as cancer therapeutics, and …
PROTAC: an effective targeted protein degradation strategy for cancer therapy
… 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). …
and summarize the PROTAC degradation strategies for different target proteins (Table 1). …
Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy
… 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, …
therapy. This article reviews PROTAC-mediated degradation of critical oncoproteins in cancer, …
PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy
… protein by hijacking the cellular protein destruction machinery. Degraders offer several
advantages for cancer therapy including resiliency to acquired mutations in the target protein, …
advantages for cancer therapy including resiliency to acquired mutations in the target protein, …
Cancer therapies based on targeted protein degradation—lessons learned with lenalidomide
… 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 …
and contribute to the efficacy of the counterintuitive combination of targeted protein degraders …
Targeting Brd4 for cancer therapy: inhibitors and degraders
… Recently, selective degradation of target proteins by small bifunctional molecules (… Brd4
degraders have been reported and showed more efficient anticancer activities than just protein …
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?
… 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. …
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 …
molecules without affecting their protein levels. An emerging therapeutic strategy that garnered …
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