Methods ligands drug screening assays antitumor. Medical search. Frequent questions

A ligand binding assay (LBA) is an assay, or an analytic procedure, which relies on the binding of ligand molecules to receptors, antibodies or other macromolecules. (wikipedia.org)
The foundations for which ligand binding assay have been built are a result of Karl Landsteiner, in 1945, and his work on immunization of animals through the production of antibodies for certain proteins. (wikipedia.org)
The former issue was often neglected prior to initiating drug discovery programmes while the latter was considered impossible because it was purported that antibodies were unsuitable to derive compounds. (cancer.gov)

One such biological target was RAS, where decades of attempts had failed (until very recently) to yield anti-cancer drugs directly interfering with RAS function. (cancer.gov)
Biological assays to test the cytotoxicity of the compound 1b combined with electroporation were performed to determine its potential for future medical applications in cancer treatment. (hindawi.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)
The biological activity of HTS02 is assessed by a tubulin polymerization assay. (cytoskeleton.com)
Protein markers are an essential component in biological research and drug development. (acrobiosystems.com)
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)

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)
Both ligands were more potent against cancer cells than in skin normal CCD-1064Sk fibroblasts. (openmedicinalchemistryjournal.com)
2013. Brine shrimp lethality assay 'an effective prescreen': Microwave-assisted synthesis, BSL toxicity and 3DQSAR studies-based designing, docking and antitumor evaluation of potent chalcones. (cytoskeleton.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)
NK cells are specialized effectors of the innate immune system that destroy their targets by antibody-dependent cell-mediated cytotoxicity, have prominent antitumor effects, and are potent killers of virally infected cells. (medscape.com)

When loaded with immune complexes (IC), consisting of tumor antigens bound to antitumor antibody, BMDC induce powerful antitumor immunity in mice. (stanford.edu)
Tumor-specific neoantigens, which are expressed on tumor cells, can induce an effective antitumor cytotoxic T-cell response and mediate tumor regression. (wjgnet.com)

DEC-205 (CD205), a member of the macrophage mannose receptor protein family, is the prototypic endocytic receptor of dendritic cells, whose ligands include phosphorothioated cytosine-guanosine (CpG) oligonucleotides, a motif often seen in bacterial or viral DNA. (uci.edu)
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)

Development and validation of an LC-MS/MS method for the determination of ARN14988, an acid ceramidase inhibitor, and its application to a pharmacokinetic study in a mouse model. (mcw.edu)
Inhibitor of checkpoint kinase CHK1 was identified as a top screen hit. (nature.com)
Herein, an electrochemical biosensor was developed for detection of T4 PNK activity and inhibitor screening based on supramolecular host-guest recognition between phosphate pillar (Dumitrache and McKinnon, 2017) [5] arene (PP5) and methylene blue (MB). (bvsalud.org)
Jin-Ching Lee, Chin-kai Tseng, Kuan-Jen Chen, Kuo-Jung Huang, Chun-Kuang Lin, Ying-Ting Lin*, "A Cell-based Reporter Assay for inhibitor screening of Hepatitis C Virus RNA dependant RNA Polymerase. (kmu.edu.tw)

These tools were initially used in RAS target validation and subsequently for isolating drug leads, guided by the intracellular antibody interaction with RAS. (cancer.gov)
We exploited the specific binding of the antibody fragment and were able to identify RAS-binding compounds in antibody-competition assays (illustrated in Fig.1). (cancer.gov)
In the first Abd technology application, we used a competitive surface plasmon resonance (cSPR) method [9] that depends on high affinity interaction of the antibody fragment with GTP-bound RAS. (cancer.gov)
The latter discovery was important for us because it suggests that the antibody combining sites could generally be accessible for implementing the Abd technology approach to drug discovery. (cancer.gov)
Aiming to exploit this effect in therapy we performed a compound screen in five breast cancer cell lines with IGF neutralising antibody xentuzumab. (nature.com)
Setting the corresponding isotype control antibody to detect non-specific binding can reduce the generation of false positive results and evaluate the possible influencing factors accurately in the drug development process. (acrobiosystems.com)
An antibody-drug conjugate (enfortumab-vedotin) directed against nectin-4 has shown marked tumor remission rates in this tumor type, which is known for high expression rates of nectin-4. (oncotarget.com)

Drug repositioning and pharmacophore identification in the discovery of hookworm MIF inhibitors. (jscimedcentral.com)
Tubulin polymerization must also be responsive to polymerization enhancers (paclitaxel) and inhibitors (nocodazole) at 5 µM drug concentration. (cytoskeleton.com)
Ying-Ting Lin*, Kuo-Jung Huang, Chin-kai Tseng, Kuan-Jen Chen, Hui-Min Wang, and Jin-Ching Lee, "Efficient In Silico Assay of Inhibitors of Hepatitis C Virus RNA-Dependent RNA Polymerase by Structure-Based Virtual Screening and In Vitro Evaluation. (kmu.edu.tw)
Molecular defects are often represented by hereditary BRCA (Breast cancer gene) mutations leading to altered DNA repair, thus presuming higher efficiency of DNA-damaging agents, such as platinum drugs and poly-ADP-ribose polymerase (PARP) inhibitors. (cttjournal.com)

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)
It will include detailed protocols for (i) immobilization of proteins with the amine coupling capture method, (ii) analyte-binding analysis, (iii) affinity/kinetics measurements, and (iv) data analysis. (bvsalud.org)

Mechanism-based target identification and drug discovery in cancer research. (jscimedcentral.com)
Organic chemistry in drug discovery. (jscimedcentral.com)
The role of the medicinal chemist in drug discovery--then and now. (jscimedcentral.com)
Terry Rabbitts is Professor of Molecular Immunology in the Centre for Cancer Drug Discovery, Institute of Cancer Research, Sutton, London, UK. (cancer.gov)
TL238) for anti-tubulin ligand drug discovery. (cytoskeleton.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)
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)

Specifically, despite the human body's endogenous receptors, hormones, and other neurotransmitters, pharmacologists utilize assays in order to create drugs that are selective, or mimic, the endogenously found cellular components. (wikipedia.org)
Ying-Ting Lin*, "A tandem regression-outlier analysis of a ligand cellular system for key structural modifications around ligand binding" Journal of Cheminformatics, (2013), 5:21. (kmu.edu.tw)
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)
Furthermore, ligand-modified-ß-CD, which can endow the ligand through complexation with PRX termini, improved the cellular uptake and genome-editing effects of the optimized PRX/Cas9 RNP in target cells. (bvsalud.org)
The data on the prognostic and predictive role of the tumor molecular biomarkers, as well as on clinically used and cellular therapy approaches and developing targeted drugs are presented, and the prospects for the future research are outlined. (cttjournal.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)

It has been proven that combining electroporation with chemotherapy potentiates the cytotoxicity of drugs when the drugs' efficacy is limited by its uptake in the cell [ 9 - 13 ]. (hindawi.com)

Such advances provide researchers with the ability not only to quantify hormones and hormone receptors, but also to contribute important pharmacological information in drug development and treatment plans. (wikipedia.org)
Radioligands are used to measure the ligand binding to receptors and should ideally have high affinity, low non-specific binding, high specific activity to detect low receptor densities, and receptor specificity. (wikipedia.org)
The gene product is a member of the nuclear hormone receptor family, a group of transcription factors regulated by small hydrophobic hormones, a subset of which do not have known ligands and are referred to as orphan nuclear receptors. (cancerindex.org)
The protein has been shown to interact with retinoid and thyroid hormone receptors, inhibiting their ligand-dependent transcriptional activation. (cancerindex.org)

Developing new techniques for screening and synthesizing peptides can result in efficient and cost-effective methods which make drugs more effective, diseases easier to cure, and lives to last longer. (peptidesguide.com)
Here huge numbers of peptides are screened so as to isolate and identify critical bioactive peptides that are used for new ways to cure diseases and cancers. (peptidesguide.com)
This method identifies peptide ligands as well as cytoxic peptides that may prove useful in developing anti-cancer agents. (peptidesguide.com)

Wolber G, Seidel T, Bendix F, Langer T. Molecule-pharmacophore superpositioning and pattern matching in computational drug design. (jscimedcentral.com)
Therefore, Src has been considered a target molecule for drug development. (oncotarget.com)
A ligand can be referred to as an «electron donor» that is attracted to the electron acceptor at the center of a complex, for which the ligand [ion or molecule] binds to a central metal atom and forms a complex. (peptidesguide.com)

This low survival may result from the metastasis of cancer cells and arising resistance to drugs. (oncotarget.com)

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)

These data identify novel therapeutic vulnerabilities and may inform future trials of IGF inhibitory drugs. (nature.com)

Ligand binding assays are used primarily in pharmacology for various demands. (wikipedia.org)

In this study, experimental studies were carried out to explore the action mechanism of the anti-cancer drug Azacitidine on the double-stranded DNA (dsDNA). (bvsalud.org)

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)
Thus, structural fine-tuning and the addition of ligand-modified-ß-cyclodextrin enabled efficient genome editing by the Cas9 RNP. (bvsalud.org)
It has been shown that the method can be used to obtain compounds with the aforementioned structural fragments separated by one or two methylene units. (edu.ua)

A detection method is used to determine the presence and extent of the ligand-receptor complexes formed, and this is usually determined electrochemically or through a fluorescence detection method. (wikipedia.org)
We also developed a method for the detection of Azacitidine at low concentrations using the differential pulse voltammetry (DPV). (bvsalud.org)
However, both methods suffer from low sensitivity and specificity, resulting in challenges for precise early detection ( 4 - 6 ). (frontiersin.org)
Recent advances in high-throughput and highly sensitive detection methods have overcome the limitation of the low concentration of most peripheral blood biomarkers. (techscience.com)
Hence, blood biomarker detection has become an efficient screening tool for the early diagnosis of OSCC. (techscience.com)

We describe antitumor activities of vitamin E succinate (VES), an anti-oxidant and fenbendazole (FBZ), a commonly used veterinary anthelmintic. (researchgate.net)
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)

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)

Some newer types are called "mix-and-measure" assays because they do not require separation of bound from unbound ligand. (wikipedia.org)

The development of platinum-drug resistance in cancer patients, the general toxicity and severe side effects of platinum drugs however required a different approach in the research of anticancer metal complexes [ 2 ]. (hindawi.com)
Treatment options are limited at best and drug resistance is common. (frontiersin.org)
Regardless of the therapeutic approach, the heterogeneity of pancreatic cancer cells and the complexity of its tumor microenvironment contribute to the emergence of drug resistance. (frontiersin.org)
The quantification of BBR is required in clinical medicine because long-term or excessive intake can lead to drug resistance and adverse effects. (bvsalud.org)
3 Click-ligated small-cyclic DNA and mini-duplexes are being explored in drug-DNA binding analysis and as potential therapeutics because of their higher resistance to nucleases, high thermal stability and better cell penetration. (biosearchtech.com)
Since it is known that inhibition of cell death mechanisms is a common event in tumour development, this poses problems for many forms of chemotherapy that utilise cell death pathways, leading to drug resistance. (gla.ac.uk)

Therefore, a rationale for treating hypertension would be to administer drugs or natural compounds which selectively inhibit ACE. (scielo.br)
This seemed much larger than would be expected for the range of space occupied by drug-like chemical compounds, estimated at 300 to 1000 Å2 [4, 5]. (cancer.gov)
Antineoplastons are drugs composed of chemical compounds that are naturally present in the urine and blood . (cancer.gov)

The main challenges left to be solved is the evaluation of restraint goodness, assigning secondary structures, restraint interconditioning, and water and ligand placement. (helsinki.fi)

Their crystal structures are similar and show a protonated amino group on the side chain of the ligand which is not very common for a simple heterocyclic derivative such as histamine. (hindawi.com)
This heterocyclic system is structurally close to 2H-1,2-benzothiazin-4-one 1,1-dioxide, which is the core of the famous non-steroidal anti-inflammatory drugs related to the "oxicam" group. (edu.ua)

Fluorescence-labelled oligonucleotides have applications as probes and primers for molecular assays such as fluorescent in situ hybridisation (FISH), quantitative PCR, sequencing and live cell imaging, which are routinely used in molecular diagnostics and drug development. (biosearchtech.com)

Conclusions These findings underscore the potential utility of this screening system for the identification of immunostimulatory drugs with anticancer effects. (bmj.com)

Methods Mol Biol. (jscimedcentral.com)

Typically, low molecular weight drugs are not recognized by the immune system, whereas protein molecules of much higher molecular weight invariably are. (genengnews.com)
Libraries in and of themselves can prove even more uniform than other methods in demonstrating full-length ligands during screening since molecular weight degeneracy can be eliminated right during the sequencing process versus during the synthesis, thus making the entirety of the technique much more simplified and less costly. (peptidesguide.com)

Derivatives of 1H-2,1-benzothiazin-4(3H)-one 2,2-dioxide are promising chemicals to search and develop drugs with the pharmacological properties required. (edu.ua)

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)

Through the development of RIA technology, researchers have been able to move beyond the use of radioactivity, and instead, use liquid- and solid-phase, competitive, and immunoradiometric assays. (wikipedia.org)
Characterisation of ER stress in PD models may be important for the current and future drug development of PD. (helsinki.fi)
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)
These findings will assist the development of anti-tumour drugs to treat lung cancer. (oncotarget.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)
Assay and Drug Development Technologies, (2011) 9, 290-298. (kmu.edu.tw)
To develop new CXCR4 antagonists a rational, ligand-based approach was taken, distinct from the more commonly used development strategy. (cnr.it)
It is a reliable and versatile technology ideal for applications in bioconjugation, probe-labelling, screening assays, and the development of pharmaceuticals. (biosearchtech.com)

Synthetizing methods for developing one-bead, one-compound (OBOC) peptide libraries have shown to be superior to that of standard assay formats and pooling strategies. (peptidesguide.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 drug binding constant (Kb) was found to be 4.13 ± 0.23 × 105 M-1 using voltammetric measurements and 1.67 ± 0.24 × 105 M-1 using the fluorescence spectroscopy. (bvsalud.org)
4 Such methods have been used to construct microarrays, fluorescence-microscopy slides and DNA-immobilised beads for diagnostics and biomedical research. (biosearchtech.com)

Ligand binding assays provide a measure of the interactions that occur between two molecules, such as protein-bindings, as well as the degree of affinity (weak, strong, or no connection) for which the reactants bind together. (wikipedia.org)
The only ligand recognized to bind MST1R (RON) is Macrophage Stimulating 1 (MST1), also known as Macrophage Stimulating Protein (MSP) or Hepatocyte Growth Factor-Like Protein (HGFL). (frontiersin.org)

Essential aspects of binding assays include, but are not limited to, the concentration level of reactants or products (see radioactive section), maintaining the equilibrium constant of reactants throughout the assay, and the reliability and validity of linked reactions. (wikipedia.org)
Click chemistry offers a quick, simple and streamlined approach to joining organic molecules without the need for heating, high pressure, and complex purification methods (there are no condensation side-products of click reactions). (biosearchtech.com)

Since melittin has multiple claimed therapeutic features and in other side, there is a limited number of studies regarding its effects on the immune system, we aimed to evaluate the immunotoxic/immunomodulatory properties of melittin in BALB/c mice with a tiered approach immunotoxicity screening. (biomedcentral.com)

Historically, ligand binding assay techniques were used extensively to quantify hormone or hormone receptor concentrations in plasma or in tissue. (wikipedia.org)

There are two common strategies that are adopted for this type of experiment: Increasing the amount of radioligand added while maintaining both the constant specific activity and constant concentration of radioligand, or decreasing the specific activity of the radioligand due to the addition of an unlabeled ligand. (wikipedia.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)

As a direct result of these monumental findings, researchers have continued the advancement of ligand binding assays in many facets in the fields of biology, chemistry, and the like. (wikipedia.org)

Antineoplastons are not approved by the U.S. Food and Drug Administration for the prevention or treatment of any disease. (cancer.gov)
Berberine (BBR) is an important anti-inflammatory drug for the treatment of intestinal diseases. (bvsalud.org)
In a study with patients with bladder cancer after treatment with platinum and anti programmed death 1/ programmed death ligand 1 therapy Nectin-4 expression was detected in all patient samples tested [ 7 ]. (oncotarget.com)
It is caused by numerous diseases that are accompanied by pain and inflammation, as well as by imperfection of the existing drugs aimed to provide treatment of these pathological conditions. (edu.ua)

Li X, Taratula O, Taratula O, Schumann C, Minko T. LHRH-Targeted Drug Delivery Systems for Cancer Therapy. (jscimedcentral.com)
These drugs may deserve to be tested for their efficacy in the control of prostate cancer using in vivo models. (researchgate.net)
Besides, recent efforts have focused on developing targeted therapies for pancreatic cancer, including drugs that target specific molecular alterations like the KRAS oncogene, which is frequently mutated in pancreatic cancer ( 9 - 11 ). (frontiersin.org)
The purpose of this study was to establish a 3D culture method for oral cancer and to verify its practicality. (medsci.org)
A commonly used in vitro experimental method in cancer research is two-dimensional (2D)-culture using dishes or flasks. (medsci.org)
and many others - see Advanced Drug Delivery Systems of Curcumin for Cancer Chemoprevention for a good overview. (blogspot.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)
From the paper: 'Carriers of pathogenic germline variants (PGV) in BRCA2 could soon be offered gastric cancer screening using gastroscopy. (cdc.gov)
In the longer term, some might even take part in lung cancer screening programs. (cdc.gov)
Methods: We used a previously published lung cancer PRS based on 80 SNPs associated with lung cancer risk in the OncoArray cohort and validated in UK Biobank. (cdc.gov)

The ligand-binding assay methodology quantified the concentration of the hormone in the test material by comparing the effects of the test sample to the results of varying amounts of known protein (ligand). (wikipedia.org)
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)

It requires that the concentration chosen must be determined empirically for a new ligand. (wikipedia.org)
The protein concentration for HTS02 in this assay is approximately 4 mg/ml. (cytoskeleton.com)

The search for new groups of anti-inflammatory and analgesic drugs is a topical issue of the current medicinal chemistry. (edu.ua)

When RON MET TAM in Mesothelioma: All Druggable for One, and One Drug for All? (frontiersin.org)

Special advances are achieved in HER-positive tumors using targeted therapy with drugs which suppress the tumor cell growth factors (trastuzumab, herceptin). (cttjournal.com)

Effective, reliable use of molecular biomarkers to inform clinical practice requires the standardisation of testing methods and careful assessment of biomarkers' predictive and prognostic value. (ersjournals.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)

Although binding assays are simple, they fail to provide information on whether or not the compound being tested affects the target's function. (wikipedia.org)

The protein encoded by this gene is an unusual orphan receptor that contains a putative ligand-binding domain but lacks a conventional DNA-binding domain. (cancerindex.org)

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