Controlling Surface Wettability for Automated In Situ Array Synthesis and Direct Bioscreening.

Area of Science:

• Biomaterials Science
• Chemical Biology
• Pharmaceutical Sciences

Background:

• In situ biomolecule synthesis on glass surfaces is crucial for pharmaceutical sciences, biomaterials, and chemical biology.
• Challenges include achieving high yields in small-feature-size combinatorial synthesis and developing compatible surfaces for synthesis and screening.

Purpose of the Study:

• To develop an advanced amphiphilic glass surface coating.
• To enable automated, high-yield in situ combinatorial synthesis of small molecules and peptides.
• To facilitate seamless transition from synthesis to protein- and cell-based bioscreening.

Main Methods:

• Coating glass surfaces with an amphiphilic layer to enhance contact angle and inhibit solvent droplet motion.
• Utilizing automated multiple rounds of combinatorial synthesis for small-molecule compounds and peptides.
• Switching the amphiphilic coating to a hydrophilic network for subsequent bioscreening.

Main Results:

• Successful in situ synthesis of small molecules and peptides on glass surfaces with enhanced droplet control.
• Demonstrated compatibility of the surface for both combinatorial synthesis and downstream bioscreening.
• Enabled rapid probing of chemical space using array technology.

Conclusions:

• The developed amphiphilic coating provides a versatile platform for automated in situ synthesis and bioscreening.
• This method significantly accelerates lead discovery and optimization in medicinal chemistry.
• It offers a novel approach for efficient biomaterial development and characterization.