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PROTACs: past, present and future
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules consisting of
one ligand that binds to a protein of interest (POI) and another that can recruit an E3 …
one ligand that binds to a protein of interest (POI) and another that can recruit an E3 …
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… - Signal transduction and …, 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 …
Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders
The von Hippel-Lindau (VHL) Cullin RING E3 ligase is an essential enzyme in the ubiquitin-
proteasome system that recruits substrates such as the hypoxia inducible factor for …
proteasome system that recruits substrates such as the hypoxia inducible factor for …
Affinity and cooperativity modulate ternary complex formation to drive targeted protein degradation
RP Wurz, H Rui, K Dellamaggiore… - Nature …, 2023 - nature.com
Targeted protein degradation via “hijacking” of the ubiquitin-proteasome system using
proteolysis targeting chimeras (PROTACs) has evolved into a novel therapeutic modality …
proteolysis targeting chimeras (PROTACs) has evolved into a novel therapeutic modality …
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 …
Driving E3 ligase substrate specificity for targeted protein degradation: lessons from nature and the laboratory
Methods to direct the degradation of protein targets with proximity-inducing molecules that
coopt the cellular degradation machinery are advancing in leaps and bounds, and diverse …
coopt the cellular degradation machinery are advancing in leaps and bounds, and diverse …
Small-molecule probes from bench to bedside: advancing molecular analysis of drug–target interactions toward precision medicine
Over the past decade, remarkable advances have been witnessed in the development of
small-molecule probes. These molecular tools have been widely applied for interrogating …
small-molecule probes. These molecular tools have been widely applied for interrogating …
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 …
High accuracy prediction of PROTAC complex structures
The design of PROteolysis-TArgeting Chimeras (PROTACs) requires bringing an E3 ligase
into proximity with a target protein to modulate the concentration of the latter through its …
into proximity with a target protein to modulate the concentration of the latter through its …
Roles and inhibitors of FAK in cancer: current advances and future directions
HH Hu, SQ Wang, HL Shang, HF Lv… - Frontiers in …, 2024 - frontiersin.org
Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that exhibits high expression
in various tumors and is associated with a poor prognosis. FAK activation promotes tumor …
in various tumors and is associated with a poor prognosis. FAK activation promotes tumor …