Basic & clinical pharmacology & toxicology · 2012
A highly soluble matrix metalloproteinase-9 inhibitor for potential treatment of dry eye syndrome.
СтатьяПоддержка исследования: вне правительства СШАНазвание и аннотация: Перевод в очереди
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Mori Mattia, De Lorenzo Emanuele, Torre Eugenio, Fragai Marco, Nativi Cristina, Luchinat Claudio, Arcangeli Annarosa
Аннотация
Dry eye syndrome (DES) or keratoconjunctivitis sicca is an eye disease caused by the chronic lack of lubrication and moisture of the eye. The pathogenesis of DES involves the over-expression and over-activity of corneal Matrix Metalloproteinase 9 (MMP-9). We propose herein a new, non-symptomatic approach for the treatment of DES based on the inhibition of MMP-9 by a new highly soluble molecule, designed as PES_103 that has been shown to inhibit MMP-9 both in vitro and in vivo. The efficacy of PES_103 in vivo and the potential benefits of this treatment in restoring tear production were studied in this work using an animal model of reduced lacrimation. PES_103 did not show any significant corneal toxicity.
Предметные рубрики MeSH
AnimalsCell LineCorneaDisease Models, AnimalDose-Response Relationship, DrugDry Eye SyndromesFemaleHumansHydroxamic AcidsKeratoconjunctivitis SiccaMatrix Metalloproteinase 2Matrix Metalloproteinase 9Matrix Metalloproteinase InhibitorsMiceMice, Inbred BALB CMice, Inbred C57BLMolecular Targeted TherapyOphthalmic SolutionsRecombinant ProteinsSolubilitySulfonamidesTears