M. Reboud-Ravaux

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Proteasome inhibitors: recent advances and new perspectives in medicinal chemistry.

M Reboud-Ravaux, J Vidal, E. Génin, 2010, Current topics in medicinal chemistry.

Towards the control of intracellular protein turnover: mitochondrial Lon protease inhibitors versus proteasome inhibitors.

B. Friguet, N. Basse, B. Pirotte, 2008, Biochimie.

Identification of a β1/β2-specific sulfonamide proteasome ligand by crystallographic screening.

M. Groll, P. Beck, M. Reboud-Ravaux, 2015, Angewandte Chemie.

Bisbenzimidazole derivatives as potent inhibitors of the trypsin-like sites of the immunoproteasome core particle.

E. S. Gromova, D. Bouvier, O. Koroleva, 2015, Biochimie.

A cyclopeptidic suicide substrate preferentially inactivates urokinase-type plasminogen activator.

M. Reboud-Ravaux, N. Boggetto, A. Vilain, 1991, Biochemical and biophysical research communications.

Identification by in silico and in vitro screenings of small organic molecules acting as reversible inhibitors of kallikreins.

B. Villoutreix, A. Hovnanian, Xiao Tan, 2013, European journal of medicinal chemistry.

Regulation of the 26S proteasome activities by peptides mimicking cleavage products.

O. Coux, D. Papapostolou, M. Reboud-Ravaux, 2002, Biochemical and biophysical research communications.

Stereoselective Synthesis of Peptidyl Trifluoromethyl Alcohols and Ketones: Inhibitory Potency Against Human Leucocyte Elastase, Cathepsin G, Porcine Pancreatic Elastase and HIV‐1 Protease

D. Bonnet-Delpon, J. Bégué, A. Amour, 1998, The Journal of pharmacy and pharmacology.

Liberation of an N-terminal proline-rich peptide from the cryptic proteinase of fibronectin by auto-proteolysis.

G. Bolbach, M. Michiel, M. Pagano, 2008, Archives of biochemistry and biophysics.

Dimerized linear mimics of a natural cyclopeptide (TMC-95A) are potent noncovalent inhibitors of the eukaryotic 20S proteasome.

M. Groll, Nerea Gallastegui, E. Génin, 2013, Journal of medicinal chemistry.

Development of lipopeptides for inhibiting 20S proteasomes.

N. Basse, Elise Bernard, R. Vanderesse, 2006, Bioorganic & medicinal chemistry letters.

Noncovalent inhibition of 20S proteasome by pegylated dimerized inhibitors.

N. Basse, E. Génin, M. Reboud-Ravaux, 2012, European journal of medicinal chemistry.

Linear TMC-95-based proteasome inhibitors.

N. Basse, J. Sobczak-Thépot, D. Papapostolou, 2007, Journal of medicinal chemistry.

Structure-based design of human immuno- and constitutive proteasomes inhibitors.

R. le Guével, E. Génin, M. Reboud-Ravaux, 2018, European journal of medicinal chemistry.

Proteasome inhibitors.

M. Reboud-Ravaux, 2002, Progress in molecular and subcellular biology.

Blockade of the malignant phenotype by β-subunit selective noncovalent inhibition of immuno- and constitutive proteasomes

B. Villoutreix, M. Miteva, Yan Cheng, 2017, Oncotarget.

Development of pseudopeptides and peptidomimetics as eukaryote proteasome inhibitors

N. Basse, Elise Bernard, R. Vanderesse, 2009 .

Acyloxybenzyl halides, inhibitors of elastases.

V. Okochi, M. Reboud-Ravaux, A. Vilain, 1991, Biochimica et biophysica acta.

Role of monocyte/macrophage derived matrix-metalloproteinases (gelatinases) in prolonged skin inflammation.

M. Reboud-Ravaux, J. Maillard, C. Favreau, 1995, Clinica chimica acta; international journal of clinical chemistry.

Piperlongumine and some of its analogs inhibit selectively the human immunoproteasome over the constitutive proteasome.

V. Bolzani, M. Furlan, C. El Amri, 2018, Biochemical and biophysical research communications.

Synthesis and Inhibition of Human Leucocyte Elastase by Functionalized N‐Aryl Azetidin‐2‐ones: Effect of Different Substituents on the Aromatic Ring

M. Reboud-Ravaux, N. Boggetto, M. Wakselman, 1996, The Journal of pharmacy and pharmacology.

Cryptic activities of fibronectin fragments, particularly cryptic proteases.

M. Pagano, M. Reboud-Ravaux, 2011, Frontiers in bioscience.

COVID-19 Therapies: Protease Inhibitions and Novel Degrader Strategies

C. El Amri, M. Reboud-Ravaux, 2022, Frontiers in Drug Discovery.

Coumarinic derivatives show anti-inflammatory effects on alveolar macrophages, but their anti-elastase activity is essential to reduce lung inflammation in vivo.

B. Pirotte, E. Bissonnette, M. Reboud-Ravaux, 2009, International immunopharmacology.

Insights into the activity control of the kallikrein-related peptidase 6: small-molecule modulators and allosterism

V. Magdolen, D. Stratmann, C. El Amri, 2018, Biological chemistry.

Metal-organic compounds: a new approach for drug discovery. N1-(4-methyl-2-pyridyl)-2,3,6-trimethoxybenzamide copper(II) complex as an inhibitor of human immunodeficiency virus 1 protease.

A. Mouithys-Mickalad, G. Deby-dupont, F. Durant, 2002, Biochemical pharmacology.

New mechanism-based inactivators of trypsin-like proteinases. Selective inactivation of urokinase by functionalized cyclopeptides incorporating a sulfoniomethyl-substituted m-aminobenzoic acid residue.

M. Reboud-Ravaux, N. Boggetto, A. Vilain, 1993, Journal of medicinal chemistry.

Irreversible inhibition and peptide mapping of urinary plasminogen activator urokinase

M. Reboud-Ravaux, F. Chapeville, G. Desvages, 1982, FEBS letters.

Introduction of polar groups on the naphthalene scaffold of molecular tongs inhibiting wild-type and mutated HIV-1 protease dimerization

R. Fanelli, N. Tonali, J. Soulier, 2014 .

Carbonylhydrazide-based molecular tongs inhibit wild-type and mutated HIV-1 protease dimerization.

R. Fanelli, B. Crousse, J. Soulier, 2012, Journal of medicinal chemistry.

Susceptibility of plasminogen activators to suicide inactivation

M. Reboud-Ravaux, J. Mazaleyrat, M. Wakselman, 1988 .

Esters and amides of 6-(chloromethyl)-2-oxo-2H-1-benzopyran-3-carboxylic acid as inhibitors of alpha-chymotrypsin: significance of the "aromatic" nature of the novel ester-type coumarin for strong inhibitory activity.

J Delarge, B. Masereel, B. Pirotte, 1996, Journal of medicinal chemistry.

Toward the first class of suicide inhibitors of kallikreins involved in skin diseases.

A. Hovnanian, B. Pirotte, Xiao Tan, 2015, Journal of medicinal chemistry.

3-Bromophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate inhibits cancer cell invasion in vitro and tumour growth in vivo

J. Foidart, A. Noël, B. Masereel, 2003, British Journal of Cancer.

Design and synthesis of hydrazinopeptides and their evaluation as human leukocyte elastase inhibitors.

J. Vidal, L. Guy, A. Amour, 1998, Journal of medicinal chemistry.

New constrained "molecular tongs" designed to dissociate HIV-1 protease dimer.

B. Collinet, J. Dumond, S. Sicsic, 2004, Journal of medicinal chemistry.

Specific inhibitors of human leukocyte elastase

B. Masereel, B. Pirotte, L. Pochet, 2000 .

Coumarinic derivatives as mechanism-based inhibitors of alpha-chymotrypsin and human leukocyte elastase.

G. Dive, J. Wouters, B. Masereel, 2000, Bioorganic & medicinal chemistry.

6-Substituted 2-oxo-2H-1-benzopyran-3-carboxylic acid as a core structure for specific inhibitors of human leukocyte elastase.

B. Pirotte, L. Pochet, M. Reboud-Ravaux, 1999, Journal of medicinal chemistry.

Esters and Amides of 6‐(Chloromethyl)‐2‐oxo‐2H‐1‐benzopyran‐3‐ carboxylic Acid as Inhibitors of α‐Chymotrypsin: Significance of the “Aromatic” Nature of the Novel Ester‐Type Coumarin for Strong Inhibitory Activity.

P. Tullio, B. Masereel, B. Pirotte, 1996 .

Interaction of human leukocyte elastase with a N-aryl azetidinone suicide substrate: Conformational analyses based on the mechanism of action of serine proteinases.

M. Reboud-Ravaux, P. Laugâa, I. Vergely, 1996, Journal of molecular graphics.

Functionalized N‐aryl azetidinones as novel mechanism‐based inhibitors of neutrophil elastase

V. Okochi, M. Reboud-Ravaux, N. Boggetto, 1991, FEBS letters.

Stereoselective synthesis and inhibitor properties towards human leucocyte elastase of chiral β-peptidyl trifluoromethyl alcohols.

D. Bonnet-Delpon, J. Bégué, A. Amour, 1994 .

De novo drug design of a new copper chelate molecule acting as HIV-1 protease inhibitor

F. Durant, M. Reboud-Ravaux, F. Lebon, 1998 .

Synthesis and structural analysis of copper(II) pyridine amide complexes as HIV-1 protease inhibitors

F. Durant, S. Sicsic, O. Kahn, 1999 .

Dimerization inhibitors of HIV-1 protease based on a bicyclic guanidinium subunit.

Michiel Van Gool, P. Prados, B. Badet, 2003, Journal of Medicinal Chemistry.

Toward the First Nonpeptidic Molecular Tong Inhibitor of Wild‐Type and Mutated HIV‐1 Protease Dimerization

L. Bannwarth, J. Soulier, S. Sicsic, 2010, ChemMedChem.

Dimer disruption and monomer sequestration by alkyl tripeptides are successful strategies for inhibiting wild-type and multidrug-resistant mutated HIV-1 proteases.

E. De Clercq, C. Pannecouque, L. Bannwarth, 2009, Biochemistry.

An alternative strategy for inhibiting multidrug-resistant mutants of the dimeric HIV-1 protease by targeting the subunit interface.

L. Bannwarth, M. Reboud-Ravaux, 2007, Biochemical Society transactions.

Disruption of the HIV-1 protease dimer with interface peptides: structural studies using NMR spectroscopy combined with [2-(13)C]-Trp selective labeling.

Ernest Giralt, Sergio Madurga, Ricard A Rodriguez-Mias, 2007, Biopolymers.

Molecular tongs containing amino acid mimetic fragments: new inhibitors of wild-type and mutated HIV-1 protease dimerization.

B. Collinet, L. Bannwarth, S. Sicsic, 2006, Journal of medicinal chemistry.

Synthesis and enzymic hydrolysis of cyclic peptides containing an anthranilic acid residue.

M. Reboud-Ravaux, J. Mazaleyrat, M. Wakselman, 2009, International journal of peptide and protein research.

Synthesis and protease-catalyzed hydrolysis of a novel hydrazinopeptide.

A. Amour, M. Reboud-Ravaux, A. Collet, 2009, International journal of peptide and protein research.

Synthesis of N-glyoxylyl peptides and their in vitro evaluation as HIV-1 protease inhibitors.

B. Badet, M. Reboud-Ravaux, N. Boggetto, 1997, Bioorganic & medicinal chemistry.

Insights into Biophysical Methods to Study Interactions Between HIV-1 Reverse Transcriptase and Non-nucleoside Reverse Transcriptase Inhibitors

J. Tronchet, M. Seman, J. Dumond, 2020 .

RNA‐acting antibiotics: in‐vitro selection of RNA aptamers for the design of new bioactive molecules less susceptible to bacterial resistance

M. Maurel, J. Décout, M. Reboud-Ravaux, 2002, The Journal of pharmacy and pharmacology.

Protection of vascular basement membrane and microcirculation from elastase-induced damage with a fluorinated beta-lactam derivative.

M. Reboud-Ravaux, J. Maillard, C. Favreau, 1992, Clinica chimica acta; international journal of clinical chemistry.

HIV-1 Protease and Reverse Transcriptase Control the Architecture of Their Nucleocapsid Partner

R. Gorelick, E. Le Cam, S. Lafosse, 2014, PloS one.

HIV-1 Protease and Reverse Transcriptase Control the Architecture of Their Nucleocapsid Partner

R. Gorelick, E. Le Cam, S. Lafosse, 2007, PLoS ONE.

Phenoxypropanolamine derivatives as selective inhibitors of the 20S proteasome β1 and β5 subunits.

D. Bouvier, G. Melikyan, Xiao Tan, 2017, Bioorganic & medicinal chemistry letters.

Inactivation of human high- and low-molecular-weight urokinases. Analysis of their active site.

M. Reboud-Ravaux, G. Desvages, 1984, Biochimica et biophysica acta.

Mutational analysis of the CG recognizing DNA methyltransferase SssI: insight into enzyme-DNA interactions.

A. Kiss, T. Rasko, O. Kirsanova, 2009, Biochimica et biophysica acta.

Synthesis and activity of HIV protease inhibitors

P. Dumy, S. Sicsic, M. Reboud-Ravaux, 1998 .

AZT and AZT-monophosphate Prodrugs Incorporating HIV-protease Substrate Fragment: Synthesis and Evaluation as Specific Drug Delivery Systems

A. Di Giorgio, M. Mehiri, A. Aubertin, 2006, Antiviral chemistry & chemotherapy.

β-Amyloid protein aggregation: its implication in the physiopathology of Alzheimer's disease

F. Bourdel, M. Reboud-Ravaux, S. Viale, 2001 .

1,2,4-Triazole derivatives as transient inactivators of kallikreins involved in skin diseases.

B. Villoutreix, A. Hovnanian, Xiao Tan, 2013, Bioorganic & medicinal chemistry letters.

Activity and inhibition mechanism of coumarin-based derivatives as protease inhibitor

B. Masereel, B. Pirotte, L. Pochet, 2000 .

Dimerization Inhibitors of HIV-1 Protease

M. Reboud-Ravaux, N. Boggetto, 2002, Biological chemistry.

New C(4)- and C(1)-derivatives of furo[3,4-c]pyridine-3-ones and related compounds: evidence for site-specific inhibition of the constitutive proteasome and its immunoisoform.

D. Bouvier, Yan Cheng, G. Melikyan, 2014, Bioorganic & medicinal chemistry letters.

Reaction of thrombin and proteinases of the fibrinolytic system with a mechanism-based inhibitor, 3,4-dihydro-3-benzyl-6-chloromethylcoumarin.

M. Reboud-Ravaux, J. Maillard, C. Favreau, 1990, Biochimica et biophysica acta.

Thyroxine-derivatives of lipopeptides: bifunctional dimerization inhibitors of human immunodeficiency virus-1 protease.

J. Dumond, W. Schramm, M. Reboud-Ravaux, 2003, Biochemical pharmacology.

The HIV-1 Nucleocapsid Regulates Its Own Condensation by Phase-Separated Activity-Enhancing Sequestration of the Viral Protease during Maturation

J. Gatell, A. Meyerhans, R. Gorelick, 2021, Viruses.

The HIV-1 ribonucleoprotein dynamically regulates its condensate behavior and drives acceleration of protease activity through membraneless granular phase separation

J. Gatell, A. Meyerhans, R. Gorelick, 2019, bioRxiv.

20S Proteasome Inhibition: Designing Noncovalent Linear Peptide Mimics of the Natural Product TMC‐95A

R. Huber, N. Basse, M. Groll, 2010, ChemMedChem.

Structural studies on the inhibitory binding mode of aromatic coumarinic esters to human kallikrein-related peptidase 7.

N. Sträter, S. Hanke, B. Pirotte, 2020, Journal of medicinal chemistry.

α- and β-hydrazino acid-based pseudopeptides inhibit the chymotrypsin-like activity of the eukaryotic 20S proteasome.

Nathalie Lagarde, B. Crousse, J. Soulier, 2013, European journal of medicinal chemistry.

Novel fluorinated pseudopeptides as proteasome inhibitors.

N. Basse, M. Reboud-Ravaux, X. Maréchal, 2009, Bioorganic & medicinal chemistry letters.

[The proteasome - structural aspects and inhibitors: a second life for a validated drug target].

M. Reboud-Ravaux, 2021, Biologie aujourd'hui.

Noncovalent fluorescent probes of human immuno- and constitutive proteasomes.

Yan Cheng, M. Reboud-Ravaux, J. Vidal, 2014, Journal of medicinal chemistry.

1,2,4-Oxadiazoles identified by virtual screening and their non-covalent inhibition of the human 20S proteasome.

M. Montès, B. Villoutreix, N. Basse, 2013, Current medicinal chemistry.

C1 and N5 derivatives of cerpegin: synthesis of a new series based on structure-activity relationships to optimize their inhibitory effect on 20S proteasome.

D. Bouvier, M. Reboud-Ravaux, The Hien Pham, 2013, Bioorganic & medicinal chemistry letters.

A new series of N5 derivatives of the 1,1,5-trimethyl furo[3,4-c]pyridine-3,4-dione (cerpegin) selectively inhibits the post-acid activity of mammalian 20S proteasomes.

D. Bouvier, M. Reboud-Ravaux, The Hien Pham, 2012, Bioorganic & medicinal chemistry letters.

N-Acetylbenzotriazole as a protein reagent. Specific behaviour towards delta-chymotrypsin.

M. Reboud-Ravaux, 1976, European journal of biochemistry.

Jatrophidin I, a cyclic peptide from Brazilian Jatropha curcas L.: isolation, characterization, conformational studies and biological activity.

V. Bolzani, H. Verli, M. Reboud-Ravaux, 2014, Phytochemistry.

Novel organic proteasome inhibitors identified by virtual and in vitro screening.

Bruno O Villoutreix, Matthieu Montes, Xavier Maréchal, 2010, Journal of medicinal chemistry.

Dimerized linear mimics of a natural cyclopeptide (TMC-95A) are potent noncovalent inhibitors of the eukaryotic 20S proteasome.

M. Groll, Nerea Gallastegui, M. Reboud-Ravaux, 2013, Journal of medicinal chemistry.

Evaluation of the Inhibitory Activity on Serine and Aspartic Proteases of 4‐Amino‐4H‐1,2,4‐triazole and 5‐Aminothiazole Derivatives Structurally Related to β‐Lactam Antibiotics

B. Masereel, B. Pirotte, M. Reboud-Ravaux, 1993, The Journal of pharmacy and pharmacology.

Cyclopeptidic inactivators for chymotrypsin-like proteinases

Juan Xie, M. Reboud-Ravaux, A. Vilain, 1991 .

beta-Amyloid protein aggregation: its implication in the physiopathology of Alzheimer's disease.

F. Bourdel, M. Reboud-Ravaux, S. Viale, 2001, Pathologie-biologie.

HIV-1 Protease and Reverse Transcriptase Control the Architecture of Their Nucleocapsid Partner

R. Gorelick, E. Le Cam, S. Lafosse, 2007, PloS one.

Efficient inactivation of urokinase with cyclopeptidic sulfonium salts

I. Gandolfi, Juan Xie, M. Reboud-Ravaux, 1993 .

Inhibition of human leukocyte elastase by functionalized N-aryl azetidin-2-ones: substituent effects at C-3 and benzylic positions

V. Okochi, M. Reboud-Ravaux, N. Boggetto, 1995 .