[PDF][PDF] Strategies for the discovery of oral PROTAC degraders aimed at cancer therapy
In the past two decades, we have witnessed the discovery and development of many potent
and efficacious proteolysis-targeting chimera (PROTAC) degraders, with several in phase I/II …
and efficacious proteolysis-targeting chimera (PROTAC) degraders, with several in phase I/II …
Recent advances in pro-PROTAC development to address on-target off-tumor toxicity
C Chen, Y Yang, Z Wang, H Li, C Dong… - Journal of Medicinal …, 2023 - ACS Publications
Proteolysis-targeting chimera (PROTAC) technology represents a novel and promising
modality for targeted protein degradation with transformative implications for the clinical …
modality for targeted protein degradation with transformative implications for the clinical …
[HTML][HTML] PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective
Abstract Mouse double minute 2 (MDM2) is an E3 ubiquitin ligase which effectively
degrades tumor suppressor p53. In the past two decades, many MDM2 inhibitors that disrupt …
degrades tumor suppressor p53. In the past two decades, many MDM2 inhibitors that disrupt …
PROTAC technology: A new drug design for chemical biology with many challenges in drug discovery
N Guedeney, M Cornu, F Schwalen, C Kieffer… - Drug Discovery …, 2023 - Elsevier
Abstract Target Protein Degradation TPD is a new avenue and revolutionary for therapeutics
because redefining the principles of classical drug discovery and guided by event-based …
because redefining the principles of classical drug discovery and guided by event-based …
Emerging targeted protein degradation tools for innovative drug discovery: From classical PROTACs to the novel and beyond
Y Zhong, F Chi, H Wu, Y Liu, Z Xie, W Huang… - European journal of …, 2022 - Elsevier
Targeted protein degradation technology has evolved a brand-new therapeutic modality
from an innovative drug discovery perspective. Though the classical PROTACs has …
from an innovative drug discovery perspective. Though the classical PROTACs has …
[HTML][HTML] Targeting the ubiquitin-proteasome system for cancer therapeutics by small-molecule inhibitors
G LaPlante, W Zhang - Cancers, 2021 - mdpi.com
Simple Summary The ubiquitin-proteasome system regulates multiple facets of protein
homeostasis to modulate signal transduction in numerous biological processes. Not …
homeostasis to modulate signal transduction in numerous biological processes. Not …
Brd4 proteolysis-targeting chimera nanoparticles sensitized colorectal cancer chemotherapy
Y He, Y Ju, Y Hu, B Wang, S Che, Y Jian… - Journal of Controlled …, 2023 - Elsevier
Abstract Bromodomain-Containing Protein 4 (BRD4) is a member of the BET family of
bromodomains, which participates in gene transcription process and is closely related to …
bromodomains, which participates in gene transcription process and is closely related to …
[HTML][HTML] Targeting androgen receptor degradation with PROTACs from bench to bedside
X Jia, X Han - Biomedicine & Pharmacotherapy, 2023 - Elsevier
Highlights•AR is a clinically fully validated target for treatment of human prostate
cancer.•PROTAC AR degraders overcome common resistance mechanisms developed …
cancer.•PROTAC AR degraders overcome common resistance mechanisms developed …
Erythroid/megakaryocytic differentiation confers BCL-XL dependency and venetoclax resistance in acute myeloid leukemia
Myeloid neoplasms with erythroid or megakaryocytic differentiation include pure erythroid
leukemia, myelodysplastic syndrome with erythroid features, and acute megakaryoblastic …
leukemia, myelodysplastic syndrome with erythroid features, and acute megakaryoblastic …