Protein degraders enter the clinic—a new approach to cancer therapy
D Chirnomas, KR Hornberger, CM Crews - Nature Reviews Clinical …, 2023 - nature.com
Heterobifunctional protein degraders, such as PROteolysis TArgeting Chimera (PROTAC)
protein degraders, constitute a novel therapeutic modality that harnesses the cell's natural …
protein degraders, constitute a novel therapeutic modality that harnesses the cell's natural …
PROTAC targeted protein degraders: the past is prologue
Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to
tackle disease-causing proteins that have historically been highly challenging to target with …
tackle disease-causing proteins that have historically been highly challenging to target with …
Chemistries of bifunctional PROTAC degraders
C Cao, M He, L Wang, Y He, Y Rao - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …
PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)
M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …
[HTML][HTML] Current therapy and drug resistance in metastatic castration-resistant prostate cancer
M Cai, XL Song, XA Li, M Chen, J Guo, DH Yang… - Drug Resistance …, 2023 - Elsevier
Castration-resistant prostate cancer (CRPC), especially metastatic castration-resistant
prostate cancer (mCRPC) is one of the most prevalent malignancies and main cause of …
prostate cancer (mCRPC) is one of the most prevalent malignancies and main cause of …
E3 ligase ligand chemistries: from building blocks to protein degraders
In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted
protein degradation, have proven their great therapeutic potential and usefulness as …
protein degradation, have proven their great therapeutic potential and usefulness as …
An overview of PROTACs: a promising drug discovery paradigm
Z Liu, M Hu, Y Yang, C Du, H Zhou, C Liu, Y Chen… - Molecular …, 2022 - Springer
Proteolysis targeting chimeras (PROTACs) technology has emerged as a novel therapeutic
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …
Discovery of ARD-2051 as a potent and orally efficacious proteolysis targeting chimera (PROTAC) degrader of androgen receptor for the treatment of advanced …
We report the discovery of ARD-2051 as a potent and orally efficacious androgen receptor
(AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM …
(AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM …
Overcoming cancer drug resistance utilizing PROTAC technology
MR Burke, AR Smith, G Zheng - Frontiers in Cell and Developmental …, 2022 - frontiersin.org
Cancer drug resistance presents a major barrier to continued successful treatment of
malignancies. Current therapies inhibiting proteins indicated in cancer progression are …
malignancies. Current therapies inhibiting proteins indicated in cancer progression are …
Advancing strategies for proteolysis-targeting chimera design
M Li, Y Zhi, B Liu, Q Yao - Journal of medicinal chemistry, 2023 - ACS Publications
Proteolysis-targeting chimeras (PROTACs) have shown great therapeutic potential by
degrading various disease-causing proteins, particularly those related to tumors. Therefore …
degrading various disease-causing proteins, particularly those related to tumors. Therefore …