[HTML][HTML] Second generation androgen receptor antagonists and challenges in prostate cancer treatment
Y Chen, Q Zhou, W Hankey, X Fang, F Yuan - Cell Death & Disease, 2022 - nature.com
Prostate cancer is a hormone-dependent malignancy, whose onset and progression are
closely related to the activity of the androgen receptor (AR) signaling pathway. Due to this …
closely related to the activity of the androgen receptor (AR) signaling pathway. Due to this …
Proteolysis-targeting chimeras in biotherapeutics: Current trends and future applications
The success of inhibitor-based therapeutics is largely constrained by the acquisition of
therapeutic resistance, which is partially driven by the undruggable proteome. The …
therapeutic resistance, which is partially driven by the undruggable proteome. The …
Radiotherapy-triggered proteolysis targeting chimera prodrug activation in tumors
C Yang, Y Yang, Y Li, Q Ni, J Li - Journal of the American …, 2022 - ACS Publications
Proteolysis targeting chimera (PROTAC) is an emerging protein degradation strategy, which
shows excellent advantages in targeting those so-called “undruggable” proteins. However …
shows excellent advantages in targeting those so-called “undruggable” proteins. However …
[HTML][HTML] DYRK1A promotes viral entry of highly pathogenic human coronaviruses in a kinase-independent manner
Identifying host genes essential for Severe Acute Respiratory Syndrome Coronavirus 2
(SARS-CoV-2) has the potential to reveal novel drug targets and further our understanding …
(SARS-CoV-2) has the potential to reveal novel drug targets and further our understanding …
Degradation of hexokinase 2 blocks glycolysis and induces gsdme-dependent pyroptosis to amplify immunogenic cell death for breast cancer therapy
R Sang, R Fan, A Deng, J Gou, R Lin… - Journal of Medicinal …, 2023 - ACS Publications
Hexokinase 2 (HK2) is the principal rate-limiting enzyme in the aerobic glycolysis pathway
and determines the quantity of glucose entering glycolysis. However, the current HK2 …
and determines the quantity of glucose entering glycolysis. However, the current HK2 …
Discovery of CBPD-268 as an exceptionally potent and orally efficacious CBP/p300 PROTAC degrader capable of achieving tumor regression
CBP/p300 proteins are key epigenetic regulators and promising targets for the treatment of
castration-resistant prostate cancer and other types of human cancers. Herein, we report the …
castration-resistant prostate cancer and other types of human cancers. Herein, we report the …
Discovery of CBPD-409 as a Highly Potent, Selective, and Orally Efficacious CBP/p300 PROTAC Degrader for the Treatment of Advanced Prostate Cancer
CBP/p300 are critical transcriptional coactivators of the androgen receptor (AR) and are
promising cancer therapeutic targets. Herein, we report the discovery of highly potent …
promising cancer therapeutic targets. Herein, we report the discovery of highly potent …
[HTML][HTML] A beginner's guide to current synthetic linker strategies towards VHL-recruiting PROTACs
NA Zografou-Barredo, AJ Hallatt, J Goujon-Ricci… - Bioorganic & Medicinal …, 2023 - Elsevier
Over the last two decades, proteolysis targeting chimeras (PROTACs) have been
revolutionary in drug development rendering targeted protein degradation (TPD) as an …
revolutionary in drug development rendering targeted protein degradation (TPD) as an …
Leveraging aptamers for targeted protein degradation
Z Yang, Q Pang, J Zhou, C Xuan, S Xie - Trends in pharmacological …, 2023 - cell.com
Targeted protein degradation (TPD) technologies, particularly proteolysis-targeting chimeras
(PROTACs), have emerged as a significant advancement in drug discovery. However …
(PROTACs), have emerged as a significant advancement in drug discovery. However …
[PDF][PDF] Targeted protein degradation in cancers: Orthodox PROTACs and beyond
Targeted protein degradation (TPD) is emerging as a strategy to overcome the limitations of
traditional small-molecule inhibitors. Proteolysis targeting chimera (PROTAC) technology …
traditional small-molecule inhibitors. Proteolysis targeting chimera (PROTAC) technology …