Article
Biochemistry & Molecular Biology
Irina Yu Strobykina, Alexandra D. Voloshina, Olga Andreeva, Anastasiia S. Sapunova, Anna P. Lyubina, Syumbelya K. Amerhanova, Mayya G. Belenok, Liliya F. Saifina, Vyacheslav E. Semenov, Vladimir E. Kataev
Summary: Four new TPP conjugates of 1,2,3-triazolyl nucleoside analogues were synthesized and evaluated for their antibacterial, antifungal, and cytotoxic activities. Two lead compounds showed high antibacterial activity against MRSA strains resistant to Ciprofloxacin and Amoxicillin, as well as high cytotoxicity against human cancer cell lines. The bactericidal effect of the lead compounds was not caused by a violation of the integrity of the cytoplasmic membrane of bacteria and their cytotoxic activity is likely associated with apoptosis induction and cell cycle arrest.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Emel Onal, Ozge Tuncel, Ipek Erdogan Vatansever, Mohamad Albakour, Gizem Gumusgoz Celik, Tugba Kucuk, Bunyamin Akgul, Ayse Gul Gurek, Serdar Ozcelik
Summary: Novel mitochondrion-targeted phthalocyanine and porphyrin photosensitizers were synthesized and their photophysical and photochemical properties were defined. The TPP-conjugated porphyrin and phthalocyanine PSs showed high singlet oxygen generation capacity and effectively killed the cells.
Article
Engineering, Biomedical
Agnieszka Dabrowska, Pawel Botwina, Emilia Barreto-Duran, Agata Kubisiak, Magdalena Obloza, Aleksandra Synowiec, Artur Szczepanski, Marta Targosz-Korecka, Krzysztof Szczubialka, Maria Nowakowska, Krzysztof Pyrc
Summary: This study proposes a method of using polymers to combat broad-spectrum viral infections. By modulating the nano-mechanical properties of cells, these polymers can interfere with viral replication and reduce infection. The effectiveness of this method was validated through experimental results, and it was found that the process is reversible.
MATERIALS TODAY BIO
(2023)
Article
Biochemistry & Molecular Biology
Yongchang Tian, Rong Zhang, Binbin Guan, Yaowei Zhu, Li Chen
Summary: In this study, a novel acid-responsive oxidized dextran-based nanoplatform (OTP NP) was developed for photodynamic antibacterial therapy. OTP NP, composed of oxidized dextran and photosensitizer monoaminoporphyrin, exhibited excellent antibacterial activity against E. coli and S. aureus. Additionally, a new mechanism of bacterial membrane damage was discovered, where the bacterial cell membrane was peeled off and formed spherical particles under the combined action of reactive oxygen species (ROS) and nanomaterials. Moreover, OTP NP showed potential as a carrier for the slightly soluble drug levofloxacin (Lev).
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Oncology
Ameet K. Mishra, Iris Kemler, David Dingli
Summary: CD126 is expressed by various tumors and CAR-T cells targeting CD126 show efficient killing of tumor cells. Binding of soluble interleukin-6 receptor (sIL-6R) by CAR-T cells can mitigate cytokine release syndrome. CD126 provides a novel therapeutic target for CAR-T cells for many tumors with low toxicity risk.
BLOOD CANCER JOURNAL
(2021)
Article
Biochemistry & Molecular Biology
Miroslawa Grymel, Anna Lalik, Alicja Kazek-Kesik, Marietta Szewczyk, Patrycja Grabiec, Karol Erfurt
Summary: The study focuses on the synthesis of molecular hybrids of betulin, a natural compound, with an alkyltriphenylphosphonium moiety. The results show that these hybrids have improved solubility and cytotoxicity, and exhibit antimicrobial properties against certain bacteria.
Article
Chemistry, Applied
Wenbo Cao, Lin Yue, Yin Zhang, Zhouping Wang
Summary: The designed M-CS-Ce6 nanocomposite showed enhanced photo-antibacterial effect against both Gram-positive and Gram-negative bacteria, making it a promising broad-spectrum antibacterial agent.
CARBOHYDRATE POLYMERS
(2022)
Article
Chemistry, Organic
Petrakis N. Chalikidi, Taimuraz T. Magkoev, Andrey V. Gutnov, Oleg P. Demidov, Maxim G. Uchuskin, Igor V. Trushkov, Vladimir T. Abaev
Summary: Two approaches have been developed for the synthesis of substituted phosphonium salts from easily available benzyl alcohols and their heterocyclic analogs. The direct mixing method is more efficient for acid-sensitive substrates, while the one-pot procedure is better for benzyl alcohols with electroneutral or electron-withdrawing substituents.
JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Rajasekaran Ganesan, Mansour A. Dughbaj, Lisa Ramirez, Steven Beringer, Teshome L. Aboye, Alexander Shekhtman, Paul M. Beringer, Julio A. Camarero
Summary: This study reports the development of a novel engineered cyclotide with effective broad-spectrum antibacterial activity against several ESKAPE bacterial strains and clinical isolates. The most active antibacterial cyclotide was extremely stable in serum, showed little hemolytic activity, and provided protection in vivo in a murine model of P. aeruginosa peritonitis. These results highlight the potential of the cyclotide scaffold for the development of novel antimicrobial therapeutic leads for the treatment of bacteremia.
CHEMISTRY-A EUROPEAN JOURNAL
(2021)
Review
Oncology
Sonja Dragojevic, Jianxiong Ji, Pankaj K. Singh, Margaret A. Connors, Robert W. Mutter, Scott C. Lester, Surabhi M. Talele, Wenjuan Zhang, Brett L. Carlson, Nicholas B. Remmes, Sean S. Park, William F. Elmquist, Sunil Krishnan, Erik J. Tryggestad, Jann N. Sarkaria
Summary: Genotoxic damage induced by radiation activates a coordinated DNA damage response, and molecular inhibitors targeting key nodes can enhance antitumor efficacy of radiation. However, these inhibitors may also increase the risk of acute and late radiation toxicities.
INTERNATIONAL JOURNAL OF RADIATION ONCOLOGY BIOLOGY PHYSICS
(2021)
Article
Chemistry, Applied
Arpita Panda, Dmytro Kobzev, Olesia Kulyk, Andrii Bazylevich, Gary Gellerman, Leonid Patsenker
Summary: Mitochondria play a crucial role in maintaining cell viability, and dysfunction can lead to serious diseases. In order to achieve selective imaging and targeted therapy, a series of novel mitochondria-specific dyes with better visualization and higher fluorescence intensity have been developed.
Article
Chemistry, Medicinal
Peng Li, Kaijing Guo, Lei Fu, Bin Wang, Baoxi Zhang, Ningbo Gong, Yang Lu, Chen Ma, Haihong Huang, Yu Lu, Gang Li
Summary: Solubility-driven optimization of nitro benzothiopyranone 1 led to the synthesis of five pharmaceutically acceptable salts. These salts exhibited increased aqueous solubility and improved oral bioavailability compared to compound 1. The maleate salt 2 demonstrated higher chemical stability, lower log P, and a better in vivo effect, making it a promising preclinical candidate for treating tuberculosis.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Microbiology
Vanessa Duncan, Daniel Smith, Laura Simpson, Emma Lovie, Laura Katvars, Leon Berge, Jennifer Robertson, Shane Smith, Carol Munro, Derry Mercer, Deborah O'Neil
Summary: Fungi cause disease in nearly one billion individuals worldwide, and current antifungal agents face challenges such as emerging and drug-resistant fungi, toxicity, and drug-drug interactions. The development of NP339, a polyarginine peptide with potent antifungal activity against various pathogenic fungi, presents a promising solution to these challenges. NP339 targets fungal cell membranes specifically, demonstrating rapid fungicidal activity without inducing resistance, suggesting its potential as a differentiated antifungal candidate for serious fungal diseases.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Article
Materials Science, Multidisciplinary
Yan-Yan Xie, Xiao-Tong Qin, Jia-Yuan Feng, Cheng Zhong, Shi-Ru Jia
Summary: Amino acid-based hydrogels formed by Fmoc-L and Fmoc-K self-assembly demonstrated significant antibacterial activity against various bacteria, with the ability to tailor the antibacterial effect by modifying the molar ratio of amino acids. This study highlights the potential of amino acid-based hydrogels as effective antibacterial agents.
JOURNAL OF MATERIALS SCIENCE
(2021)
Article
Biochemistry & Molecular Biology
Mario Cano-Munoz, Daniel Polo-Megias, Ana Camara-Artigas, Jose A. Gavira, Maria J. Lopez-Rodriguez, Geraldine Laumond, Sylvie Schmidt, Julien Demiselle, Seiamak Bahram, Christiane Moog, Francisco Conejero-Lara
Summary: The SARS-CoV-2 spike protein plays a crucial role in virus attachment and fusion with cells. The HR1 and HR2 regions of the spike protein are potential therapeutic targets for COVID-19. A study designed chimeric proteins that mimic stable HR1 helical trimers and strongly bind to HR2, showing broad inhibitory activity against different virus strains. Antibody responses against the HR1 mimetic proteins were found in sera from COVID-19 convalescent donors, but not in sera from uninfected donors.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2022)