Trends in kinase drug discovery: targets, indications and inhibitor design
The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …
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 …
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 …
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 …
Attacking the PI3K/Akt/mTOR signaling pathway for targeted therapeutic treatment in human cancer
Cancer is the second leading cause of human death globally. PI3K/Akt/mTOR signaling is
one of the most frequently dysregulated signaling pathways observed in cancer patients that …
one of the most frequently dysregulated signaling pathways observed in cancer patients that …
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 …
Recent developments in PROTAC‐mediated protein degradation: from bench to clinic
Abstract Proteolysis‐targeting chimeras (PROTACs), an emerging paradigm‐shifting
technology, hijacks the ubiquitin‐proteasome system for targeted protein degradation …
technology, hijacks the ubiquitin‐proteasome system for targeted protein degradation …
At a crossroads: how to translate the roles of PI3K in oncogenic and metabolic signalling into improvements in cancer therapy
N Vasan, LC Cantley - Nature Reviews Clinical Oncology, 2022 - nature.com
Numerous agents targeting various phosphatidylinositol 3-kinase (PI3K) pathway
components, including PI3K, AKT and mTOR, have been tested in oncology clinical trials …
components, including PI3K, AKT and mTOR, have been tested in oncology clinical trials …
PI3K/AKT/mTOR-targeted therapy for breast cancer
K Zhu, Y Wu, P He, Y Fan, X Zhong, H Zheng, T Luo - Cells, 2022 - mdpi.com
Phosphatidylinositol 3-kinase (PI3K), protein kinase B (PKB/AKT) and mechanistic target of
rapamycin (mTOR)(PAM) pathways play important roles in breast tumorigenesis and confer …
rapamycin (mTOR)(PAM) pathways play important roles in breast tumorigenesis and confer …
Signaling pathways in cancer: therapeutic targets, combinatorial treatments, and new developments
Molecular alterations in cancer genes and associated signaling pathways are used to inform
new treatments for precision medicine in cancer. Small molecule inhibitors and monoclonal …
new treatments for precision medicine in cancer. Small molecule inhibitors and monoclonal …