Abstract
Small molecule covalent inhibitors, or called as irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity. Nevertheless, these agents may also exhibit larger toxicity once off-target effects arise. This "double-edged swords" property often leads drug researchers to avoid attaching them. In recent years, some problems such as drug resistance are difficult to be solved with reversible inhibitors leading researchers to pay more attention on the covalent inhibitors. In this review, we shall make a short summary to the recent research progress of covalent inhibitors and the interaction modes between covalent inhibitors and their target protein residues.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Amino Acids / chemistry*
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / therapeutic use
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Antiviral Agents / chemical synthesis
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Antiviral Agents / chemistry
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Antiviral Agents / therapeutic use
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Drug Discovery*
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Drug Resistance
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / therapeutic use
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ErbB Receptors / antagonists & inhibitors*
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Hepatitis C / drug therapy
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Humans
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Molecular Structure
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Neoplasms / drug therapy
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Protein Binding
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / chemistry*
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Protein Kinase Inhibitors / therapeutic use
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Serine Proteinase Inhibitors / chemical synthesis
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Serine Proteinase Inhibitors / chemistry*
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Serine Proteinase Inhibitors / therapeutic use
Substances
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Amino Acids
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Antineoplastic Agents
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Antiviral Agents
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Enzyme Inhibitors
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Protein Kinase Inhibitors
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Serine Proteinase Inhibitors
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ErbB Receptors