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Modification of Connection between Nucleobase and Backbone

Modification of Connection between Nucleobase and Backbone

The bases in PNA are generally bound to the backbone through acetyl groups. Changing the connection method and position of the base and the backbone will cause certain changes in the structure of the PNA, which may affect the stability of hybridization.

Modification of Connection between Nucleobase and Backbone

Now, because the modification of PNA is expected to solve the difficulties in its development and utilization in many fields, it is necessary to pay attention to the development and design of PNA. Creative Peptides is committed to providing tailor-made PNA research according to the needs of specific products.

Connection Methods

The PNA monomer usually first forms the base into the base acetic acid, and then connects it to the unprotected N atom on the backbone by condensation. The performance of PNA may be optimized by modifying the connection method, the following are several modification schemes.

Method

Application

Structure

The unprotected N on the bone frame reacts with chloroacetic acid to form acid chloride, and then directly reacts with the base

Improve affinity

The base and backbone connection method

Use propionyl group instead of acetyl group to attach thymine to the PNA backbone

Improve affinity

The base and backbone connection method

Use ethyl group instead of acetyl group to connect, and introduce carboxylic acid ester in the bone frame

Enhance water solubility

The base and backbone connection method

Connection Position

In addition to changing the connection mode, the base can also be combined with the backbone by changing the connection position. Here are some examples that have been successfully transformed.

Method

Application

Structure

Synthesize a new type of PNA monomer by U-4CR method, and its base was connected to the α position of PNA backbone

Selectively hydrolyzed

The base and backbone connection position

Connect the bases to the PNA backbone through a ring structure

Improve hybridity

The base and backbone connection position

Our Highlights

  • We will cooperate with customers at each stage of PNA development, provide a complete test plan, select the appropriate program and process, and monitor the entire test process.
  • We provide modification strategies based on product diversity and inherent biological characteristics. A professional operation team with rich experimental experience can provide active solutions to the complexity of PNA synthesis and modification, and perform experiments efficiently.
  • In addition to customized services, we also provide a series of quality assurance studies, such as GC-MS, HPLC analysis, to achieve quality monitoring and understanding of the effects of finished products. In order to further ensure the effectiveness of the product, we will test it.

Creative Peptides is committed to providing comprehensive PNA development services to design and customize, synthesize and modify, so as to promote your PNA development plan. If you are interested in our services, please feel free to contact us to discuss how we can participate in your PNA development plan.

Reference

  • Zeng F. et al. Progress in the synthesis of modified peptide nucleic acids. Chinese Pharmaceutical Journal. 2015, 50(22):1936-1945.

Notice: Products and services are used only for scientific research.