Issue 81, 2021

The C29–C34 parts of antitumor macrolide aplyronine A serve as versatile actin-affinity tags

Abstract

Anticancer drug development inspired by natural products based on protein–protein interactions (PPI) is a promising strategy. We developed structurally-simplified C29–C34 side-chain analogs of aplyronine A (ApA), an antitumor marine macrolide. Among them, the analog possessing the C23 acyloxy group, the C29 N,N-dimethyl-L-alanine ester and the C34 N-methyl enamide showed potent actin-depolymerizing activity. Binding kinetics, molecular docking, and affinity-purification experiments revealed that they are versatile actin-affinity tags to accelerate studies on the mode of action related to cytoskeletal dynamics and the development of PPI-based drug leads.

Graphical abstract: The C29–C34 parts of antitumor macrolide aplyronine A serve as versatile actin-affinity tags

Supplementary files

Article information

Article type
Communication
Submitted
04 Aug 2021
Accepted
16 Sep 2021
First published
17 Sep 2021

Chem. Commun., 2021,57, 10540-10543

The C29–C34 parts of antitumor macrolide aplyronine A serve as versatile actin-affinity tags

D. H. Utomo, A. Fujieda, K. Tanaka, M. Takahashi, K. Futaki, K. Tanabe, H. Kigoshi and M. Kita, Chem. Commun., 2021, 57, 10540 DOI: 10.1039/D1CC04259A

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