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Morphological profiling of small molecules.

Slava Ziegler¹, Sonja Sievers¹, Herbert Waldmann²

¹Max-Planck Institute of Molecular Physiology, Department of Chemical Biology, Otto-Hahn-Strasse 11, 44227 Dortmund, Germany.

Cell Chemical Biology

|March 19, 2021

Summary

This summary is machine-generated.

Morphological profiling uses automated imaging to detect cellular changes induced by small molecules, aiding drug discovery. This unbiased approach helps predict compound activity and targets early in development.

Keywords:

biological activity mode of action morphology profiling targets

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Area of Science:

Cellular imaging and analysis
Pharmacology
Drug discovery

Background:

Small-molecule bioactivity profiling, including gene expression and proteome profiling, provides unbiased insights into cellular states.
Automated imaging and image analysis offer high-throughput detection of morphological alterations induced by small molecules.

Purpose of the Study:

To review current morphological profiling approaches.
To discuss the types of bioactivity detectable and predictable through morphological profiling.
To highlight the growing importance of morphological profiling in drug discovery.

Main Methods:

High-throughput screening using automated microscopy.
Image analysis to quantify hundreds of morphological features.
Generation of small-molecule bioactivity profiles based on cellular morphology.

Main Results:

Morphological profiling enables detection of bioactivity in compound collections within a broader biological context.
This method aids in predicting the mode of action or targets of novel compounds.
Unanticipated activities of known small molecules can be uncovered.

Conclusions:

Morphological profiling is a valuable, unbiased tool for early-stage compound evaluation in drug discovery.
It offers a powerful method for understanding small-molecule effects and predicting their biological relevance.
The review synthesizes current knowledge on morphological profiling techniques and their applications.