Review
Chemistry, Medicinal
Shrawan Kumar Mangawa, Shailja Singh
Summary: Despite scientific progress, malaria remains a global burden that causes thousands of deaths annually. The only option for reducing malaria mortality and morbidity is chemotherapy, but due to drug resistance and toxicity, scientists must explore beyond conventional medicinal chemistry. Metal-based hybrids, including ferrocene compounds, have shown potential as antimalarial agents, with Ferroquine being the most advanced organometallic compound developed and showing great potency in clinical trials against both drug-sensitive and drug-resistant malaria.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2023)
Review
Infectious Diseases
Kasem Kulkeaw
Summary: This article summarizes current in vitro hepatic models and tools for assaying antimalarial drug activity. While primary human cells are more physiologically relevant, they face limitations. Advances in stem cell technologies and multidimensional culture provide new avenues for modeling human infectious diseases.
Article
Chemistry, Analytical
Robert Domes, Torsten Frosch
Summary: Deep ultraviolet resonance Raman experiments were conducted to investigate the antimalarial drug FQ. The drug's behavior in different pH environments and membrane polarities was simulated using buffered aqueous solutions. Density functional theory calculations were performed to analyze the drug's microspeciation and shifts in Raman signals. The study found that FQ exists in different forms in polar and nonpolar environments and determined the limit of detection at different pH values.
ANALYTICAL CHEMISTRY
(2023)
Article
Microbiology
Silvia Parapini, Silvio Paone, Emanuela Erba, Loredana Cavicchini, Manoochehr Pourshaban, Francesco Celani, Alessandro Contini, Sarah D'Alessandro, Anna Olivieri
Summary: Malaria causes numerous cases and deaths annually, and the search for novel antimalarial drugs is essential. This study tested a series of Rac1 inhibitors and found that EHop-016 exhibited the most effective inhibitory activity against Plasmodium falciparum, without affecting red blood cell invasion but impacting parasite growth internally.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2022)
Review
Pharmacology & Pharmacy
Hannah C. Zierden, Rachel L. Shapiro, Kevin DeLong, Davell M. Carter, Laura M. Ensign
Summary: Preterm birth is defined as delivery before 37 weeks of gestation, with 15 million infants born prematurely globally each year, increasing the risk of mortality and health challenges. While the only FDA approved therapy for preventing preterm birth in the U.S. has faced recent setbacks, interdisciplinary efforts are underway to develop next generation therapies to prevent preterm birth and save infant lives. This research aims to better identify women at risk for preterm birth, prevent premature labor, and ultimately improve outcomes for newborns.
ADVANCED DRUG DELIVERY REVIEWS
(2021)
Review
Oncology
E. Elizabeth Patton, Kristen L. Mueller, David J. Adams, Niroshana Anandasabapathy, Andrew E. Aplin, Corine Bertolotto, Marcus Bosenberg, Craig J. Ceo, Christin E. Burd, Ping Chi, Meenhard Herlyn, Sheri L. Holmen, Florian A. Karreth, Charles K. Kaufman, Shaheen Khan, Sebastian Kobold, Eleonora Leucci, Carmit Levy, David B. Lombard, Amanda W. Lund, Kerrie L. Marie, Jean-Christophe Marine, Richard Marais, Martin McMahon, Carla Daniela Robles-Espinoza, Ze'ev A. Ronai, Yardena Samuels, Maria S. Soengas, Jessie Villanueva, Ashani T. Weeraratna, Richard M. White, Iwei Yeh, Jiyue Zhu, Leonard Zon, Marc S. Hurlbert, Glenn Merlino
Summary: The current state of melanoma models encompass various types which can address challenges such as metastasis, drug resistance, immune response, etc. Building models for rare subtypes of melanomas is an important yet unmet need.
Article
Oncology
Alex O. Haber, Aditi Jain, Chinnadurai Mani, Avinoam Nevler, Lebaron C. Agostini, Talia Golan, Komaraiah Palle, Charles J. Yeo, William H. Gmeiner, Jonathan R. Brody
Summary: CF10 is a novel drug for treating PDAC, more potent than 5-FU, effective in inhibiting PDAC cell survival by inhibiting TS and strong Top1 cleavage complex formation, and shows single-agent activity in murine models.
MOLECULAR CANCER RESEARCH
(2021)
Review
Engineering, Biomedical
Molly Klimak, Robert J. Nims, Lara Pferdehirt, Kelsey H. Collins, Natalia S. Harasymowicz, Sara J. Oswald, Lori A. Setton, Farshid Guilak
Summary: Immunoengineering has advanced new approaches for treating joint diseases such as osteoarthritis and rheumatoid arthritis, emphasizing the importance of precise targeting and controlled delivery strategies for better therapeutic outcomes. By leveraging biomaterials and genetic engineering, immunoengineering has the potential to revolutionize the understanding, treatment, and prevention of joint diseases.
ACTA BIOMATERIALIA
(2021)
Article
Biology
Ines Bouzon-Arnaiz, Yunuen Avalos-Padilla, Arnau Biosca, Omar Cano-Prades, Lucia Roman-Alamo, Javier Valle, David Andreu, Diana Moita, Miguel Prudencio, Elsa M. Arce, Diego Munoz-Torrero, Xavier Fernandez-Busquets
Summary: This study found that inhibiting protein aggregation significantly reduces the viability of the malaria parasite in vitro. A compound called YAT2150 demonstrated powerful anti-malarial activity, inhibiting the growth of the parasite in different developmental stages by affecting its protein composition. Due to its novel structure and potential targeting of multiple gene products, the evolution of resistance to YAT2150 is unlikely, making it a promising compound for the post-artemisinin era.
Article
Multidisciplinary Sciences
Louai Labanieh, Crystal L. Mackall
Summary: The development of next-generation CAR immune cell technologies has greatly improved the efficacy, safety, and accessibility of CAR therapies. Multispecific, logic-gated, and regulatable CARs show promise in overcoming resistance and increasing safety. Stealth, virus-free, and in vivo gene delivery platforms may reduce costs and improve access to cell therapies. The success of CAR T cells in liquid cancers is driving the development of more sophisticated immune cell therapies for solid cancers and non-malignant diseases in the future.
Article
Immunology
Camila Fabbri, Glenda Quaresma Ramos, Djane Clarys Baia-da-Silva, Alexandre Oliveira Trindade, Luis Carlos Salazar-Alvarez, Juliana Costa Ferreira Neves, Ivanildes dos Santos Bastos, Allyson Guimaraes Costa, Marcus Vinicius Guimaraes Lacerda, Wuelton Marcelo Monteiro, Fabio Trindade Maranhao Costa, Stefanie Costa Pinto Lopes
Summary: This study evaluated the potential of methylene blue (MB) against the asexual and sexual forms of Plasmodium vivax. The results showed that MB had high efficacy against the asexual stages and demonstrated some inhibition in the sexual forms. These findings suggest that MB may be a potential drug for the treatment of vivax malaria.
FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY
(2023)
Article
Chemistry, Multidisciplinary
Enrico Mastrobattista
Summary: This article introduces the author's research work and future research plans at the Department of Pharmaceutical Sciences at Utrecht University, focusing on the administration and fate control of biotherapeutics. The author's research interests include formulation of biotherapeutics into nanomedicines, intracellular delivery of nucleic acids and protein therapeutics, and targeted delivery of biotherapeutics beyond the liver. Additionally, the author provides an outlook on how current developments in drug delivery and gene therapy may lead to sustainable and cost-effective dosing regimens for biotherapeutics.
JOURNAL OF CONTROLLED RELEASE
(2021)
Article
Chemistry, Medicinal
Thanh-Hoang Nguyen-Vo, Quang H. Trinh, Loc Nguyen, Trang T. T. Do, Matthew Chin Heng Chua, Binh P. Nguyen
Summary: This study proposes a novel molecular encoding scheme for predicting antimalarial natural products. By training and comparing machine learning algorithms, the results show that this encoding scheme is highly accurate and effective, and can be used in other biomedical applications.
JOURNAL OF CHEMICAL INFORMATION AND MODELING
(2022)
Article
Microbiology
Chatpong Pethrak, Navaporn Posayapisit, Jutharat Pengon, Nattida Suwanakitti, Atiporn Saeung, Molnipha Shorum, Kittipat Aupalee, Kritsana Taai, Yongyuth Yuthavong, Sumalee Kamchonwongpaisan, Natapong Jupatanakul
Summary: This study provides important insights into the activity of antifolates as a chemopreventive therapeutic which could lead to a more efficient and cost-effective treatment regime.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2022)
Article
Biochemistry & Molecular Biology
Giulia Degiacomi, Laurent Roberto Chiarelli, Deborah Recchia, Elena Petricci, Beatrice Gianibbi, Ersilia Vita Fiscarelli, Lanfranco Fattorini, Fabrizio Manetti, Maria Rosalia Pasca
Summary: The study focused on the essential mycolic acids transporter MmpL3 and identified mefloquine as a potential new drug against Mycobacterium abscessus. Mefloquine was found to interfere with mycolic acids biosynthesis and showed activity against other nontuberculous mycobacteria. Repurposing the well-known antimalarial agent mefloquine could help reduce the time and cost of discovering novel drug candidates.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Charlotte Dubois, Kateryna Kondratska, Artem Kondratskyi, Angela Morabito, Lina Mesilmany, Valerio Farfariello, Robert-Alain Toillon, Nathalie Ziental Gelus, Emilie Laurenge, Fabien Vanden Abeele, Loic Lemonnier, Natalia Prevarskaya
Summary: Changes in cytosolic free Ca2+ concentration play a central role in cellular processes. ORAI3 channels are expressed in both normal and pancreatic ductal adenocarcinoma cell lines, affecting store-operated calcium entry (SOCE). Silencing ORAI3 increases SOCE in PDAC cell lines and decreases SOCE in normal pancreatic cell line, impacting proliferation, cell cycle, viability, mitotic catastrophe, and cell death.
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH
(2021)
Article
Plant Sciences
Oriane Morel, Cedric Lion, Godfrey Neutelings, Jonathan Stefanov, Fabien Baldacci-Cresp, Clemence Simon, Christophe Biot, Simon Hawkins, Corentin Spriet
Summary: This article introduces a methodology called REPRISAL for mapping the lignification capacity of plant cell walls in detail. REPRISAL combines three separate approaches, including chemical reporters labeling, automatic segmentation algorithm, and ratiometric analysis, to analyze the distribution and proportions of monolignol reporters in different cell wall zones. The methodology is applied to study the lignification capacity in Arabidopsis, Populus, flax, and maize, as well as the incorporation of a fucose reporter into noncellulosic cell wall polymers.
Article
Multidisciplinary Sciences
Valerio Farfariello, Dmitri Gordienko, Lina Mesilmany, Yasmine Touil, Emmanuelle Germain, Ingrid Fliniaux, Emilie Desruelles, Dimitra Gkika, Morad Roudbaraki, George Shapovalov, Lucile Noyer, Mathilde Lebas, Laurent Allart, Nathalie Zienthal-Gelus, Oksana Iamshanova, Franck Bonardi, Martin Figeac, William Laine, Jerome Kluza, Philippe Marchetti, Bruno Quesnel, Daniel Metzger, David Bernard, Jan B. Parys, Loic Lemonnier, Natalia Prevarskaya
Summary: This study reveals the mechanism of how alterations in mitochondrial function and calcium signaling contribute to cellular senescence and tumor growth. The downregulation of TRPC3 protein in senescent fibroblasts leads to increased mitochondrial calcium load and oxidative phosphorylation, promoting cellular senescence. The downregulation of TRPC3 in stromal cells also affects secretome and tumor progression, highlighting its importance in cancer development.
NATURE COMMUNICATIONS
(2022)
Article
Biochemistry & Molecular Biology
Di Wu, Pierre-Andre Gilormini, Sakura Toda, Christophe Biot, Cedric Lion, Yann Guerardel, Chihiro Sato, Ken Kitajima
Summary: This study investigated the role of the C-domain in the CMP-Kdn-dependent inhibition in rainbow trout and mice. The results showed that the C-domain affects the catalytic activity of rtCSS when using Kdn as a substrate, and the inhibition is C-domain-dependent.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2022)
Article
Oncology
Sarah Trouvilliez, Julien Cicero, Romain Leveque, Leo Aubert, Cyril Corbet, Alexandre Van Outryve, Karolin Streule, Pierre-Olivier Angrand, Pamela Volkel, Romain Magnez, Guillaume Brysbaert, Caroline Mysiorek, Fabien Gosselet, Roland Bourette, Eric Adriaenssens, Xavier Thuru, Chann Lagadec, Jerome de Ruyck, Veronique Orian-Rousseau, Xuefen Le Bourhis, Robert-Alain Toillon
Summary: Our study revealed that CD44v3 forms a complex with TrkA in response to NGF stimulation in breast cancer, and a CD44v3 mimetic peptide can inhibit tumor growth and metastasis, suggesting a potential therapeutic option for triple-negative breast cancers.
JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH
(2022)
Article
Oncology
Giorgia Chinigo, Guillaume P. Grolez, Madelaine Audero, Alexandre Bokhobza, Michela Bernardini, Julien Cicero, Robert-Alain Toillon, Quentin Bailleul, Luca Visentin, Federico Alessandro Ruffinatti, Guillaume Brysbaert, Marc F. Lensink, Jerome De Ruyck, Anna Rita Cantelmo, Alessandra Fiorio Pla, Dimitra Gkika
Summary: This study reveals that the TRPM8 channel inhibits cell migration and adhesion in prostate cancer by interacting with the small GTPase Rap1A. The interaction between TRPM8 and Rap1A is critical for the motility control of cancer cells and could potentially be targeted for therapy in various types of tumors.
Article
Immunology
Alice Capuz, Melodie-Anne Karnoub, Sylvain Osien, Melanie Rose, Celine Meriaux, Isabelle Fournier, David Devos, Fabien Vanden Abeele, Franck Rodet, Dasa Cizkova, Michel Salzet
Summary: A study found that different types of IgG immunoglobulins appeared in the spinal cord after spinal cord injury in rats, influencing the growth of neuronal synapses. By investigating the mechanism of action of immunoglobulins on neurons, a novel potential strategy for treating spinal cord injury was proposed.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Vincent Rigolot, Yannick Rossez, Christophe Biot, Cedric Lion
Summary: Most Escherichia coli strains associated with neonatal meningitis express the K1 capsule, a sialic acid polysaccharide that is directly related to their pathogenicity. However, bacterial capsules are seldom targeted despite their important role as virulence factors, and the K1 polysialic acid (PSA) antigen that shields bacteria from the immune system still remains untackled. In this study, we develop a fluorescence microplate assay that combines metabolic oligosaccharide engineering (MOE) and bioorthogonal chemistry to detect K1 capsules. The assay is optimized, validated, and can be used for screening approaches to identify novel capsule-targeted antibiotics.
RSC CHEMICAL BIOLOGY
(2023)
Editorial Material
Biochemistry & Molecular Biology
Marie Lopez, Yung-Sing Wong, Christophe Biot, Boris Vauzeilles
Summary: Chemical biology is a growing field that uses chemical and physicochemical tools to address biological questions at the molecular level. Chemical biologists design and develop molecular tools to understand and modify biological processes, and observe their effects in complex biological environments. This field finds applications in areas such as healthcare and the environment.
Review
Oncology
Sarah Trouvilliez, Chann Lagadec, Robert-Alain Toillon
Summary: This review summarizes the failures of targeted therapies against TrkA, focusing on non-genomic resistance. It highlights that overexpression of TrkA can lead to ligand-independent activation, bypassing the effect of kinase inhibitors, resulting in treatment failures. These observations suggest that genetics alone cannot explain all therapeutic failures, and new hypotheses are needed to understand these failures.
Article
Oncology
Martin Morisse, Thomas Bourhis, Romain Leveque, Mathieu Guilbert, Julien Cicero, Martine Palma, Dominique Chevalier, Xuefen le Bourhis, Robert-Alain Toillon, Francois Mouawad
Summary: Head and Neck Squamous Cell Carcinoma (HNSCC) is a cancer with a poor prognosis, but targeted anti-EGFR therapies have limited efficacy. Our study investigated the interaction between Sortilin and EGFR and found that Sortilin expression is associated with reduced survival. ProNGF was shown to reduce the effects of EGF on cell growth by inducing the internalization of EGFR.
FRONTIERS IN ONCOLOGY
(2023)
Article
Biochemical Research Methods
Marie Denoulet, Mathilde Brule, Francois Anquez, Audrey Vincent, Julie Schnipper, Eric Adriaenssens, Robert-Alain Toillon, Xuefen Le Bourhis, Chann Lagadec
Summary: The study develops a new R-based tool called ABSP for analyzing CpG methylation levels in bisulfite sequencing PCR data. The tool can process both direct-BSP and cloning-BSP data, and provides an automated analysis process and user-friendly interface.
Article
Oncology
Julien Cicero, Sarah Trouvilliez, Martine Palma, Gaetan Ternier, Laurine Decoster, Eloise Happernegg, Nicolas Barois, Alexandre Van Outryve, Lucie Dehouck, Roland P. Bourette, Eric Adriaenssens, Chann Lagadec, Cagatay Mehmet Tarhan, Dominique Collard, Zied Souguir, Elodie Vandenhaute, Gregory Maubon, Francois Sipieter, Nicolas Borghi, Fumitaka Shimizu, Takashi Kanda, Paolo Giacobini, Fabien Gosselet, Nathalie Maubon, Xuefen Le Bourhis, Isabelle Van Seuningen, Caroline Mysiorek, Robert-Alain Toillon
Summary: This study demonstrates for the first time that the precursor of Nerve Growth Factor (proNGF) is involved in brain metastasis of triple-negative breast cancer (TNBC), and identifies the TrkA/EphA2 complex as a potential therapeutic target. These findings provide important insights into the mechanisms underlying brain metastasis.
EXPERIMENTAL HEMATOLOGY & ONCOLOGY
(2023)
Article
Biochemical Research Methods
Nadine V. Conchinha, Liliana Sokol, Laure-Anne Teuwen, Koen Veys, Sybastien J. Dumas, Elda Meta, Melissa Garcia-Caballero, Vincent Geldhof, Rongyuan Chen, Lucas Treps, Mila Borri, Pauline de Zeeuw, Kim D. Falkenberg, Charlotte Dubois, Magdalena Parys, Laura P. M. H. de Rooij, Katerina Rohlenova, Jermaine Goveia, Luc Schoonjans, Mieke Dewerchin, Guy Eelen, Xuri Li, Joanna Kalucka, Peter Carmeliet
Summary: Endothelial cells (ECs) have distinct phenotypical and functional characteristics depending on their tissue localization, playing crucial roles in diseases of various organs. Rapid and reproducible purification of blood vessel ECs can be achieved through mechanical and enzymatic digestion, providing important tools for research.
Article
Biochemical Research Methods
Sebastien J. Dumas, Elda Meta, Nadine V. Conchinha, Liliana Sokol, Rongyuan Chen, Mila Borri, Laure-Anne Teuwen, Koen Veys, Melissa Garcia-Caballero, Vincent Geldhof, Lucas Treps, Pauline de Zeeuw, Kim D. Falkenberg, Charlotte Dubois, Magdalena Parys, Laura P. M. H. de Rooij, Katerina Rohlenova, Jermaine Goveia, Luc Schoonjans, Mieke Dewerchin, Guy Eelen, Xuri Li, Joanna Kalucka, Peter Carmeliet
Summary: Endothelial cells exhibit tissue-specific phenotypes and functions, making their isolation essential for studies in the vascular field. Tailored protocols for highly purified ECs from kidney, spleen, and testis tissues are provided for scRNA sequencing, utilizing magnetic- and fluorescence-activated cell sorting for rapid and reproducible purification.