Article
Biotechnology & Applied Microbiology
Neelam Mishra, Kavita Rana, Siva Deepthi Seelam, Rakesh Kumar, Vijyendra Pandey, Bharathi P. Salimath, Dayanand Agsar
Summary: Pseudomonas aeruginosa DNM50 was identified as a biosurfactant-producing bacterium with 12 different congeners of rhamnolipid identified through structural characterization. The rhamnolipid showed radical scavenging activity with an IC50 value of 101.8 μg/ml and exhibited cytotoxic activity against MDA-MB-231 breast cancer cell line with a low IC50 of 0.05 μg/ml at 72 h of treatment. This suggests that DNM50RL may have potential in breast cancer treatment by targeting inhibition of p38MAPK.
FRONTIERS IN BIOENGINEERING AND BIOTECHNOLOGY
(2021)
Article
Environmental Sciences
Chun-Wen Cheng, Gwo-Tarng Sheu, Jing-Shiuan Chou, Pei-Han Wang, Yu-Chun Cheng, Chane-Yu Lai
Summary: The study demonstrated that soluble PM2.5 from building demolition sites can promote the survival and metastasis of triple-negative breast cancer cells, with increased cell viability, migration capacity, and activation of malignant signaling pathways in cancer cells exposed to the particulates.
Article
Biophysics
Rahman Hallaj, Zhaleh Ghafary, Osama kamal Mohammed, Raheleh Shakeri
Summary: The study developed an electrochemical biosensor for detecting the endogenous protein of breast cancer cells using RNA-cleaving DNAzymes. Thionine-modified gold nanoparticles and modified magnetic nanoparticles were used to prepare a probe, which was then pulled to the electrode surface with the help of a magnetic field. The presence of gold nanoparticle-thionine hybrid as an electroactive label ensured strong detection signals. The biosensor showed a linear range of (1.0E-06 to 1.0E+01) pg/ml for the protein marker and a detection limit of (1.0129E-07 pg/ml) using differential pulse voltammetry and electrochemical impedance spectroscopy (EIS).
BIOSENSORS & BIOELECTRONICS
(2023)
Article
Multidisciplinary Sciences
Xingjian Zhang, Trevor Chan, Michael Mak
Summary: This study investigated the phenotypes of highly aggressive cancer cells in confined microenvironments, revealing two distinct migratory phenotypes in fast migrating single cells and an increase in protrusions at the leading edge of cells under geometric confinement. The findings elucidate the impact of geometric constraints on cell behavior and morphodynamics associated with different cell phenotypes.
SCIENTIFIC REPORTS
(2021)
Article
Biochemistry & Molecular Biology
Kamylla Fernanda Souza de Souza, Danilo Tofoli, Indiara Correia Pereira, Kelly Juliana Filippin, Ana Tereza Gomes Guerrero, Edgar Julian Paredes-Gamero, Maria de Fatima Cepa Matos, Walmir Silva Garcez, Fernanda Rodrigues Garcez, Renata Trentin Perdomo
Summary: The study isolated three compounds from the leaves of Aniba heringeri, with compound 3 showing strong cytotoxicity against breast cancer cells and a high selective index. This compound exhibited promising apoptosis induction effects on triple-negative breast cancer cells, demonstrating potential as a prototype for targeting TNBC cells that are usually resistant to conventional therapies.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Cell Biology
Florian Keller, Roman Bruch, Franziska Clauder, Mathias Hafner, Ruediger Rudolf
Summary: The study found that extracellular matrix components play a significant role in regulating BSP expression, suggesting mechanisms for the formation of bone-associated metastasis in breast cancer that may involve local control of BSP levels through extracellular matrix degradation and release of growth factors.
Article
Cell Biology
Marco A. Lacerda-Abreu, Thais Russo-Abrahao, Raissa Leite Tenorio Aguiar, Robson de Queiroz Monteiro, Franklin D. Rumjanek, Jose R. Meyer-Fernandes
Summary: Breast cancer is associated with genetic mutations that lead to uncontrolled growth of breast cells. Tumor cells have rewired energy metabolism compared to normal cells, with inorganic phosphate playing a crucial role in cancer cell proliferation. Understanding the activity of ectophosphatase can provide insights into cancer cell energy requirements and growth mechanisms.
CELL BIOLOGY INTERNATIONAL
(2021)
Article
Biology
Fatma Mousa AlGhalban, Amir Ali Khan, Muhammad Nasir Khan Khattak
Summary: The latex of Ficus salicifolia and Ficus carica exhibit anti-proliferative and anti-metastatic effects in TNBC cells. They differ in the level of toxicity and molecular mechanisms involved in their anti-cancer activity.
SAUDI JOURNAL OF BIOLOGICAL SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
C. Cantonero, P. J. Camello, G. M. Salido, J. A. Rosado, P. C. Redondo
Summary: TMEM97 is involved in the proliferation of breast cancer cells by regulating calcium influx and promoting cholesterol uptake. It acts by influencing the interaction between SOCE calcium channel and cholesterol in cancer cells.
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS
(2021)
Article
Oncology
Rahil Ghanbarnasab Behbahani, Amir Danyaei, Ali Teimoori, Mohammad Javad Tahmasbi, Niloofar Neisi
Summary: This study investigated the synergistic effects of OPN gene knockout and radiotherapy in MDA-MB-231 breast cancer cells using CRISPR/Cas9 technique. The results showed that the combination of OPN gene knockout and radiotherapy promoted cell apoptosis, suppressed downstream gene expression, reduced cell viability, and inhibited cell cycle progression. Additionally, this approach substantially altered DNA damage responses.
JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY
(2023)
Article
Chemistry, Inorganic & Nuclear
Tina Rabizadeh, Reyhaneh Varshochian, Athar Mahdieh, Mahsa Rezaei, Negin Pazouki, Mahsa Zardkanlou, Shiva Irani, Rassoul Dinarvand
Summary: In this study, polydopamine-coated superparamagnetic iron oxide nanoparticles were used to deliver the immunomodulatory drug teriflunomide to breast cancer cells. The nanoparticles showed promising potential by increasing cytotoxicity and gene expression in the cells. The study suggests that the designed teriflunomide-loaded nanoparticles could be considered for future breast cancer therapy research.
JOURNAL OF CLUSTER SCIENCE
(2023)
Article
Biochemistry & Molecular Biology
Hadi Chavoshi, Mahsa Taheri, Murphy Lam Yim, Mehdi Sabzichi
Summary: Triple-negative breast cancer (TNBC) is a highly lethal subtype of breast cancer. Crocin-loaded liposomes showed enhanced cytotoxicity when combined with chemotherapy drug doxorubicin (DOX) in MDA-MB-231 cells. The liposome formulation had monodisperse distribution with an average size of 80 nm, about 70% encapsulation efficiency, and 11% loading capacity. The study suggested that crocin-loaded liposomes can be a promising approach against tumor cells, especially when combined with DOX.
PROCESS BIOCHEMISTRY
(2023)
Article
Biotechnology & Applied Microbiology
Ling Chen, Li-Quan Ren, Zhong Liu, Xin Liu, Han Tu, Xu-Ying Huang
Summary: This study investigated the anti-cancer mechanism of Schisandrin A in breast cancer through bio-informatics analysis and in vitro experiments. The results showed that SchA could promote cell migration and inhibit apoptosis by regulating specific targets, making it a potential adjuvant treatment for breast cancer.
Article
Biochemistry & Molecular Biology
Ana-Isabel Naranjo, Maria-Julia Gonzalez-Gomez, Victoriano Baladron, Jorge Laborda, Maria-Luisa Nueda
Summary: DLK2 expression levels can affect the tumor properties and growth dynamics of MDA-MB-231 breast cancer cells by regulating NOTCH signaling and other cell signaling pathways.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Food Science & Technology
Ling Xie, Jun Yi, Yongjia Song, Mengyao Zhao, Liqiang Fan, Liming Zhao
Summary: GOLM1 has been identified as a prime target for cancer therapy, and EGCG is the first natural product found to downregulate GOLM1 expression, inhibiting MDA-MB-231 cell migration through the HGF/HGFR/AKT/GSK-3/ beta-catenin/c-Myc signaling pathway.
FOOD AND CHEMICAL TOXICOLOGY
(2021)
Article
Chemistry, Medicinal
Camilla Pecoraro, Michele De Franco, Daniela Carbone, Davide Bassani, Matteo Pavan, Stella Cascioferro, Barbara Parrino, Girolamo Cirrincione, Stefano Dall'Acqua, Stefano Moro, Valentina Gandin, Patrizia Diana
Summary: Metabolic deregulation is a key mechanism in promoting cancer resistance and progression. In this study, novel hybrid molecules were synthesized and evaluated for their ability to inhibit PDK, resulting in the suppression of pancreatic cancer cell growth and spread. These compounds also showed promising results in animal models, reducing tumor growth without significant side effects.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Editorial Material
Biochemistry & Molecular Biology
Valentina Gandin, James D. Hoeschele, Nicola Margiotta
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Daniela Carbone, Michele De Franco, Camilla Pecoraro, Davide Bassani, Matteo Pavan, Stella Cascioferro, Barbara Parrino, Girolamo Cirrincione, Stefano Dall'Acqua, Stefano Moro, Valentina Gandin, Patrizia Diana
Summary: A library of 3-amino-1,2,4-triazine derivatives was designed and synthesized, which showed potent and selective inhibition of PDK. These compounds proved to be effective in inducing cancer cell death, especially in human pancreatic KRAS mutated cancer cells.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Francesca Moret, Luca Menilli, Celeste Milani, Giorgia Di Cintio, Chiara Dalla Torre, Vincenzo Amendola, Marta De Zotti
Summary: In the field of bioactive peptides, peptaibols are a unique class of compounds produced by Trichoderma fungi that are membrane-active and can induce plant defense responses. Among these compounds, trichogin analogs have shown potent activity against phytopathogens and potential as a sustainable alternative to copper-based plant protection. This study investigated the activity of trichogin analogs against breast cancer cells and normal cells, finding that certain analogs displayed cytotoxicity against cancer cells and could be anchored to gold nanoparticles for targeted drug delivery.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Maura Pellei, Carlo Santini, Luca Bagnarelli, Miriam Caviglia, Paolo Sgarbossa, Michele De Franco, Mirella Zancato, Cristina Marzano, Valentina Gandin
Summary: The conversion of two acids into ester derivatives and their use for synthesizing silver(I) complexes with significant in vitro antitumor activity, particularly against small-cell lung carcinoma, is described. Mechanistic studies show that these complexes can accumulate in cancer cells and selectively target Thioredoxin (TrxR), leading to redox homeostasis imbalance and cancer cell death through apoptosis.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Alisa Zanin, Giacomo Meneghetti, Luca Menilli, Annachiara Tesoriere, Francesco Argenton, Maddalena Mognato
Summary: A coordinated action between nuclear and mitochondrial activities is crucial for the cellular response to genotoxic stress. This study examined the role of mitochondrial STAT3 (mitoSTAT3) in the DNA damage response to UVC radiation. The results showed that stable expression of mitoSTAT3 enhanced cell proliferation and improved cell survival after UVC irradiation by minimizing oxidant cellular stress.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Daniela Carbone, Michele De Franco, Camilla Pecoraro, Davide Bassani, Matteo Pavan, Stella Cascioferro, Barbara Parrino, Girolamo Cirrincione, Stefano Dall'Acqua, Stefania Sut, Stefano Moro, Valentina Gandin, Patrizia Diana
Summary: Pancreatic ductal adenocarcinoma (PDAC) is a highly aggressive cancer type with poor prognosis and drug resistance. Cell metabolism alteration plays a key role in PDAC progression, leading to cell proliferation, invasion, and chemotherapy resistance. In this study, a new series of indolyl-7-azaindolyl triazine compounds were synthesized, inspired by marine bis-indolyl alkaloids. These compounds were found to inhibit the enzymatic activity of pyruvate dehydrogenase kinases (PDKs), with a high selectivity against KRAS-mutant PDAC. Molecular docking analysis and cell growth inhibition assays demonstrated the potential of these derivatives as therapeutic options for PDAC.
Article
Biochemistry & Molecular Biology
Stephen Barrett, Michele De Franco, Chiara Donati, Cristina Marzano, Valentina Gandin, Diego Montagner
Summary: The interest in using copper as a metal scaffold for developing novel chemotherapeutics has grown in recent years due to its lower toxicity compared to platinum drugs, different mechanisms of action, and lower cost. Many copper-based complexes, including the copper bis-phenanthroline [Cu(phen)(2)](2+) developed by D.S. Sigman, have been developed and screened as anticancer agents. Specifically, copper(phen) derivatives have shown high interest for their ability to interact with DNA through nucleobase intercalation. In this study, we report the synthesis and chemical characterization of four novel copper(II) complexes functionalized with phenanthroline derivatives containing biotin, which has receptors overexpressed in many tumor cells. A detailed biological analysis, including cytotoxicity, cellular drug uptake, DNA interaction, and morphological studies, is discussed.
Article
Pharmacology & Pharmacy
Greta Avancini, Luca Menilli, Adele Visentin, Celeste Milani, Francesca Mastrotto, Francesca Moret
Summary: Despite improvements in breast cancer treatment, alternative therapies are needed for advanced-stage patients. Photodynamic therapy (PDT) is gaining attention as a selective and low off-target option. Polymeric nanoparticles (NPs) can overcome the solubility and circulation challenges of hydrophobic photosensitizers (PSs).
Article
Chemistry, Multidisciplinary
Amrita Sarkar, Vojtech Novohradsky, Moumita Maji, Tomer Babu, Lenka Markova, Hana Kostrhunova, Jana Kasparkova, Valentina Gandin, Viktor Brabec, Dan Gibson
Summary: A multitargeting prodrug (2) that releases gemcitabine, oxaliplatin, and doxorubicin in their active form in cancer cells is a potent cytotoxic agent. It selectively targets cancer cells with high selectivity indices and induces the release of DAMPs in CT26 cells. The prodrug also inhibits tumor growth in murine models with lower body weight loss compared to FDA drugs.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Biochemistry & Molecular Biology
Irene Varponi, Stefania Ferro, Luca Menilli, Alessandro Grapputo, Francesca Moret, Francesca Mastrotto, Oriano Marin, Federica Sandrelli
Summary: This study reports the biological properties of D-Q53 CecB, which is an all-D enantiomer of the silkworm natural peptide Q53 CecB. Compared to the L-variant, D-Q53 CecB shows enhanced bactericidal activity against P. aeruginosa planktonic bacteria and resistance to in vitro degradation by humans and P. aeruginosa elastases. It is thermostable and maintains its antimicrobial activity at high salt concentrations and in the presence of divalent cations or fetal-bovine serum. In addition, D-Q53 CecB shows cytotoxic phenomena at higher concentrations against different types of human cells. It is also effective in inhibiting and degrading biofilms, making it a favorable candidate for anti-Pseudomonas therapy.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Laura Morbiato, Celeste Quaggia, Luca Menilli, Chiara Dalla Torre, Antonio Barbon, Marta De Zotti
Summary: Peptaibols are proteolysis-resistant, membrane-active peptides with stable helical 3D structures. Medium-length peptaibols are of interest for studying peptide-membrane interaction. Electron paramagnetic resonance (EPR) is used for this purpose, but it requires synthesis of spin-labeled medium-length peptaibols.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang
Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon
Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai
Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang
Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho
Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski
Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun
Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan
Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)