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Reversible ketomethylene-based inhibitors of human neutrophil proteinase 3.

Abstract：

:Neutrophil serine proteases, proteinase 3 (PR3) and human neutrophil elastase (HNE), are considered as targets for chronic inflammatory diseases. Despite sharing high sequence similarity, the two enzymes have different substrate specificities and functions. While a plethora of HNE inhibitors exist, PR3 specific inhibitors are still in their infancy. We have designed ketomethylene-based inhibitors for PR3 that show low micromolar IC50 values. Their synthesis was made possible by amending a previously reported synthesis of ketomethylene dipeptide isosteres to allow for the preparation of derivatives suitable for solid phase peptide synthesis. The best inhibitor (Abz-VADnV[Ψ](COCH2)ADYQ-EDDnp) was found to be selective for PR3 over HNE and to display a competitive and reversible inhibition mechanism. Molecular dynamics simulations show that the interactions between enzyme and ketomethylene-containing inhibitors are similar to those with the corresponding substrates. We also confirm that N- and C-terminal FRET groups are important for securing high inhibitory potency toward PR3.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Budnjo A,Narawane S,Grauffel C,Schillinger AS,Fossen T,Reuter N,Haug BE

doi

10.1021/jm500782s

subject

Has Abstract

pub_date

2014-11-26 00:00:00

pages

9396-408

issue

22

eissn

0022-2623

issn

1520-4804

journal_volume

57

pub_type

杂志文章

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