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Issue 19, 2021
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Facile synthesis of rapamycin-peptide conjugates as mTOR and Akt inhibitors

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Abstract

A simple and straightforward process for the synthesis of rapamycin peptide conjugates in a regio and chemoselective manner was developed. The methodology comprises the tagging of chemoselective functionalities to rapamycin and peptides which enables the conjugation of free peptides, without protecting the functionality of the side chain amino acids, in high yield and purity. From this methodology, we successfully conjugate free peptides containing up to 15 amino acids. Rapamycin is also conjugated to the peptides known for inhibiting the kinase activity of Akt protein. These conjugates act as dual target inhibitors and inhibit the kinase activity of both mTOR and Akt.

Graphical abstract: Facile synthesis of rapamycin-peptide conjugates as mTOR and Akt inhibitors

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Article information


Submitted
23 Jan 2021
Accepted
06 Apr 2021
First published
07 Apr 2021

Org. Biomol. Chem., 2021,19, 4352-4358
Article type
Paper

Facile synthesis of rapamycin-peptide conjugates as mTOR and Akt inhibitors

S. Singh, R. Ali, J. Miyan, V. Singh, S. Meena, M. Hasanain, S. Bhadauria, D. Datta, J. Sarkar and W. Haq, Org. Biomol. Chem., 2021, 19, 4352
DOI: 10.1039/D1OB00132A

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