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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 …
[HTML][HTML] Current therapy and drug resistance in metastatic castration-resistant prostate cancer
M Cai, XL Song, XA Li, M Chen, J Guo, DH Yang… - Drug Resistance …, 2023 - Elsevier
Castration-resistant prostate cancer (CRPC), especially metastatic castration-resistant
prostate cancer (mCRPC) is one of the most prevalent malignancies and main cause of …
prostate cancer (mCRPC) is one of the most prevalent malignancies and main cause of …
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 …
An overview of PROTACs: a promising drug discovery paradigm
Proteolysis targeting chimeras (PROTACs) technology has emerged as a novel therapeutic
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …
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 …
Cell cycle on the crossroad of tumorigenesis and cancer therapy
Aberrancy in cell cycle progression is one of the fundamental mechanisms underlying
tumorigenesis, making regulators of the cell cycle machinery rational anticancer therapeutic …
tumorigenesis, making regulators of the cell cycle machinery rational anticancer therapeutic …
Advances in targeting 'undruggable'transcription factors with small molecules
MJ Henley, AN Koehler - Nature Reviews Drug Discovery, 2021 - nature.com
Transcription factors (TFs) represent key biological players in diseases including cancer,
autoimmunity, diabetes and cardiovascular disease. However, outside nuclear receptors …
autoimmunity, diabetes and cardiovascular disease. However, outside nuclear receptors …
Targeting FAK in anticancer combination therapies
JC Dawson, A Serrels, DG Stupack… - Nature Reviews …, 2021 - nature.com
Focal adhesion kinase (FAK) is both a non-receptor tyrosine kinase and an adaptor protein
that primarily regulates adhesion signalling and cell migration, but FAK can also promote …
that primarily regulates adhesion signalling and cell migration, but FAK can also promote …
Targeted protein degradation: expanding the toolbox
M Schapira, MF Calabrese, AN Bullock… - Nature reviews Drug …, 2019 - nature.com
Proteolysis-targeting chimeras (PROTACs) and related molecules that induce targeted
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …
PROTACs: great opportunities for academia and industry
X Sun, H Gao, Y Yang, M He, Y Wu, Y Song… - Signal transduction and …, 2019 - nature.com
Although many kinds of therapies are applied in the clinic, drug-resistance is a major and
unavoidable problem. Another disturbing statistic is the limited number of drug targets, which …
unavoidable problem. Another disturbing statistic is the limited number of drug targets, which …