Activation of MMP‐9 by neutrophil elastase in an in vivo model of acute lung injury
- G. Ferry, M. Lonchampt, Laurence Pennel, G. de Nanteuil, E. Canet, G. C. Tucker
- Biology, MedicineFEBS Letters
- 27 January 1997
New prolyl endopeptidase inhibitors: in vitro and in vivo activities of azabicyclo[2.2.2]octane, azabicyclo[2.2.1]heptane, and perhydroindole derivatives.
- B. Portevin, A. Benoist, G. de Nanteuil
- Chemistry, BiologyJournal of Medicinal Chemistry
- 7 June 1996
A series of potent and selective prolylendopeptidase (PEP) inhibitors of the alpha-keto heterocyclic type has been obtained by replacing the classical central proline of…
S 17092-1, a highly potent, specific and cell permeant inhibitor of human proline endopeptidase.
- H. Barelli, A. Petit, F. Checler
- Biology, ChemistryBiochemical and Biophysical Research…
- 21 April 1999
It is established that S17092-1 behaves as a highly potent, specific and cell permeant inhibitor of human proline endopeptidase and can be seen as a probe to examine PE contribution in Alzheimer's disease.
Pharmacodynamic and pharmacokinetic profile of S 17092, a new orally active prolyl endopeptidase inhibitor, in elderly healthy volunteers. A phase I study.
- P. Morain, J. Robin, G. de Nanteuil, R. Jochemsen, V. Heidet, D. Guez
- MedicineBritish Journal of Clinical Pharmacology
- 24 December 2001
S 17092 had a potent, dose-dependent inhibitory effect on plasmatic PEP, increased alpha band EEG at the 100 mg dose and improved performance in two verbal memory tests at the 1200 mg dose while there were disruption to the vigilance task.
S 17092: a prolyl endopeptidase inhibitor as a potential therapeutic drug for memory impairment. Preclinical and clinical studies.
- P. Morain, P. Lestage, P. Boyer
- Biology, PsychologyCNS drug reviews
- 7 June 2006
The preclinical and clinical effects of S 17092 have suggested a promising role for this compound as an agent for the treatment of cognitive disorders associated with cerebral aging.
Effects of ceramide on apoptosis, proteoglycan degradation, and matrix metalloproteinase expression in rabbit articular cartilage.
- M. Sabatini, G. Rolland, J. Bonnet
- Biology, MedicineBiochemical and Biophysical Research…
- 7 January 2000
The hypothesis that ceramide might play a mediatory role in both matrix degradation and apoptosis in processes of cartilage loss such as those observed in osteoarthritis is supported.
Effect of inhibition of matrix metalloproteinases on cartilage loss in vitro and in a guinea pig model of osteoarthritis.
- M. Sabatini, C. Lesur, P. Pastoureau
- Biology, MedicineArthritis & Rheumatism
- 2005
In both treated animal groups, S-34219 significantly prevented the loss of cartilage thickness, probably by inhibiting collagen breakdown that normally leads to the erosion of fibrillated superficial areas.
Further evidence for a dissociation between different forms of mnemonic expressions in a mouse model of age-related cognitive decline: effects of tacrine and S 17092, a novel prolyl endopeptidase…
- A. Marighetto, K. Touzani, P. Morain
- Psychology, BiologyLearning & memory (Cold Spring Harbor, N.Y.)
- 1 May 2000
It is concluded that the specific patterns of drug effects on the three indices of discriminative performance might suggest that each index is associated with a distinct form of mnemonic expression relying on separate neural systems.
Effects of ceramide on aggrecanase activity in rabbit articular cartilage.
- M. Sabatini, M. Thomas, J. Bonnet
- BiologyBiochemical and Biophysical Research…
- 25 May 2001
Results show that, similarly to IL-1 and TNF, ceramide-induced aggrecan degradation is mainly due to Aggrecanases, and support the hypothesis that cytokine-induced ceramide could play a mediatory role in situations of increased degradation of cartilage matrix.
Low molecular weight activated protein C inhibitors as a potential treatment for hemophilic disorders.
- G. de Nanteuil, P. Gloanec, T. Verbeuren
- Chemistry, BiologyJournal of Medicinal Chemistry
- 25 July 2006
Benzamidine-containing derivatives were found to be potent aPC inhibitors, some of them showing selectivity against the procoagulant proteaseThrombin, and compound 1 significantly restored the generation of thrombin in hemophiliac plasma.
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