13 results on '"Moumné R"'
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2. Amide Alkaloids as Privileged Sources of Senomodulators for Therapeutic Purposes in Age-Related Diseases.
- Author
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Dotou M, L'honoré A, Moumné R, and El Amri C
- Subjects
- Amides, Plant Extracts pharmacology, Alkaloids pharmacology, Piper
- Abstract
Nature is an important source of bioactive compounds and has continuously made a large contribution to the discovery of new drug leads. Particularly, plant-derived compounds have long been identified as highly interesting in the field of aging research and senescence. Many plants contain bioactive compounds that have the potential to influence cellular processes and provide health benefits. Among them, Piper alkaloids have emerged as interesting candidates in the context of age-related diseases and particularly senescence. These compounds have been shown to display a variety of features, including antioxidant, anti-inflammatory, neuroprotective, and other bioactive properties that may help counteracting the effects of cellular aging processes. In the review, we will put the emphasis on piperlongumine and other related derivatives, which belong to the Piper alkaloids, and whose senomodulating potential has emerged during the last several years. We will also provide a survey on their potential in therapeutic perspectives of age-related diseases.
- Published
- 2024
- Full Text
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3. Analytical Tools for Dynamic Combinatorial Libraries of Cyclic Peptides.
- Author
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Peker T, Zagiel B, Rocard L, Bich C, Sachon E, and Moumné R
- Subjects
- Tandem Mass Spectrometry, Peptide Library, Peptides, Peptides, Cyclic chemistry, Combinatorial Chemistry Techniques
- Abstract
Target-directed dynamic combinatorial chemistry is a very attractive strategy for the discovery of bioactive peptides. However, its application has not yet been demonstrated, presumably due to analytical challenges that arise from the diversity of a peptide library with combinatorial side-chains. We previously reported an efficient method to generate, under biocompatible conditions, large dynamic libraries of cyclic peptides grafted with amino acid's side-chains, by thiol-to-thioester exchanges. In this work, we present analytical tools to easily characterize such libraries by HPLC and mass spectrometry, and in particular to simplify the isomers' distinction requiring sequencing by MS/MS fragmentations. After structural optimization, the cyclic scaffold exhibits a UV-tag, absorbing at 415 nm, and an ornithine residue which favors the regioselective ring-opening and simultaneous MS/MS fragmentation, in the gas-phase., (© 2023 The Authors. ChemBioChem published by Wiley-VCH GmbH.)
- Published
- 2023
- Full Text
- View/download PDF
4. Dynamic Amino Acid Side-Chains Grafting on Folded Peptide Backbone.
- Author
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Zagiel B, Peker T, Marquant R, Cazals G, Webb G, Miclet E, Bich C, Sachon E, and Moumné R
- Subjects
- Combinatorial Chemistry Techniques methods, Peptides chemistry, Proteins, Amino Acids, Peptide Library
- Abstract
An efficient strategy for the synthesis of large libraries of conformationally defined peptides is reported, using dynamic combinatorial chemistry as a tool to graft amino acid side chains on a well-ordered 3D (3-dimension) peptide backbone. Combining rationally designed scaffolds with combinatorial side chains selection represents an alternative method to access peptide libraries for structures that are not genetically encodable. This method would allow a breakthrough for the discovery of protein mimetic for unconventional targets for which little is known., (© 2022 Wiley-VCH GmbH.)
- Published
- 2022
- Full Text
- View/download PDF
5. Small AntiMicrobial Peptide With in Vivo Activity Against Sepsis.
- Author
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Boullet H, Bentot F, Hequet A, Ganem-Elbaz C, Bechara C, Pacreau E, Launay P, Sagan S, Jolivalt C, Lacombe C, Moumné R, and Karoyan P
- Subjects
- Amino Acids chemistry, Animals, Anti-Infective Agents chemistry, Anti-Infective Agents pharmacology, Antimicrobial Cationic Peptides chemistry, Antimicrobial Cationic Peptides pharmacology, Disease Models, Animal, Drug Design, Gram-Negative Bacteria drug effects, Gram-Positive Bacteria drug effects, Humans, Mice, Microbial Sensitivity Tests, Molecular Mimicry, Proteolysis, Sepsis etiology, Sepsis microbiology, Anti-Infective Agents administration & dosage, Anti-Infective Agents chemical synthesis, Antimicrobial Cationic Peptides administration & dosage, Antimicrobial Cationic Peptides chemical synthesis, Sepsis drug therapy
- Abstract
Antimicrobial peptides (AMPs) are considered as potential therapeutic sources of future antibiotics because of their broad-spectrum activities and alternative mechanisms of action compared to conventional antibiotics. Although AMPs present considerable advantages over conventional antibiotics, their clinical and commercial development still have some limitations, because of their potential toxicity, susceptibility to proteases, and high cost of production. To overcome these drawbacks, the use of peptides mimics is anticipated to avoid the proteolysis, while the identification of minimalist peptide sequences retaining antimicrobial activities could bring a solution for the cost issue. We describe here new polycationic β-amino acids combining these two properties, that we used to design small dipeptides that appeared to be active against Gram-positive and Gram-negative bacteria, selective against prokaryotic versus mammalian cells, and highly stable in human plasma. Moreover, the in vivo data activity obtained in septic mice reveals that the bacterial killing effect allows the control of the infection and increases the survival rate of cecal ligature and puncture (CLP)-treated mice., Competing Interests: Declare conflicts of interest or state “The authors declare no conflict of interest.”
- Published
- 2019
- Full Text
- View/download PDF
6. Thrombospondin-1 Mimetic Agonist Peptides Induce Selective Death in Tumor Cells: Design, Synthesis, and Structure-Activity Relationship Studies.
- Author
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Denèfle T, Boullet H, Herbi L, Newton C, Martinez-Torres AC, Guez A, Pramil E, Quiney C, Pourcelot M, Levasseur MD, Lardé E, Moumné R, Ogi FX, Grondin P, Merle-Beral H, Lequin O, Susin SA, and Karoyan P
- Subjects
- Amino Acid Sequence, Apoptosis drug effects, Cell Line, Tumor, Humans, Models, Molecular, Neoplasms drug therapy, Neoplasms metabolism, Structure-Activity Relationship, Thrombospondin 1 metabolism, Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Peptides chemistry, Peptides pharmacology, Thrombospondin 1 agonists
- Abstract
Thrombospondin-1 (TSP-1) is a glycoprotein considered as a key actor within the tumor microenvironment. Its binding to CD47, a cell surface receptor, triggers programmed cell death. Previous studies allowed the identification of 4N1K decapeptide derived from the TSP-1/CD47 binding epitope. Here, we demonstrate that this peptide is able to induce selective apoptosis of various cancer cell lines while sparing normal cells. A structure-activity relationship study led to the design of the first serum stable TSP-1 mimetic agonist peptide able to trigger selective programmed cell death (PCD) of at least lung, breast, and colorectal cancer cells. Altogether, these results will be of valuable interest for further investigation in the design of potent CD47 agonist peptides, opening new perspectives for the development of original anticancer therapies.
- Published
- 2016
- Full Text
- View/download PDF
7. CD47 agonist peptides induce programmed cell death in refractory chronic lymphocytic leukemia B cells via PLCγ1 activation: evidence from mice and humans.
- Author
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Martinez-Torres AC, Quiney C, Attout T, Boullet H, Herbi L, Vela L, Barbier S, Chateau D, Chapiro E, Nguyen-Khac F, Davi F, Le Garff-Tavernier M, Moumné R, Sarfati M, Karoyan P, Merle-Béral H, Launay P, and Susin SA
- Subjects
- Aged, Aged, 80 and over, Animals, Female, Humans, Leukemia, Lymphocytic, Chronic, B-Cell blood, Leukemia, Lymphocytic, Chronic, B-Cell drug therapy, Male, Mice, Mice, Inbred NOD, Middle Aged, Peptides therapeutic use, Thrombospondin 1 therapeutic use, Apoptosis drug effects, B-Lymphocytes metabolism, CD47 Antigen metabolism, Drug Resistance, Neoplasm, Leukemia, Lymphocytic, Chronic, B-Cell metabolism, Peptides pharmacology, Phospholipase C gamma metabolism
- Abstract
Background: Chronic lymphocytic leukemia (CLL), the most common adulthood leukemia, is characterized by the accumulation of abnormal CD5+ B lymphocytes, which results in a progressive failure of the immune system. Despite intense research efforts, drug resistance remains a major cause of treatment failure in CLL, particularly in patients with dysfunctional TP53. The objective of our work was to identify potential approaches that might overcome CLL drug refractoriness by examining the pro-apoptotic potential of targeting the cell surface receptor CD47 with serum-stable agonist peptides., Methods and Findings: In peripheral blood samples collected from 80 patients with CLL with positive and adverse prognostic features, we performed in vitro genetic and molecular analyses that demonstrate that the targeting of CD47 with peptides derived from the C-terminal domain of thrombospondin-1 efficiently kills the malignant CLL B cells, including those from high-risk individuals with a dysfunctional TP53 gene, while sparing the normal T and B lymphocytes from the CLL patients. Further studies reveal that the differential response of normal B lymphocytes, collected from 20 healthy donors, and leukemic B cells to CD47 peptide targeting results from the sustained activation in CLL B cells of phospholipase C gamma-1 (PLCγ1), a protein that is significantly over-expressed in CLL. Once phosphorylated at tyrosine 783, PLCγ1 enables a Ca2+-mediated, caspase-independent programmed cell death (PCD) pathway that is not down-modulated by the lymphocyte microenvironment. Accordingly, down-regulation of PLCγ1 or pharmacological inhibition of PLCγ1 phosphorylation abolishes CD47-mediated killing. Additionally, in a CLL-xenograft model developed in NOD/scid gamma mice, we demonstrate that the injection of CD47 agonist peptides reduces tumor burden without inducing anemia or toxicity in blood, liver, or kidney. The limitations of our study are mainly linked to the affinity of the peptides targeting CD47, which might be improved to reach the standard requirements in drug development, and the lack of a CLL animal model that fully mimics the human disease., Conclusions: Our work provides substantial progress in (i) the development of serum-stable CD47 agonist peptides that are highly effective at inducing PCD in CLL, (ii) the understanding of the molecular events regulating a novel PCD pathway that overcomes CLL apoptotic avoidance, (iii) the identification of PLCγ1 as an over-expressed protein in CLL B cells, and (iv) the description of a novel peptide-based strategy against CLL.
- Published
- 2015
- Full Text
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8. 3-Substituted prolines: from synthesis to structural applications, from peptides to foldamers.
- Author
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Mothes C, Caumes C, Guez A, Boullet H, Gendrineau T, Darses S, Delsuc N, Moumné R, Oswald B, Lequin O, and Karoyan P
- Subjects
- Proline analogs & derivatives, Protein Structure, Secondary, Peptides chemistry, Proline chemical synthesis, Proline chemistry
- Abstract
Among the twenty natural proteinogenic amino acids, proline is unique as its secondary amine forms a tertiary amide when incorporated into biopolymers, thus preventing hydrogen bond formation. Despite the lack of hydrogen bonds and thanks to conformational restriction of flexibility linked to the pyrrolidine ring, proline is able to stabilize peptide secondary structures such as b-turns or polyproline helices. These unique conformational properties have aroused a great interest in the development of proline analogues. Among them, proline chimeras are tools combining the proline restriction of flexibility together with the information brought by natural amino acids side chains. This review will focus on the chemical syntheses of 3-substituted proline chimeras of potential use for peptide syntheses and as potential use as tools for SAR studies of biologically active peptides and the development of secondary structure mimetics. Their influence on peptide structure will be briefly described.
- Published
- 2013
- Full Text
- View/download PDF
9. Investigation of RNA-ligand interactions by 19F NMR spectroscopy using fluorinated probes.
- Author
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Lombès T, Moumné R, Larue V, Prost E, Catala M, Lecourt T, Dardel F, Micouin L, and Tisné C
- Subjects
- Fluorine chemistry, Ligands, Magnetic Resonance Spectroscopy, Aminoglycosides chemistry, Fluorescent Dyes chemistry, Framycetin chemistry, Neomycin chemistry, Paromomycin chemistry, RNA chemistry
- Published
- 2012
- Full Text
- View/download PDF
10. Fragment-based design of small RNA binders: promising developments and contribution of NMR.
- Author
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Moumné R, Catala M, Larue V, Micouin L, and Tisné C
- Subjects
- Humans, Ligands, Drug Design, Magnetic Resonance Spectroscopy methods, RNA metabolism, Small Molecule Libraries chemistry, Small Molecule Libraries metabolism
- Abstract
Fragment-based drug design has become increasingly popular over the last decade. We review here the use of this approach to design small RNA binders. In addition, we discuss the use of NMR to detect the binding of small molecules on RNA targets and to guide chemists in the design of compounds targeting RNA., (Copyright © 2012 Elsevier Masson SAS. All rights reserved.)
- Published
- 2012
- Full Text
- View/download PDF
11. Stereoselective synthesis of fluorinated 1,3-cis-diaminocyclopentanes.
- Author
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Pasco M, Moumné R, Lecourt T, and Micouin L
- Subjects
- Amination, Halogenation, Molecular Structure, Stereoisomerism, Cyclopentanes chemical synthesis
- Abstract
Several fluorinated 1,3-diaminocyclopentanes, previously reported to be useful RNA structural probes, can be prepared in a diastereoselective manner from a single bicyclic hydrazine precursor, in 3 to 9 steps.
- Published
- 2011
- Full Text
- View/download PDF
12. Fluorinated diaminocyclopentanes as chiral sensitive NMR probes of RNA structure.
- Author
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Moumné R, Pasco M, Prost E, Lecourt T, Micouin L, and Tisné C
- Subjects
- Base Sequence, Molecular Probes, Nucleic Acid Conformation, Cyclopentanes chemistry, Fluorine chemistry, Magnetic Resonance Spectroscopy methods, RNA chemistry
- Abstract
The supramolecular chiral recognition between rac-2a and several structured RNA leads to a distinct (19)F NMR signal splitting. The (19)F NMR analysis of the diastereomeric pairs formed upon binding of this racemic probe delivers a topological footprint of the RNA. This phenomenon can be exploited to investigate dynamic events involving structural equilibria, as demonstrated in a melting experiment. This work provides a proof of concept that small fluorinated moderate binders can act as external probes of RNA structures.
- Published
- 2010
- Full Text
- View/download PDF
13. Tether influence on the binding properties of tRNALys3 ligands designed by a fragment-based approach.
- Author
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Moumné R, Larue V, Seijo B, Lecourt T, Micouin L, and Tisné C
- Subjects
- Binding Sites, HIV drug effects, Ligands, Models, Molecular, Nuclear Magnetic Resonance, Biomolecular, RNA, Transfer, Amino Acyl chemistry, RNA, Viral chemistry, Reverse Transcription drug effects, HIV Infections drug therapy, RNA, Transfer, Amino Acyl metabolism, RNA, Viral metabolism, Triazoles chemistry, Triazoles pharmacology
- Abstract
A small library of 1,5-triazole derivatives linking a diaminocyclopentadiol and aromatic ketones has been prepared and screened using NMR and fluorescent techniques against tRNA(Lys)(3), the HIV reverse transcription primer. The comparison of their binding properties to those of their 1,4-triazole isomers, previously discovered in a fragment-based approach, outlines the influence of the linker on affinity and binding selectivity in such an approach.
- Published
- 2010
- Full Text
- View/download PDF
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