Advancing targeted protein degradation for cancer therapy

B Dale, M Cheng, KS Park, HÜ Kaniskan… - … Reviews Cancer, 2021 - nature.com
cancer and AR + breast cancer xenograft models 90,91 . These preclinical findings suggest
that AR degradation may provide a potential therapeutic strategy … prostate cancer that small-…

[HTML][HTML] 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). …

Targeted protein degradation: an emerging therapeutic strategy in cancer

SH Barghout - … Current Medicinal Chemistry-Anti-Cancer …, 2021 - ingentaconnect.com
… molecules without affecting their protein levels. An emerging therapeutic strategy that
garnered attention in recent years is the induction of Targeted Protein Degradation (TPD) of …

[HTML][HTML] Targeted protein degradation: mechanisms, strategies and application

L Zhao, J Zhao, K Zhong, A Tong, D Jia - … and targeted therapy, 2022 - nature.com
… , extracellular proteins, and protein aggregates, thus greatly … a simple introduction of protein
degradation mechanisms. We … BTK is an established target in both inflammation and cancer

[PDF][PDF] Targeted protein degradation: A promise for undruggable proteins

KTG Samarasinghe, CM Crews - Cell chemical biology, 2021 - cell.com
Targeted Protein Degradation (TPD) strategies have also been explored to target previously
undruggable proteins, … Targeting antiapoptotic proteins in cancer therapy has long been an …

Phthalimide conjugation as a strategy for in vivo target protein degradation

GE Winter, DL Buckley, J Paulk, JM Roberts, A Souza… - Science, 2015 - science.org
… an efficacious therapeutic strategy, in particular for cancer, … chemical strategy for endogenous
target protein degradation. … -dependent posttranslational degradation with exquisite target-…

[HTML][HTML] Protein degradation technology: a strategic paradigm shift in drug discovery

H Li, J Dong, M Cai, Z Xu, XD Cheng, JJ Qin - Journal of Hematology & …, 2021 - Springer
… technologies that achieve selective degradation of target proteins using heterobifunctional
small … and more attention because of its great potential in cancer treatment [17]. PROTAC is a …

[PDF][PDF] Targeted protein degradation: from chemical biology to drug discovery

PM Cromm, CM Crews - Cell chemical biology, 2017 - cell.com
strategy translates the SERD mode of degradation into smallmolecule probes capable of
targeting various proteins for … drug target in prostate cancer, was selectively degraded using an …

Protein degradation: a validated therapeutic strategy with exciting prospects

H Lebraud, TD Heightman - Essays in biochemistry, 2017 - portlandpress.com
… are already approved for treatment of cancer patients. The … of lysine residues in the target
protein, to form an isopeptide … inducing protein degradation (Figure 1), from targeted protein

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

X Li, Y Song - Journal of hematology & oncology, 2020 - Springer
… Given these limitations, strategies have been developed for targeted protein reduction as
an alternative approach to cancer therapy. Targeted protein reduction may be readily …