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 …
Advancing targeted protein degradation for cancer therapy
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 …
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 …
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …
PROTAC: an effective targeted protein degradation strategy for cancer therapy
Proteolysis targeting chimeric (PROTAC) technology is an effective endogenous protein
degradation tool developed in recent years that can ubiquitinate the target proteins through …
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
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 …
COVID-19, employs two key host proteins to gain entry and replicate within cells …
PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …
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
Proteolysis targeting chimera (PROTAC) small-molecule degraders have emerged as a
promising new type of therapeutic agents, but the design of PROTAC degraders with …
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 …
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 …
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 …
malignancies. Current therapies inhibiting proteins indicated in cancer progression are …