Testing for drug-human serum albumin binding using fluorescent probes and other methods

Area of Science:

• Pharmacology
• Biochemistry

Background:

• Drug plasma protein binding is critical in drug development.
• Existing methods lack the throughput for large compound libraries.
• Early-stage evaluation of ADME necessitates higher-throughput assays.

Purpose of the Study:

• To review recent advancements in drug plasma binding profiling methods.
• To emphasize fluorescent probes and high-throughput methodologies.

Main Methods:

• Fluorescent probe displacement assays offer flexibility and scalability for high-throughput screening.
• Homogenous time-resolved fluorescence and aggregation-induced emission probes enhance assay sensitivity.
• Microscale thermophoresis and QSAR modeling are emerging alternative techniques.

Main Results:

• High-throughput assays have been developed to meet increased demands for compound profiling.
• Fluorescent probe assays are adaptable for large compound libraries.
• Recent fluorescence technologies improve assay sensitivity.

Conclusions:

• Assay technology selection depends on laboratory capabilities and data requirements.
• Fluorescent probes are a key technology for scalable drug plasma protein binding assessment.
• Emerging techniques like microscale thermophoresis and QSAR modeling provide valuable alternatives.