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Search Results: 1 - 10 of 9542 matches for " drug discovery "
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Olhando para trás: um novo caminho possível para a descoberta de drogas em psicofarmacologia
Shorter, Edward;
Revista de Psiquiatria do Rio Grande do Sul , 2004, DOI: 10.1590/S0101-81082004000200009
Abstract: the history of psychopharmacology is littered with type ii errors - the rejection of effective compounds in the specious belief that they were inefficacious because they had failed to beat placebo in a controlled trial. revisiting some of these drugs to establish their receptor profile, and then determining what patentable compounds now on the shelf match that profile, might represent a possible future pathway to drug discovery. this article looks at the special circumstances in which numerous potentially effective drugs were withdrawn in the united states.
HCS strategy targeting dysregulation of the VHL/HIF pathway for drug discovery  [PDF]
Bastien Cautain, Nuria de Pedro, Maria Mu?oz de Escalona, Jose R. Tormo, Olga Genilloud, Francisca Vicente
Advances in Bioscience and Biotechnology (ABB) , 2013, DOI: 10.4236/abb.2013.43053
Abstract:

One-third of top-selling drugs are derived from natural products. When only a fraction of the bioactive natural products diversity has been explored, huge opportunities still remain for discovering novel leads for the development of new drugs. Clear cell renal cell carcinoma (ccRCC) is a highly vascular tumour arising from epithelial elements. Mutations in the Von Hippel-Lindau (VHL) gene are responsible for VHL disease and arise in the majority of Renal Cell Carcinoma (RCC) as well as in other types of cancer. Renal carcinoma cell lines with naturally occurring VHL mutations (RCC4 VA) and their genetically matched wild-type VHL (RCC4 VHL) counterparts were seeded onto 96-well plates and allowed to attach overnight. Fungal extracts were tested on both cell lines. Clinically useful antitumor agents were used as positive controls and as reference points to establish the efficacy and selectivity of the new compounds. Renal cell carcinoma cell lines expressing VHL or not were treated with Carboxyfluorescein succinimidyl ester (CFSE). The day after cell inoculation, extracts were added and during the following days of incubation, fluorescence intensity was measured as a surrogate marker for cell viability. The most promising extracts selectively inhibited growth of pVHL-defi- cient cells but not of wild-type VHL cells. We used High Content Bio-imaging, a complete cellular imaging workflow that integrates instruments and software to acquire and analyze images, to evaluate their effect. Cell imaging can reveal effects that would be overlooked by other cell assay approaches. This target-based whole cell screen is a new strategy, which ensures cell permeability and target selectivity especially in natural product screening where natural product purification is a labour of extensive work. This approach permitted a dynamic study where fluorescence was measured without affecting cell viability and enabling a better detection of cytotoxic effects such as autophagy, senescence or late apoptosis.

Strategizing the Development of Alzheimer’s Therapeutics  [PDF]
Justin Davis, Robin Couch
Advances in Alzheimer's Disease (AAD) , 2014, DOI: 10.4236/aad.2014.33011
Abstract: Alzheimer’s Disease is a complex, progressive condition with symptoms that do not reveal themselves until significant changes to neuronal morphology have already occurred. The delayed manifestation of cognitive decline makes determination of the true etiological origins difficult. As a result, identification of ideal drug targets becomes seemingly impossible. The existing treatments for Alzheimer’s Disease may temporarily suppress the rate of cognitive decline, but do little to slow or halt neuronal decay. While many believe that the current approaches to identifying a cure for the disease are too narrow-minded, focusing heavily on the physical manifestations of the diseased brain such as amyloid plaques and neurofibrillary tangles, this review asserts the status of Alzheimer’s research as rational and multi-faceted.
Small Molecule Inhibitors as Countermeasures for Botulinum Neurotoxin Intoxication
Bing Li,Norton P. Peet,Michelle M. Butler,James C. Burnett,Donald T. Moir,Terry L. Bowlin
Molecules , 2011, DOI: 10.3390/molecules16010202
Abstract: Botulinum neurotoxins (BoNTs) are the most potent of known toxins and are listed as category A biothreat agents by the U.S. CDC. The BoNT-mediated proteolysis of SNARE proteins inhibits the exocytosis of acetylcholine into neuromuscular junctions, leading to life-threatening flaccid paralysis. Currently, the only therapy for BoNT intoxication (which results in the disease state botulism) includes experimental preventative antibodies and long-term supportive care. Therefore, there is an urgent need to identify and develop inhibitors that will serve as both prophylactic agents and post-exposure ‘rescue’ therapeutics. This review focuses on recent progress to discover and develop small molecule inhibitors as therapeutic countermeasures for BoNT intoxication.
In Vivo magnetic resonance techniques and drug discovery
Beckmann, Nicolau;
Brazilian Journal of Physics , 2006, DOI: 10.1590/S0103-97332006000100006
Abstract: the long and resource intensive process of drug discovery and development is confronted with the basic challenge of providing effective and safe therapies at reasonably low costs. the better the mechanism of a disease is known, the higher the probability to find an appropriate therapy. also, the better and earlier a disease can be diagnosed and characterized, the higher the chance to be able to interfere in this process with a chemical entity. this reasoning sets the framework for the use of imaging in drug discovery. we discuss the relevance of magnetic resonance imaging and spectroscopy to derive anatomical, functional, metabolic and target-related information in the context of pharmacological research in vivo.
CURRENT TRENDS IN DRUG DISCOVERY: TARGET IDENTIFICATION TO CLINICAL DEVELOPMENT OF THE DRUG
Athar Mohd,Das Amar Jyoti
International Research Journal of Pharmacy , 2012,
Abstract: The practice of the drug discovery process has been revolutionized with the involvement of some newer techniques. Target based drug design is more advantageous, time consuming and effective. With the use of High Throughput Screening (HTS) technique a large number of compounds screened for their biological activity with the discovered)) target, which are synthesized by combinatorial chemistry, these are called hits. Quantitative Structure Activity Relationships (QSAR) constitutes immense importance in discovering new drug candidate called analogues which shows high affinity with the target. Various advanced techniques and Modern research disciplines such as genomics, proteomics, metabolomics, chemogenomics, and others improve the quality of the drug discovery process. The main objective of this article is to highlight the steps and trends followed in drug discovery process and also to understand the mechanism for searching the ailment of disease.
ANTIBACTERIAL AND PHYTOCHEMICAL EVALUATION OF HARUNGANA MADAGASCARIENSIS L (HYPERICACEAE) SEEDS
Afieroho O.E.,Izontimi Susan S.,Okoroafor Dorcas O.,Caleb Blessing
International Research Journal of Pharmacy , 2012,
Abstract: Clinical cases of resistance to orthodox drugs are on the rise. Medicinal plants are a source of lead compounds in drug discovery. Harungana madagascariensis is known for its ethno medicinal uses in the treatment of dysentery and related bacterial infections. In view of this, investigating its antibacterial drug lead potential is an imperative .The crude methanol extract of the fresh seeds was fractionated with n-hexane, chloroform, ethyl acetate and acetone successively. Agar dilution method was used for the antibacterial evaluation with clinical and ATCC strains of .E. coli and S.aureus as test microorganisms. Phytochemical methods were by using standard phytochemical screening reagents.The Chloroform fraction was the most active against the test pathogenic organisms with observed minimum inhibitory concentration MIC trend: chloroform (0.03125 mg/ml) > ethyl acetate (0.50000 mg/ml). Anthraquinones were found only in the most active chloroform fraction with some amount of flavonoids aglycones, and triterpenoids. This study showed that anthraquinones and/or flavonoids aglycones could be responsible for the antibacterial activity with possible synergistic effect from flavonoids and terpenoids. This further confirmed its ethnomedicinal uses.
PHARMACOGENOMICS AND ITS IMPACT ON DRUG DISCOVERY
Ashish Baldi,Yogendra Tailor
Journal of Global Pharma Technology , 2009, DOI: 10.1234/jgpt.v1i1.23
Abstract: Pharmacogenomics is derived from integration of genomics, medical, pharmacological and biotechnological principles to develop ideal, safe, efficacious drugs with personalized approach based on the genetic variations that exist in all human beings. It plays an important role in design and discovery of “future pharmaceuticals” through understanding of newer and specific target identification, better clinical trials, and individualized consideration of drug response and their genetic interactions. The present article will provide insights on pharmacogenomics and its role in development of target oriented personalized drugs based on genetic polymorphism.
In Vivo magnetic resonance techniques and drug discovery
Beckmann Nicolau
Brazilian Journal of Physics , 2006,
Abstract: The long and resource intensive process of drug discovery and development is confronted with the basic challenge of providing effective and safe therapies at reasonably low costs. The better the mechanism of a disease is known, the higher the probability to find an appropriate therapy. Also, the better and earlier a disease can be diagnosed and characterized, the higher the chance to be able to interfere in this process with a chemical entity. This reasoning sets the framework for the use of imaging in drug discovery. We discuss the relevance of magnetic resonance imaging and spectroscopy to derive anatomical, functional, metabolic and target-related information in the context of pharmacological research in vivo.
Application of Computer-Aided Drug Design to Traditional Chinese Medicine  [PDF]
Jie Yang
International Journal of Organic Chemistry (IJOC) , 2013, DOI: 10.4236/ijoc.2013.31A001
Abstract:

Computer-aided drug design (CADD) is an interdisciplinary subject, playing a pivotal role during new drug research and development, especially the discovery and optimization of lead compounds. Traditional Chinese Medicine (TCM) modernization is the only way of TCM development and also an effective approach to the development of new drugs and the discovery of potential drug targets (PDTs). Discovery and validation of PTDs has become the “bottle-neck” restricted new drug research and development and is urgently solved. Innovative drug research is of great significance and bright prospects. This paper mainly discusses the “druggability” and specificity of PTDs, the “druglikeness” of drug candidates, the methods and technologies of the discovery and validation of PTDs and their application. It is very important to achieve the invention and innovation strategy “from gene to drug”. In virtue of modern high-new technology, especially CADD, combined with TCM theory, research and develop TCM and initiate an innovating way fitting our country progress. This paper mainly discusses CADD and their application to drug research, especially TCM modernization.

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