• 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)
  • Though chemotherapy drugs show initial positive response, tumor acquires resistance gradually and patients experience continued tumor growth and metastatic disease. (springernature.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)
  • Chemotherapeutic drugs target cancer-specific characteristics, such as alterations in DNA repair, which has complicated roles in oncogenesis and tumor progression. (biomedcentral.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)
  • 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)
  • 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)
  • 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)
  • We studied the chemosensitivity of these two MCSP tumor xenografts to anticancer drugs in vivo. (ox.ac.uk)
  • Targeted cancer therapies are used to inhibit the growth, progression, and metastasis of the tumor by interfering with specific molecular targets and are currently the focus of anticancer drug development. (spandidos-publications.com)
  • Direct damage to cancer cell DNA occurs through high-LET (linear energy transfer) charged particles such as proton, boron, carbon or neon ions which have an antitumor effect which is independent of tumor oxygen supply because these particles act mostly via direct energy transfer usually causing double-stranded DNA breaks. (medicalmarijuana.com)
  • 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)
  • Drug repositioning and pharmacophore identification in the discovery of hookworm MIF inhibitors. (jscimedcentral.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)
  • The discovery process of Akt inhibitors has evolved from adenosine triphosphate (ATP)‑competitive agents to alternative approaches employing allosteric sites in order to overcome the high degree of structural similarity between Akt isoforms in the catalytic domain, and considerable structural analogy to the AGC kinase family. (spandidos-publications.com)
  • We explore the pipeline of Akt inhibitors and their preclinical and clinical examination status, presenting the potential clinical application of these agents as a monotherapy or in combination with ionizing radiation, other targeted therapies, or chemotherapy. (spandidos-publications.com)
  • 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)
  • 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)
  • Among the many regulatory factors, overexpression of pro-survival Bcl-2 family members may promote resistance to chemotherapeutic drugs in many tumors. (oncotarget.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)
  • OBJECTIVE: Synthesis and in-silico studies of 4-Phenyl thiazol-2-amine derivatives as anti-breast cancer agents and molecular docking was used to assess the compounds' capacity to bind ER-α protein target. (bvsalud.org)
  • RESULTS: Most of the synthesized compounds have shown dock scores ranging from -6.658 to - 8.911 kcal/mol, which is better than the standard drug tamoxifen (-6.821 kcal/mol). (bvsalud.org)
  • According to molecular docking, all compounds fit in the protein's active site and have the same hydrophobic pocket as the standard drug tamoxifen. (bvsalud.org)
  • Organophosphorus compounds represent significant importance as biologically active agents. (japsonline.com)
  • Antineoplastons are drugs composed of chemical compounds that are naturally present in the urine and blood . (cancer.gov)
  • 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)
  • These potent effects are driven by curcumin's ability to induce G2/M cell cycle arrest, induce autophagy, activate apoptosis, disrupt molecular signaling, inhibit invasion and metastasis, and increase the efficacy of current chemotherapeutics. (hindawi.com)
  • 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)
  • The present invention isa new solid phase method for the preparation of DAT to make this lead molecule as a new class of small molecules as a potent antimitotic agents for the control of cytoskeletal functions and cell proliferation. (rgcb.res.in)
  • 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)
  • This review summarizes the intracellular functions of Akt as a pivotal point of converging signaling pathways involved in cell growth, proliferation, apoptotis and neo‑angiogenesis, and focuses on the drug design strategies to develop potent anticancer agents targeting Akt. (spandidos-publications.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)
  • Tetrazolium reduction and resazurin assays are the mainstay of routine in vitro toxicity batteries. (cdc.gov)
  • Considering the side effects of this class of drugs for humans, therapeutic drug monitoring (TDM) becomes important. (bvsalud.org)
  • Overall, our study offers a novel conceptual framework for biomimetic NPs using a DoE strategy and consolidates the high therapeutic potential of leukosomes as a viable drug delivery system for anti-inflammatory and antineoplastic applications. (frontiersin.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)
  • 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)
  • 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)
  • 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)
  • 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)
  • Thiazole scaffolds are gaining popularity in drug discovery due to their broad range of biological activity. (bvsalud.org)
  • 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)
  • ACAT activity T was in an assay mixture, which tested two.5 mg ml BSA in buffer A and 20 M Ls Ure with beauveriolide I or III, and the microsomal fraction or the membrane fraction. (mirnamimics.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)
  • 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)
  • 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)
  • 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)
  • 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)
  • The results obtained indicate that the developed method proves to be successful in the effective separation of anticancer drugs. (bvsalud.org)
  • Anticancer drugs: Keeping one step ahead. (jscimedcentral.com)
  • Triticum aestivum L. root growth inhibition test and Allium cepa L. assay were used to assess the cytotoxic potential of phosphonates. (japsonline.com)
  • With greater control over where exogenous agents are delivered, diagnostic and treatment therapies are more effective and cause fewer side effects. (wikipedia.org)
  • Industrial Relevance: This study presents an example of the successful integration of a well- known herbal supplement, AHCC, with traditional western medicine cytotoxic agent, pegylated liposomal doxorubicin, for the treatment of recurrent ovarian cancer. (researchgate.net)
  • Importantly, each of these pathways is known to respond effectively to different therapeutic agents, thus personalized diagnosis equates to personalized treatment. (nih.gov)
  • Although, taxanes are among the most active agents, the absolute benefit of taxane-based treatment is modest (3-5%) and has to be balanced according to serious side-effects. (justia.com)
  • Antineoplastons are not approved by the U.S. Food and Drug Administration for the prevention or treatment of any disease. (cancer.gov)
  • Chemotherapeutic regimens for treatment of MCSP have not been established. (ox.ac.uk)
  • Arencibia JM, Pastor-Flores D, Bauer AF, Schulze JO and Biondi RM: AGC protein kinases: From structural mechanism of regulation to allosteric drug development for the treatment of human diseases. (spandidos-publications.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)
  • Billingsley ML. Druggable targets and targeted drugs: enhancing the development of new therapeutics. (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)
  • 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)
  • Mitsiades CS, Mitsiades N and Koutsilieris M: The Akt pathway: Molecular targets for anti-cancer drug development. (spandidos-publications.com)
  • Curr Cancer Drug Targets. (spandidos-publications.com)
  • For biomedical applications, we are combining rational design and combinatorial methods to create designer protein therapeutics and diagnostic agents. (stanford.edu)
  • 50 years of preclinical anticancer drug screening:empirical to target-driven approaches. (jscimedcentral.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)
  • 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)
  • There are varying dose recommendations for Kyprolis for multiple myeloma, depending on line of therapy and combination with other agents. (aetna.com)
  • There are varying dose recommendations for Kyprolis for Waldenstrom's macroglobulinemia, depending on line of therapy and combination with other agents. (aetna.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)
  • 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)
  • 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)
  • 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)
  • 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)
  • Antiangiogenic agents as second-line therapy for advanced non-small cell lung cancer. (jscimedcentral.com)
  • Aggarwal C, Somaiah N, Simon G. Antiangiogenic agents in the management of non-small cell lung cancer: where do we stand now and where are we headed? (jscimedcentral.com)
  • Much research has been devoted to overcoming hypoxia including the use of high pressure oxygen tanks, blood substitutes that carry increased oxygen, hypoxic cell radiosensitizer drugs such as misonidazole and metronidazole, and hypoxic cytotoxins (tissue poisons), such as tirapazamine. (medicalmarijuana.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)
  • 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)
  • 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)
  • 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)
  • In particular, the discovery of the new use of artemisinin derivatives as excellent anti-cancer drugs is also reviewed. (anti-agingfirewalls.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)
  • Sawa M, Masai H. Drug design with Cdc7 kinase: a potential novel cancer therapy target. (jscimedcentral.com)
  • To date, many different chemotherapeutic agents have been widely used as common treatments for oral cancers. (oncotarget.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)
  • 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)
  • Specifically, the use of leukocyte-derived membrane proteins to functionalize nanovesicles (leukosomes) can enable their long circulation and target the inflamed endothelium present in many inflammatory pathologies and tumors, making them a promising and versatile drug delivery system. (frontiersin.org)
  • 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)
  • 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)
  • Drugs of natural origin have been classified as (i) original natural products, (ii) products derived or chemically synthesized from natural products or (iii) synthetic products based on natural product structures. (microbialtec.com)
  • The contribution of synthetic organic chemistry to anticancer drug development. (jscimedcentral.com)
  • Mechanism-based target identification and drug discovery in cancer research. (jscimedcentral.com)
  • Further more, one of the most recent approaches in drug discovery from microorganisms is cocultivation. (microbialtec.com)
  • However, their therapeutic effects have been disappointing, and these agents may have unwanted side effects. (oncotarget.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)
  • 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)
  • The US Preventive Services Task Force (USPSTF) recommends against screening (with serum CA125 level or transvaginal ultrasonography) for ovarian cancer in the general population. (medscape.com)
  • Hence, blood biomarker detection has become an efficient screening tool for the early diagnosis of OSCC. (techscience.com)
  • In 2D culture, all cells can proliferate at a relatively constant rate in a planar space, and can be provided uniform access to nutrients, oxygen or drugs. (medsci.org)
  • These successful examples validate the concept of understanding the genetic profile of patients most likely to benefit from a targeted agent and preferentially selecting those patients for therapy. (ersjournals.com)