Synthetic combinatorial OPA-cyclic peptide library

Cyclic peptides have a rising popularity as novel drug due to its improved stability and lower entropic cost for binding.In order to look for potential cyclic peptide drug, a high-throughput screening on various drug target can be done using a cyclic peptide library.Among various types of peptide library, we have chosen to synthesize a cyclic peptide library using the One-Bead-One-Compound (OBOC) strategy.In the design of our cyclic peptide library, we utilized ortho-phthalaldehyde (OPA) to do an on-resin peptide cyclization 1 .After the cyclic peptide library has been synthesized, we conducted a bead-based biological screening on various drug targets, for example, BamA and Walk-EPAS.We have successfully screened a few potential binders through this technique.

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Publication Details

Published
2024-09-20
DOI
https://doi.org/10.17952/37eps.2024.p1031
Primary Topic
Chemical Synthesis and Analysis
Type
article
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article

Synthetic combinatorial OPA-cyclic peptide library

Carina Hey Pui Cheung, Xuechen Li, Kin Nam Adrian Chu
Chemical Synthesis and Analysis
article

Synthetic combinatorial OPA-cyclic peptide library

Carina Hey Pui Cheung, Xuechen Li, Kin Nam Adrian Chu
article en

Abstract

Cyclic peptides have a rising popularity as novel drug due to its improved stability and lower entropic cost for binding.In order to look for potential cyclic peptide drug, a high-throughput screening on various drug target can be done using a cyclic peptide library.Among various types of peptide library, we have chosen to synthesize a cyclic peptide library using the One-Bead-One-Compound (OBOC) strategy.In the design of our cyclic peptide library, we utilized ortho-phthalaldehyde (OPA) to do an on-resin peptide cyclization 1 .After the cyclic peptide library has been synthesized, we conducted a bead-based biological screening on various drug targets, for example, BamA and Walk-EPAS.We have successfully screened a few potential binders through this technique.

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