Article
Chemistry, Multidisciplinary
Li Gao, Haixia Shi, Cheng Liu, Ni Xia, Jia Cheng, Lei Liu
Summary: A sensitive, selective, and simple sensor platform was established in this study for detecting chymotrypsin using pyrene as a fluorescent dye for peptides and based on the covalent binding of peptides to gold nanoparticles and GO. The method achieved a detection limit of 7.394 pg mL(-1) and could be applied to real samples.
NEW JOURNAL OF CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Lorenzo Cianni, Fernanda Dos Reis Rocho, Vinicius Bonatto, Felipe Cardoso Prado Martins, Jeronimo Lameira, Andrei Leitao, Carlos A. Montanari, Anwar Shamim
Summary: In this study, a new set of peptide-like nitrile-based cathepsin inhibitors were synthesized using a knowledge-based design approach. Three compounds showed nanomolar inhibition of CatB with selectivity over other cysteine proteases. Through a structure-based design, selective CatB inhibition was achieved, and successful bioisosteric replacement of the amide bond for a sulfonamide one was demonstrated.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Shengrong Li, Chengjun Zhu, Qian Zhao, Zhi-Min Zhang, Pinghua Sun, Zhengqiu Li
Summary: Chemical cross-linking of proteins coupled with mass spectrometry analysis (CXMS) is a powerful method for studying protein structure and protein-protein interactions (PPIs). However, the available chemical probes and zero-length cross-linkers are limited. To overcome this, researchers developed a new coupling reagent, sulfonyl amide, which efficiently connects carboxyl residues (D/E) with lysine (K) to form amide bonds without any catalyst. This new reagent showed significant improvement in cross-linking efficiency and specificity compared to traditional methods.
ACS CHEMICAL BIOLOGY
(2023)
Article
Plant Sciences
Chin-Soon Phan, Jakia Jerin Mehjabin, Andrea Roxanne J. Anas, Masahiro Hayasaka, Reiko Onoki, Juting Wang, Taiki Umezawa, Kenji Washio, Masaaki Morikawa, Tatsufumi Okino
Summary: Chemical investigation of the cyanobacterium Dolichospermum sp. NIES-1697 resulted in the discovery of two new compounds, nostosin G (1) and spiroidesin B (2), which were characterized and studied for their structure and biosynthesis.
JOURNAL OF NATURAL PRODUCTS
(2022)
Article
Chemistry, Organic
Huidan Geng, Fei Chen, Yonglong Zhao, Bing Guo, Lei Tang, Yuan-Yong Yang
Summary: A protecting-group-free protocol was developed for the efficient diversification of the Meridianin alkaloid, leading to the synthesis of Meridianin B. The protocol tolerates a broad range of substituents, resulting in moderate to high product yields. Furthermore, preliminary studies demonstrate the potential of Meridianin derivatives in inhibiting Acinetobacter baumannii biofilm and enhancing antibiotic efficacy.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Organic
Huidan Geng, Fei Chen, Yonglong Zhao, Bing Guo, Lei Tang, Yuan -Yong Yang
Summary: A protecting-group-free method was developed for the diversification of Meridianin alkaloid in a time and step efficient manner. A wide range of substituents were successfully incorporated, leading to moderate to high product yields and the first synthesis of Meridianin B. This simple method enables the rapid construction of a Meridianin derivative library for antibiofilm evaluation. Preliminary results demonstrate the ability of Meridianin derivatives to inhibit Acinetobacter baumannii biofilms and synergistically lower the antibiotic MIC.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Analytical
Zhi'ang Chen, Yi Wee Lim, Jin Yong Neo, Rachel Shu Ting Chan, Li Quan Koh, Tsz Ying Yuen, Yee Hwee Lim, Charles W. Johannes, Zachary P. Gates
Summary: A chemical linearization method was applied to sequence synthetic peptide macrocycles, and it was found that linearized macrocycles can be accurately sequenced with lower recall compared to linear peptides. This study demonstrates the potential of using chemical linearization for de novo sequencing.
ANALYTICAL CHEMISTRY
(2023)
Article
Chemistry, Organic
Nitin Bagra, Rahul Jain
Summary: A new structural class of phenylalanine derivatives was synthesized using copper-ligand catalysis and microwave irradiation. The developed protocol enabled the efficient synthesis of the target products through regioselective copper-catalyzed azide-terminal alkyne cycloaddition.
SYNTHETIC COMMUNICATIONS
(2022)
Article
Multidisciplinary Sciences
Leandro da Costa Clementino, Guilherme Felipe Santos Fernandes, Igor Muccilo Prokopczyk, Wilquer Castro Laurindo, Danyelle Toyama, Bruno Pereira Motta, Amanda Martins Baviera, Flavio Henrique-Silva, Jean Leandro dos Santos, Marcia A. S. Graminha
Summary: Leishmaniasis is a neglected disease affecting 12 million people mainly in developing countries. The synthesized compound 4f showed promising antileishmanial activity, possibly acting through a dual mechanism against L. infantum.
Article
Biochemical Research Methods
Ahlame Saidi, Mylene Wartenberg, Jean-Baptiste Madinier, Guy Ilango, Seda Seren, Brice Korkmaz, Fabien Lecaille, Vincent Aucagne, Gilles Lalmanach
Summary: The near-infrared fluorescent substrate-based probe (pro3-SBP) is a convenient tool for monitoring hPR3 activity, showing high specificity and sensitivity in detecting human neutrophil activation processes. It can be successfully hydrolyzed by activated human neutrophils and provides a strong signal under confocal microscopy.
BIOCONJUGATE CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Xujie Zhang, Lin Sun, Megan E. Meuser, Waleed A. Zalloum, Shujing Xu, Tianguang Huang, Srinivasulu Cherukupalli, Xiangyi Jiang, Xiao Ding, Yucen Tao, Dongwei Kang, Erik De Clercq, Christophe Pannecouque, Alexej Dick, Simon Cocklin, Xinyong Liu, Peng Zhan
Summary: A series of novel dimerized phenylalanine derivatives were designed, synthesized, and studied as HIV-1 capsid inhibitors, with Q-c4 identified as the most potent compound. These dimerized phenylalanines show promise as a platform for future HIV-1 CA inhibitors with considerable potential for optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Qiongna Cai, Qian Yu, Wanxin Liang, Haizhou Li, Jiayong Liu, Hongxia Li, Yongzhi Chen, Shanfang Fang, Rongcui Zhong, Shouping Liu, Shuimu Lin
Summary: Antibiotic resistance is a global public health concern, and the development of novel antimicrobials is urgently needed. In this study, a series of new peptidomimetic antimicrobials were designed and synthesized, with compound 51 identified as the lead compound due to its potent antibacterial activity, low toxicity, and avoidance of bacterial resistance development. Compound 51 also significantly reduced microbial burden in a murine model of keratitis infected by Staphylococcus aureus or Pseudomonas aeruginosa. This design strategy provides a promising and effective solution to overcome antibiotic resistance.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Minglong Liu, Richard Morewood, Ryoji Yoshisada, Mirte N. Pascha, Antonius J. P. Hopstaken, Eliza Tarcoveanu, David A. Poole, Cornelis A. M. de Haan, Christoph Nitsche, Seino A. K. Jongkees
Summary: Peptide display technologies are powerful for discovering bioactive sequences, but instability can be an issue. This study explores the use of meta-cyanopyridylalanine (mCNP) for ribosomal incorporation into peptides, forming stable macrocycles. The researchers also demonstrate compatibility with thioether macrocyclisation and the potential for chemical modification of the peptides. This innovative approach provides a valuable addition to the peptide discovery toolbox.
Article
Chemistry, Multidisciplinary
Minglong Liu, Richard Morewood, Ryoji Yoshisada, Mirte N. Pascha, Antonius J. P. Hopstaken, Eliza Tarcoveanu, David A. Poole, Cornelis A. M. de Haan, Christoph Nitsche, Seino A. K. Jongkees
Summary: This study demonstrates a new method for peptide discovery, utilizing ribosomal incorporation of mCNP to macrocyclize peptides during translation. This method improves peptide stability and plays a crucial role in chemical modification of in vitro translated peptides.
Article
Chemistry, Multidisciplinary
Yulei Li, Jie Heng, Demeng Sun, Baochang Zhang, Xin Zhang, Yupeng Zheng, Wei-Wei Shi, Tong-Yue Wang, Jiu-Yi Li, Xiaoou Sun, Xiangyu Liu, Ji-Shen Zheng, Brian K. Kobilka, Lei Liu
Summary: This study presents a practical synthesis method for differentially modified, full-length beta(2)AR receptors. The success in preparing a range of homogeneous samples with distinct modification patterns, including a full-length beta(2)AR bearing both monoubiquitination and octaphosphorylation modifications, provides valuable insights into the structure and interactions of beta(2)AR complexes.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2021)
Article
Biochemistry & Molecular Biology
Natalia Gruba, Lech Stachurski, Adam Lesner
Summary: Bladder cancer is a common cancer with high recurrence rate and poor prognosis, usually asymptomatic and requiring invasive and expensive regular re-examinations. The study used chromogenic substrates for qualitative determination of urine enzyme activity in healthy individuals and bladder cancer patients, finding proteolytic activity in cancer patients but not in healthy volunteers.
CHEMISTRY & BIODIVERSITY
(2021)
Letter
Respiratory System
Seda Seren, Lohann Derian, Irem Keles, Antoine Guillon, Adam Lesner, Loic Gonzalez, Thomas Baranek, Mustapha Si-Tahar, Sylvain Marchand-Adam, Dieter E. Jenne, Christophe Paget, Youenn Jouan, Brice Korkmaz
EUROPEAN RESPIRATORY JOURNAL
(2021)
Review
Biochemistry & Molecular Biology
Vincent Mariaule, Aicha Kriaa, Souha Soussou, Soufien Rhimi, Houda Boudaya, Juan Hernandez, Emmanuelle Maguin, Adam Lesner, Moez Rhimi
Summary: Proteolytic imbalance is often linked to diseases, especially in digestive inflammation. Serine proteases and matrix metalloproteases play crucial roles in inflammatory responses, but the imbalance between these enzymes and their inhibitors could contribute to disease pathogenesis.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Natalia Stach, Abdulkarim Karim, Przemyslaw Golik, Radoslaw Kitel, Katarzyna Pustelny, Natalia Gruba, Katarzyna Groborz, Urszula Jankowska, Sylwia Kedracka-Krok, Benedykt Wladyka, Marcin Drag, Adam Lesner, Grzegorz Dubin
Summary: By studying the substrate specificity and structure of SplF, it was found that the enzyme has a strict preference for long aliphatic sidechains at the P1 subsite and significant selectivity for aromatic residues at P3, with its crystal structure defining the structural basis of this substrate specificity. Comparisons with other Spl proteases suggest that the spl operon encodes a unique extracellular proteolytic system.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Anita Romanowska, Katarzyna Wegrzyn, Katarzyna Bury, Emilia Sikorska, Aleksandra Gnatek, Agnieszka Piwkowska, Igor Konieczny, Adam Lesner, Magdalena Wysocka
Summary: Novel polycationic polymers composed of N-substituted L-2,3-diaminopropionic acid residues were synthesized and their cell permeability, cytotoxicity, and DNA-binding ability were investigated in this study. The compounds showed efficient cell membrane penetration, dsDNA binding, and minimal cytotoxicity. The interaction with plasmid DNA and the length of the main chain of the compounds influenced the formation of unique nanostructures.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Biochemistry & Molecular Biology
Hela Mkaouar, Vincent Mariaule, Soufien Rhimi, Juan Hernandez, Aicha Kriaa, Amin Jablaoui, Nizar Akermi, Emmanuelle Maguin, Adam Lesner, Brice Korkmaz, Moez Rhimi
Summary: Inflammatory bowel diseases are incurable disorders with increasing prevalence and global socioeconomic impact. Gut microbiota dysbiosis and increased activity of serine proteases may play roles in the onset and maintenance of the disease, with potential therapeutic relevance of gut microbiota serpins.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Mladena Glavas, Agata Gitlin-Domagalska, Dawid Debowski, Natalia Ptaszynska, Anna Legowska, Krzysztof Rolka
Summary: This article discusses the synthesis and functions of human neurohormone vasopressin (AVP), as well as the efforts and applications in finding AVP analogues. Natural and synthetic AVP analogues play important therapeutic roles in medicine, such as lypressin and terlipressin. Recent research also explores the potential applications of AVP analogues in the treatment of SARS-CoV-2.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Iga Biskupek, Adam Sieradzan, Cezary Czaplewski, Adam Liwo, Adam Lesner, Artur Gieldon
Summary: This manuscript proposes a two-stage infection mechanism of the SARS-CoV-2 virus, highlighting the crucial role of the interaction between the virus and the ACE2 receptor in the infection process, and identifies the importance of three key residues.
Review
Cell Biology
Aicha Kriaa, Vincent Mariaule, Amin Jablaoui, Soufien Rhimi, Hela Mkaouar, Juan Hernandez, Brice Korkmaz, Adam Lesner, Emmanuelle Maguin, Ali Aghdassi, Moez Rhimi
Summary: Inflammatory bowel diseases (IBDs) are a global public health problem with limited effective therapeutic options. Changes in gut microbiota composition and alterations in bile acids (BAs) have been identified as important factors in dysregulated intestinal immunity and the pathogenesis of IBDs. This review explores the interactions between BAs and gut microbiota in IBDs and discusses how the gut microbiota-BA-host axis may influence digestive inflammation.
Article
Pharmacology & Pharmacy
Wioletta Brankiewicz, Joanna Okonska, Katarzyna Serbakowska, Jan Lica, Marek Drab, Natalia Ptaszynska, Anna Legowska, Krzysztof Rolka, Piotr Szweda
Summary: This study reported five conjugates composed of fluconazole and cell penetrating or antimicrobial peptide, showing high antifungal activity, especially against fluconazole-resistant strains, with low cytotoxicity.
Article
Chemistry, Medicinal
Agata Gitlin-Domagalska, Dawid Debowski, Aleksandra Maciejewska, Sergey Samsonov, Martyna Maszota-Zieleniak, Natalia Ptaszynska, Anna Legowska, Krzysztof Rolka
Summary: In this study, five new peptide furin inhibitors with strong inhibitory action and stability were obtained using combinatorial chemistry. Inhibitor 5 showed the highest activity and was more resistant to proteolysis compared to the reference furin inhibitor described in the literature. It also reduced furin-like activity in PANC-1 cell lysate. Molecular dynamics simulations were performed to analyze the furin-inhibitor complexes in detail.
ACS MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Multidisciplinary Sciences
Sylwia Wojcik-Mieszawska, Kinga Lewtak, Ewa Skwarek, Dawid Debowski, Agata Gitlin-Domagalska, Jakub Nowak, Jerzy Wydrych, Jaroslaw Pawelec, Marta J. Fiolka
Summary: The present studies demonstrate the impact of Venetin-1 protein-polysaccharide complex from earthworm coelomic fluid on Candida albicans cells. The action of Venetin-1 led to reduced survival rate, enlarged and deformed cells, and an increase in cells with enlarged vacuoles. Autophagy process was observed through different microscopy techniques. Changes in vacuoles were accompanied by alterations in mitochondrial size, possibly due to oxidative stress.
SCIENTIFIC REPORTS
(2023)
Article
Biochemistry & Molecular Biology
Mladena Glavas, Agata Gitlin-Domagalska, Natalia Ptaszynska, Dominika Starego, Sylwia Freza, Dawid Debowski, Aleksandra Helbik-Maciejewska, Anna Legowska, Chaim Gilon, Krzysztof Rolka
Summary: Arginine increases peptides' hydrophilicity and enables interactions with charged molecules, but its presence may reduce permeability through biological membranes. Temporary coverage of peptide charge with lipophilic, enzyme-sensitive alkoxycarbonyl groups can resolve this issue. We present a new, optimized strategy to obtain arginine building blocks with increased lipophilicity.