Alfa Chemistry is an expert in the field of drug discovery and has established an advanced DNA-encoded libraries (DELs) technology platform dedicated to building and synthesizing a large number of novel, diverse, drug-like compound libraries.
We can provide synthesis services of DELs of peptidomimetic macrocycles. Our world-class laboratories and scientists can support your unique synthetic needs and help you apply peptidomimetic macrocycle DELs to enable affinity screening against targeted proteins for hit discovery.
What are Peptidomimetic Macrocycles?
Peptidomimetic macrocycles are a class of peptidomimetics that are characterized by their macrocyclic structure that consists of rings of atoms typically containing 12 or more core scaffold atoms. These larger, more flexible structures enable macrocyclic peptidomimetics to reach binding hotspots on the protein surface and interact with biological targets with high affinity and selectivity. Peptidomimetic macrocycles such as cyclosporine A and certain antibiotics have demonstrated therapeutic efficacy in various disease conditions. In a word, peptidomimetic macrocycles have great potential in the development of new drugs [1].
Macrocycles have always been one of the most popular research directions in the field of supramolecular chemistry. However, it is extremely challenging to construct macrocycles simply and efficiently, since they are structurally complex in nature, which may pose significant synthetic obstacles [1].
In addition, difficulties in developing analogs of synthetic peptidomimetic macrocycles, much like natural product macrocycles, include difficulties in predicting the unique folding mechanisms responsible for function and cell permeability.
Our Capabilities
Based on the valuable DELs technology platform, Alfa Chemistry provides professional synthesis services for DELs of peptidomimetic macrocycles. Our experienced team of chemists utilize state-of-the-art technologies and methods to design and custom-synthesize a compound library of peptidomimetic macrocycles with diverse chemical structures and properties based on customer needs. By leveraging our expertise in peptidomimetic chemistry and DELs, we can effectively generate large DNA-encoded peptidomimetic macrocycle libraries for screening against specific biological targets.
Custom synthesis of peptidomimetic macrocycle DELs
Most DELs are synthesized by DNA-tagged combinatorial chemistry. A series of chemical building blocks (BBs) combine chemical synthesis and DNA encoding through split-and-pool methods to ultimately synthesize compound libraries efficiently, cost-effectively, and quickly.
Alfa Chemistry utilizes split-and-pool DNA synthesis to generate large libraries of DNA-tagged peptidomimetic-based macrocycles, whose BBs are typically a combination of natural and unnatural amino acid-like structures. The peptidomimetic macrocycle DELs enables in vitro affinity-based selection against protein targets of interest to discover hits.
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Reference
- Connors, W. H.; et al. DNA-encoded chemical libraries of macrocycles. Curr Opin Chem Biol. 2015, 26: 42-7.