imaging in drug discovery and development
DRUG DISCOVERY AND DEVELOPMENT – PRESENT AND FUTURE pptx
... and quality of life and relieving pain and suffering However, the process is very complex, time consuming, and resource intensive, requiring multi-disciplinary expertise and innovative approaches ... the drug for longer periods and so retain drugs in the body for longer times Intermediate metabolizers retain drugs in the body for normal time periods Extensive metabolizers (EM) retain drugs in ... throughput DNA sequencing, gene mapping, and bioinformatics to identify the actual genetic basis of ‘interindividual’ and ‘interracial’ variation in drug efficacy and metabolism and holds promise...
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In silico methodologies for selection and prioritization of compounds in drug discovery
... to extensive in vitro and in vivo testing to determine if it is safe enough for human testing In the next step, the candidate drug enters the development process (clinical trials) in which it ... scoring scheme Dashed lines and circles denote aromatic bonds and atoms respectively Continuous lines and circles denote aliphatic bonds and atoms respectively Curly lines denote any bond type and ... The top 10 fingerprint keys of the AKT1 validation and test sets selected by the scoring scheme Dashed lines and circles denote aromatic bonds and atoms respectively Continuous lines and circles...
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Biointormatics of targeted therapeutics and applications in drug discovery
... light in drug discovery Bioinformatics approaches to collect relevant drug combination data from literature and to analyse the pathways and molecular interaction profiles involved in drug combinations ... phase of drug discovery From hit to lead to clinical trial drugs and to approved drugs, the drug discovery process is still time and money consuming (48) and methods to identify drug candidates ... including drug targets, drug chemicals, natural products and biomarkers The drug and target information stored in TTD was updated constantly to include recent approvals into clinical trials and...
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Báo cáo khoa học: Nuclear localization of human spermine oxidase isoforms – possible implications in drug response and disease etiology pptx
... overexpressing SMO cells further confirmed the increased SMO activity, with decreases in intracellular spermine pools and increased spermidine levels in SMO1 and SMO5 cells These changes in spermine and ... oxidation of spermine to spermidine diminishes nuclear spermine pools Because spermine has essential roles in the the protection of DNA, including free radical scavenging and DNA shielding, this reduction ... cells were maintained in RPMI 1640 media (Mediatech, Inc., Herndon, VA, USA) containing 9% iron-supplemented fetal bovine serum (Hyclone, Logan, UT, USA) and 1% penicillin and streptomycin Beas2B...
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Antibiotic Discovery and Development pptx
... Antibiotic Drug Development: Moving Forward into the Clinic 1071 Jane E Ambler and Greg G Stone Part IX 37 Antibiotic Drug Development The Economics and Incentives of Antibiotic Drug Discovery ... The drug was discovered in 1909 and amazingly (by today’s standards) was in clinical use by the following year It was extremely successful in treating syphilis, especially when compared with standard ... Daptomycin Erythromycin Novobiocin Fig 1.4 Antibiotics produced by Actinomycetes Lincomycin Spectinomycin The Early History of Antibiotic Discovery: Empiricism Ruled Rifamycin SV Streptomycin Vancomycin...
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MASS SPECTROMETRY IN DRUG METABOLISM AND DISPOSITION docx
... Drug- Metabolizing Enzymes, Transporters, and Drug Drug Interactions 83 Steven W Louie and Magang Shou Experimental Models of Drug Metabolism and Disposition 151 Gang Luo, Chuang Lu, Xinxin Ding, ... in drug discovery and development Drug Metab and Dispos 1998;26:1213À1216 Wu CY, Benet LZ Predicting Drug Disposition via Application of BCS: Transport/ Absorption/Elimination Interplay and Development ... via chlorination) some drugs and physiological substrates Depending on the remaining structure, the formed radical products of drugs can yield quinones, quinone imines, diimines, dimers (and other...
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Báo cáo khoa học: Role of the plasma membrane leaflets in drug uptake and multidrug resistance ppt
... data reported in the present study, and obtained in living cells, confirm the finding obtained in reconstituted proteoliposomes [11,12] and isolated membranes [29,30] indicating that Pgp and a bacterial ... anthracyclines, are positively charged and therefore bind to acidic groups in proteins and membranes Thus, their movement into the cell can be envisaged as a series of binding and releasing events ... is expected to handle incoming drugs more efficiently compared to drugs already present in the cell interior By contrast, in the case where drug concentrations in the cytoplasm and the cytoplasmic...
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ONCOGENOMICS AND CANCER PROTEOMICS – NOVEL APPROACHES IN BIOMARKERS DISCOVERY AND THERAPEUTIC TARGETS IN CANCER pot
... Wnt/βcatenin and cadherin pathway genes including N-cadherin and P-cadherin but low E-cadherin protein expression This finding demonstrated the highgrade serous ovarian cancer contained messenchymal ... which will be discussed in details below a Chromosomal instability (CIN) Chromosomal instability lead to increase rate of losing or gaining chromosomes during cell division and accounts for 15% ... aneupploidy and cellular transformation in vitro (40) AURKA interacts with TPX2 and plays a role in centrosome maturation and spindle formation (41) The polo-like kinase (PLK1) is important in spindle...
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fragment based drug discovery and x-ray crystallography
... cysteine is introduced into a protein and used to capture fragments that bind in the vicinity, thus providing some information on the binding site It is also possible to measure fragments binding ... Pyridine Cyclohexane Pyrimidine N N 1,3,5-triazine H N Piperidine H N H N N N N Indole 1H-indazole N N Benzimidazole N Purine N N N Napthalene Fig (continued) Quinoline Isoquinoline N Quinazoline ... letter in Drug Discovery Today by Andrew Hopkins and coworkers [78]: LE ¼ (free energy of ligand binding)/(number of heavy atoms) The “free energy of ligand binding” is normally expressed in kilocalories...
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Báo cáo y học: "Potential involvement of oxidative stress in cartilage senescence and development of osteoarthritis: oxidative stress induces chondrocyte telomere instability and downregulation of chondrocyte function" pptx
... 4°C, and then paraffin blocks were prepared using standard histological procedures For nitrotyrosine staining, the sections were deparaffinized and hydrated, and then were immunostained using ... oxidative stress induces telomere instability and dysfunction in chondrocytes, subsequently resulting in cartilage ageing and the development of OA through a mechanism involving the acceleration ... nitrotyrosine Nitrotyrosine was present both within chondrocytes and in the cartilage matrix, and was seen mainly in the more superficial regions The degree of immunostaining for nitrotyrosine (number...
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Báo cáo y học: "Global transcriptome analysis reveals circadian regulation of key pathways in plant growth and development" potx
... transcripts, including the following: RNA processing; DNA synthesis and chromatin structure; protein synthesis, secretion, and ubiquitin-mediated degradation; G-proteinmediated signaling; and cell ... -tocopherol Phytol phytol -tocopherol -carotene Zeinoxanthin zeinoxanthin -carotene Zeaxanthin zeaxanthin Lutein lutein Violaxanthin violaxanthin ABA Figure Circadian co-regulation of metabolic ... Possible links between the clock and hormone signaling The gaseous hormone ethylene plays well-known roles in fruit ripening and the triple response during seedling emergence; in addition, it is involved...
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Provision, discovery and development of ubiquitous services and applications
... Universal Business Registry (UBR) for all publicly available Web services UBR stores four types of information, including business information, service information, binding information and information ... realized and tested for assisting people’s daily living The combination of mobile and ubiquitous computing, or referred to as Mobile Ubiquitous Computing in this thesis, is emerging as a promising ... For instance, assume Kate is currently doing a sharing of information regarding the general election in Singapore Keith, a Singaporean currently on a business trip to USA, is particularly interested...
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Knowledge discovery in biomedical research and drug design the development and application of biological databases
... rationalized and focused experiments The interaction between molecules, including protein-protein, proteinnucleic acids and protein-ligand, is normally identified by binding experiments and kinetic ... understand of disease etiology and better therapy 1.4 Role of Databases in Facilitating Drug Discovery 1.4.1 Overview of emerging technologies of drug discovery Drug discovery is complex and costly ... toxicity inducing drug candidates It is expected that a series of target databases like DART are useful in facilitating rational drug discovery Three kinds of target proteins are important for drug discovery: ...
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Tài liệu Lipases and Phospholipases in Drug Development pptx
... 81 Mg2+-independent Neutral Sphingomyelinases 84 Alkaline Sphingomyelinase from the Intestinal Tract 85 Bacterial Sphingomyelinase-phospholipase C 85 Sphingomyelinase Mechanism 85 Binding of Magnesium ... Alonso Introduction and Scope Sphingomyelinases 80 Types of Sphingomyelinases 80 Acid Sphingomyelinase (aSMase) 80 Secretory Sphingomyelinase (sSMase) 81 Neutral, Mg2+-dependent Sphingomyelinases ... Ions 85 Binding of Substrate 85 Mechanism of Catalysis 86 Sphingomyelinase Assay 88 Sphingomyelinase Inhibitors 89 Sphingomyelinase–Membrane Interactions 89 Lipid Effects on Sphingomyelinase Activity...
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Báo cáo y học: " Effectiveness of antiretroviral therapy and development of drug resistance in HIV-1 infected patients in Mombasa, Kenya" doc
... molecular work and sequence analysis and prepared the manuscript SL and CV assisted in designing the study and drafting the manuscript KD and JR performed viral loads and genotyping KM supervised ... Prevalence and risk factors for developing K65R mutations among HIV-1 infected patients who fail an initial regimen of fixed-dose combination of stavudine, lamivudine, and nevirapine J Clin Virol ... genotyping of HIV RNA was performed by nested RT-PCR and an in- house sequencing assay as described elsewhere [4] The interpretations of genotyping data and subtyping were performed using Smartgene™...
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báo cáo khoa học: " The first set of EST resource for gene discovery and marker development in pigeonpea (Cajanus cajan L.)" ppsx
... proteins with bi-functional role in lysozyme/chitinase activity involved in random hydrolysation of N-aetyl-beta-D-glucosaminide-beta linkages in chitin and chitodextrins during systemic acquired resistance ... [17,64] and therefore we used this approach for mining SNPs in this study By using in silico mining approach in a total of 871 contigs coming from 10,376 ESTs (9,888 generated in this study and 908 ... proteins (22.5%), developmental proteins (19.7%), cellular proteins (15.4%), metabolic proteins (14.0%), defence/stimulus responsive proteins (4.3%), protein specific binding proteins (2.8%) and...
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Báo cáo y học: "Optical tomographic imaging discriminates between disease-modifying anti-rheumatic drug (DMARD) and non-DMARD efficacy in collagen antibody-induced arthritis" pptx
... following criteria of redness and swelling: = no swelling or redness (normal paws), = swelling and/ or redness in one digit or in the ankle, = swelling and/ or redness in one or two digits and ankle, ... (MMPSense680), including MMP-3, MMP-9, and MMP-13 These agents were administered via intravenous route (2 nmol (fluorophore) in 150 μl saline) in all imaging studies A third NIR imaging agent that ... advances in rodent arthritis models as well as in imaging technology to establish non-invasive optical tomographic imaging as a robust and accurate means of assessing inflammation and bone changes in...
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Báo cáo y học: "Distribution patterns of small-molecule ligands in the protein universe and implications for origin of life and drug discovery" doc
... ligand-protein binding Power-law behaviors of ligand-protein binding The number of ligands (N) decays with an increase in the number (L) of (a) domains and (b) folds that bind the ligand and ... during protein folding [74,75] Thus, the free energy release during ligand binding may meet the free energy demand during protein folding It is tempting to examine the conjecture of ligand-induced ... protein-ligand binding ture-function relationships of proteins First, binding sites and ligands are quite flexible and plastic [39-41], and therefore, binding-site selection is, to certain extent,...
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