Leupeptazin, a highly modified tripeptide isolated from cultures of a Streptomyces sp. inhibits cathepsin K.

Natasha Kruglyak, David E Williams, Henry Chen, Simon Law, Jadwiga Kaleta, Ivan Villanueva, Julian E Davies, Raymond J Andersen, Dieter Brömme

Bioorganic & medicinal chemistry letters 2017 Mar 15

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Using a human cathepsin K-targeting inhibitor screen, a new leupeptin analogue, leupeptazin (1), containing an unprecedented piperidinotriazine moiety, was isolated from a liquid culture of soil Streptomyces sp. IS2-4 collected in northern Italy. The structure of leupeptazin was established using HRESIMS as well as 1D and 2D NMR data. The inhibitory activity of the compound towards the collagenase cathepsin K was tested in vitro to reveal moderate activity with an inhibition constant, Ki, of 44μM. Copyright © 2017 Elsevier Ltd. All rights reserved.

Citation

Natasha Kruglyak, David E Williams, Henry Chen, Simon Law, Jadwiga Kaleta, Ivan Villanueva, Julian E Davies, Raymond J Andersen, Dieter Brömme. Leupeptazin, a highly modified tripeptide isolated from cultures of a Streptomyces sp. inhibits cathepsin K. Bioorganic & medicinal chemistry letters. 2017 Mar 15;27(6):1397-1400