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

Outcomes for patients with melanoma have improved over the past decade with the clinical development and approval of immunotherapies targeting immune checkpoint receptors such as programmed death-1 (PD-1), programmed death ligand 1 (PD-L1) or cytotoxic T lymphocyte antigen-4 (CTLA-4). (biomedcentral.com)
EGFR, PBRM1 , LKB1 , JAK1/2 , and B2M mutations), complex rearrangements/copy number variations (e.g. programmed death ligand 1/2 [PD-L1/2] amplification), microsatellite instability, and TMB-related metrics can be detected in blood using next-generation sequencing (NGS) analysis of circulating tumor DNA. (biomedcentral.com)

Tumor-specific neoantigens, which are expressed on tumor cells, can induce an effective antitumor cytotoxic T-cell response and mediate tumor regression. (wjgnet.com)
Triticum aestivum L. root growth inhibition test and Allium cepa L. assay were used to assess the cytotoxic potential of phosphonates. (japsonline.com)

The interaction of human topoisomerase 1B and dimethylmyricacene, a compound prepared semisynthetically from myricanol extracted from Myrica cerifera root bark, was investigated using enzymatic activity assays and molecular docking procedures. (mdpi.com)
Description: Inhibition of RIPK1 enzymatic activity in vitro determined using Eurofins' KinaseProfiler assay. (guidetopharmacology.org)

Furthermore, a novel fluorescence "light-up" sensor for assaying BBR was established based on the interaction between BBR and SiO2@NH2@CNCl NPs. (bvsalud.org)
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)

Identification of a Vitamin-D Receptor Antagonist, MeTC7, which Inhibits the Growth of Xenograft and Transgenic Tumors In Vivo . (mcw.edu)
Our previous work allowed the identification of the first positive marker for MF and SS cutaneous and circulating malignant T cells, namely the NK cell receptor KIR3DL2. (hipi-lab-saint-louis.fr)
This switching off happens when the PD1 receptor binds to the other cells' PDL1 or PDL2 ligands (also proteins). (timesofisrael.com)
Drug-induced ubiquitination and degradation erbB receptor tyrosine kinases. (mirnamimics.com)
The efficient use of tyrosine kinase inhibitors (TKI) of the epidermal growth factor receptor (EGFR) as therapeutical agents in advanced non-small cell lung cancer (NSCLC) depends on identification of patients likely to show clinical benefit from these specific treatments. (biomedcentral.com)
Identification of Toll-like receptor signaling inhibitors based on selective activation of hierarchically acting signaling proteins. (createuky.net)
This antimicrobial gene encodes a chemokine of the CXC subfamily and ligand for the receptor CXCR3. (cancerindex.org)

Drug repositioning and pharmacophore identification in the discovery of hookworm MIF inhibitors. (jscimedcentral.com)
However, drug resistance to these inhibitors is developed resulting in only short-term improvement of patients' survival 15 . (nature.com)
Identification of Plasmodium falciparum heat shock 90 inhibitors via molecular docking. (createuky.net)
Bromodomain-Selective BET Inhibitors Are Potent Antitumor Agents against MYC-Driven Pediatric Cancer. (createuky.net)
A high-throughput screen indicates gemcitabine and JAK inhibitors may be useful for treating pediatric AML. (createuky.net)
Chemical array screening for small molecule inhibitors. (riken.jp)
Robust and systematic drug screening method using chemical arrays and protein library: Identification of novel inhibitors of carbonic anhydrase II. (riken.jp)

The activity of this enzyme is commonly assayed using a leucine arylamide chromogenic substrate such as leucyl beta-naphthylamide. (lookformedical.com)
Of these, RNA-seq, flow and mass cytometry, and enzyme-linked immunosorbent assay-based multiplex technologies are frequently utilized to identify peripheral immune markers associated with clinical response to immune modulating therapies. (biomedcentral.com)

When loaded with immune complexes (IC), consisting of tumor antigens bound to antitumor antibody, BMDC induce powerful antitumor immunity in mice. (stanford.edu)

Combined to our long-lasting and strong collaboration with the Onco-Dermatology Department of Saint Louis Hospital, our results would ultimately lead to the identification of novel targets both on the tumor and immune side and allow the development of innovative therapies. (hipi-lab-saint-louis.fr)
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)
Combination therapies with anti-PD-1 treatment in TNBC-bearing mice reduced tumor growth in multi-drug cohorts. (bmj.com)
This symposium presents a remarkable opportunity to convene with other researchers, clinicians, and industry leaders to discuss the extraordinary progress and immense potential of new drug therapies and technologies in paving the way for a brighter future in cancer treatment. (nyas.org)
This mini-review summarizes the resistance mechanisms of gliomas to platinum drugs, as well as molecules and therapies that can improve the sensitivity of gliomas to platinum drugs. (eurekaselect.com)
The present study aimed to assess the feasibility of developing low-cost multipurpose iron oxide/TiO2 nanocomposites (NCs) for use in combined antitumor therapies and water treatment applications. (infim.ro)

Chemotherapy is commonly used clinically to treat colorectal cancer, but it is usually prone to drug resistance, so novel drugs need to be developed continuously to treat colorectal cancer. (bvsalud.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)
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)
Treatment options are limited at best and drug resistance is common. (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)
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)
However, the results of gliomas chemotherapy are unsatisfactory, and resistance to platinum drugs is one of the important reasons. (eurekaselect.com)
The resistance of gliomas to platinum drugs is the result of a combination of influencing factors. (eurekaselect.com)
miRNAs and lncRNAs control drug sensitivity and the development of tumor resistance towards platinum drugs. (eurekaselect.com)
The long-term effectiveness of most antibiotic treatments is restricted by both pathogen drug resistance and non-target effects on the host's commensal microbial community. (nature.com)
Anti-infective drugs that do not perturb survival or viability of bacterial pathogens should be less likely to promote resistance than conventional antibiotics 1 , 2 . (nature.com)
Natural bioactive compounds derived from plant species show promising therapeutic properties to combat the emerging resistance in microbial pathogens, which can be exploited as next generation anti-infective drugs. (nature.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)
The success of inorganic nanomaterial-based therapeutic agents depends on the degree to which these nanostructures satisfy general requirements for drug safety regarding biocompatibility, biodegradability, and stability and on their antitumor efficacy. (infim.ro)

Berberine (BBR) is an important anti-inflammatory drug for the treatment of intestinal diseases. (bvsalud.org)
The search for new groups of anti-inflammatory and analgesic drugs is a topical issue of the current medicinal chemistry. (edu.ua)
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)
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)

Guidebook on molecular modeling in drug design: Academic Press. (jscimedcentral.com)
Ooms F. Molecular modeling and computer aided drug design. (jscimedcentral.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)
The identification of Pathogen-Associated Molecular Patterns (PAMPs) has greatly advanced our understanding of how adjuvants work beyond the simple concept of extended antigen release and has accelerated the development of novel adjuvants. (mdpi.com)
Molecular docking studies suggest that cranberry-derived proanthocyanidin binds to QS transcriptional regulators, mainly interacting with their ligand binding sites. (nature.com)

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)

Description: Inhibition of recombinant RIPK1 in an in vitro ADP-Glo assay (Promega). (guidetopharmacology.org)
Description: Inhibition of recombinant human RIPK1 using ADP-Glo assay. (guidetopharmacology.org)

However, in 1990, Jon A. Wolff demonstrated the idea of nucleic acid-encoded drugs by direct injecting in vitro transcribed (IVT) mRNA or plasmid DNA (pDNA) into the skeletal muscle of mice which expressed the encoded protein in the injected muscle. (wikipedia.org)
Here we introduce CODD-Pred (COmprehensive Drug Design Predictor), an online web server with well-curated data sets from the GOSTAR database, which is designed with a dual purpose of predicting potential protein drug targets and computing bioactivity values of small molecules. (bvsalud.org)
These drugs are designed to break down the protein "checkpoints" that cancer cells create to protect themselves from antibodies that seek to destroy them. (timesofisrael.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)
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)
This photo-cross-linked microarray format was found to be useful not merely for ligand screening but also to study the structure-activity relationship, that is, the relationship between the structural motif (or pharmacophore) found in small molecules and its binding affinity toward a protein, by taking advantage of the nonselective nature of the photo-cross-linking process. (riken.jp)
Photo-cross-linked small-molecule microarrays as chemical genomic tools for dissecting protein-ligand interactions. (riken.jp)

Second, we collected 56 targets closely related to the occurrence and development of cancer, metabolic diseases, and inflammatory immune diseases and developed a multi-model self-validation activity prediction (MSAP) framework that enables accurate bioactivity quantification predictions for small-molecule ligands of these 56 targets. (bvsalud.org)
Billingsley ML. Druggable targets and targeted drugs: enhancing the development of new therapeutics. (jscimedcentral.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)

Hence, blood biomarker detection has become an efficient screening tool for the early diagnosis of OSCC. (techscience.com)
Detection of "hit ligands" is done by merged display analysis. (riken.jp)

Description: Determined in an in vitro fluorescent polarization based binding assay. (guidetopharmacology.org)

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)

Therefore, a rationale for treating hypertension would be to administer drugs or natural compounds which selectively inhibit ACE. (scielo.br)

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)

Target identification and bioactivity prediction are critical steps in the drug discovery process. (bvsalud.org)

The major concern of chemotherapy is the side effects of existing drugs ( Baldo and Pham, 2013 ). (japsonline.com)
Chemotherapy with platinum drugs such as cisplatin, carboplatin, oxaliplatin, or a combination thereof is used to treat a variety of tumors. (eurekaselect.com)

While tumor sampling is widely implemented for biomarker identification and analysis, obtaining tissue is challenging because of limited accessibility, multiple lesions, heterogeneity of the biopsy site, and patient condition. (biomedcentral.com)

Many diagnostic and prognostic assays have begun to show clinical applicability providing additional tools to optimize and individualize treatments. (biomedcentral.com)

50 years of preclinical anticancer drug screening:empirical to target-driven approaches. (jscimedcentral.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)
Compared with more neoantigens in melanoma, the paucity and inefficient identification of effective neoantigens in hepatocellular carcinoma (HCC) remain enormous challenges in effectively treating this malignancy. (wjgnet.com)

Research has begun to explore RNAs potential to be used for therapeutic benefit, and unique challenges have occurred during drug discovery and implementation of RNA therapeutics. (wikipedia.org)
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)

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)
Identification and investigation of potential biomarkers that may predict sensitivity to immunotherapy is an area of active research. (biomedcentral.com)
In addition to the identification of new biomarkers, the platforms and assays required to accurately and reproducibly measure biomarkers play a key role in ensuring consistency of measurement both within and between patients. (biomedcentral.com)

The anti-PD1 agent given in ICI therapy prevents the binding of the ligands and receptors and boosts the body's immune response. (timesofisrael.com)
But what's more important is the functionality of the binding of the ligands and receptors. (timesofisrael.com)
The method is based on the immobilization of one of the binding partners, called the "ligand," on a dedicated sensor surface. (bvsalud.org)
Description: Binding constant determined by KINOMEscan assay. (guidetopharmacology.org)
Description: Binned value determined in a fluorescent polarization hRIPK1 binding assay. (guidetopharmacology.org)

Platinum drugs are a class of chemotherapeutic drugs that affect the cell cycle, and the main site of action is the DNA of cells, which are common chemotherapeutic drugs in clinical practice. (eurekaselect.com)

We found that Ponatinib, an FDA-approved drug, is an effective inhibitor of BRAF monomers and dimers. (nature.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)
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)
Fourteen drugs were identified as having synergy with TRAIL, including those whose TRAIL sensitization activities were previously unknown in either prostate or pancreatic cancer cells or both. (biomedcentral.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)

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)

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)

The contribution of synthetic organic chemistry to anticancer drug development. (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)
Radiotheranostics, injectable radiopharmaceuticals with antitumour effects, have seen rapid development over the past decade. (harvard.edu)

The research and medical communities are enthusiastic about the potential for immunotherapy and hundreds of drug trials are ongoing in the US. (timesofisrael.com)

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

Over the last decade, research on antimicrobials has shifted towards an alternative approach to combat pathogens using anti-infective drugs that selectively interrupt virulence pathways to help prevent or cure bacterial infections. (nature.com)

With this approach, photo-cross linked microarrays of 2000 natural products and drugs were constructed. (riken.jp)

Demand for FISH assays in formalin-fixed, paraffin-embedded tissues has been increasing, mainly in conditions in which diagnosis is not achieved in cell smears or tissue imprints, such as solid tumors. (biomedcentral.com)
Decreased intracellular drug concentration, enhanced function of cell processing active products, enhanced repair ability of cellular DNA damage, and blockage of related apoptosis pathways play an important role in it. (eurekaselect.com)

Drug target analysis based on proteomic analysis by 2D-DIGE. (riken.jp)
Proteomic profiling system for drug target analysis using 2D-DIGE. (riken.jp)
Proteomics accelerating the identification of the target molecule of bioactive small molecules. (riken.jp)

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)

Both ligands were more potent against cancer cells than in skin normal CCD-1064Sk fibroblasts. (openmedicinalchemistryjournal.com)
Cancer cells tend to have many PDL1 and PDL2 ligands, so they can evade attack from the T cells. (timesofisrael.com)
You need to know how many of the ligands can suppress the T cells. (timesofisrael.com)
It is known that the pathogenic properties of glioma cells and the response of glioma towards platinum-based drugs are strongly influenced by non-coding RNAs, particularly, by microRNAs (miRNAs) and long non-coding RNAs (lncRNAs). (eurekaselect.com)

Analysis of variance was used to identify drugs that exhibited synergy with TRAIL. (biomedcentral.com)

Rapid repurposing of drugs for COVID-19. (createuky.net)

and diagnostics and drug delivery for low-resource environments (Euliano et al. (harvard.edu)

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)

Anatomy22

Organisms15

Diseases29

Chemicals and Drugs100

Analytical, Diagnostic and Therapeutic Techniques and Equipment46

Phenomena and Processes50

Disciplines and Occupations2

Technology, Industry, Agriculture2

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Death ligand2

Cytotoxic2

Enzymatic activity2

Fluorescence2

Receptor7

Inhibitors7

Enzyme2

Induce1

Therapies6

Resistance12

Efficacy2

Anti-inflammatory5

Molecular5

Biological2

Inhibition2

Protein7

Targets3

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20001

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Activity1

Cells4

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