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Protein degradation technology: a strategic paradigm shift in drug discovery
by
Li, Haobin
, Qin, Jiang-Jiang
, Cai, Maohua
, Xu, Zhiyuan
, Cheng, Xiang-Dong
, Dong, Jinyun
in
Animals
/ Binding sites
/ Breast cancer
/ Cancer Research
/ Cancer therapies
/ Cell cycle
/ Degradation
/ Degradation pathway
/ Degradation technology
/ Drug development
/ Drug discovery
/ Drug Discovery - methods
/ Drug resistance
/ Enzymes
/ Hematology
/ Humans
/ Kinases
/ Ligands
/ materials
/ Medicine
/ Medicine & Public Health
/ molecular engineering for drug discovery
/ Molecular Targeted Therapy
/ Molecular weight
/ Monomeric degraders
/ Mutation
/ New developments in delivery technology
/ Oncology
/ Prostate cancer
/ PROTAC
/ Protein degradation
/ Proteins
/ Proteins - antagonists & inhibitors
/ Proteins - metabolism
/ Proteolysis
/ Proteolysis - drug effects
/ Review
/ Signal transduction
/ Small Molecule Libraries - chemistry
/ Small Molecule Libraries - pharmacology
/ Transcription factors
/ Tumors
2021
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Protein degradation technology: a strategic paradigm shift in drug discovery
by
Li, Haobin
, Qin, Jiang-Jiang
, Cai, Maohua
, Xu, Zhiyuan
, Cheng, Xiang-Dong
, Dong, Jinyun
in
Animals
/ Binding sites
/ Breast cancer
/ Cancer Research
/ Cancer therapies
/ Cell cycle
/ Degradation
/ Degradation pathway
/ Degradation technology
/ Drug development
/ Drug discovery
/ Drug Discovery - methods
/ Drug resistance
/ Enzymes
/ Hematology
/ Humans
/ Kinases
/ Ligands
/ materials
/ Medicine
/ Medicine & Public Health
/ molecular engineering for drug discovery
/ Molecular Targeted Therapy
/ Molecular weight
/ Monomeric degraders
/ Mutation
/ New developments in delivery technology
/ Oncology
/ Prostate cancer
/ PROTAC
/ Protein degradation
/ Proteins
/ Proteins - antagonists & inhibitors
/ Proteins - metabolism
/ Proteolysis
/ Proteolysis - drug effects
/ Review
/ Signal transduction
/ Small Molecule Libraries - chemistry
/ Small Molecule Libraries - pharmacology
/ Transcription factors
/ Tumors
2021
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Protein degradation technology: a strategic paradigm shift in drug discovery
by
Li, Haobin
, Qin, Jiang-Jiang
, Cai, Maohua
, Xu, Zhiyuan
, Cheng, Xiang-Dong
, Dong, Jinyun
in
Animals
/ Binding sites
/ Breast cancer
/ Cancer Research
/ Cancer therapies
/ Cell cycle
/ Degradation
/ Degradation pathway
/ Degradation technology
/ Drug development
/ Drug discovery
/ Drug Discovery - methods
/ Drug resistance
/ Enzymes
/ Hematology
/ Humans
/ Kinases
/ Ligands
/ materials
/ Medicine
/ Medicine & Public Health
/ molecular engineering for drug discovery
/ Molecular Targeted Therapy
/ Molecular weight
/ Monomeric degraders
/ Mutation
/ New developments in delivery technology
/ Oncology
/ Prostate cancer
/ PROTAC
/ Protein degradation
/ Proteins
/ Proteins - antagonists & inhibitors
/ Proteins - metabolism
/ Proteolysis
/ Proteolysis - drug effects
/ Review
/ Signal transduction
/ Small Molecule Libraries - chemistry
/ Small Molecule Libraries - pharmacology
/ Transcription factors
/ Tumors
2021
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Protein degradation technology: a strategic paradigm shift in drug discovery
Journal Article
Protein degradation technology: a strategic paradigm shift in drug discovery
2021
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Overview
Targeting pathogenic proteins with small-molecule inhibitors (SMIs) has become a widely used strategy for treating malignant tumors. However, most intracellular proteins have been proven to be undruggable due to a lack of active sites, leading to a significant challenge in the design and development of SMIs. In recent years, the proteolysis-targeting chimeric technology and related emerging degradation technologies have provided additional approaches for targeting these undruggable proteins. These degradation technologies show a tendency of superiority over SMIs, including the rapid and continuous target consumption as well as the stronger pharmacological effects, being a hot topic in current research. This review mainly focuses on summarizing the development of protein degradation technologies in recent years. Their advantages, potential applications, and limitations are also discussed. We hope this review would shed light on the design, discovery, and clinical application of drugs associated with these degradation technologies.
Publisher
BioMed Central,BioMed Central Ltd,Springer Nature B.V,BMC
Subject
/ Enzymes
/ Humans
/ Kinases
/ Ligands
/ Medicine
/ molecular engineering for drug discovery
/ Mutation
/ New developments in delivery technology
/ Oncology
/ PROTAC
/ Proteins
/ Proteins - antagonists & inhibitors
/ Review
/ Small Molecule Libraries - chemistry
/ Small Molecule Libraries - pharmacology
/ Tumors
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