• The search for targeted drugs for cancer treatment includes consideration of natural products, which may provide new opportunities for antitumor cytotoxicity as single agents or in combination therapy. (cancer.gov)
  • Based on this method, we performed cytotoxicity assays on 42 AsPCs grown both as monolayers and spheroids. (biomedcentral.com)
  • The ability of lovastatin, mevastatin and simvastatin to inhibit the melanoma cell proliferation was examined using cytotoxicity and apoptosis assays. (biomedcentral.com)
  • The current investigation aimed to demonstrate how interpretation of results from several standard cytotoxicity and proliferation assays vary in dependence on contributions from the pentose phosphate pathway (PPP). (cdc.gov)
  • Non-tumorigenic Beas-2B cells were treated with graded concentrations of benzo[a]pyrene (B[a]P) for 24 and 48h prior to cytotoxicity and proliferation assessment with commonly used MTT, MTS, WST1, and Alamar Blue assays. (cdc.gov)
  • The ethanolic extracts of the plant were examined for the presence of bioactive components and their total flavonoid content, with focusing on quercetin detection using thin layer bioautography (TLB) and brine shrimp lethality assay (BSLA) for cytotoxicity. (who.int)
  • Alternatively, miR-21 aggravates cyst development by suppressing cyst epithelial apoptosis (15). (baxkyardgardener.com)
  • Role of PDL-1 in NSCLC chemoresistance was assessed using CRISPR/Cas9 knockdown and various functional assays including MTT, cell invasion, sphere formation, and cell apoptosis. (cdc.gov)
  • Decreased intracellular drug concentration, enhanced function of cell processing active products, enhanced repair ability of cellular DNA damage, and blockage of related apoptosis pathways play an important role in it. (eurekaselect.com)
  • A recent in vitro screening of the Phoneutria nigriventer spider venom (PnV) antitumor effects by our group has shown that the venom significantly affected glioblastoma cell lines. (nature.com)
  • Scientific Methods: In vitro growth inhibition assays were completed with AHCC alone and in combination with PLD in panel of human cancer cell lines and findings confirmed in vivo in an ovarian cancer xenograft mouse model. (researchgate.net)
  • Major Findings: The in vitro growth inhibition assays demonstrated additive activity when AHCC is co-administered with PLD. (researchgate.net)
  • Integration of a machine learning-derived signature of response with in vitro assessment of LP-184 efficacy facilitated the derivation of manageable yet robust biomarkers which can be used to predict drug sensitivity with high accuracy and clinical value. (biomedcentral.com)
  • We examined the effects of statin drugs on in vitro proliferation, migration and invasion of melanoma cells. (biomedcentral.com)
  • On the other hand, removing Compact disc8+ T cells from an ADPKD mouse model or excluding stroma from in vitro PKD organoid ethnicities aggravates cyst development (9, 10). (baxkyardgardener.com)
  • Tetrazolium reduction and resazurin assays are the mainstay of routine in vitro toxicity batteries. (cdc.gov)
  • The identification, optimization and synthesis of antineoplastic drugs from PnV molecules may lead to a new multitarget chemotherapy. (nature.com)
  • To date, the multidrug resistant features of stem cells have been characterized only in vertebrates, where there is a critical need to understand how cancer stem cells thwart chemotherapy drugs. (marksteinlab.org)
  • The major concern of chemotherapy is the side effects of existing drugs ( Baldo and Pham, 2013 ). (japsonline.com)
  • Our finding supports PDL-1 in CAFs as a chemotherapy response biomarker and as a drug delivery and therapeutic target for chemoresistant NSCLC. (cdc.gov)
  • Although chemotherapy is accepted as standard treatment, large scale of patients suffers from the severe side effects, and drug resistance is commonly observed after long-term treatment. (jcancer.org)
  • Chemotherapy with platinum drugs such as cisplatin, carboplatin, oxaliplatin, or a combination thereof is used to treat a variety of tumors. (eurekaselect.com)
  • However, the results of gliomas chemotherapy are unsatisfactory, and resistance to platinum drugs is one of the important reasons. (eurekaselect.com)
  • Triticum aestivum L. root growth inhibition test and Allium cepa L. assay were used to assess the cytotoxic potential of phosphonates. (japsonline.com)
  • The differentiation of naive CD8 T cells into effector cytotoxic T lymphocytes upon antigen stimulation is necessary for successful antiviral, and antitumor immune responses. (marksteinlab.org)
  • The active compound curcumin is believed to have a wide range of biological effects including anti-inflammatory, antioxidant, antitumor, antibacterial, and antiviral activities, which have shown a lot of potential for use in clinical medicine. (blogspot.com)
  • Wnt/β-catenin signaling is a branch of a functional network that is involved in a broad range of biological systems including stem cells, embryonic development and adult organs. (chemdiv.com)
  • A growing body of evidence points to the importance of the functional diversity of immune and structural cells during tumor development. (biomedcentral.com)
  • These interactions begin during the early stages of embryonic development and coordinate events such as cell proliferation and differentiation in complex tissues, crucial processes for the functional maintenance of whole organs [ 10 ]. (biomedcentral.com)
  • We have developed a 3D (spheroid) functional assay to assess the sensitivity of two PARPis (niraparib and olaparib) in ascites-derived primary cell cultures (AsPCs) from HGSOC patients. (biomedcentral.com)
  • Global gene expression comparison of 6 PARPi-resistant and 6 PARPi-sensitive 3D AsPCs was indicative for the predominant downregulation of numerous genes and networks with previously demonstrated roles in EOC chemoresistance, suggesting that the PARPis-sensitive AsPCs could display enhanced sensitivity to other chemotherapeutic drugs, commonly applied in cancer management. (biomedcentral.com)
  • Consistently, inactivating mutations ENOblock (AP-III-a4) in various NER genes cause the autosomal recessive syndrome xeroderma pigmentosum (XP), which is Nos1 usually associated with UV sensitivity and susceptibility to skin cancer development (4). (colinsbraincancer.com)
  • miRNAs and lncRNAs control drug sensitivity and the development of tumor resistance towards platinum drugs. (eurekaselect.com)
  • This mini-review summarizes the resistance mechanisms of gliomas to platinum drugs, as well as molecules and therapies that can improve the sensitivity of gliomas to platinum drugs. (eurekaselect.com)
  • For example, kinases that regulate response to fibroblast growth factor receptor (FGFR) inhibitor have been found in gastric cancer [ 11 ], and the Wnt-FZD5 signaling pathway that regulates drug sensitivity has been identified in RNF43-mutant pancreatic tumors [ 12 ]. (ijbs.com)
  • Cell proliferation, migration, and invasion were measured with cell counting kit-8 (CCK-8), wound healing, and transwell assays. (jcancer.org)
  • Emerging evidence suggests that they provide a cellular mechanism for induction and emergence of drug resistance and contribute to increased invasive and metastatic potential. (frontiersin.org)
  • Using a novel in vivo efflux assay and multiple drug challenges, we show that stem cells in the fly intestine depend on two ABC transporters-one constitutively expressed and the other induced-for efflux and multidrug resistance. (marksteinlab.org)
  • Among the many regulatory factors, overexpression of pro-survival Bcl-2 family members may promote resistance to chemotherapeutic drugs in many tumors. (oncotarget.com)
  • Chemotherapeutic drugs result in not only strong resistance but also more side effects [ 4 ]. (hindawi.com)
  • The resistance of gliomas to platinum drugs is the result of a combination of influencing factors. (eurekaselect.com)
  • Sorafenib is the standard first-line drug for the treatment of advanced hepatocellular carcinoma (HCC), however, its therapeutic efficacy is not satisfactory due to primary or secondary resistance of HCC cells. (ijbs.com)
  • In the present study, we identified Metaxin 1 (MTX1) as a new regulator of sorafenib resistance in HCC through genome-scale CRISPR activation (CRISPRa) screening. (ijbs.com)
  • Nevertheless, the clinical efficacy of sorafenib is frequently limited by drug resistance in a considerable number of HCC patients [ 5 , 6 ]. (ijbs.com)
  • In the present work, in order to identify genes which are essential to sorafenib resistance in HCC, we conducted CRISPR-Pool™ SAM human library comprising 70,290 SAM-sgRNAs upon HCC cells to amplify genes for screening purposes. (ijbs.com)
  • Our researchers are now extracting bacterial DNA from soil and marine habitats, cloning large fragments into, for example, bacterial artificial chromosomes, expressing in a host bacterium and screening the library for new compounds. (microbialtec.com)
  • assists in identifying natural products and synthetic compounds that may serve as bioprobes for chemical genetics, proteomics, target validation and potential lead compounds for clinical development. (cancer.gov)
  • Compounds of interest include not only classical "drug-like" organic small molecules, but also peptides, proteins, and other bioactive chemical classes. (cancer.gov)
  • This library represents a selection of drug-like compounds aimed at modulating protein-protein interaction (PPI) of β-catenin with different proteins involved in significant physiological processes. (chemdiv.com)
  • The discovery of vitamin-mediated drug targeting in plants led to the hypothesis that folate-targeted therapies could be of clinical use. (wikipedia.org)
  • The Part 2 post in this series is concerned with mainline anti-cancer drug interventions that simultaneously address multiple growth pathways, ones that are entering clinical practice. (anti-agingfirewalls.com)
  • Application of machine learning in early phases of preclinical development is likely to allow a better positioning and ultimate clinical success of molecules. (biomedcentral.com)
  • Therapies tailored to specific genetic lesions and diagnostic tests that assay for their respective molecular targets are now an established part of clinical practice across various tumour types, including chronic myeloid leukaemia 1 , gastrointestinal stromal tumours and epithelial tumours, such as breast and colon cancer 2 . (ersjournals.com)
  • The application of this assay and the potential biomarkers with possible predictive significance to PARPis therapy of EOC patients now need testing in the setting of a clinical trial. (biomedcentral.com)
  • Epidemiological and clinical studies have suggested that cancer could be prevented or significantly reduced by treatment with anti-oxidant and anti-inflammatory drugs, therefore, curcumin, a principal component of turmeric (a curry spice) showing strong anti-oxidant and anti-inflammatory activities, might be a potential candidate for the prevention and/or treatment of cancer and other chronic diseases. (blogspot.com)
  • Platinum drugs are a class of chemotherapeutic drugs that affect the cell cycle, and the main site of action is the DNA of cells, which are common chemotherapeutic drugs in clinical practice. (eurekaselect.com)
  • Finally, several clinical trials are currently ongoing using MEK inhibitors in combination with chemotherapeutic drugs (including dacarbazine or paclitaxel). (biomedcentral.com)
  • Both ikarugamycin and astemizole improved the anticancer activity of the immunogenic chemotherapeutic agent oxaliplatin in a T cell-dependent fashion. (bmj.com)
  • 20423 bioactive compound berberine was determined by MTT assay, and the oxidative stress was determined by lipid peroxidation method along with assessment of changes in the enzymatic and non enzymatic antioxidant status. (pdfplayer.org)
  • Finally, the efficacy of certain potential drugs was predicted using the pRRophetic algorithm, and the results in the high- and low-risk groups were compared. (hindawi.com)
  • While some drugs and radioimaging agents are delivered to cells as folate conjugates in a one-to-one folate-to-conjugate ratio, folate-targeted liposomes allow for the delivery of larger amounts of chemotherapeutic agents. (wikipedia.org)
  • Microtubule binding drugs are of special interest as they have important roles in the modulation of cellular functions and many of them act as anticancer agents. (rgcb.res.in)
  • Their current application in oncology has revolutionized cancer treatment by improving the antitumor activity of several chemotherapeutic agents. (mdpi.com)
  • Microbial metabolites are among the most important of the cancer chemotherapeutic agents. (microbialtec.com)
  • To date, many different chemotherapeutic agents have been widely used as common treatments for oral cancers. (oncotarget.com)
  • On the basis of this information, we established a screening system using N18-RE-105 cells to identify therapeutic agents that can protect cells from glutamate toxicity. (researchgate.net)
  • Abstract Circulating tumor cells (CTCs) are essential biomarkers for liquid biopsies, which are important in the early screening, prognosis, and real-time monitoring of cancer. (techscience.com)
  • Different OSCC-related biomarkers have been reported in circulation in the peripheral blood that support the occurrence and development of OSCC. (techscience.com)
  • Based on the natural high affinity of folate for the folate receptor protein (FR), which is commonly expressed on the surface of many human cancers, folate-drug conjugates also bind tightly to the FR and trigger cellular uptake via endocytosis. (wikipedia.org)
  • Molecules from animal venoms are promising candidates for the development of new drugs. (nature.com)
  • Studies in progress are selecting the venom molecules with antitumor and immunomodulatory effects and trying to better understand their mechanisms. (nature.com)
  • Therefore, there is substantial interest in developing chemotherapeutic drugs that directly target pro-survival Bcl-2 proteins by mimicking the BH3 domain and unleashing pro-apoptotic molecules in tumor cells. (oncotarget.com)
  • Cisplatin showed concentration-dependent antitumor effects due to loss of cell adhesion and spheroid disruption in each cell line, while cetuximab exhibited antitumor effects that correlated with EGFR expression in each cell line. (medsci.org)
  • 50 years of preclinical anticancer drug screening:empirical to target-driven approaches. (jscimedcentral.com)
  • The contribution of synthetic organic chemistry to anticancer drug development. (jscimedcentral.com)
  • His achievements in understanding the role of physiochemical properties in drug activity, more precisely in the disposition of medicines ought to be particularly recognised. (efmc.info)
  • Unfortunately, some targets with potent oncogenic activity fall into this category, and currently little is known about how to solve this problem, which largely hampered drug research on human cancers. (techscience.com)
  • Some Mek inhibitors showed promising antitumor activity, although schedules and doses associated with low systemic toxicity need to be defined. (biomedcentral.com)
  • The statins are group of drugs routinely used in the treatment of lipid disorders, including hypercholesterolemia. (biomedcentral.com)
  • There is considerable effort dedicated to finding a way to make curcumin/turmeric more bioavailable, including lipid delivery systems, self-microemulsifying drug delivery system (SMEDDS) , nanoparticulate delivery systems. (blogspot.com)
  • The Molecular Targets Program (MTP) provides the focus and infrastructure that enables CCR investigators to pursue molecularly targeted drug discovery research by promoting an interdisciplinary, collaborative, team-oriented approach to identifying and validating potential cancer-pertinent targets. (cancer.gov)
  • Library has been assembled using in house structural biology insight, molecular stimulation-modeling, virtual screening of ChemDiv's novel chemistries and medicinal chemistry filtering/ranking of the resulting hits. (chemdiv.com)
  • Guidebook on molecular modeling in drug design: Academic Press. (jscimedcentral.com)
  • Ooms F. Molecular modeling and computer aided drug design. (jscimedcentral.com)
  • In this sense, the lack of technologies that would allow for molecular screening of individual stromal cell types poses a major challenge for the development of therapies targeting the tumor microenvironment. (biomedcentral.com)
  • From a mechanistic perspective, the FR functions to concentrate exogenous ligands (e.g. folates and folate-drug conjugates) into the cell cytosol by endocytosis. (wikipedia.org)
  • In order to confirm the effect of the extract on motility of human endothelial cells, cell migration assay was conducted. (emanresearch.org)
  • Open data on the gene expression of the NCI-60 cell lines, provides a unique opportunity to add another dimension to the preclinical development of such drugs by interrogating correlations with gene expression patterns. (biomedcentral.com)
  • Method For immunopharmacological screening campaigns, we built an artificial miniature immune system in which dendritic cells (DCs) derived from immature precursors present MHC (major histocompatibility complex) class I-restricted antigen to a T-cell hybridoma that then secretes interleukin-2 (IL-2). (bmj.com)
  • N- trans -Feruloyloctopamine (FO), a natural compound, was reported in our previous study to inhibit a tumor cell malignant phenotype by AKT- and EMT-related signals and might be used as a promising drug for HCC treatment. (hindawi.com)
  • Additional screens for MMTV provirus entry sites in tumors revealed several other upregulated genes that are associated with other gene development pathways such as INT2, INT3, and INT4 [4,5,6]. (chemdiv.com)
  • Therefore, there have been recent attempts to develop effective anticancer strategies targeting apoptotic signaling pathways [ 2 ], such as through inhibiting anti-apoptotic survival factors, which are likely overexpressed in many tumors and may confer drug-resistant phenotypes [ 2 , 3 ]. (oncotarget.com)
  • Results The screening of three drug libraries relevant to known signaling pathways, FDA (Food and Drug Administration)-approved drugs and neuroendocrine factors yielded two major hits, astemizole and ikarugamycin. (bmj.com)
  • The genome-wide screening is an effective and unbiased approach to determine genes or pathways involved in biological processes [ 10 ]. (ijbs.com)
  • One of the key oncogenic pathways involved in melanoma aggressiveness, development and progression is the RAS/BRAF/MEK pathway, whose alterations are found in most patients. (biomedcentral.com)
  • Jacob et al [ 9 ] examined the association between use of cholesterol-lowering drugs and colorectal cancer incidence among 132,136 men and women in the Cancer Prevention Study II Nutrition Cohort. (biomedcentral.com)
  • Current or 5 year use of cholesterol-lowering drugs was not associated with colorectal cancer incidence. (biomedcentral.com)
  • Early detection through widely applied screening programs is the most important factor in the recent decline of colorectal cancer in developed countries (see Overview/Epidemiology ). (medscape.com)
  • This knowledge is slowly making its way into the clinic and being employed to better stratify individual risks of developing colorectal cancer, discover better screening methodologies, allow for better prognostication, and improve the ability to predict benefit from new anticancer therapies. (medscape.com)
  • In the present work, the effects of PnV on tumor development were established in vivo using a xenogeneic model. (nature.com)
  • Since in classic chemotherapies it is observed a decrease in immune response, methotrexate (MTX) was used only to compare the PnV effects on innate immune cells with a highly immunosuppressive antineoplastic drug. (nature.com)
  • Therefore, it would be relevant to establish the effects of PnV on tumor development in vivo , considering the complex neoplastic microenvironment. (nature.com)
  • To the best of our knowledge, this is the first demonstration of the antitumor effects of ABT-737 on human oral cancers. (oncotarget.com)
  • Conclusions These findings underscore the potential utility of this screening system for the identification of immunostimulatory drugs with anticancer effects. (bmj.com)
  • The harmful effects of chemicals and the side effects of chemical drugs on human health have a widely focused global attention on herbal drugs and medicinal plants. (researchgate.net)
  • The antitumor effects of radix Actinidia chinensis is that its root contains a large amount of terpenes, including ursolic acid, oleanolic acid and their derivatives [ 12 - 14 ]. (jcancer.org)
  • Drug repositioning and pharmacophore identification in the discovery of hookworm MIF inhibitors. (jscimedcentral.com)
  • We hypothesized that a high fat diet in non-human primates would induce changes in hepatic chromatin structure resulting in altered expression of fetal genes critical to the development of childhood and adult obesity. (nih.gov)
  • Screening with RNA-Seq in Huh7 cells treated with FO revealed that 317 genes were modulated, of which 188 genes were upregulated and 129 genes were downregulated. (hindawi.com)
  • Herein, genome-wide transcriptome profiling (RNA-Seq) was used to screen the differentially expressed genes (DEGs) in FO-treated Huh7 cells, with the aim of uncovering the pharmacologic pattern. (hindawi.com)
  • Finally, the antitumor effect of the leaves ethanolic extract was evaluated using in vivo human tumor xenograft model. (emanresearch.org)
  • LP-184 is a highly potent novel alkylating agent where the preclinical development is being guided by a dedicated machine learning-derived response signature. (biomedcentral.com)
  • The applica tion of new genetic tools also led to the discovery of an important familial neuroblastoma cancer gene, ALK , which is mutated in approximately 8% of sporadic tumors, and genome-wide association studies have unveiled loci with risk alleles for neuroblastoma development. (biomedcentral.com)
  • Billingsley ML. Druggable targets and targeted drugs: enhancing the development of new therapeutics. (jscimedcentral.com)
  • This lack of success may result in part from the fact that most studies focus on tumor cells as potential therapeutic targets and neglect the complex microenvironment that undergoes profound changes during tumor development. (biomedcentral.com)
  • Progress in microenvironment genetic studies represents a formidable opportunity for the development of new selective drugs because stromal cells have lower mutation rates than malignant cells, and should prove to be good targets for therapy. (biomedcentral.com)
  • However, the drug targets and the detailed mechanisms have been masked. (hindawi.com)
  • The venom was effective at impairing tumor development in murine xenogeneic model, activating the innate immune response and increasing tumor infiltrating macrophages. (nature.com)
  • The antitumor effect of ethanol extracted from radix of Actinidia chinensis (EERAC) were identified in human colon cancer cells, but the underlying mechanism remains unclear. (jcancer.org)
  • Colon cancer is now often detected during screening procedures. (medscape.com)
  • Unresponsiveness may result, at least in part, because these therapies only target cancer cells and neglect the complex microenvironment around tumors that undergo drastic changes during disease development [ 7 ]. (biomedcentral.com)
  • Further applications are possible in various areas of pharmacology, developments catalyzed by the use of simple enzyme assays for screening before testing in intact animals. (microbialtec.com)
  • Curcumin can be developed as a therapeutic drug through improvement in formulation properties or delivery systems, enabling its enhanced absorption and cellular uptake. (blogspot.com)
  • This review mainly focuses on the anti-inflammatory potential of curcumin and recent developments in dosage form and nanoparticulate delivery systems with the possibilities of therapeutic application of curcumin for the prevention and/or treatment of cancer. (blogspot.com)
  • Therefore, there is an urgent need for development of more effective therapies that may rely on molecularly targeted individualized treatments. (biomedcentral.com)
  • The recent successes in unraveling the genetic basis of neuroblastoma are now opening opportunities for development of targeted therapies. (biomedcentral.com)
  • Many developments were achieved, and new methodologies were developed, leading to advancements in phytotherapy. (interesjournals.org)
  • Amongst all the marine invertebrates, sponges represent the most described group with potential application in medicinal chemistry, representing a valid starting point for new drug leads due to their chemical defense mechanisms. (microbialtec.com)
  • Sawa M, Masai H. Drug design with Cdc7 kinase: a potential novel cancer therapy target. (jscimedcentral.com)
  • We observed intracellular reactive oxygen species(ROS) level by DCFH-DA method, mitochondrial membrane potential alteration by rhodamine 123 staining and apoptotic morphological changes by acridine orang/ethidium bromine dual staining method and Hoest staining assay and comet assay. (pdfplayer.org)
  • In the future, it may become possible to produce tumor spheroids from tissue samples of oral cancer patients, and then apply them to drug screening and to develop individualized diagnostic and treatment methods. (medsci.org)
  • Cancer research has been conducted using cultured cells as part of drug discovery testing, but conventional two-dimensional culture methods are unable to reflect the complex tumor microenvironment. (medsci.org)
  • Furthermore, an unfortunate association of factors such as tumor genetic complexity, overestimation of biomarker and drug potentials, as well as a poor understanding of tumor microenvironment in diagnosis and prognosis leads to the current levels of treatment failure regarding a vast majority of cancer types. (biomedcentral.com)
  • How this altered pericystic microenvironment affects cyst development is another query of significant curiosity. (baxkyardgardener.com)
  • Mechanism-based target identification and drug discovery in cancer research. (jscimedcentral.com)
  • Chemotherapeutic drugs target cancer-specific characteristics, such as alterations in DNA repair, which has complicated roles in oncogenesis and tumor progression. (biomedcentral.com)
  • Dr. Cochran's translational interests span protein-based drug discovery and development for applications in oncology and regenerative medicine, and the development of new technologies for high-throughput protein analysis and engineering. (stanford.edu)
  • While genetic deletion of miR-214 does not affect kidney development or homeostasis, surprisingly, its inhibition in expression and enhanced pericystic macrophage accumulation. (baxkyardgardener.com)
  • EFMC would like to remind his efforts, joint with Henk Timmerman and Han van de Waterbeemd, to launch the successful series of EFMC Short Course in Medicinal Chemistry in 2009 with a very successful course on "Improving Compound Quality: Physical Chemistry and DMPK Properties in Drug Discovery. (efmc.info)
  • The role of the medicinal chemist in drug discovery--then and now. (jscimedcentral.com)
  • Importantly, manipulation of the recycling pathway influenced the response of drug-sensitive cells to doxorubicin treatment. (up.pt)
  • EERAC might be a promising chemotherapeutic agent for CRC treatment. (jcancer.org)
  • Further more, one of the most recent approaches in drug discovery from microorganisms is cocultivation. (microbialtec.com)