• 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 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)
  • 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)
  • 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)
  • Tetrazolium reduction and resazurin assays are the mainstay of routine in vitro toxicity batteries. (cdc.gov)
  • 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)
  • Tulp, M. and Bohlin, L. (2002) Functional versus Chemical Diversity: Is Biodiversity Important for Drug Discovery? (scirp.org)
  • 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)
  • 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)
  • 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)
  • Though chemotherapy drugs show initial positive response, tumor acquires resistance gradually and patients experience continued tumor growth and metastatic disease. (springernature.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)
  • Previously, Kinases are known to play important role in regulating several phenotypes of carcinogenesis including growth, proliferation, angiogenesis, metastasis and evasion of antitumor immune responses [5]. (springernature.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)
  • Tests that demonstrate the relative effectiveness of chemotherapeutic agents against specific parasites. (nih.gov)
  • Any tests that demonstrate the relative efficacy of different chemotherapeutic agents against specific microorganisms (i.e., bacteria, fungi, viruses). (bvsalud.org)
  • 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)
  • The concept has now been extended to embrace synthetic lethal drug sensitivity, such as that observed with PARP inhibitors in combination with DNA-damaging chemotherapy in a variety of BRCA defective tumors 10 . (nature.com)
  • In the end, to have a potential therapeutic approach, we looked for an efficient inhibitor against the target kinase in the international union of basic and clinical pharmacology (IUPHAR) database, where a screen of 72 inhibitors against 456 human kinases binding activity is provided. (springernature.com)
  • Some Mek inhibitors showed promising antitumor activity, although schedules and doses associated with low systemic toxicity need to be defined. (biomedcentral.com)
  • Finally, several clinical trials are currently ongoing using MEK inhibitors in combination with chemotherapeutic drugs (including dacarbazine or paclitaxel). (biomedcentral.com)
  • Drug repositioning and pharmacophore identification in the discovery of hookworm MIF inhibitors. (jscimedcentral.com)
  • Phytochemical screening test revealed the presence of terpenoid, flavonoid, tannin, saponin and phenolic compound in all the stem bark extracts of C. odontophyllum. (scirp.org)
  • MINK1 drives 5FU resistance via AKT/MDM2/p53 axis : Reveals a high throughput kinome knockout screening in OSCC. (springernature.com)
  • Here using high-throughput screening, we identified MINK1 as a driver of 5FU resistance through AKT/MDM2/p53 axis. (springernature.com)
  • Reprogramming resistant cells to undergo drug induced cell death is a feasible approach to overcome drug resistance. (springernature.com)
  • To understand the role of potential kinase signaling in 5FU resistance in OSCC, a CRISPR based kinome-wide high throughput screening was performed using a lentiviral sgRNA library knocking out 840 kinases individually with a total number of 3214 sgRNA constructs, followed by treatment with a sub lethal dose of 5FU for 48h after which cell death was measured in high content analyzer using a fluorescent cell viability dye. (springernature.com)
  • Chemotherapeutic drugs result in not only strong resistance but also more side effects [ 4 ]. (hindawi.com)
  • 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)
  • Their current application in oncology has revolutionized cancer treatment by improving the antitumor activity of several chemotherapeutic agents. (mdpi.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)
  • Both ikarugamycin and astemizole improved the anticancer activity of the immunogenic chemotherapeutic agent oxaliplatin in a T cell-dependent fashion. (bmj.com)
  • 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)
  • 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)
  • 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)
  • Antineoplastons are drugs composed of chemical compounds that are naturally present in the urine and blood . (cancer.gov)
  • 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)
  • The chemotherapeutic regimen used for OSCC are cisplatin, 5FU and Docetaxel (TPF)(3). (springernature.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)
  • 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)
  • 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)
  • The identification, optimization and synthesis of antineoplastic drugs from PnV molecules may lead to a new multitarget chemotherapy. (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)
  • MDR is a phenomenon by which tumor cells become resistant to several unrelated drugs. (up.pt)
  • Further more, one of the most recent approaches in drug discovery from microorganisms is cocultivation. (microbialtec.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)
  • 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)
  • 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)
  • 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)
  • 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)
  • This can be achieved by identifying the causative factors for acquired chemoresistance and discovering novel agents to target critical causative factors, which will restore drug-induced cell death in chemoresistant OSCC. (springernature.com)
  • To confirm the finding from the kinome screening, cell viability and cell death assays were performed which suggest that knocking out MINK1 (MINK1 KO) significantly resenitized chemoresistant cells to 5FU (Fig. 2A&B). (springernature.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)
  • FDA-approved drugs were screened for their ability to sensitize TRAIL resistant prostate cancer cells to TRAIL using an MTT assay for cell viability. (biomedcentral.com)
  • Drugs demonstrating the highest synergy were selected as leads and tested in different prostate and pancreatic cancer cell lines, and one immortalized human pancreatic epithelial cell line. (biomedcentral.com)
  • 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)
  • 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)
  • However, the drug targets and the detailed mechanisms have been masked. (hindawi.com)
  • Billingsley ML. Druggable targets and targeted drugs: enhancing the development of new therapeutics. (jscimedcentral.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)
  • 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)
  • In the current work, we screened a small library of fifty-five FDA and foreign-approved anti-neoplastic drugs in order to identify candidates that sensitized resistant prostate and pancreatic cancer cells to TRAIL-induced apoptosis. (biomedcentral.com)
  • Sequential and simultaneous dosing modalities were investigated and the annexin V/propidium iodide assay, in concert with fluorescence microscopy, was employed to visualize cells undergoing apoptosis. (biomedcentral.com)
  • Colon cancer is now often detected during screening procedures. (medscape.com)
  • 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)
  • 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)
  • To date, many different chemotherapeutic agents have been widely used as common treatments for oral cancers. (oncotarget.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)
  • 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)
  • 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)
  • 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)
  • Studies in progress are selecting the venom molecules with antitumor and immunomodulatory effects and trying to better understand their mechanisms. (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 identification of a number of FDA-approved drugs as TRAIL sensitizers can expand chemotherapeutic options for combination treatments in prostate and pancreatic cancer diseases. (biomedcentral.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)
  • Molecules from animal venoms are promising candidates for the development of new drugs. (nature.com)
  • The plant can be used as promising candidate for anti-neoplasic drug development. (emanresearch.org)
  • 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)
  • 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)
  • 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)
  • 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)
  • 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)
  • Importantly, manipulation of the recycling pathway influenced the response of drug-sensitive cells to doxorubicin treatment. (up.pt)
  • 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)
  • Antineoplastons are not approved by the U.S. Food and Drug Administration for the prevention or treatment of any disease. (cancer.gov)
  • Chemotherapeutic drugs target cancer-specific characteristics, such as alterations in DNA repair, which has complicated roles in oncogenesis and tumor progression. (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)
  • Targeted drug therapy is advantageous because it deposits the drug at the specific location where it can be most useful in treating the disease. (wikipedia.org)
  • Mechanism-based target identification and drug discovery in cancer research. (jscimedcentral.com)
  • 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)
  • 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)
  • 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)
  • Hexane extract of the stem bark and ethanolic leaves extract profoundly inhibited the sprouting of microvessels (by 89.56% and 87.12% respectively) in rat aortic ring assay. (emanresearch.org)
  • Hence, blood biomarker detection has become an efficient screening tool for the early diagnosis of OSCC. (techscience.com)
  • Finally, the antitumor effect of the leaves ethanolic extract was evaluated using in vivo human tumor xenograft model. (emanresearch.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)
  • Microbial metabolites are among the most important of the cancer chemotherapeutic agents. (microbialtec.com)
  • Folate targeting is a method utilized in biotechnology for drug delivery purposes. (wikipedia.org)
  • Li X, Taratula O, Taratula O, Schumann C, Minko T. LHRH-Targeted Drug Delivery Systems for Cancer Therapy. (jscimedcentral.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)
  • and many others - see Advanced Drug Delivery Systems of Curcumin for Cancer Chemoprevention for a good overview. (blogspot.com)
  • Norwati, D., Harmy, M.Y., Mohd Noor, N. and Amry, A.R. (2014) Colorectal Cancer Screening Practices of Primary Care Providers: Results of a National Survey in Malaysia. (scirp.org)
  • Our results showed that MDR cells released more EVs than their drug-sensitive counterparts and also that the drug-sensitive cells captured more EVs than their MDR counterparts. (up.pt)