Article
Biochemistry & Molecular Biology
Hao Yin, Xing-Yan Fu, Han-Yu Gao, Yan-Nan Ma, Jing-Fang Yao, Shan-Shan Du, Yun-Kun Qi, Ke-Wei Wang
Summary: Nitrogen mustards are important chemotherapeutic drugs widely used in cancer treatment. However, their reactivity with proteins and phospholipids within the cell membrane limits their effectiveness in reaching the nucleus and interacting with DNA. The hybridization of nitrogen mustards with membranolytic agents could potentially enhance their penetration of the cell membrane.
BIOORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Fernando Calzada, Elihu Bautista, Sergio Hidalgo-Figueroa, Normand Garcia-Hernandez, Elizabeth Barbosa, Claudia Velazquez, Rosa Maria Ordonez-Razo, Angel Giovanni Arietta-Garcia
Summary: The study demonstrated that IA exhibits high antilymphoma activity and lethality through BSL, with strong interactions in molecular docking studies. Additionally, IA showed low acute toxicity in mice.
Article
Pharmacology & Pharmacy
Joanne Heade, Fiona McCartney, Miguel Chenlo, Olga Moreno Marro, Maja Severic, Robert Kent, Sinead B. Bleiel, Clara Alvarez, Brendan T. Griffin, David J. Brayden
Summary: The study aimed to develop a convenient oral delivery system for insulin and peptides, investigating the encapsulation and release properties of insulin entrapped in dWPI-based beads. Results showed promising potential for the dWPI-based beads as an oral peptide delivery system with high encapsulation efficiency and controlled release profile.
Article
Pharmacology & Pharmacy
Pimthanya Wanichawan, Jonas Skogestad, Marianne Lunde, Thea Parsberg Stole, Maria Stensland, Tuula A. Nyman, Ivar Sjaastad, Ole M. Sejersted, Jan Magnus Aronsen, Cathrine Rein Carlson
Summary: The study focused on analyzing the binding affinities and kinetics of PLM-NCX1 and pSer68-PLM-NCX1 interactions using surface plasmon resonance (SPR), as well as developing a proteolytically stable NCX1 activator peptide. The findings showed that both PLM and pSer68-PLM bind strongly to NCX1 with similar affinities, but PLM exhibited higher binding rates. The developed peptide, NOPT, increased NCX1 activity in cardiomyocytes isolated from normal and heart failure mice by disrupting the inhibitory pSer68-PLM-NCX1 interaction.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Microbiology
Jih-Chao Yeh, Prakash Kishore Hazam, Chu-Yi Hsieh, Po-Hsien Hsu, Wen-Chun Lin, Yun-Ru Chen, Chao-Chin Li, Jyh-Yih Chen
Summary: In our in vitro studies, one dual stapled peptide (TP4-3: FIIXKKSXGLFKKKAGAXKKKXIKK) showed significant activity, low toxicity, and high stability in 50% human serum. In a mouse model of polymicrobial sepsis, TP4-3 improved survival and enhanced the activity of meropenem against sepsis. This study highlights the potential of TP4-based stapled peptides for clinical applications.
MICROBIOLOGY SPECTRUM
(2023)
Article
Computer Science, Hardware & Architecture
Irith Pomeranz
Summary: Iterative synthesis involves making local design modifications to improve design parameters or correct design errors. This study suggests that a fast procedure for identifying undetectable faults is effective in predicting the deterioration of testability due to local design modifications, without the need for test generation.
IEEE TRANSACTIONS ON VERY LARGE SCALE INTEGRATION (VLSI) SYSTEMS
(2023)
Article
Engineering, Biomedical
Dennis Kundrat, Giulio Dagnino, Trevor M. Y. Kwok, Mohamed E. M. K. Abdelaziz, Wenqiang Chi, Anh Nguyen, Celia Riga, Guang-Zhong Yang
Summary: The research successfully developed a novel endovascular robotic platform for remote manipulation of endovascular instrumentation in MR environments, demonstrating high success rates in cannulating different vascular anatomies. The robotic dexterity involving pneumatic actuation concepts enabled successful remote cannulation with lower interaction forces compared to manual cannulation.
IEEE TRANSACTIONS ON BIOMEDICAL ENGINEERING
(2021)
Article
Biochemistry & Molecular Biology
Jesica Ramirez-Santos, Fernando Calzada, Jessica Elena Mendieta-Wejebe, Rosa Maria Ordonez-Razo, Rubria Marlen Martinez-Casares, Miguel Valdes
Summary: This study evaluated the antitumor activity of three acyclic terpenoids obtained from Annona macroprophyllata, suggesting their potential as new treatments for non-Hodgkin's lymphoma.
Article
Chemistry, Medicinal
Claudia De Fusco, Marianne Schimpl, Ulf Borjesson, Tony Cheung, Iain Collie, Laura Evans, Priyanka Narasimhan, Christopher Stubbs, Mercedes Vazquez-Chantada, David J. Wagner, Michael Grondine, Matthew G. Sanders, Sharon Tentarelli, Elizabeth Underwood, Argyrides Argyrou, James M. Smith, James T. Lynch, Elisabetta Chiarparin, Graeme Robb, Sharan K. Bagal, James S. Scott
Summary: MAT2a is an enzyme that synthesizes the essential metabolite SAM, making it an attractive target for treating MTAP-deleted cancers sensitive to its inhibition. Through structure-guided design and systematic SAR exploration, a potent series of MAT2a inhibitors has been developed, demonstrating promising antitumor response in in vivo studies.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Victor A. Naumenko, Daniil A. Vishnevskiy, Aleksei A. Stepanenko, Anastasiia O. Sosnovtseva, Anastasiia A. Chernysheva, Tatiana O. Abakumova, Marat P. Valikhov, Anastasiia Lipatova, Maxim A. Abakumov, Vladimir P. Chekhonin
Summary: Hepatotoxicity is a problem in adenovirus cancer therapy, caused by Kupffer cell death and hepatocyte transduction. The interaction between adenovirus and liver cells is not well understood. This study used intravital microscopy to track the infection and immune response in mouse livers after adenovirus injection, and found that Ad5-RGD and Ad5/3 caused macrophage deformation and virus release, but neutrophils and CD8+ T cells did not affect the rate or dynamics of liver infection. Ad5-RGD failed to complete the replicative cycle in hepatocytes, but enhanced liver transduction during hepatic regeneration.
Article
Multidisciplinary Sciences
Stanley C. Xie, Riley D. Metcalfe, Hirotake Mizutani, Tanya Puhalovich, Eric Hanssen, Craig J. Morton, Yawei Du, Con Dogovski, Shih-Chung Huang, Jeffrey Ciavarri, Paul Hales, Robert J. Griffin, Lawrence H. Cohen, Bei-Ching Chuang, Sergio Wittlin, Ioanna Deni, Tomas Yeo, Kurt E. Ward, Daniel C. Barry, Boyin Liu, David L. Gillett, Benigno F. Crespo-Fernandez, Sabine Ottilie, Nimisha Mittal, Alisje Churchyard, Daniel Ferguson, Anna Caroline C. Aguiar, Rafael V. C. Guido, Jake Baum, Kirsten K. Hanson, Elizabeth A. Winzeler, Francisco-Javier Gamo, David A. Fidock, Delphine Baud, Michael W. Parker, Stephen Brand, Lawrence R. Dick, Michael D. W. Griffin, Alexandra E. Gould, Leann Tilley
Summary: The study identifies the Plasmodium falciparum proteasome as a potential antimalarial drug target and develops a series of potent inhibitors with high efficacy against malaria parasites and low likelihood of resistance. These findings offer insights for designing potent and selective antimalarial proteasome inhibitors.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2021)
Article
Nanoscience & Nanotechnology
Shan Huang, Bingtao Zhai, Yu Fan, Jing Sun, Jiangxue Cheng, Junbo Zou, Xiaofei Zhang, Yajun Shi, Dongyan Guo
Summary: The study successfully prepared and optimized paeonol-loaded liposomes to improve the oral absorption of paeonol, which showed significantly improved anti-inflammatory activity in vitro and in vivo, laying the groundwork for the further development of paeonol as an oral anti-inflammatory drug.
INTERNATIONAL JOURNAL OF NANOMEDICINE
(2022)
Article
Food Science & Technology
Ying Zhu, Yuyang Huang, Meiying Li, Bingyu Sun, Linlin Liu, Mingshou Lv, Min Qu, Huanan Guan, Xiuqing Zhu
Summary: The high Fischer (F) ratio hemp peptide (HFHP) was prepared using activated carbon adsorption, ultrafiltration, and gel filtration chromatography. HFHP showed strong scavenging abilities for DPPH, hydroxyl free radicals, and superoxide. Mouse experiments demonstrated that HFHP increased the activity of superoxide dismutase and glutathione peroxidase, and improved swimming performance by reducing lactic acid, serum urea nitrogen, and malondialdehyde levels while increasing liver glycogen.
FOOD RESEARCH INTERNATIONAL
(2023)
Article
Immunology
Md Kamal Hossain, Majid Davidson, Jack Feehan, George Deraos, Kulmira Nurgali, John Matsoukas, Vasso Apostolopoulos
Summary: This article introduces the development and characterization of a novel METH vaccine. Through confirmation of chemical reaction steps and support from animal studies, an effective METH vaccine was successfully developed.
Article
Pharmacology & Pharmacy
Chenyu Zhang, Xiang Li, Zhenjian Xing, Honglan Zhong, Dianbao Yu, Rui Yu, Xin Deng
Summary: In this study, an anticancer AMP (Mastoparan) and its derivatives were designed and evaluated. Preliminary studies showed that the Mastoparan analogue KM8 exhibited selective antitumor effects but had metabolic instability. By substituting the 9Ala residue in KM8, a long-acting derivative KM8-Aib was generated, which showed higher metabolic stability, potent anticancer activity, and lower toxicity. Therefore, KM8-Aib is suggested as a potential antimalignant agent for further study.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Review
Chemistry, Multidisciplinary
John S. Mjoen Svendsen, Thomas M. Grant, David Rennison, Margaret A. Brimble, Johan Svenson
ACCOUNTS OF CHEMICAL RESEARCH
(2019)
Article
Biochemical Research Methods
Myagmarsuren Sengee, J. Johannes Eksteen, Silje Lillemark Nergard, Terje Vasskog, Leiv K. Sydnes
BIOCONJUGATE CHEMISTRY
(2019)
Article
Oncology
Wei Xie, Laura Mondragon, Brynjar Mauseth, Yan Wang, Jonathan Pol, Sarah Levesque, Heng Zhou, Takahiro Yamazaki, Johannes J. Eksteen, Laurence Zitvogel, Baldur Sveinbjornsson, Oystein Rekdal, Oliver Kepp, Guido Kroemer
Article
Chemistry, Medicinal
Marianne H. Paulsen, Dominik Ausbacher, Annette Bayer, Magnus Engqvist, Terkel Hansen, Tor Haug, Trude Anderssen, Jeanette H. Andersen, Johanna U. Ericson Sollid, Morten B. Strom
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2019)
Article
Chemistry, Multidisciplinary
J. Johannes Eksteen, Dominik Ausbacher, Terje Vasskog, Oystein Rekdal, John S. M. Svendsen
Article
Chemistry, Medicinal
Marianne H. Paulsen, Magnus Engqvist, Dominik Ausbacher, Trude Anderssen, Manuel K. Langer, Tor Haug, Glenn R. Morello, Laura E. Liikanen, Hans-Matti Blencke, Johan Isaksson, Eric Juskewitz, Annette Bayer, Morten B. Strom
Summary: This study presents a series of synthetic cationic amphipathic barbiturates with potent antimicrobial activity against multi-resistant bacteria. Inspired by the pharmacophore model of small antimicrobial peptides and marine antimicrobials, these compounds show promising in vivo antibiotic efficacy and strong membrane disruptive effects. The results suggest that the design strategy based on small AMPs and marine compounds can lead to the development of highly effective peptidomimetics against multi-drug resistant bacteria.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Infectious Diseases
Anne Sofie Laulund, Franziska Angelika Schwartz, Lars Christophersen, Niels Hoiby, John Sigurd Mjoen Svendsen, Wenche Stensen, Kim Thomsen, Jorunn Pauline Cavanagh, Claus Moser
Summary: This study aimed to investigate whether adjunctive AMC-109 could augment the ciprofloxacin effect in a chronic Pseudomonas aeruginosa wound model. The results showed that the combined treatment group had a lower bacterial load, decreased pro-inflammatory response, and improved tissue remodeling.
JOURNAL OF GLOBAL ANTIMICROBIAL RESISTANCE
(2022)
Article
Infectious Diseases
Eskil Andre Karlsen, Wenche Stensen, Eric Juskewitz, Johan Svenson, Mattias Berglin, John Sigurd Mjoen Svendsen
Summary: The study demonstrated that antimicrobial peptides covalently attached to a gold surface can effectively reduce bacterial colonization, offering promising strategies for combating healthcare-associated infections.
Article
Chemistry, Medicinal
Wenche Stensen, Ulli Rothweiler, Richard Alan Engh, Melissa R. Stasko, Ilya Bederman, Alberto C. S. Costa, Anders Fugelli, John S. Mjoen Svendsen
Summary: Down syndrome is a complex genetic disorder with substantial physical, cognitive, and behavioral challenges. While treatment options for physical co-morbidities have improved, cognitive deficits in individuals with DS cannot be addressed pharmacologically, and all individuals with DS develop early onset Alzheimer's disease pathology by the age of 40. The study introduces a novel inhibitor for the protein kinase DYRK1A, which is a key controlling kinase associated with DS.
Article
Multidisciplinary Sciences
Susannah von Hofsten, Marianne Hagensen Paulsen, Synnove Norvoll Magnussen, Dominik Ausbacher, Mathias Kranz, Annette Bayer, Morten B. Strom, Gerd Berge
Summary: Bioprospecting contributes to the discovery of new molecules with anticancer properties. In this study, a new natural product mimic called MPM-1 was found to rapidly kill cancer cells and induce the release of DAMPs, suggesting its potential as a novel anticancer compound.
SCIENTIFIC REPORTS
(2022)
Article
Pharmacology & Pharmacy
Susannah von Hofsten, Manuel K. Langer, Katja Korelin, Synnove Magnussen, Dominik Ausbacher, Trude Anderssen, Tuula Salo, Morten B. Strom, Annette Bayer, Ahmed Al-Samadi, Gerd Berge
Summary: This study explores the anticancer activity of a panel of novel compounds (marine product mimics, MPMs) against head and neck squamous cell carcinoma (HNSCC) cell lines. The results indicate that these novel MPMs are more potent than the previously reported MPM-1 and can activate the integrated stress response associated with immunogenic cell death. Cell surface expression of calreticulin and release of HMGB1 and ATP, hallmarks of immunogenic cell death, were also demonstrated. The MPMs show potential as interesting candidates for future HNSCC cancer therapies.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Multidisciplinary Sciences
Adela Melcrova, Sourav Maity, Josef Melcr, Niels A. W. de Kok, Mariella Gabler, Jonne van der Eyden, Wenche Stensen, John S. M. Svendsen, Arnold J. M. Driessen, Siewert J. Marrink, Wouter H. Roos
Summary: This study investigates the mechanism of action of the antimicrobial cationic tripeptide AMC-109. It was found that AMC-109 self-assembles into stable aggregates with a cationic surface, and then inserts into the bacterial membrane disrupting membrane nanodomains, thus affecting membrane function without forming pores. The results suggest that AMC-109 is a peptide with enhanced selectivity for bacterial membranes.
NATURE COMMUNICATIONS
(2023)
Article
Biochemistry & Molecular Biology
Martin Jakubec, Fredrik G. Rylandsholm, Philip Rainsford, Mitchell Silk, Maxim Bril'kov, Tone Kristoffersen, Eric Juskewitz, Johanna U. Ericson, John Sigurd M. Svendsen
Summary: Antimicrobial peptides (AMPs) are compounds that disrupt bacterial membranes. The initial interaction between AMPs and Gram-negative E. coli is driven by lipopolysaccharides (LPS) which act as kinetic barriers. Cationic AMPs first bind to LPS before reaching the bacterial membrane. The potency of AMPs is diminished if the initial LPS-binding is too strong, while their antimicrobial activity is dependent on effective interaction with the membrane.
