the drug development pipeline discovery to testing in humans
DRUG DISCOVERY docx
... clinically used drugs may cause flavonoid -drug interactions by modulating the pharmacokinetics of certain drugs, which results in an increase in their toxicity or a decline in their therapeutic effect, ... protect the gastrointestinal tract against damage by reactive species present in foods or generated within the stomach and intestines However, they may be beneficial in the Fruit/Vegetable -Drug Interactions: ... metabolism in humans are expressed predominantly in the liver However, they are also present in the large and small intestine, lungs and brain [34] CYP proteins are categorized into families...
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scientific american - 2001 08 - cyber cells - simulating life for drug discovery
... of the disease— a protein largely responsible for the cellular stickiness The protein, called thrombospondin, binds to red blood cells and provokes them into releasing molecules that increase the ... determining the cause of death by focusing on either the chest or the head area and then working rapid-fire through the half a dozen major causes of death “He’s telling me there was a pain in the ... start, Myriad plans to make its data commercially available only to collaborators and paying customers 16 The Post-Genome Project f the proof of the pudding is in the eating, then the proof that biology...
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computational medicinal chemistry for drug discovery - p. bultinck, et al., (marcel dekker, 2004)
... bringing a medicine to the market The title of this book refers to two topics, namely, Computational Medicinal Chemistry and Drug Design It unites these topics by giving an overview of the main ... unit of most force elds is the atom type, determining what parameters to apply for all interactions involving the same constituent atom types The various interaction types include bond lengths, angles, ... 17] Furthermore, there is currently an increasing interest in polarizable force elds incorporating electrostatics dependent on the surroundings [18] A major problem lies in the fact that atomic...
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fragment based drug discovery and x-ray crystallography
... 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 to proteins via ... expected, the acetohydroxamic acid chelates the Fig 11 Fragment linking to discover ABT-518 Introduction to Fragment-Based Drug Discovery 23 active site zinc while the biaryl binds in the S10 pocket The ... natural and synthetic ligands to a number of proteins [80] By plotting the binding energy against the number of heavy atoms in the ligand, they found a roughly linear relation for the smallest...
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DRUG DISCOVERY RESEARCH IN PHARMACOGNOSY ppt
... origin, including whole plants or their parts, animal parts and minerals, are used as medicines, either alone or in combination In addition, various other measures are used in an attempt to maintain ... used in the analysis of essential oil in herbal medicines With the GC–MS, not only a chromatographic fingerprint of the essential oil of the herbal medicine can be obtained but also the information ... spectrometer Information features of chromatographic fingerprints of herbal medicines Hence there are many chromatographic techniques, including the hyphenated chromatographies, available for us to the instrumental...
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DRUG DISCOVERY AND DEVELOPMENT – PRESENT AND FUTURE pptx
... whether to continue the development or to select the optimum candidate or formulation for development [22] One of the major initiatives in an effort to improve the efficiency and success in drug ... Toxicity Testing in the 21(st) Century Altex-Alternatives to Animal Experimentation 28: 17-44 [24] Wagner JA (2008) Back to the future: driving innovation in drug development Clin Pharmacol Ther ... drug to the market There is a growing urgency to identify and develop more effective, efficient, and expedient ways to bring safe and effective products to the market The drug discovery and developmental...
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In silico drug discovery on computational Grids for finding novel drugs against neglected diseases
... 8- Amino Quinolines Primaquine, Tafenoquine Hypnozoites, Gametocytes 4- Amino Quinolines Chloroquine, Amidoquine Intra-erythrocytic stages, Gametocytes Quinoline-alcohols Quinine, Mefloquine Erythrocytic ... Delivering the drugs to the patients in need of the drugs f Effective combination therapies that are frontline treatments are too expensive to be paid by the patients g No new drugs in the past ... ligand, then it requires preparing the binding site of the protein by taking ~6–8 °A from the co-crystallized ligand, taking care the significant amino acids for the activity are included in the binding...
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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
... behaviors of ligand-protein binding From the factor loadings, we see that the first factor, explaining 52.8% of the variance, contains high loadings (>0.9; shown in bold in Table 1) from constitutional ... likely to have originated independently of proteins [56-59], the binding of ligands with primordial proteins would also be a critical step in the origin of life Thus, it is intriguing to explore the ... 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...
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Báo cáo y học: "Meeting the challenges of drug discovery: a multidisciplinary re-evaluation of current practices" pptx
... drug reactions After describing the power of the technique in general terms, he presented an informative case study on determining the toxicity of potential inhibitors to the chemokine receptor ... receptor used by the human immunodeficiency virus (HIV) to enter cells Making the right clinical decisions There remains the challenge of matching the “right drug to the right patient” Good clinical ... early in the drug discovery process to predict toxicity in vivo Roger Ulrich (Rosetta Inpharmatics, Seattle, USA) is applying microarray technology to toxicogenomics with the goal of reducing adverse...
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Báo cáo y học: "Digital drug discovery" pot
... the challenges in integrating microarray data into drug development and medicine Investigators at Harvard Medical School and at the National Institute for Standards and Technology (NIST, Gaithersburg, ... extending today’s healthcare paradigm of diagnosis and therapy to include predisposition screening, targeted monitoring, and an emphasis on preventive medicine In an attempt to identify genes influencing ... mimicking blood flow in the liver This threedimensional bioreactor more faithfully replicates the in vivo complexity of the liver itself, resulting in an improved in vitro model Bioreactors have...
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Drug discovery metformin and the control of diabetes
... carbon chain would render the compounds less toxic, whilst maintaining the hypoglycaemic effect of the guanidine groups However, they weren’t nontoxic enough Their debilitating effects on the liver ... extremities Poor sensation in the feet, for instance, can lead to minor injuries, such as stubbing the toes, going unrecognised Infection, Testing blood glucose levels combined with poor circulation ... became increasingly resistant to it The supply of the drug – it was imported from Java – was also inconsistent during periods of global unrest By the 1930s, the search was on to find alternatives to...
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In silico methodologies for selection and prioritization of compounds in drug discovery
... based on the following points within a molecule: the centroid, the closest atom to the centroid, the furthest atom from the centroid and the furthest atom from the furthest atom from the centroid ... 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 ... considerable investments in the storage, retrieval and interpretation of the data into useful information As such, the application of data mining methods to analyse these data will guide the medicinal...
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Chemical and pharmacological studies of ardisia elliptica antiplatelet, anticoagulant activities and multivariate data analysis for drug discovery
... 2009 14 Sanguinarine Sanguinaria canadensis Taxinine, taxinine A, taxinine B, Taxus cuspidata 2-deacetoxytaxinine B, taxacin, taxchinin B, taxol Inhibit collagen, U46619 and thrombin-induced Jeng ... complex at the site of tissue injury via the extrinsic pathway The intrinsic pathway is initiated by the interaction of factor XII, high molecular weight kininogen (HMWK) and prekallikrein to form ... protein kinase (ERK), p38 mitogenactivated protein kinase (MAPK) and protein kinase C (PKC)α (Medeiros et al., 2007) α-amyrin was shown to inhibit platelet activating factor (PAF) receptor binding...
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Development of database and computational methods for disease detection and drug discovery
... Bioinformatics and cheminformatics in drug discovery The combination of random screening and rational drug design have played an important role in drug discovery [44] The traditional drug discovery ... derived to attempt [79] to estimate the binding tightness of the ligand and the protein in bound complexes Docking and scoring algorithms are combined to detect the compounds with higher affinity ... the number of true hits found in the hit list respect to the total number of compounds in the hit list; and the enrichment factor (EF) is the hit rate divided by the total number of hits in the...
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Biointormatics of targeted therapeutics and applications in drug discovery
... targeted therapeutics included in TTD will facilitate target and drug discovery The aim of updating TTD is to make it into a more useful target and drug discovery resource in complement to other ... enter the next 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 ... have been injected into drug discovery, in the hope of finding new drugs Statistics show that R&D expenditures in pharmaceutical industry has been growing at an annual growth of 13% since 1970,...
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Pharmacokinetics pharmacodynamics driven approach for lead optimization in anti mycobacterial and anti malarial drug discovery
... lactone) Biguanides Diaminopyrimidines Antimalarial drug Quinine (Cinchona alkaloids) Quinidine Mefloquine Halofantrine Benflumetol (Lumefantrine) Chloroquine Amodiaquine Pyronaridine Primaquine ... causing inhibition of nucleic acid and adenosine triphosphate synthesis Inhibits early stages of protein synthesis similar to macrolides Inhibitors of aminoacyl-tRNA binding during protein synthesis ... Infected female Anopheles mosquitos transmit the parasites to humans The mosquitos inject sporozoites into the bloodstream of the human host These sporozoites reach to the liver and rapidly invade...
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Implementation of a drug discovery tool for the evaluation of anti fibrotic compounds application in fibrovascular disorders
... the instrument for the fluorescence measurement: Reading direction: FLUOstar offers the flexibility in the reading direction: top-top, top-bottom, bottombottom, bottom-top (the first referred to ... engineering The presence of collagen fibrils in tissue constructs is essential in maintaining the mechanical strength and defining the shape and form of the tissues Unfortunately, due to the ... referred to the excitation source point and the latter referred to the emission reading point) After optimization, top-bottom and top-top reading direction offered the best reading for the experimental...
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Human embryonic stem cells as a cellular model for osteogenesis in implant testing and drug discovery
... mounting (containing Dapi, Invitrogen) was performed to stain the nucleus Staining was examined under fluorescent microscope (Olympus IX70, Tokyo, Japan) 2.1.6 Teratoma formation and staining ... molecular implants These included substituted purines, pyrimidines, indoles, quinazolines, pyrazines, pyrrolopyrimidines, pyrazolopyrimidines, phthalazines, pyridazines and quinoxalines[55] High-throughput ... differentiation into osteoblast lineage is still unknown, either from murine or human origin In this study, we investigated the efficiency of purmorphamine in differentiating human embryonic stem cell into...
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