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Design, synthesis and analysis of charged RGD derivatives



Bonaventure Mujyambere1, Subasri Mohanakrishnan1, Shoufia Jabeen Mubarak2, Hemamalini Vedagiri2, Sivasamy Ramasamy3 & Suja Samiappan1*



1Department of Biochemistry & 2Department of Bioinformatics & 3Department of Human Genetics and Molecular Biology, Bharathiar University, Coimbatore, Tamilnadu, India; *Corresponding author



Bonaventure Mujyambere E-mail: mubona@gmail.com

Subasri Mohanakrishnan - E-mail: subamohan025@gmail.com

Shoufia Jabeen E-mail: shoufiamdu@gmail.com

Hemamalini Vedagiri E-mail: hemamalini@buc.edu.in

Sivasamy Ramasamy E-mail: rshgmb@buc.edu.in

Suja Samiappan E-mail: suja.s@buc.edu.in


Article Type

Research Article



Received September 1, 2023; Revised September 30, 2023; Accepted September 30, 2023, Published September 30, 2023



In the present study, negatively charged N-Biotin-RGD and positively charged C-Biotin-RGD were designed, synthesized, and characterized with docking analysis. The fixation of MDA-MB-231 cells with formalin made their cell surface neutrally charged thus removing the electrostatic interactions between charged biotinylated RGD derivatives and MDA-MB-231 cells. The results of the binding affinity of biotinylated RGD derivatives against MDA-MB-231 cells showed that N-Biotin-RGD had higher binding affinity than C-Biotin-RGD. The cytotoxic effect was analyzed by incubating charged biotinylated RGD derivatives with live MDA-MB-231 cells. MDA-MB-231 cell surface is negatively charged due to high hypersialyliation of polyglycans and Warburg effect. The results of their cytotoxic activities against live MDA-MB-231 cells were found to be electrostatic in nature. C-Biotin-RGD had an attractive interaction with the MDA-MB-231 cell surface resulting in a higher cytotoxic effect. In comparison, N-Biotin-RGD had a repulsive interaction with the MDA-MB-231 cell surface resulting in a lower cytotoxic effect. Hence, positively charged C-Biotin-RGD is a better cytotoxic agent than a negatively charged N-Biotin-RGD against MDA-MB-231 cells.



Design, synthesis, analysis, charged RGD derivatives



Mujyambere et al. Bioinformation 19(9): 918-924 (2023)


Edited by

P Kangueane






Biomedical Informatics



This is an Open Access article which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited. This is distributed under the terms of the Creative Commons Attribution License.