Microarray-based enzyme profiling: Recent advances and applications (Review)

Area of Science:

• Biochemistry
• Molecular Biology
• Drug Discovery

Background:

• Enzymes are crucial biological molecules, representing a significant portion of expressed proteins in eukaryotes.
• Many enzymes are implicated in diseases, making them key drug targets, yet most remain poorly understood.
• A gap exists in understanding enzyme functions, substrate specificities, and interactions, hindering their therapeutic potential.

Purpose of the Study:

• To present microarray methods as a high-throughput solution for enzyme characterization.
• To facilitate the biological investigation and drug target adoption of enzymes.
• To bridge the knowledge gap regarding the roles and properties of diverse enzyme classes.

Main Methods:

• Adoption of microarray techniques for high-throughput enzyme profiling.
• Focus on profiling major enzyme classes: kinases, phosphatases, and proteases.
• Development of specific chemical tools, including peptide substrates, activity-based probes, and compound libraries using combinatorial synthesis and click chemistry.

Main Results:

• Demonstration of microarray applicability for profiling kinases, phosphatases, and proteases.
• Successful assembly of chemical tools and libraries for enzyme characterization.
• Establishment of microarrays as a powerful platform for enzyme study and modulation.

Conclusions:

• Microarray-based profiling offers a robust approach to investigate enzyme properties and functions.
• These methods accelerate the characterization of enzyme classes like kinases, phosphatases, and proteases.
• Microarrays enable the discovery of small molecules to modulate enzyme activity, advancing drug discovery efforts.