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A series of novel 2-[(5-phenyl-1,3,4-thiadiazole-2-imino)substituted benzene]diazenyl benzene sulphonamide derivatives (VII)6-10 weresynthesized and FT-IR, 1H NMR, 13C NMR and GC-MS spectral data were used to investigate the structures of the synthesized sulphonamide derivatives. The antioxidant activity of 2-[(5-phenyl-1,3,4-thiadiazole-2-imino)su...
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Integrin-mediated focal adhesions are the primary architectures that transmit forces between the extracellular matrix (ECM) and the actin cytoskeleton. Although focal adhesions are abundant on rigid and flat substrates that support high mechanical tensions, they are sparse in soft three-dimensional (3D) environments. Here we report curvature-depend...
Article
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Piano-stool-{CpRu} complexes containing 1,3,5-triaza-7-phosphaadamantane (PTA), N-methyl-1,3,5-triaza-7-phosphaadamantane (mPTA), and 3,7-dimethyl-1,3,7-triaza-5-phosphabyciclo[3.3.1]nonane (dmoPTA) were evaluated as drugs against breast cancer. The evaluated compounds include two new examples of this family, the complexes [RuCp(DMSO-κS)(HdmoPTA)(P...
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Background Quantum dots are usually particles smaller than 100 nm and have a low toxic effect. This study aimed to bioconjugate the anticancer effective melatonin agonist to quantum dots and demonstrate its effects in two cancer lines. This is the first study that aims to examine the anticancer activity of ramelteon bioconjugation to quantum dots,...
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Cellular deformability is a promising biomarker for evaluating the physiological state of cells in medical applications. Microfluidics has emerged as a powerful technique for measuring cellular deformability. However, existing microfluidic-based assays for measuring cellular deformability rely heavily on image analysis, which can limit their scalab...
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Drug resistance is a challenge in anticancer therapy. In many cases, cancers can be resistant to the drug prior to exposure, i.e., possess intrinsic drug resistance. However, we lack target-independent methods to anticipate resistance in cancer cell lines or characterize intrinsic drug resistance without a priori knowledge of its cause. We hypothes...
Preprint
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Treatment regimens are regularly evolving, together with novel therapies and drugs. Such evolution is necessary to circumvent resistance mechanisms and to give patients the best possible health care. When dealing with cancer, most regimens involve multiple treatments (surgery, radiation therapy, chemotherapy, immunotherapy, etc.). The purpose of th...
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Chemotherapy is a classical method of cancer treatment. Cisplatin-based chemotherapy is a traditional and essential therapeutic approach in gastric cancer treatment. However, the development of drug resistance during treatment is a major obstacle that limits their further application, and molecular changes have occurred in the development of drug r...
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The most common in vitro model for absorption, distribution, metabolism, and excretion (ADME) purposes is currently the Caco-2 cell line. However, clear differences in gene and protein expression towards the small intestine and an, at best, fair prediction accuracy of intestinal drug absorption restrict the usefulness of a model for intestinal epit...
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T cell leukemia homeobox 2 (TLX2) plays an important role in some tumors. Bioinformatics and experimental validation represent a useful way to explore the mechanisms and functions of TLX2 gene in the cancer disease process from a pan cancer perspective. TLX2 was aberrantly expressed in pan cancer and cell lines and correlated with clinical stage. H...
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Acquired resistance to chemotherapeutic drugs in gallbladder cancer (GBC) results in therapy failure. This study is aimed to establish oxaliplatin (OXA)-resistant GBC cell lines and uncover their gene expression profiles. First, two OXA-resistant GBC cell lines (GBC-SD/OXA and SGC996/OXA) were established by gradually increasing the drug concentrat...
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Cells of two molecular genetic types of breast cancer—hormone-dependent breast cancer (ZR-75 cell line) and triple-negative breast cancer (BT-20 cell line)—were studied using atomic force microscopy and an optical nanomotion detection method. Using the Peak Force QNM and Force Volume AFM modes, we revealed the unique patterns of the dependence of Y...
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As one of the triterpene extracts of Taraxacum, a traditional Chinese plant, taraxerol (TRX) exhibits antitumor activity. In this study, we evaluated the effects of TRX on the migration and invasion of MDA-MB-231 cells, analyzed the molecular mechanism through network pharmacology and molecular docking, and finally verified it by in vitro experimen...
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Cancer occurs due to uncontrolled growth and proliferation of abnormal cells, which is a result of molecular alterations in genes associated with a variety of cellular processes. In order to support the development of incipient tumors, cancer cells are expected to require a constant and increasing supply of nutrients. Although it is evident that th...
Article
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Eight new scalarane sesterterpenes, phyllofenones F–M (1–8), together with two known analogues, carteriofenones B and A (9–10), were isolated from the marine sponge Phyllospongia foliascens collected from the South China Sea. The structures of these compounds were determined based on extensive spectroscopic and quantum chemical calculation analysis...
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Objectives: In this study we explored Bryonia alba as a new anti-cancer agent against liver cancer cells. Material and Methods: The Bryonia 6C - an alternative medicine was applied on HepG2 liver cancer cell line to find out its effectiveness indicating morphological and cytokine changes by observing cytopathic effect and RT-PCR study. Results: The...
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Applying a multistep approach, novel indolin-2-ones (IND) that possess an arylidene motif have been synthesized. Eight compounds were chosen for different biological tests (antimicrobial and cytotoxicity). IND containing 2-thienyl (4h) fragment have been found to exhibit good antimicrobial activity against B. cereus. Molecules that have 3-aminophen...
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Background Metformin is the most frequently prescribed medication for the treatment of type II diabetes mellitus and has played an anti-tumor potential in a variety of cancer types. Metformin can inhibit the growth of many cancer cells through various mechanisms, including ferroptosis. However, it is still unclear whether metformin can induce ferro...
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Protein complexes are responsible for the enactment of most cellular functions. For the protein complex to form and function, its subunits often need to be present at defined quantitative ratios. Typically, global changes in protein complex composition are assessed with experimental approaches that tend to be time consuming. Here, we have developed...
Preprint
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Background Cancer cells favour glycolysis and lactate production over mitochondrial metabolism despite the presence of oxygen (the Warburg effect). Increased pyruvate dehydrogenase kinase (PDK) activity contributes to this glycolytic phenotype. Dichloroacetate (DCA) is a PDK inhibitor with anti-cancer potential that inhibits all four isoforms of PD...
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Piperlongumine and derivatives are being developed as anticancer agents which act primarily as inducers of reactive oxygen species (ROS) in cancer cell lines. Many of the anticancer activities of piperlongumine resemble those observed for bis-indole derived compounds that bind the orphan nuclear receptor 4A1 (NR4A1) and act as inverse receptor agon...
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Pancreatic cancer is one of the deadliest diseases in human malignancies. Among total pancreatic cancer patients, ~10% of patients are categorized as familial pancreatic cancer (FPC) patients, carrying germline mutations of the genes involved in DNA repair pathways (e.g., BRCA2). Personalized medicine approaches tailored toward patients’ mutations...
Article
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KLHL5 was a member of kelch-repeat protein family and was involved in the initiation of progression of a plethora of cancers. However, its specific role in gastric cancer was not explicitly illustrated. In this context, we aimed to investigate the biological role and mechanisms about KLHL5 in gastric cancer. qRT-PCR and western blot were used to in...
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Vasculogenic mimicry (VM) is an intriguing phenomenon observed in tumor masses, in which cancer cells organize themselves into capillary-like channels that closely resemble the structure and function of blood vessels. Although VM is believed to contribute to alternative tumor vascularization, the detailed regulatory mechanisms controlling these cel...
Preprint
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Alterations of metabolism are a well appreciated hallmark of many cancers, including changes in mitochondrial and glutathione (GSH) metabolism. Mitochondrial GSH (mGSH) transport is a poorly characterized aspect of GSH metabolism, which we investigate in the context of cancer. Here, we apply hybrid machine learning (ML) models and leverage cancer c...
Preprint
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Canine mammary tumors represent one of the leading malignant pathology in female dogs, displaying the importance of efficient therapeutic findings, beside the golden standard surgery, able to limit the development of the disease. Studies in human cancers demonstrated that Doxorubicin presents a good effect in different biological processes like apo...
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The benzo[d]thiazole derivatives 4a–c were synthesized and used for the synthesis of thiophene derivatives 6a–f. They form the arylhydrazone derivatives 8a–i which were capable to form pyridazine derivatives 9a–i and 10a–i. The latter compounds reacted with thioglycolic acid to produce the thiazole derivatives 12a–i and 13a–i, respectively. The thi...
Article
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Marine-derived cyclic imine toxins, portimine A and portimine B, have attracted attention because of their chemical structure and notable anti-cancer therapeutic potential1–4. However, access to large quantities of these toxins is currently not feasible, and the molecular mechanism underlying their potent activity remains unknown until now. To addr...
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Viscosity is an essential parameter that regulates bio-molecular reaction rates of diffusion-driven cellular processes. Hence, abnormal viscosity levels are often associated with various diseases and malfunctions like cancer. For this reason, monitoring intracellular viscosity becomes vital. While several approaches have been developed for in vitro...
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Purpose Genome-wide association studies have identified SMAD7 as a colorectal cancer (CRC) susceptibility gene. However, its underlying mechanism has not yet been characterized. This study screened functional SNPs (fSNPs) related to colorectal cancer through Reel-seq and obtained regulatory proteins on functional SNPs. Methods The candidate fSNPs...
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Despite significant advancements in cancer treatment, there is a constant need for new and effective therapeutic options. One such potential weapon in the fight against cancer is ruthenium complex II. In this article, we synthesized, characterized, and studied the activity of dithiocyanato-N-bis[8-(diphenylphosphino)quinoline]ruthenium (II) [Ru(N-P...
Preprint
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Transcriptomics, and in particular RNA-Seq, has become a widely used approach to assess the molecular state of biological systems. To facilitate its analysis, many tools have been developed for different steps, such as filtering lowly expressed genes, normalisation, differential expression, and enrichment. While numerous studies have examined the i...
Preprint
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HSF1 is a well-known Heat Shock Protein expression regulator in response to stress. It also regulates processes important for growth, development, or tumorigenesis. Here, we studied the HSF1 influence on the phenotype of non-tumorigenic human mammary epithelial (MCF10A and MCF12A) and several triple-negative breast cancer cell lines. MCF10A and MCF...
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Skin cancer, which includes melanoma and non-melanoma cancer types (basal cell and squamous cell carcinomas), is the most common type of neoplasia worldwide with massive calls for exploring chemoprevention strategies. Research suggests that chronic inflammation is a critical component of cancer progression in which over expression of COX-2 has been...
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Eight rifamycin-related polyketides were isolated from the culture broth of a marine-derived bacterium Salinispora arenicola, including five known (2–5 and 8) and three new derivatives (1, 6, and 7). The structures of the new compounds were determined by means of spectroscopic methods (HRESIMS and 1D, 2D NMR) and a comparison of their experimental...
Preprint
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The BRG/Brahma-associated factors (BAF or mSWI/SNF) family of chromatin remodeling complexes are critical regulators of gene expression and are major determinants of cancer and other diseases. Two paralog ATPases, SMARCA4 and SMARCA2 (BRG1 and BRM, respectively), provide the enzymatic activity required for chromatin remodeling. Here, we discover an...
Preprint
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Antimicrobial peptides (AMPs) are small, naturally occurring molecules that play a vital role in the innate immune systems of various organisms, ranging from bacteria to humans. Additionally, artificial AMPs are also designed and synthesized based on the common structure-activity relationships (SARs) found in natural ones. As part of our ongoing ef...
Preprint
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Chemo-immunotherapy combinations have been regarded as one of the most practical ways to improve immunotherapy response in cancer patients. In this study, we integrated the transcriptomics data from immunotherapy-treated tumors and compound-treated cell lines to systematically identify chemo-immunotherapy synergisms and their underlying mechanisms....
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Background One of the most popular anti-inflammatory and anti-leukemic medications is 6-mercaptopurine, along with its riboside derivatives. Because of their potent adverse effects and limited biological half-life, they are rarely used. These problems might be solved by a novel medication delivery technique based on gold nanoparticles (AuNPs). In p...
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Motivation Backsplicing of RNA results in circularized rather than linear transcripts, known as circular RNA (circRNA). A recently discovered and poorly understood subset of circRNAs that are composed of multiple genes, termed fusion-derived circular RNAs (fcircRNAs), represent a class of potential biomarkers shown to have oncogenic potential. Dete...
Preprint
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Breast cancer is the most common malignancy in women worldwide and the leading cause of cancer-related mortality in women Breast cancer aggressiveness can be regulated by miRNAs, which are encoded in the genome as pre-miRNAs. One pre-miRNA can give rise to several functionally distinct mature miRNA species. miR-1307-3p has been described to promote...
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This study aimed to investigate the cytotoxic and apoptotic effects of Ganoderma lucidum, Pleurotus ostreatus, Pleurotus eryngii, and Inonotus hispidus fungal extracts on HT-29 and HCT-116 colorectal cancer cell lines and to search the DNA damage and oxidative stress caused by these extracts. Accordingly, mushroom extracts were applied to colorecta...
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A green and low-cost approach was run to synthesize zinc nanoparticles (NPs) using rosemary extract. The NPs were identified by various methods, i.e., ultraviolet-visible and Fourier transform infrared spectroscopy, FE-scanning electron microscope imaging, X-ray diffraction, and energy-dispersive X-ray analysis. The radical scavenging activity and...
Preprint
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Uncontrolled cell proliferation is the key feature of tumours. Because experimental measures provide only a partial view to the underlying proliferative processes, such as cell cycling, cell quiescence and cell death, mathematical modelling aims to provide a unifying view of the data with a quantitative description of the contributing basic process...
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The ketone bodies, sodium and lithium salts of acetoacetate (AcAc) and sodium 3-hydroxybutyrate (3-HB; commonly called beta-hydroxybutyrate) have been found to inhibit the proliferation of cancer cells. Previous studies have suggested that lithium itself may be an inhibiting agent but may be additive or synergistic with the effect of AcAc. We previ...
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The synthesis, anticancer, and antioxidant activities of a series of indole-derived hybrid chalcones are reported here. First, using the well-known Claisen–Schmidt condensation method, a set of 29 chalcones has been designed, synthesized, and consequently characterized. Subsequently, screening for the antiproliferative activity of the synthesized h...
Preprint
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High-throughput drug screens are a powerful tool for cancer drug development. However, the results of such screens are often made available only as raw data, which is intractable for researchers without informatic skills, or as highly processed summary statistics, which can lack essential information for translating screening results into clinicall...
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The emergence of multidrug-resistant bacteria has severely increased the burden on the global health system, and such pathogenic infections are considered a great threat to human well-being. Antimicrobial peptides, due to their potent antimicrobial activity and low possibility of inducing resistance, are increasingly attracting great interest. Here...
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We describe herein the synthesis of eight new ester-coupled hybrid compounds from thymoquinone and protoflavone building blocks, and their bioactivity testing against multiple cancer cell lines. Among the hybrids, compound 14 showed promising activities in all cell lines studied. The highest activities were recorded against breast cancer cell lines...
Article
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With the increasing global burden of diabetes mellitus type 2, the search for the new drugs, with better pharmacological profile is continued. As a part of this surge, the synthesis, pharmacological in vitro and computational evaluation of five, simple carbamate derivatives, against carbohydrate digestive enzyme a-glucosidase, is disclosed herein....
Preprint
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Sufficient numbers of activated replication origins are essential for successful DNA replication. While normal cells load replication origins in abundance to the genome, cancer cells often load fewer origins of replication due to genomic alterations such as CCNE1 amplifications. Here we exploit this feature to sensitize cancer cells to ATR inhibiti...
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Background Enzalutamide, a next-generation antiandrogen agent, is approved for the treatment of metastatic castration-resistant prostate cancer (CRPC). While enzalutamide has been shown to improve time to progression and extend overall survival in men with CRPC, the majority of patients ultimately develop resistance to treatment. Immunotherapy appr...
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Metastatic (as well as tumor) microenvironments contain both cancer‐promoting and cancer‐restraining factors. The balance between these opposing forces determines the fate of cancer cells that disseminate to secondary organ sites. In search for microenvironmental drivers or inhibitors of metastasis, we identified, in a previous study, the beta subu...
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Background: 5-Fluorouracil (5-FU) is a widely used chemotherapeutic drug in clinical cancer treatment, including hepatocellular carcinoma (HCC). A correct understanding of the mechanisms leading to a low or lack of sensitivity of HCC to 5-FU-based treatment is a key element in the current personalized medical treatment. Methods: Weighted gene co-ex...
Article
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Four diastereomers of 16-azidomethyl substituted 3-O-benzyl estradiol (1–4) and their two estrone analogs (16AABE and 16BABE) were tested for their antiproliferative properties against human gynecological cancer cell lines. The estrones were selected for additional experiments based on their outstanding cell growth-inhibiting activities. Both compo...
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Among different neoplastic lesions, hepatocellular carcinoma plays a pivotal role due to the extreme difficulty of treating it in advanced conditions. Research shows that there is a high intractability towards chemotherapy for this disease. Therefore, using medicinal plants can be another approach to fend off this grim scenario and pave a new way t...
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TP53 is the most frequently mutated gene in human cancers. Most TP53 genomic alterations are missense mutations, which cause a loss of its tumour suppressor functions while providing mutant p53 (mut_p53) with oncogenic features (gain-of-function). Loss of p53 tumour suppressor functions alters the transcription of both protein-coding and non-protei...
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SVIL is a member of the villin/gelsolin superfamily and is responsible for encoding supervillin. It has been reported to be closely related to the occurrence and development of various tumors. However, the mechanism of SVIL in bladder cancer has not been reported yet. In this research, we evaluated the relationship between SVIL expression and bladd...
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An altered expression of miR-143-3p has been previously reported in prostate cancer where it is purported to play a tumor suppressor role. Evidence from other cancers suggests miR-143-3p acts as an inhibitor of epithelial-to-mesenchymal transition (EMT), a key biological process required for metastasis. However, in prostate cancer the interaction b...
Preprint
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Background: Myocardial infarction (MI) and heart failure (HF) are associated with an increased incidence of cancer. The mechanism is complex and unclear. Here, we aimed to test our hypothesis that cardiac small extracellular vesicles (sEVs), particularly cardiac mesenchymal stromal cells-derived sEVs (cMSC-sEVs), contribute to the link between post...
Article
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Two series of pyrazolo[3,4-b]pyridine derivatives, 9a–h and 14a–h, are synthesized and evaluated for their anti-cancer potency towards Hela, MCF7, and HCT-116 cancer cell lines. Compound 9a showed the highest anticancer activity with IC50 = 2.59 µM against Hela when compared with doxorubicin (IC50 = 2.35 µM). Compound 14g revealed cytotoxicity IC50...
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According to World Health Organisation data, cancer is one of the most influential diseases that goes head to head with heart diseases in the ranking of causes of death, causing approximately 10 million deaths annually and accounting for 20% of all deaths. Lung cancer is a leading cause of cancer-related deaths globally for both men and women. In s...