Issue 40, 2023

Catalytic olefin metathesis in blood

Abstract

The direct synthesis of drugs in vivo enables drugs to treat diseases without causing side effects in healthy tissues. Transition-metal reactions have been widely explored for uncaging and synthesizing bioactive drugs in biological environments because of their remarkable reactivity. Nonetheless, it is difficult to develop a promising method to achieve in vivo drug synthesis because blood cells and metabolites deactivate transition-metal catalysts. We report that a robust albumin-based artificial metalloenzyme (ArM) with a low loading (1–5 mol%) can promote Ru-based olefin metathesis to synthesize molecular scaffolds and an antitumor drug in blood. The ArM retained its activity after soaking in blood for 24 h and provided the first example of catalytic olefin cross metathesis in blood. Furthermore, the cyclic-Arg-Gly-Asp (cRGD) peptide-functionalized ArM at lower dosages could still efficiently perform in vivo drug synthesis to inhibit the growth of implanted tumors in mice. Such a system can potentially construct therapeutic drugs in vivo for therapies without side effects.

Graphical abstract: Catalytic olefin metathesis in blood

Supplementary files

Article information

Article type
Edge Article
Submitted
22 7 2023
Accepted
05 9 2023
First published
27 9 2023
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY-NC license

Chem. Sci., 2023,14, 11033-11039

Catalytic olefin metathesis in blood

I. Nasibullin, H. Yoshioka, A. Mukaimine, A. Nakamura, Y. Kusakari, T. Chang and K. Tanaka, Chem. Sci., 2023, 14, 11033 DOI: 10.1039/D3SC03785A

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