PROTAC: targeted drug strategy. Principles and limitations
OA Koroleva, YV Dutikova, AV Trubnikov… - Russian Chemical …, 2022 - Springer
Abstract The PROTAC (PROteolysis TArgeting Chimera) technology is a method of targeting
intracellular proteins previously considered undruggable. This technology utilizes the …
intracellular proteins previously considered undruggable. This technology utilizes the …
Small-molecule PROTACs for cancer immunotherapy
Z Liu, Y Zhang, Y Xiang, X Kang - Molecules, 2022 - mdpi.com
Unsatisfactory physicochemical properties of macromolecular drugs seriously hinder their
application in tumor immunotherapy. However, these problems can be effectively solved by …
application in tumor immunotherapy. However, these problems can be effectively solved by …
Roles of Cullin-RING ubiquitin ligases in cardiovascular diseases
Maintenance of protein homeostasis is crucial for virtually every aspect of eukaryotic biology.
The ubiquitin-proteasome system (UPS) represents a highly regulated quality control …
The ubiquitin-proteasome system (UPS) represents a highly regulated quality control …
[HTML][HTML] The PROTAC selectively degrading Bcl-xL represents a novel Hedgehog pathway inhibitor with capacity of combating resistance to Smoothened inhibitors …
S Zhang, Y Chen, Z Xu, J Yang, R Sun, J Wang… - Theranostics, 2022 - ncbi.nlm.nih.gov
Rationale: Primary and acquired resistance to Smoothened (Smo) inhibitors largely
hampered their clinical efficacy. Given the important functions of hedgehog (Hh) pathway in …
hampered their clinical efficacy. Given the important functions of hedgehog (Hh) pathway in …
Proteolysis-targeting chimaeras (PROTACs) as pharmacological tools and therapeutic agents: advances and future challenges
C Wang, Y Zhang, T Zhang, L Shi… - Journal of Enzyme …, 2022 - Taylor & Francis
Proteolysis-targeting chimaeras (PROTACs) have been developed to be an emerging
technology for targeted protein degradation and attracted the favour of academic institutions …
technology for targeted protein degradation and attracted the favour of academic institutions …
[HTML][HTML] MDM2-BCL-XL PROTACs enable degradation of BCL-XL and stabilization of p53
Inhibition or degradation of anti-apoptotic protein BCL-X L is a viable strategy for cancer
treatment. Despite the recent development of PROTACs for degradation of BCL-X L, the E3 …
treatment. Despite the recent development of PROTACs for degradation of BCL-X L, the E3 …
BCL-XL PROTAC degrader DT2216 synergizes with sotorasib in preclinical models of KRASG12C-mutated cancers
KRAS mutations are the most common oncogenic drivers. Sotorasib (AMG510), a covalent
inhibitor of KRASG12C, was recently approved for the treatment of KRASG12C-mutated non …
inhibitor of KRASG12C, was recently approved for the treatment of KRASG12C-mutated non …
Developing PROteolysis TArgeting Chimeras (PROTACs) for hematologic malignancies
Y Wu, J Zhang, X Zhu, Y Zhang - Cancer Letters, 2022 - Elsevier
Abstract PROteolysis TArgeting Chimeras (PROTACs) degrade target proteins via the
ubiquitin-proteasome system, providing novel insights into drug development for …
ubiquitin-proteasome system, providing novel insights into drug development for …
What can we learn from mice lacking pro-survival BCL-2 proteins to advance BH3 mimetic drugs for cancer therapy?
K Brinkmann, AP Ng, CA de Graaf… - Cell Death & …, 2022 - nature.com
In many human cancers the control of apoptosis is dysregulated, for instance as a result of
the overexpression of pro-survival BCL-2 proteins. This promotes tumorigenesis by …
the overexpression of pro-survival BCL-2 proteins. This promotes tumorigenesis by …