Related Experiment Video
Updated: Jul 3, 2026

Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase
Published on: November 23, 2016
Structures of human arylamine N-acetyltransferases
1Department of Pharmacology and Toxicology, University of Toronto, 1 King's College Circle, Toronto, Ontario M5S1A8, Canada. denis.grant@utoronto.ca
Human arylamine N-acetyltransferases NAT1 and NAT2 (N-acetyltransferases) are crucial for drug metabolism. Understanding their structure and function aids in predicting therapeutic and toxic outcomes of related chemicals.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Over 80 years of research has elucidated human arylamine N-acetyltransferases (NAT1 and NAT2) structure-function relationships.
- Key groundwork includes biochemical studies, enzyme kinetics, gene cloning, and structural analysis of prokaryotic orthologues.
Purpose of the Study:
- To provide a historical overview of human NAT1 and NAT2 research.
- To summarize current knowledge on human NAT1 and NAT2 structures and functions.
- To explore future applications in predicting therapeutic and toxicological outcomes.
Main Methods:
- Biochemical and enzyme kinetic studies in various model systems.
- Cloning and amino acid sequence determination of NAT enzymes.
- Characterization of natural and mutated human NAT forms.
- Crystal structure elucidation of prokaryotic NAT orthologues.
- Cross-species comparisons and direct structural analysis of human NAT1 and NAT2.
Main Results:
- Significant insights into the structure-function correlation of human NAT1 and NAT2 have been gained.
- Crystallization and structural analysis of human NAT1 and NAT2 in 2007 substantially advanced research.
- A comprehensive understanding of NAT enzyme mechanisms and substrate specificities has been developed.
Conclusions:
- Knowledge of human NAT1 and NAT2 structures and functions is vital for understanding chemical acetylation.
- This information can be applied to predict the therapeutic efficacy and toxicity of aromatic amine and hydrazine compounds.
- Further research can optimize drug development and safety assessments.
Related Concept Videos
Phase II Reactions: Acetylation Reactions
The substrates for acetylation are typically drugs or their metabolites with an amino, sulfonamide, or hydrazine functional group. Acetylation can occur at several points in the drug molecule, including primary, secondary, and...
Pharmacogenetics of Phase II Enzymes: N-acetyltransferase, Thiopurine S-methyltransferase, UDP-glucuronosyltransferase
Nomenclature of Aryl and Heterocyclic Amines
Physical Properties of Amines
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of the aromatic...
Structure of Amines

