• 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 negative results for cytotoxic and antimicrobial assays indicated possible low cytotoxicity to the extract. (researchgate.net)
  • 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)
  • Figure 6: Antimitotic drugs induce different mitotic and interphase phenotypes. (nature.com)
  • When loaded with immune complexes (IC), consisting of tumor antigens bound to antitumor antibody, BMDC induce powerful antitumor immunity in mice. (stanford.edu)
  • We studied the chemosensitivity of these two MCSP tumor xenografts to anticancer drugs in vivo. (ox.ac.uk)
  • Secarna Pharmaceuticals, an IZB-based biopharmaceutical company focusing on the discovery and development of next-generation antisense oligonucleotide (ASO) therapies to address challenging or previously undruggable targets via its LNAplus™ platform, announced the publication of striking new preclinical data demonstrating that bimodal ASOs can enable efficacious long-term antitumor immunity in tumor models compared to current immune checkpoint inhibitors. (izb-online.de)
  • The combined downregulation of PD-L1 expression in a single-molecule approach resulted in exceptional antitumor activity in different tumor models. (izb-online.de)
  • Collectively, these data show that IM-T9P1 leads to long-lasting, adaptive antitumor immunity that can be further improved when combined with T cell-targeting immune checkpoint inhibitors and can have efficacy against large, established tumors in preclinical tumor models. (izb-online.de)
  • Treatment with IM-T9P1 resulted in the sustained activation of a specific type of tumor infiltrating cell, dendritic cells 3 (DC3s), which can promote antitumor immunity by supporting T cells with survival signals and enabling them to perform their effector functions. (izb-online.de)
  • 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)
  • Furthermore, the Genomics of Drug Sensitivity in Cancer database was used to explore the relationship between the risk model and anti-tumor drug sensitivity. (biomedcentral.com)
  • Though chemotherapy drugs show initial positive response, tumor acquires resistance gradually and patients experience continued tumor growth and metastatic disease. (springernature.com)
  • Increasing amounts of evidence indicate that autophagy is induced by a number of stressors in tumor cells, such as starvation, growth factor deprivation, hypoxia, damage stimulation and therapeutic drugs, and is an important survival mechanism in response to cellular stress ( 9 ). (spandidos-publications.com)
  • We investigate the cellular and molecular mechanisms involve in cellular transformation and tumor escape, with a special focus on pathways leading to resistance or relapse upon therapies and inhibition of anti-tumor immune responses. (hipi-lab-saint-louis.fr)
  • Osteosarcoma is a particularly chemotherapy-resistant tumor that only responds to high doses of chemotherapy and rapidly acquires resistance [ 11 - 12 ]. (ijbs.com)
  • These results demonstrate the importance of DCs in overcoming ICI resistance and achieving effective and durable antitumor responses and, in many cases, antitumor immunity. (izb-online.de)
  • We also examined the expression of multidrug resistance-related proteins such as p-glycoprotein (Pgp) and multidrug resistance-associated protein (MRP) by immunohistochemical analysis. (ox.ac.uk)
  • 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)
  • Although the RAS family of proteins was discovered nearly four decades ago there has not been a viable drug therapy developed to effectively blocks mutant RAS dysfunction. (cytoskeleton.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)
  • 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)
  • Cell viability assays, colony formation assays, wound healing assays, and Transwell assays demonstrated that ebastine elicited antitumor effects in osteosarcoma cells. (ijbs.com)
  • The objective of this review was to analyze the results from preclinical and clinical trials of these drugs for the treatment of cancer. (frontiersin.org)
  • Aslthough all these drugs have produced good results in preclinical studies of multiple cancers, the outcomes of clinical trials have not been similar. (frontiersin.org)
  • 50 years of preclinical anticancer drug screening:empirical to target-driven approaches. (jscimedcentral.com)
  • METHODS: A drug array was used to recognize compounds that can suppress the cisplatin-induced and radiation-induced PD-L1 expression in NSCLC via the flow cytometry-based assay. (bvsalud.org)
  • RESULTS: BRD4 inhibitors JQ1 and ARV-771 were identified as the most promising drugs both in the cisplatin and radiation screening projects in two NSCLC cell lines. (bvsalud.org)
  • With over 50 compounds in development and 40 disease areas being studied, diverse and unique career opportunities are available in areas from Small Molecule Drug Discovery to Nonclinical, and Translational Research. (bms.com)
  • Mechanism-based target identification and drug discovery in cancer research. (jscimedcentral.com)
  • Drug repositioning and pharmacophore identification in the discovery of hookworm MIF inhibitors. (jscimedcentral.com)
  • Organic chemistry in drug discovery. (jscimedcentral.com)
  • The role of the medicinal chemist in drug discovery--then and now. (jscimedcentral.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)
  • Recently, a drug that targets mutant RAS G12C specifically has shown promising clinical results and is now the first FDA approved RAS-targeting drug for the treatment of NSCLC, read on for a summary of this drugs journey from discovery to approval, and roadblocks that still lie ahead. (cytoskeleton.com)
  • S. K. Chakrabarti and B. Mukherjee, "Search for Anticancer Drug from Indian Medicinal Plants," Indian Journal of Medical Research, Vol. 56, No. 4, 1968, pp. 445-455. (scirp.org)
  • The contribution of synthetic organic chemistry to anticancer drug development. (jscimedcentral.com)
  • These include EpiScreen™, a T-cell epitope mapping technology that screens peptides for their immunostimulatory properties, and EpiScreen DC:T cell assay, which screens biologics for their immunogenicity. (genengnews.com)
  • We applied our workflow to quantify cell-cycle effects of three antimitotic cancer drugs over 8 d in HT-1080 fibrosarcoma xenografts in living mice using a data set of 38,000 cells and compared the induced phenotypes. (nature.com)
  • These drugs inhibit immune-suppressive signals and reinstate cancer immunosurveillance. (izb-online.de)
  • The studies described in the publication evaluated the use of ASOs as potential immunomodulators and their role in overcoming immune checkpoint inhibitor resistance through its dual mechanism of action. (izb-online.de)
  • Typically, low molecular weight drugs are not recognized by the immune system, whereas protein molecules of much higher molecular weight invariably are. (genengnews.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)
  • In contrast to results with 2D culture, observed mitotic arrest was relatively low, suggesting involvement of additional mechanisms in their antitumor effect in vivo . (nature.com)
  • If ER stress is a significant factor that affects the disease development, it would be important to find a drug that alters these mechanisms and UPR. (helsinki.fi)
  • Although these diseases arise from the transformation of different cell types (namely melanocytes, CD4+ T cell and epithelial cells), they share common features such as a partially elucidated pathophysiology, a lack of treatment at advanced stages, a need to understand the mechanisms leading to relapse or resistance upon currently available treatments and consequently a need for alternative therapies. (hipi-lab-saint-louis.fr)
  • This low survival may result from the metastasis of cancer cells and arising resistance to drugs. (oncotarget.com)
  • We provide experimental evidence demonstrating that ebastine has antitumor activity in osteosarcoma and promotes autophagy by activating the AMPK/ULK1 signaling pathway, which is IPMK dependent. (ijbs.com)
  • Sphingolipid-targeting drugs have been tested alone or in combination with chemotherapy, exhibiting antitumor activity alone and in synergism with chemotherapy in vitro and in vivo . (frontiersin.org)
  • These data further support the versatility of our LNAplus™ ASO platform and its ability to offer novel therapeutic solutions to overcome cancer treatment resistance. (izb-online.de)
  • The effectiveness or lack of a major therapeutic effect of sphingolipid modulation by some drugs as a cancer therapy and other aspects related to their mechanism of action are discussed in this review. (frontiersin.org)
  • BACKGROUND: Chemoradiotherapy-induced PD-L1 upregulation leads to therapeutic resistance and treatment failure. (bvsalud.org)
  • The mitophagy-related lncRNA signature can help estimate the survival and drug sensitivity, the ceRNA network may provide novel therapeutic targets for patients with OC. (biomedcentral.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)
  • Pharmacophore-based activity profiling screen demonstrated some biological targets that MS44-53 may modulate their biological response, and thus can be considered as potential drugs to treat different kinds of diseases, such as carcinoma, diabetes type II, bacterial infection and cardiovascular diseases. (openmedicinalchemistryjournal.com)
  • To confirm this popular use, ethanol extract from leaves of G. globosa L. was prepared by maceration and analyzed by some phytochemical and biological assays, including cardiovascular activity. (researchgate.net)
  • Billingsley ML. Druggable targets and targeted drugs: enhancing the development of new therapeutics. (jscimedcentral.com)
  • Alternative drugs have been developed to target Farnesyl transferase and downstream MEK targets, but these have failed for various reasons (reviewed in (1, 2)) . (cytoskeleton.com)
  • They confer resistance against many different viruses, inhibit proliferation of normal and malignant cells, impede multiplication of intracellular parasites, enhance macrophage and granulocyte phagocytosis, augment natural killer cell activity, and show several other immunomodulatory functions. (lookformedical.com)
  • Analysis of mitosis and antimitotic drug responses in tumors by in vivo microscopy and single-cell pharmacodynamics. (nature.com)
  • Single-cell and subcellular pharmacokinetic imaging allows insight into drug action in vivo . (nature.com)
  • The drug underwent significant rounds of modifications to produce a drug suitable for in vivo applications, these efforts resulted in ARS-1620 which has been used by the scientific community to further define the utility of this class of drugs (5) . (cytoskeleton.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)
  • Next, Ectopic expression of MINK1 efficiently rescued the 5FU resistance phenotypes in MINK1 KD (knock down) OSCC (Fig. 2C&D), which further depicts MINK1 dependency of 5FU resistance in OSCC. (springernature.com)
  • Next, MINK1 kinase inhibitor lestaurtinib was found to reverse 5FU resistance in OSCC. (springernature.com)
  • 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)
  • 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)
  • When RON MET TAM in Mesothelioma: All Druggable for One, and One Drug for All? (frontiersin.org)
  • However, studies relating kinase mediators of 5FU resistance in OSCC are limited. (springernature.com)
  • The goal of this study is to find out the potential kinase(s) those are major driver(s) of 5FU resistance in OSCC. (springernature.com)
  • Further, to understand the kinase driven mechanism regulating 5FU resistance, we performed a phosphorylation profiling using a phospho-antibody array in presence or absence of the target kinase. (springernature.com)
  • Sawa M, Masai H. Drug design with Cdc7 kinase: a potential novel cancer therapy target. (jscimedcentral.com)
  • Figure 5: Pharmacodynamics of antimitotic drugs in the HT-1080 xenograft system. (nature.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)
  • To understand the mechanism by which MINK1 regulates 5FU resistance, we performed a high-throughput phosphorylation profiling in MINK1 WT and MINK1 KO 5FU resistant cells (Fig. 3A&B). From this study, we found p- p53 (Ser33) and p-53(Ser15) to be significantly up-regulated in MINK1KO cells whereas p-AKT (Ser473) and p-MDM2 (Ser166) were found to be down-regulated in MINK1KO cells as compared to MINK1WT cells. (springernature.com)
  • Diagnostic testing continues to improve, but multi-drug resistance to treatment is an increasing challenge. (cdc.gov)
  • Here, we first used high-throughput screening and had screened one compound candidate, ebastine (a H1-histamine receptor antagonist), for osteosarcoma therapy. (ijbs.com)
  • Li X, Taratula O, Taratula O, Schumann C, Minko T. LHRH-Targeted Drug Delivery Systems for Cancer Therapy. (jscimedcentral.com)
  • These findings will assist the development of anti-tumour drugs to treat lung cancer. (oncotarget.com)
  • In the longer term, some might even take part in lung cancer screening programs. (cdc.gov)
  • Human-derived hepatic cell lines are a valuable alternative to primary hepatocytes for drug metabolism, transport and toxicity studies. (cancerindex.org)
  • Potent cell growth inhibitory properties were shown by ligands MS47 and MS49 against human melanoma MDA-MB-435, colon cancer HCT-116 and COLO 205, and pancreatic cancer MIA PaCa-2 cell lines, as evidenced by MTT assay. (openmedicinalchemistryjournal.com)
  • Figure 4: Quantitative analysis of drug response to paclitaxel treatment at a single-cell level. (nature.com)
  • Therefore, Src has been considered a target molecule for drug development. (oncotarget.com)
  • Characterisation of ER stress in PD models may be important for the current and future drug development of PD. (helsinki.fi)
  • Mitophagy and long non-coding RNAs (lncRNAs) play pivotal roles in tumorigenesis, development, and drug resistance. (biomedcentral.com)
  • Patients can usually be treated with nonsteroidal anti-inflammatory drugs (NSAIDs) alone. (msdmanuals.com)
  • The most effective drugs are fenretinide and α-galactosylceramide (α-GalCer). (frontiersin.org)
  • Using cDNA microarray screens and northern blot analysis, a previous study showed that Beclin 1 is upregulated in liver cancer tissues ( 11 ). (spandidos-publications.com)