Negative allosteric modulators

Negative allosteric modulators (NAMs) are a type of pharmacological agent that decrease the activity of proteins, typically receptors, by binding to a site on the protein that is distinct from the active site. This site is referred to as an allosteric site. NAMs are a type of allosteric modulator, which also includes positive allosteric modulators (PAMs) and neutral allosteric ligands (NALs).

Mechanism of Action

NAMs function by binding to an allosteric site on a protein. This binding changes the protein's conformation, or shape, which in turn reduces the protein's activity. This is in contrast to competitive inhibition, where the inhibitor binds directly to the active site of the protein and prevents the natural ligand from binding.

NAMs can have a variety of effects on the protein's function. They can decrease the protein's affinity for its ligand, decrease the efficacy of the ligand, or both. The specific effect depends on the nature of the NAM and the protein to which it binds.

Applications

NAMs have a wide range of potential applications in medicine. They can be used to modulate the activity of a variety of proteins, including enzymes and receptors. This makes them potentially useful for treating a wide range of conditions, including neurological disorders, cancer, and infectious diseases.

For example, NAMs that target the GABA receptor are being investigated for their potential use in treating anxiety and insomnia. Similarly, NAMs that target the glutamate receptor could potentially be used to treat schizophrenia and other psychiatric disorders.

See Also

• Positive allosteric modulator
• Allosteric regulation
• Pharmacology
• Receptor (biochemistry)

Resources

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Source: Data courtesy of the U.S. National Library of Medicine. Since the data might have changed, please query MeSH on Negative allosteric modulators for any updates.

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