Article
Agriculture, Multidisciplinary
Wu-Bin Shao, Rong-Shuang Luo, Jiao Meng, Xiao-Kang Lv, Hong-Mei Xiang, Wan-Lin Xiao, Xiang Zhou, Li-Wei Liu, Zhi-Bing Wu, Song Yang
Summary: Phenothiazine derivatives showed excellent bioactivity against different bacteria and demonstrated potential as pesticide candidates for plant diseases. Compound C-2 had high effectiveness against rice leaf blight, outperforming commonly used pesticides.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
Article
Multidisciplinary Sciences
Karianne Giller Fleten, J. Johannes Eksteen, Brynjar Mauseth, Ketil Andre Camilio, Terje Vasskog, Baldur Sveinbjornsson, Oystein Rekdal, Gunhild M. Maelandsmo, Kjersti Flatmark
Summary: The study found that oncolytic peptides showed promising activity in treating CRC and produced good therapeutic effects in mouse models. Experimental evidence demonstrated that these oncolytic peptides can trigger lasting anticancer immune responses and prevent the occurrence of liver metastases, making them potentially promising drugs for the treatment of colorectal cancer in the future.
SCIENTIFIC REPORTS
(2021)
Article
Chemistry, Multidisciplinary
Jeffrey Y. -K. Wong, Raja Mukherjee, Jiayuan Miao, Olena Bilyk, Vivian Triana, Mark Miskolzie, Antoine Henninot, John J. Dwyer, Serhii Kharchenko, Anna Iampolska, Dmitriy M. Volochnyuk, Yu-Shan Lin, Lynne-Marie Postovit, Ratmir Derda
Summary: In this manuscript, a novel technology called TSL was developed to convert phage-displayed peptide libraries made of 20 common amino acids to genetically-encoded libraries of bicyclic peptides. Utilizing this technology, several bicyclic macrocycles were discovered in vitro to specifically antagonize NODAL-induced signaling in cancer cells. This study demonstrates the potential of TSL-constrained peptides in expanding the repertoire of phage-displayed bicyclic architectures for the discovery of proteolytically stable bicyclic inhibitors for various protein targets.
Review
Immunology
Diana Ivonne Duarte-Mata, Mario Cesar Salinas-Carmona
Summary: Intracellular bacteria cause difficult-to-resolve infections, and standard therapy antibiotics are often ineffective due to poor cellular uptake. Antimicrobial peptides (AMPs) show promise as a therapeutic approach because of their bactericidal properties and ability to modulate immune responses. This review focuses on AMPs used to treat intracellular bacterial infections and their impact on immune mechanisms.
FRONTIERS IN IMMUNOLOGY
(2023)
Article
Biochemistry & Molecular Biology
D. R. G. Koppalu R. Puneeth Kumar, Sachin A. Nalawade, Saikat Pahan, Manjeet Singh, Dillip K. Senapati, Souvik Roy, Sanjit Dey, Sandip U. Toraskar, Srinivasarao Raghothama, Hosahudya N. Gopi
Summary: In this study, a 15-residue hybrid peptide was found to inhibit the aggregation of soluble Aβ(42) and disintegrate the aggregated fibrils. The peptide also rescued neuronal cells from Aβ(42) toxicity and showed resistance against trypsin digestion. CD analysis revealed that the peptide induced a helix-type conformation in Aβ(42). These findings have potential implications for designing new therapeutics for Alzheimer's disease.
ACS CHEMICAL NEUROSCIENCE
(2023)
Article
Biochemistry & Molecular Biology
DRGKoppalu R. Puneeth Kumar, Sachin A. Nalawade, Saikat Pahan, Manjeet Singh, Dillip K. Senapati, Souvik Roy, Sanjit Dey, Sandip U. Toraskar, Srinivasarao Raghothama, Hosahudya N. Gopi
Summary: In this study, a 15-amino acid peptide was reported to not only inhibit the aggregation of A beta(42) into fibrils, but also disintegrate the pre-formed fibrils into smaller assemblies. The peptide rescued neuronal cells from the toxicity of A beta(42) at equimolar concentrations. Furthermore, the peptide showed resistance against trypsin digestion and induced a helix-type conformation in A beta(42).
ACS CHEMICAL NEUROSCIENCE
(2023)
Review
Biochemistry & Molecular Biology
Matthew Drayton, Julia P. Deisinger, Kevin C. Ludwig, Nigare Raheem, Anna Mueller, Tanja Schneider, Suzana K. Straus
Summary: The rapid rise of multidrug-resistant bacteria has raised concerns about the effectiveness of traditional antibiotics. Antimicrobial peptides, with their diverse mechanisms of actions, offer a promising solution to combat these pathogens. This review discusses the mechanisms of antibiotic resistance and the potential of antimicrobial peptides in providing a more robust treatment of bacterial infections.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Immunology
Aetas Amponnawarat, Chalatip Chompunud Na Ayudhya, Hydar Ali
Summary: Pseudomonas aeruginosa infections are difficult to treat due to biofilm formation and antibiotic resistance, but a lipidated HDP mimetic called murepavadin has shown antibacterial activity against multi-drug-resistant strains. Murepavadin activates human MCs via MRGPRX2 and murine MCs via MrgprB2, potentially contributing to bacterial clearance and wound healing.
FRONTIERS IN IMMUNOLOGY
(2021)
Article
Biology
Jin Wang, Jiayi Xie, Daosong Wang, Xue Han, Minqi Chen, Guojun Shi, Linjia Jiang, Meng Zhao
Summary: Using single-cell sequencing, researchers identified a specific subpopulation of megakaryocytes (MKs) that highly expressed CXCR4 and exhibited both immune characteristics and MK-specific features. These CXCR4(high) MKs interacted with myeloid cells to promote their migration and enhance bacterial phagocytosis, and they were also capable of antigen presentation to activate T cells. Furthermore, in response to bacterial infection, these CXCR4(high) MKs could exit circulation and infiltrate into the spleen, liver, and lung. The ablation of MKs suppressed the innate immune response and impaired the anti-bacterial effects of T cells in mice.
Review
Agronomy
Fernando Lobo, Alicia Boto
Summary: Host-defense peptides (HDP) are emerging as promising phytosanitaries due to their potency, low toxicity, and low induction of antimicrobial resistance. They are natural compounds that have been used by animals and plants for millions of years to defend against pathogens. HDPs are being discovered through genome mining and produced using biofactories. Truncated or modified peptides have been developed to improve their bioactivities and reduce production costs. The combination of HDP and other antimicrobials, as well as the development of hybrid molecules, has shown promising results. However, cautionary measures need to be taken for the sustainable use of HDPs.
Article
Chemistry, Multidisciplinary
Suemin Lee, Bethany R. Schefter, Sattar Taheri-Araghi, Bae-Yeun Ha
Summary: In this study, a biophysical model was used to quantitatively demonstrate the dependence of antimicrobial peptide (AMP) selectivity on the presence and density of host cells and peptide trapping in a mixture of bacteria and host cells. The results showed that the selectivity increases with increasing host-cell density, but decreases with bacterial cell density. The model also clarified the difference between cell selectivity and membrane selectivity of AMPs.
Article
Multidisciplinary Sciences
Joni M. Prasad, Oscar Negron, Xinli Du, Eric S. Mullins, Joseph S. Palumbo, Jessica M. Gilbertie, Magnus Hook, Steven P. Grover, Rafal Pawlinski, Nigel Mackman, Jay L. Degen, Matthew J. Flick
Summary: This study identifies the essential role of the fibrinogen in combating Staphylococcus aureus infection, which relies on the coagulant function of thrombin. The bacteria-derived prothrombin activator vWbp is crucial for the fibrinogen-mediated bacterial clearance.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2021)
Article
Biochemistry & Molecular Biology
Marta Kinga Lemieszek, Marcin Golec, Jacek Zwolinski, Jacek Dutkiewicz, Janusz Milanowski
Summary: Pulmonary fibrosis is a challenging disease with poor prognosis and low survival rate. Studies suggest that cathelicidin may be beneficial in preventing and treating pulmonary fibrosis by suppressing epithelial-mesenchymal transition, however, it cannot completely neutralize all negative changes.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Pharmacology & Pharmacy
Hashem Etayash, Robert E. W. Hancock
Summary: Amphiphilic antimicrobial polymers and surface engineered polymeric-brush-tethered HDP are promising strategies that aim to overcome limitations of HDPs, enhance physicochemical properties and therapeutic performance, and address unmet therapeutic needs.
Review
Infectious Diseases
Isabel Tobin, Guolong Zhang
Summary: The rise of antimicrobial resistance has led to an urgent need for antibiotic alternatives in disease control and prevention. Host defense peptides (HDPs), with their antimicrobial and immunomodulatory properties, offer a promising solution to treating infections without the risk of developing resistance. Polyphenols, natural compounds found in plants, have been found to stimulate HDP synthesis and show potential as antibiotic alternatives.
Article
Surgery
Patrick Trevidic, Joely Kaufman-Janette, Susan Weinkle, Raymond Wu, Benji Dhillon, Stephanie Antunes, Emilie Mace, Pauline Maffert
Summary: This article highlights the importance of midface rejuvenation and the use of hyaluronic acid fillers in this area. It describes the advantages of this treatment method, including noninvasive procedures, immediate results, and minimal downtime. The article emphasizes the need for a tailored treatment approach based on the patient's characteristics and a thorough understanding of anatomical structures to minimize procedural risks and achieve natural-looking results.
AESTHETIC SURGERY JOURNAL
(2022)
Article
Dermatology
Patrick Trevidic, Wayne Carey, Anthony Benedetto, John H. Joseph, Laura Eaton, Stephanie Antunes, Pauline Maffert
Summary: This study aimed to develop a reliable lip fullness rating scale and validate its reliability and sensitivity. The results showed that the scale had high repeatability and consistency, making it suitable for classifying lip fullness in clinical trials and routine patient care.
JOURNAL OF COSMETIC DERMATOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Lorene Tallet, Emilie Frisch, Megane Bornerie, Claire Medemblik, Benoit Frisch, Philippe Lavalle, Gilles Guichard, Celine Douat, Antoine Kichler
Summary: There is an urgent need to develop new therapeutic strategies to combat multidrug resistant bacteria. The use of urea-based foldamers has shown promising antibacterial and antifungal properties.
Article
Chemistry, Multidisciplinary
Franziska R. Traube, Marcel Stern, Annika J. Toelke, Martina Rudelius, Ernesto Mejias-Perez, Nada Raddaoui, Beate M. Kuemmerer, Celine Douat, Filipp Streshnev, Manuel Albanese, Paul R. Wratil, Yasmin Gaertner, Milda Nainyte, Grazia Giorgio, Stylianos Michalakis, Sabine Schneider, Hendrik Streeck, Markus Mueller, Oliver T. Keppler, Thomas Carell
Summary: In this study, chemically stabilized siRNA against SARS-CoV-2 was synthesized and modified with peptides, reducing viral loads and virus-induced cytotoxicity. The siRNA was also able to reduce virus replication and virus-induced apoptosis in 3D mucociliary lung microtissues. The adjustment of siRNA sequence allows rapid adaptation to different variants, and conjugation with receptor ligands via click-chemistry enables the construction of targeted siRNAs for a flexible antiviral defense strategy.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Chemistry, Multidisciplinary
Sebastian Dengler, Celine Douat, Ivan Huc
Summary: In this study, hybrid sequences consisting of a peptide with multiple Cys residues and an aromatic foldamer helix with multiple chloroacetamide functions were synthesized. The reactive sites on the structurally defined helix were strategically placed to selectively stitch the peptide to form different macrocycles, resulting in mostly one preferred product. The reaction trails, involving identical reaction sites successively due to precise positioning in space, can be predicted based on structural considerations and the assumption that smaller macrocycles form faster.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Chemistry, Multidisciplinary
Valentina Corvaglia, Florian Sanchez, Friedericke S. Menke, Celine Douat, Ivan Huc
Summary: Helically folded oligoamides composed of up to 41 units were efficiently prepared using optimized manual solid-phase synthesis (SPS) protocols. The high yield and purity of the products, as well as the validation of analytical methods including H-1 NMR, contribute to the efficiency of these protocols. Implementation of SPS on a commercial peptide synthesizer through in situ acid chloride activation under Appel's conditions dramatically reduces the labor required for producing long sequences, representing a breakthrough for the development of helical aromatic oligoamide foldamers.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Chemistry, Multidisciplinary
Nagendar Pendem, Yella-Reddy Nelli, Leonie Cussol, Claude Didierjean, Brice Kauffmann, Christel Dolain, Gilles Guichard
Summary: Oligomers with a helix-turn-helix super-secondary structure were prepared by covalently bridging aliphatic oligourea foldamer helices with either rigid aromatic or flexible aliphatic spacers. The relative orientation of the helices in these dimers was studied using high-resolution X-ray diffraction analysis. Racemic crystallography was employed in some cases to facilitate crystallization and structure determination. All structures were solved using direct methods. Well-defined parallel helical hairpin motifs were observed in all cases when 4,4'-methylene diphenyl diisocyanate was used as a dimerizing agent, regardless of the primary sequence and chain length.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Polymer Science
Mohamed Samir Zaky, Gilles Guichard, Daniel Taton
Summary: This study investigates the stereoselective ring-opening polymerization (ROP) of racemic lactide (rac-LA) using a series of chiral amino(thio)ureas and phosphazene organic bases. The chiral binary organocatalytic pairs showed fast and highly selective ROP of rac-LA, resulting in semicrystalline and metal-free stereoblock-like materials based on polylactide (PLA). The reaction rates and stereocontrol were found to be influenced by the components of the pairs and the phosphazene bases used.
Article
Physics, Fluids & Plasmas
C. Douat, S. Ponduri, T. Boumans, O. Guaitella, S. Welzel, E. Carbone, R. Engeln
Summary: This study investigates the dissociation of CO2 in a symmetric pin-to-pin dielectric barrier discharge (DBD). The number of filaments per half cycle follows a power-law as a function of the injected power and remains constant regardless of pressure or other process parameters. The CO2 conversion is found to be proportional to specific energy input (SEI) even at the single filament level.
PLASMA SOURCES SCIENCE & TECHNOLOGY
(2023)
Article
Chemistry, Multidisciplinary
Sebastian Dengler, Ryan T. Howard, Vasily Morozov, Christos Tsiamantas, Wei-En Huang, Zhiwei Liu, Christopher Dobrzanski, Vojislava Pophristic, Sophie Brameyer, Celine Douat, Hiroaki Suga, Ivan Huc
Summary: Expanding the chemical diversity of peptide macrocycle libraries through the inclusion of a large aromatic helical foldamer has been implemented. A hybrid macrocyclic nanomolar binder to the C-lobe of the E6AP HECT domain was selected, and its crystal structure and molecular dynamics simulations revealed an intriguing reciprocal helical folding of the peptide and foldamer. The results represent a significant extension in the chemical space amenable to display selection and highlight the potential benefits of incorporating an aromatic foldamer into a peptide macrocycle for protein recognition.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Chemistry, Multidisciplinary
Marie E. Perrin, Bo Li, Johanne Mbianda, May Bakail, Christophe Andre, Gwenaelle Moal, Pierre Legrand, Virginie Ropars, Celine Douat, Francoise Ochsenbein, Gilles Guichard
Summary: In this study, we investigated the substitution of 4 α-residues with 3-urea segments in a short α-helical peptide known to bind ASF1. By analyzing the effects of different foldamer replacements, we discovered new binding modes for the peptide-urea chimeras with ASF1.
CHEMICAL COMMUNICATIONS
(2023)
Article
Chemistry, Organic
Binhao Teng, Joan Atcher, Lars Allmendinger, Celine Douat, Yann Ferrand, Ivan Huc
Summary: Aromatic oligoamide foldamers were designed to fold into helical structures through local conformation preferences and solvophobic effects. Solid phase synthesis allowed for efficient synthesis of the desired sequences. Solvent-driven conformational transitions of the foldamers were observed using NMR and UV absorption spectroscopy, varying with sequence length.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Binhao Teng, Pradeep K. Mandal, Lars Allmendinger, Celine Douat, Yann Ferrand, Ivan Huc
Summary: This study designed and synthesized water-soluble helically folded aromatic oligoamides. By replacing charged side chains with neutral methoxy groups, various aggregates were formed and studied using different experimental methods. The results showed that the hydrophobic effect was the main driving force for aggregation and could be finely modulated by the presence or absence of charges.
Meeting Abstract
Biochemistry & Molecular Biology
Bo Li, Marie E. Perrin, Johanne Mbianda, May Bakail, Christophe Andre, Celine Douat, Raphael Guerois, Francoise Ochsenbein, Gilles Guichard
JOURNAL OF PEPTIDE SCIENCE
(2022)
Article
Chemistry, Multidisciplinary
Aline Delamare, Guillaume Naulet, Brice Kauffmann, Gilles Guichard, Guillaume Compain
Summary: The hexafluoroisobutyl group is a commonly found hydrophobic group in drugs, and its introduction can provide new advantages to compounds. However, the lack of a general and practical synthetic methodology has hindered the exploration of this modification. In this study, the first general method for introducing the hexafluoroisobutyl group into various compounds was reported. This method overcomes the usual fluoride beta-elimination observed with other CF3-vinyl groups, and it has been successfully applied to the multigram-scale synthesis of enantiopure (S)-5,5,5,5',5',5'-hexafluoroleucine.
