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Dual function inhibitors of relevance to chronic obstructive pulmonary disease.

ABSTRACT: The general strategy and rationale underlying the design of COPD therapeutics that possess protease inhibitory activity and are also capable of releasing a species that attenuates inflammation by inhibiting caspase-1, are described. The synthesis and in vitro biochemical evaluation of a dual function molecule that sequentially inhibits HNE and caspase-1 in a time-dependent manner is reported.

SUBMITTER: Dou D

PROVIDER: S-EPMC3147253 | biostudies-literature | 2011 May

REPOSITORIES: biostudies-literature

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Dual function inhibitors of relevance to chronic obstructive pulmonary disease.

Dou Dengfeng D He Guijia G Alliston Kevin R KR Groutas William C WC

Bioorganic & medicinal chemistry letters 20101210 10

The general strategy and rationale underlying the design of COPD therapeutics that possess protease inhibitory activity and are also capable of releasing a species that attenuates inflammation by inhibiting caspase-1, are described. The synthesis and in vitro biochemical evaluation of a dual function molecule that sequentially inhibits HNE and caspase-1 in a time-dependent manner is reported. ...[more]

PMID: 21511470

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