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 o...

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Bibliographic Details
Main Authors: Alexander V. Vakhrushev, Dmitry A. Gruzdev, Alexander M. Demin, Galina L. Levit, Victor P. Krasnov
Format: Article
Language:English
Published: MDPI AG 2023-04-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/28/8/3467
Description
Summary: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 <i>N</i>- and <i>C</i>-protected RGD peptide containing 3-amino-<i>closo</i>-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.
ISSN:1420-3049