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 …

Advancing targeted protein degradation for cancer therapy

B Dale, M Cheng, KS Park, HÜ Kaniskan… - Nature Reviews …, 2021 - nature.com
The human proteome contains approximately 20,000 proteins, and it is estimated that more
than 600 of them are functionally important for various types of cancers, including nearly 400 …

Proteolysis-targeting chimeras (PROTACs) in cancer therapy

X Li, W Pu, Q Zheng, M Ai, S Chen, Y Peng - Molecular cancer, 2022 - Springer
Proteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …

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
Proteolysis targeting chimeric (PROTAC) technology is an effective endogenous protein
degradation tool developed in recent years that can ubiquitinate the target proteins through …

Targeting transcriptional regulation of SARS-CoV-2 entry factors ACE2 and TMPRSS2

Y Qiao, XM Wang, R Mannan… - Proceedings of the …, 2021 - National Acad Sciences
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the virus responsible for
COVID-19, employs two key host proteins to gain entry and replicate within cells …

PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy

JM Kelm, DS Pandey, E Malin, H Kansou, S Arora… - Molecular Cancer, 2023 - Springer
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …

Strategies toward discovery of potent and orally bioavailable proteolysis targeting chimera degraders of androgen receptor for the treatment of prostate cancer

X Han, L Zhao, W Xiang, C Qin, B Miao… - Journal of medicinal …, 2021 - ACS Publications
Proteolysis targeting chimera (PROTAC) small-molecule degraders have emerged as a
promising new type of therapeutic agents, but the design of PROTAC degraders with …

Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges

S Zeng, W Huang, X Zheng, Z Zhang, J Wang… - European journal of …, 2021 - Elsevier
Proteolysis targeting chimera (PROTAC), hijacking protein of interest (POI) and recruiting E3
ligase for target degradation via the ubiquitin-proteasome pathway, is a novel drug …

Remodeling oncogenic transcriptomes by small molecules targeting NONO

SG Kathman, SJ Koo, GL Lindsey, HL Her… - Nature chemical …, 2023 - nature.com
Much of the human proteome is involved in mRNA homeostasis, but most RNA-binding
proteins lack chemical probes. Here we identify electrophilic small molecules that rapidly …

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 …