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Related Experiment Video

Updated: Mar 20, 2026

Creating Highly Specific Chemically Induced Protein Dimerization Systems by Stepwise Phage Selection of a Combinatorial Single-Domain Antibody Library

Creating Highly Specific Chemically Induced Protein Dimerization Systems by Stepwise Phage Selection of a Combinatorial Single-Domain Antibody Library

Published on: January 14, 2020

Development of a large peptoid-DOTA combinatorial library.

Jaspal Singh¹, Daniel Lopes², D Gomika Udugamasooriya^3,4,5,6

¹Department of Pharmacological and Pharmaceutical Sciences, University of Houston, Houston, TX, 77204.

|June 4, 2016

Summary

Researchers developed a novel method to create large libraries of potential theranostic agents. This approach combines therapeutic peptoids with imaging DOTA components on beads for efficient screening and drug discovery.

Keywords:

DOTA combinatorial imaging peptoids theranostics

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Last Updated: Mar 20, 2026

Creating Highly Specific Chemically Induced Protein Dimerization Systems by Stepwise Phage Selection of a Combinatorial Single-Domain Antibody Library

Creating Highly Specific Chemically Induced Protein Dimerization Systems by Stepwise Phage Selection of a Combinatorial Single-Domain Antibody Library

Published on: January 14, 2020

Split-and-pool Synthesis and Characterization of Peptide Tertiary Amide Library

Split-and-pool Synthesis and Characterization of Peptide Tertiary Amide Library

Published on: June 20, 2014

Synthesis of Information-bearing Peptoids and their Sequence-directed Dynamic Covalent Self-assembly

Synthesis of Information-bearing Peptoids and their Sequence-directed Dynamic Covalent Self-assembly

Published on: February 6, 2020

Area of Science:

Medicinal Chemistry
Combinatorial Chemistry
Biotechnology

Background:

Conventional one-bead one-compound (OBOC) libraries are primarily used for identifying therapeutic molecules.
The development of molecules with combined therapeutic and imaging capabilities (theranostic agents) using OBOC synthesis has been underexplored.
Designing molecules with both therapeutic and imaging functions for specific targets is challenging.

Purpose of the Study:

To develop a combinatorial library of molecules with fused therapeutic and imaging components for theranostic applications.
To create an on-bead library of Peptoid-DOTA compounds for screening and identification of theranostic candidates.
To establish a facile synthesis method for large peptidomimetic-DOTA libraries.

Main Methods:

Synthesized an on-bead library of 153,600 Peptoid-DOTA compounds.
Utilized TentaGel beads, attaching the DOTA scaffold to one arm and building a 6-mer peptoid library on the remaining three arms.
Evaluated synthesis and mass spectrometric sequencing of compounds and the library.

Main Results:

Compounds exhibited unique ionization patterns, including DOTA scaffold fragmentation, enabling clear sequence decoding.
Demonstrated successful synthesis and characterization of the Peptoid-DOTA library.
Confirmed the feasibility of on-bead development for large peptidomimetic-DOTA libraries.

Conclusions:

The developed approach facilitates the on-bead synthesis of large peptidomimetic-DOTA libraries.
This method enables the screening of molecules for potential theranostic agent identification.
The study offers a pathway for discovering novel theranostic agents against biological targets.