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Synthesis of Novel Carborane-Containing Derivatives of RGD Peptide

Short peptides containing the Arg-Gly-Asp (RGD) fragment can selectively bind to integrins on the surface of tumor cells and are attractive transport molecules for the targeted delivery of therapeutic and diagnostic agents to tumors (for example, glioblastoma). We have demonstrated the possibility of obtaining the N- and C-protected RGD peptide containing 3-amino-closo-carborane and a glutaric acid residue as a linker fragment. The resulting carboranyl derivatives of the protected RGD peptide are of interest as starting compounds in the synthesis of unprotected or selectively protected peptides, as well as building blocks for preparation of boron-containing derivatives of the RGD peptide of a more complex structure.

 

Comments:

That's fascinating! It seems like you're discussing the potential use of short peptides containing the Arg-Gly-Asp (RGD) fragment for targeted delivery of therapeutic and diagnostic agents to tumors, specifically glioblastoma. The RGD sequence is known to selectively bind to integrins on the surface of tumor cells, making it an attractive option for targeted delivery.

You mentioned the possibility of obtaining N- and C-protected RGD peptides containing 3-amino-closo-carborane and a glutaric acid residue as a linker fragment. These carboranyl derivatives of the protected RGD peptide can serve as valuable starting compounds in the synthesis of unprotected or selectively protected peptides. They can also be used as building blocks for the preparation of boron-containing derivatives of the RGD peptide with more complex structures.

The incorporation of boron atoms into peptides can offer unique properties and potential applications, particularly in the field of boron neutron capture therapy (BNCT), where boron-containing compounds are used to selectively destroy tumor cells through the release of high-energy particles upon neutron irradiation.

By utilizing the RGD peptide sequence and modifying it with boron-containing compounds, there is potential to enhance the targeting specificity and therapeutic efficacy in the treatment of glioblastoma and other types of tumors.

It's important to note that the information you provided seems to be a description of research or a scientific study. If you have any specific questions or would like further information on a particular aspect, please let me know!

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Integrin