MiceResistanceDoxorubicinMolecularPeptidesCellularVitroPancreatic cancerTherapeuticTargetsLibrariesVivoPrimarilyAnticancerTumorBiomimeticPharmacologicalComputational approachesInteractions2017Anti-inflammatoryEfficacyTissueDMARDsTreatmentProteinsFindingsInhibitorsClinicalResponsesPatientsFood and Drug AdminSpecificCompoundsTopicalImmuneDevelopmentIncludeDiseasesHumanStudiesSuccessfulCellsDiscoveryRequireRelevantNumerousUtilityPharmaceuticalChemical
Mice2
- The same methodology was applied to MEL mice treated with the clinically approved anti-fibrotic drug nintedanib. (ibecbarcelona.eu)
- lipid carriers (C-D-NLC) inhibited the growth of LLC tumors in mice and reduced drug toxicity. (ajol.info)
Resistance3
- Diagnostic testing continues to improve, but multi-drug resistance to treatment is an increasing challenge. (cdc.gov)
- 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)
- Mitophagy and long non-coding RNAs (lncRNAs) play pivotal roles in tumorigenesis, development, and drug resistance. (biomedcentral.com)
Doxorubicin1
- In cultured primary fibroblasts and cancer cells, the chemotherapeutic drug doxorubicin causes mtDNA damage and release, which leads to cGAS STING dependent ISG activation. (regenerativemedicine.net)
Molecular6
- 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)
- 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)
- 3 The development of molecular targeted therapies aimed at these molecular alterations has generated great optimism for the treatment of cancers such as NSCLC, and drugs targeting the EGFR tyrosine kinase domain are now available. (bmj.com)
- This Perspective will focus on the molecular and computational approaches that underpin drug design by medicinal chemists to promote understanding and collaboration with clinical scientists. (springeropen.com)
- As a clear proof of such translational success of multi-target drugs into the clinic, we have performed an analysis of the US Food and Drug Administration (FDA)-approved new molecular entities (NMEs) from 2015 to 2017 (status September 2017), following a similar analysis (from 2000 to 2015) made by Lin et al. (springeropen.com)
- We publish articles in pharmaceutical sciences and related disciplines (including biotechnology, cell and molecular biology, drug utilization including adverse drug events, medical and other life sciences, and related engineering fields). (ajol.info)
Peptides2
- Besides the isolation and identification of major histocompatibility complex I-restricted peptides from the surface of cancer cells, one of the challenges is eliciting an effective antitumor CD8+ T-cell-mediated response as part of therapeutic cancer vaccine. (elifesciences.org)
- Indeed, the use of peptides for eliciting specific antitumor adaptive immunity is hindered by two main limitations: the efficient selection of the most optimal candidate peptides and the use of a highly immunogenic platform to combine with the peptides to induce effective tumor-specific adaptive immune responses. (elifesciences.org)
Cellular2
- 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)
- CYP387 is another just indicated JAK chemical with moderate selectivity for JAK1/2 over JAK3 in enzyme assays, and it's been proven to inhibit wild type JAK2 as well as JAK2V617F in cellular assays, but this element has yet to be evaluated in myeloma models. (igfprotein.com)
Vitro1
Pancreatic cancer1
- Together, the data provide new insight into mechanisms by which statins constrain proliferation in cancer and establish the effectiveness of a novel screening platform to identify small molecules of clinical relevance in pancreatic cancer. (oncotarget.com)
Therapeutic7
- 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 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)
- However, the complexity of the current incurable pathologies has clearly demonstrated that such single-target drugs are inadequate to achieve a therapeutic effect [ 1 , 2 ]. (springeropen.com)
- Here we focused on a drug-centered approach by predicting the therapeutic class of FDA-approved compounds, not considering data concerning the diseases. (biomedcentral.com)
- Successful drug repositioning requires that a known drug has a positive impact on a different disease, but its highest value resides in that its use for the novel indication surpasses the currently available therapeutic options for that condition. (biomedcentral.com)
- Aiming at enhancing the predictive power of the available computational methods, we have developed a novel approach based on machine-learning classification algorithms, where mismatches between known and predicted drug classifications are purposely interpreted as potential alternative therapeutic indications. (biomedcentral.com)
- There are a few other goals of therapeutic interest to produce effective IS that in conjunction with other drugs are highly desirable for immune tolerance induction. (igfprotein.com)
Targets5
- Our findings highlight fibronectin and tumor ECM mechanics as attractive targets in cancer therapy and support the need to identify new anti-fibrotic drugs to abrogate aberrant ECM mechanics in metastases. (ibecbarcelona.eu)
- Modern drug discovery has the power to identify potential modulators for multiple targets from millions of compounds. (springeropen.com)
- On this basis, the concept of drugs interacting with multiple targets has long been flagged as undesirable, as it was inherently associated with adverse side effects. (springeropen.com)
- We have integrated multiple layers of information: i) on the distances of the drugs based on how similar are their chemical structures, ii) on how close are their targets within the protein-protein interaction network, and iii) on how correlated are the gene expression patterns after treatment. (biomedcentral.com)
- Experimental approaches to drug repositioning generally involve high-throughput assays where libraries of approved compounds are tested against biological targets of interest. (biomedcentral.com)
Libraries1
- 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)
Vivo1
- We studied the chemosensitivity of these two MCSP tumor xenografts to anticancer drugs in vivo. (ox.ac.uk)
Primarily2
- Ligand binding assays are used primarily in pharmacology for various demands. (wikipedia.org)
- In order to overcome such limitations, in this study we have decided to establish a methodological approach focusing primarily on drug characteristics. (biomedcentral.com)
Anticancer1
- Conclusions These findings underscore the potential utility of this screening system for the identification of immunostimulatory drugs with anticancer effects. (bmj.com)
Tumor4
- 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)
- One strategy to increase cure rates is the identification of patient-specific drug responses in tissue models that mimic the interaction between patient cancer cells and tumor environment. (regenhu.com)
- potent anti-cancer drugs, combretastatin A-4 (CA-4) and docetaxel (DTX), against tumor cells and vasculature. (ajol.info)
- and anti-tumor assays. (ajol.info)
Biomimetic2
- The development of biomimetic nanoparticles (NPs) has revolutionized the concept of nanomedicine by offering a completely new set of biocompatible materials to formulate innovative drug delivery systems capable of imitating the behavior of cells. (frontiersin.org)
- This study presents an in-silico model replicating a microfluidic assay where endothelial cells sprout into a biomimetic extracellular matrix, specifically, a large-pore, low-concentration fibrin-based porous hydrogel, influenced by chemotactic factors. (ibecbarcelona.eu)
Pharmacological2
- 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)
- 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)
Computational approaches2
- Computational approaches more specifically aimed at drug repositioning have been designed to find correlations between disease-associated and drug-associated expression signatures under the assumption that an effective drug should be able to counterbalance the perturbations caused by a disease. (biomedcentral.com)
- Although the above studies have demonstrated that computational approaches to drug repositioning are feasible, there are still large margins for improvement. (biomedcentral.com)
Interactions3
- 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)
- For instance, deriving drug repositioning from drug-disease interactions alone can be difficult due to the complexity, variability and sparsity of data currently available for the diseases, and to the intrinsic nature of publicly available gene expression data, which derive from patients already treated with other drugs in most of the cases. (biomedcentral.com)
- studied to evaluate potential drug interactions. (ajol.info)
20171
- Building on such accumulating evidence, the concept of multi-target drugs has made rapid and spectacular progress from being an emerging paradigm when first enunciated at the beginning of 2000 [ 3 , 4 , 5 ], to one of the hottest topics in drug discovery in 2017. (springeropen.com)
Anti-inflammatory3
- 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)
- Optimal care of patients with rheumatoid arthritis (RA) requires an integrated approach that includes both nonpharmacologic therapies and pharmacologic agents such as nonbiologic and biologic disease-modifying antirheumatic drugs (DMARDs), nonsteroidal anti-inflammatory drugs (NSAIDs), analgesics, and corticosteroids. (medscape.com)
Efficacy3
- Dopamine receptor occupancy using [ 11 C]-raclopride PET is familiar to neuroscientists when used 10 as a PD biomarker of antipsychotic drug efficacy. (drugtargetreview.com)
- In rheumatology, change in the transfer constant K trans in dynamic contrast-enhanced MRI is used ( Panel 2 ) as a PD biomarker of drug efficacy in synovitis, in addition to its more familiar use in oncology. (drugtargetreview.com)
- In this regard, compounds that have passed through phases II or III in the drug discovery pipeline but never made it to the market due to efficacy issues bear great potential for drug repositioning approaches. (biomedcentral.com)
Tissue1
- Historically, ligand binding assay techniques were used extensively to quantify hormone or hormone receptor concentrations in plasma or in tissue. (wikipedia.org)
DMARDs2
- Updated treatment recommendations for the therapy of rheumatoid arthritis (RA) in South Africa advocate early diagnosis, prompt initiation of disease-modifying anti-rheumatic drugs (DMARDs), and an intense treatment strategy where disease activity is assessed with a composite score such as the Simplified Disease Activity Index (SDAI). (samj.org.za)
- and ( iii ) the emergence of biologic disease-modifying anti-rheumatic drugs (DMARDs). (samj.org.za)
Treatment4
- 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)
- Methods The literature related to PMS were collected from China Knowledge Network (CNKI), Wanfang database and Weipu database in the past 20 years, the herbal compound prescriptions for the treatment of PMS were screened and a relevant database were established and analyzed by SPSS. (bvsalud.org)
- The study consists of a maximum 6-week screening period, a 52-week treatment period (including the 26-week tapering), and an 8-week safety follow-up, with primary and secondary endpoint assessments at week 28. (biomedcentral.com)
- Existing computational methods for drug repositioning either rely only on the gene expression response of cell lines after treatment, or on drug-to-disease relationships, merging several information levels. (biomedcentral.com)
Proteins2
- 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 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)
Findings2
- 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)
- To translate these findings for clinical utility, we developed a high throughput screening platform to identify small molecule inducers of Class I/II bHLH activity. (oncotarget.com)
Inhibitors1
- Prominent among the hits were members of the statin class of HMG-CoA reductase inhibitors, cholesterol lowering drugs that are also being evaluated in cancer. (oncotarget.com)
Clinical3
- Drug developers sometimes think of imaging as an emerging discipline, full of esoteric technologies of marginal relevance to real-world clinical drug development. (drugtargetreview.com)
- Figure 1: Six imaging modalities most likely to be encountered in clinical drug development. (drugtargetreview.com)
- The FDA and EMA want evidence that a new drug improves how the patients feels , functions, or survives , so almost anything else measured in a clinical trial is considered a biomarker. (drugtargetreview.com)
Responses1
- The responses from experienced 'reliability experts' had been statistically validated for consistency and reliability. (ijsrp.org)
Patients1
- These recommendations provide practical suggestions for the screening and management of TB and other comorbidities, and offer an approach to monitoring of RA patients. (samj.org.za)
Food and Drug Admin1
- Bacillus subtilis is one of the main sources of probiotics and is classified as GRAS (Generally Recognized as Safe) by the US Food and Drug Administration (FDA). (biomedcentral.com)
Specific2
- Despite the complexity of causative factors that can lead to these disease states, the tools of modern drug discovery have the power to cover millions of compounds or fragments and determine their potential association with a target before specific chemical synthesis and biological testing is done. (springeropen.com)
- A survey among the expert professionals attached to the inter-disciplinary tasks of managing assets' reliability reveals that 116 items in 4 constructs suit this core specific purpose. (ijsrp.org)
Compounds1
- Drug discovery in the 21st century has the disadvantage that it is very difficult to get new compounds into the clinic. (springeropen.com)
Topical1
- Sesame oil is a potential lipophilic component in emulgel formulations for topical delivery of hydrophobic drugs. (ajol.info)
Immune2
- 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)
- That is based on the reliability of either or both JAK1 and JAK2 in numerous homodimeric or heterodimeric signaling complexes associated with various cytokine and growth factors along with the potential liability of immune suppression pan HDAC inhibitor associated with JAK3 inhibition. (igfprotein.com)
Development7
- 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)
- In fact, the opposite is true: imaging measurements (imaging biomarkers) are used daily in drug development and in personalised medicine. (drugtargetreview.com)
- In recent years an even wider array of imaging technologies has been transforming drug development. (drugtargetreview.com)
- Imaging tests are increasingly used as pharmacodynamic (PD) and safety biomarkers in early drug development. (drugtargetreview.com)
- Efficient drug repurposing has the potential to significantly impact the whole field of drug development. (biomedcentral.com)
- This practice, usually referred to as drug repositioning, is highly attractive because of its potential to speed up the process of drug development, hence reducing costs in addition to providing new treatments for unmet medical needs [ 2 ]. (biomedcentral.com)
- In contrast, the presence Bax inhibitor of neutralizing antibodies to AAV2 didn't stop local FIX gene transfer and transgene expression following IM injection of AAV2 development human FIX in human subjects with hemophilia B. The use of drugs targeting B cells prior Lymph node to vector delivery to subjects with high titer antibodies to the vector hasn't been tested yet. (igfprotein.com)
Include1
- 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)
Diseases1
- The success of drug design for complex diseases depends on an interdisciplinary and collaborative approach, and on scientists and clinicians who are willing to communicate and work together throughout the process. (springeropen.com)
Human1
- Antiviral screening assays for human herpesviruses 6 and 7. (unt.edu)
Studies1
- The need to control all these variables often leads to time-consuming and very expensive screening studies that require the analysis of a single variable at a time. (frontiersin.org)
Successful1
- The first successful ligand binding assay was reported in 1960 by Rosalyn Sussman Yalow and Solomon Berson. (wikipedia.org)
Cells1
- on LLC cells, superior to a single drug or solution group. (ajol.info)
Discovery1
- Indeed, in the years, these concepts have triggered the interest of the drug discovery community both in academia and pharmaceutical companies to such a point that a plethora of multi-target drugs are already available on the market. (springeropen.com)
Require1
- Some newer types are called "mix-and-measure" assays because they do not require separation of bound from unbound ligand. (wikipedia.org)
Relevant1
- Results The relevant literatures contains 184 Chinese medicine prescriptions/proprietary Chinese medicines, 122 flavors of traditional Chinese medicines, and the drug categories were mainly tonic drugs, antipyretic drugs, astringent drugs, and tranquilizers. (bvsalud.org)
Numerous1
- There are numerous types of ligand binding assays, both radioactive and non-radioactive. (wikipedia.org)
Utility1
- Our data indicate that the utility of risk-based screening for mpox in persons without skin lesions or rash via pharyngeal swabs, rectal swabs, and/or blood is likely limited. (cdc.gov)
Pharmaceutical1
- Despite the enormous increase of financial investments in pharmaceutical R&D, the number of newly approved drugs has greatly diminished during the past decade [ 1 ]. (biomedcentral.com)
Chemical1
- A physico-chemical screening test for chemical carcinogens: The ke test. (cdc.gov)