Genomics

Dataset Information

0

Homo sapiens


ABSTRACT: Attenuation of Global Transcript Changes Induced by Elastase with Symplostatin 5 Cotreatment

ORGANISM(S): Homo sapiens  

PROVIDER: PRJNA177674 | ENA |

REPOSITORIES: ENA

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Publications

Potent elastase inhibitors from cyanobacteria: structural basis and mechanisms mediating cytoprotective and anti-inflammatory effects in bronchial epithelial cells.

Salvador Lilibeth A LA   Taori Kanchan K   Biggs Jason S JS   Jakoncic Jean J   Ostrov David A DA   Paul Valerie J VJ   Luesch Hendrik H  

Journal of medicinal chemistry 20130128 3


We discovered new structural diversity to a prevalent, yet medicinally underappreciated, cyanobacterial protease inhibitor scaffold and undertook comprehensive protease profiling to reveal potent and selective elastase inhibition. Structure-activity relationship (SAR) studies and X-ray cocrystal structure analysis allowed a detailed assessment of critical and tunable structural elements. To realize the therapeutic potential of these cyclodepsipeptides, we probed the cellular effects of a novel a  ...[more]

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