Patent review.

abstract：:Arylamine N-acetyltransferases (NATs) are a family of enzymes found in eukaryotes and prokaryotes. While the precise endogenous function of NAT remains unknown for most organisms, recent evidence has shown that the expression of human NAT1 is up-regulated in estrogen receptor positive breast cancer. Additionally, NAT ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Westwood IM,Kawamura A,Russell AJ,Sandy J,Davies SG,Sim E

更新日期：2011-02-01 00:00:00

abstract：:African trypanosomes are extracellular blood parasites that cause sleeping sickness in humans and Nagana in cattle. The therapeutics used to control and treat these diseases are very ineffective and thus, the development of new drugs is urgently needed. We have previously suggested to use trypanosome-specific RNA apta...

journal_title：Combinatorial chemistry & high throughput screening

authors： Homann M,Lorger M,Engstler M,Zacharias M,Göringer HU

更新日期：2006-08-01 00:00:00

abstract：:The GoLoco motif is a short Galpha-binding polypeptide sequence. It is often found in proteins that regulate cell-surface receptor signaling, such as RGS12, as well as in proteins that regulate mitotic spindle orientation and force generation during cell division, such as GPSM2/LGN. Here, we describe a high throughput...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kimple AJ,Yasgar A,Hughes M,Jadhav A,Willard FS,Muller RE,Austin CP,Inglese J,Ibeanu GC,Siderovski DP,Simeonov A

更新日期：2008-06-01 00:00:00

abstract：:Crucial to the success of directed evolution of enantioselective enzymes for use as catalysts in synthetic organic chemistry is the availability of high-throughput assays for determining the enantiopurity of thousands of samples. Although several such ee-assays are available, they entail time and effort, which means t...

journal_title：Combinatorial chemistry & high throughput screening

authors： Reetz MT,Wang LW

更新日期：2006-05-01 00:00:00

abstract：:There is increasing evidence that redox regulation of transcription, particularly activator protein-1 (AP-1) and nuclear factor kappa B (NF-kappaB), is important in inflammatory diseases. Human thioredoxin (TRX), a member of the oxidoreductase superfamily, was initially identified, as a factor which augments the produ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Eguchi M,McMillan M,Nguyen C,Teo JL,Chi EY,Henderson WR Jr,Kahn M

更新日期：2003-11-01 00:00:00

abstract：:The Emory Chemical Biology Discovery Center (ECBDC) aims to accelerate high throughput biology and translation of biomedical research discoveries into therapeutic targets and future medicines by providing high throughput research platforms to scientific collaborators worldwide. ECBDC research is focused at the interfa...

journal_title：Combinatorial chemistry & high throughput screening

authors： Johns MA,Meyerkord-Belton CL,Du Y,Fu H

更新日期：2014-03-01 00:00:00

abstract：:Among the chemometric tools used in rational drug design, we find artificial neural network methods (ANNs), a statistical learning algorithm similar to the human brain, to be quite powerful. Some ANN applications use biological and molecular data of the training series that are inserted to ensure the machine learning,...

journal_title：Combinatorial chemistry & high throughput screening

authors： Scotti L,Ishiki H,Mendonça Júnior FJ,da Silva MS,Scotti MT

更新日期：2015-01-01 00:00:00

abstract：AIM AND OBJECTIVE:The Dendrobium officinalis flower (DOF) is popular in China due to common belief in its anti-aging properties and positive effects on "nourish yin". However, there have been relatively few confirmatory pharmacological experiments conducted to date. The aim of this work was to evaluate whether DOF has ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Li LZ,Lei SS,Li B,Zhou FC,Chen YH,Su J,Lv GY,Chen SH

更新日期：2020-01-01 00:00:00

abstract：:Cell-based screening using phenotypic assays is a useful means of identifying bioactive chemicals for use as tools to elucidate complex cellular processes. However, the chemicals must display sufficient selectivity and their targets have to be identified. We describe how cell-based screening assays can be designed to ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Schriemer DC,Kemmer D,Roberge M

更新日期：2008-09-01 00:00:00

abstract：:For years, the physicochemical properties of drug candidates have been used to predict their in vivo pharmacokinetic behaviors. Several theories and empirical correlations have been established by various researchers with the overall goal of expediting the drug candidate selection process, with greater confidence and ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Chiang PC,Hu Y

更新日期：2009-03-01 00:00:00

abstract：:Cyclic peptides have been often utilized as metabolically stable, conformationally restricted mimics of different kinds of biologically active peptides, including peptide antibiotics, endogenous opioid peptides, integrin inhibitors, peptide hormones, anticancer peptides, and so on. And in particular, cyclic compounds ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Gentilucci L,Cardillo G,Tolomelli A,Squassabia F,De Marco R,Chiriano G

更新日期：2009-12-01 00:00:00

abstract：BACKGROUND:The fruit pulp decoction of Crescentia cujete, commonly known as calabash, is traditionally used for the treatment of several respiratory diseases and is available as syrup formulations. Unfortunately, there is no detailed investigation on analytical methods for warranting the quality of these products. AIM...

journal_title：Combinatorial chemistry & high throughput screening

authors： Rivera-Mondragón A,Caballero-George C,Pieters L,Foubert K

更新日期：2020-12-06 00:00:00

abstract：:Generation of in vitro cellular assays using fluorescence measurements at heterologously expressed NMDA receptors would speed up the process of ligand characterization and enable high-throughput screening. The major drawback to the development of such assays is the cytotoxicity caused by Ca(2+)-flux into the cell via ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Hansen KB,Bräuner-Osborne H,Egebjerg J

更新日期：2008-05-01 00:00:00

abstract：:This review describes the design process from conception through realisation and optimisation of a minibody'--a minimised antibody. The result was a proteinaceous molecule of novel fold and metal binding activity. We explain how combinatorial approaches, using phage display libraries, were used to randomise loop regio...

journal_title：Combinatorial chemistry & high throughput screening

authors： Vaughan CK,Sollazzo M

更新日期：2001-08-01 00:00:00

abstract：:Cervical cancer is the second largest form of cancer to infest the leading cause of death in women worldwide. There are many causes of cancer but viruses are the most common among them. Human papillomaviruses (HPVs) are found to be the causative organism in almost 99.7% of the cases. HPV16 is the most frequent HPV typ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Choudhury AD,Choudhury MD,Chetia P,Chowdhury A,Talukdar AD

更新日期：2014-01-01 00:00:00

abstract：:Therapeutic options for many infections are extremely limited and at crisis point. We run the risk of entering a second pre-antibiotic era. There had been no miracle drug for the patients infected by resistant microbial pathogens. Most of the very few new drugs under development have problems with their toxicity, or p...

journal_title：Combinatorial chemistry & high throughput screening

authors： Phougat N,Khatri S,Singh A,Dangi M,Kumar M,Dabur R,Chhillar AK

更新日期：2014-01-01 00:00:00

abstract：BACKGROUND:Lead (Pb) remains a common contaminant in the environment in many parts of the world. Pb exposure adversely affects many human organs, including the gonads, via oxidant and inflammatory marker propagation in affected tissues. Moringa oleifera leaf extract (MOE) is a rich source of antioxidants reported to ha...

journal_title：Combinatorial chemistry & high throughput screening

authors： Albasher G,Alrajhi R,Alshammry E,Almeer R

更新日期：2020-09-23 00:00:00

abstract：:The molecular recognition behaviors of some representative bile salts by three 3,6'-bridged beta-cyclodextrin dimers with oligo(ethylenediamino) linkers in different lengths, i.e. 3,6'-(ethylenediamino-bridged) beta-cyclodextrin dimer (1), 3,6'-(diethylenetriamino-bridged) beta-cyclodextrin dimer (2), and 3,6'-(trieth...

journal_title：Combinatorial chemistry & high throughput screening

authors： Liu Y,Kang S,Chen Y,Cao R,Shi J

更新日期：2007-06-01 00:00:00

abstract：:Trivalent lanthanide ions (Ln(3+)) doped inorganic nanocrystals (NCs) have currently attracted reviving interest and come to the forefront in nanophotonics owing to their potential applications in diverse fields such as luminescent biodetection and bioimaging. As an alternative to conventional biolabels, Ln(3+)-doped ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Ju Q,Tu D,Liu Y,Zhu H,Chen X

更新日期：2012-08-01 00:00:00

abstract：:Lipopolysaccharides (LPS), otherwise termed 'endotoxins', are outer-membrane constituents of Gram-negative bacteria. Lipopolysaccharides play a key role in the pathogenesis of 'Septic Shock', a major cause of mortality in the critically ill patient. Therapeutic options aimed at limiting downstream systemic inflammator...

journal_title：Combinatorial chemistry & high throughput screening

authors： Wood SJ,Miller KA,David SA

更新日期：2004-05-01 00:00:00

abstract：AIM AND OBJECTIVE:To determine the mechanisms present in the etiopathogenesis of nasal polyposis. It is not clear whether amino acids contribute in a causal way to the development of the disease. Therefore, the aim of this study was to determine the plasma-free amino acid profile in patients with nasal polyposis and to...

journal_title：Combinatorial chemistry & high throughput screening

authors： Celik M,Şen A,Koyuncu İ,Gönel A

更新日期：2019-01-01 00:00:00

abstract：:Due to the numerous challenges in hit identification from random RNAi screening, we have examined current practices with a discovery of a variety of methodologies employed and published in many reports; majority of them, unfortunately, do not address the minimum associated criteria for hit nomination, as this could po...

journal_title：Combinatorial chemistry & high throughput screening

authors： Bhinder B,Djaballah H

更新日期：2012-11-01 00:00:00

abstract：:G protein-coupled receptors (GPCRs) are signaling molecules with a wide variety of skills. Members of this large family of membrane protein have been shown to regulate the activities of the different signaling pathways of the ligand specific manner. α2-adrenoceptors (α2-ARs) are one of the GPCRs and the stimulation of...

journal_title：Combinatorial chemistry & high throughput screening

authors： Yang H,He L,Yan M,He JG,Yu T

更新日期：2013-06-28 00:00:00

abstract：:The high level of attrition of drugs in clinical development has led pharmaceutical companies to increase the efficiency of their lead identification and development through techniques such as combinatorial chemistry and high-throughput (HTP) screening. Since the major reasons for clinical drug candidate failure other...

journal_title：Combinatorial chemistry & high throughput screening

authors： Shearer TW,Smith KS,Diaz D,Asher C,Ramirez J

更新日期：2005-02-01 00:00:00

abstract：:Protein Kinase C βII (PKCβII) overexpression has been linked to various diabetic microvascular complications viz. retinopathy, neuropathy, and cardiomyopathy. Novel and potent small molecules with preferential selective inhibitory property of PKCβII will be helpful in treatment as well as understanding insight of PKCβ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Grewal BK,Sobhia ME

更新日期：2014-01-01 00:00:00

abstract：AIM AND OBJECTIVE:The present method is simple, green and highly efficient for the synthesis of 2-amino-4H-pyran derivatives which are achieved by a one pot three component cyclocondensation of aldehyde, malanonitrile and ethyl acetoacetate or methyl acetoacetate using DABCO under solvent free with grinding conditions ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Waghmare AS,Pandit SS,Suryawanshi DM

更新日期：2018-01-01 00:00:00

abstract：BACKGROUND:Diabetes mellitus is one of the most common endocrine metabolic disorder diseases. The application of herbal medicine to control glucose levels and improve insulin action might be a useful approach in the treatment of diabetes. Mulberry leaves (ML) has been reported to exert important activities of anti-diab...

journal_title：Combinatorial chemistry & high throughput screening

authors： Wu Q,Hu Y

更新日期：2020-09-13 00:00:00

abstract：:The recent success of the human genome project and the continued accomplishment in obtaining DNA sequences for a vast array of organisms is providing an unprecedented wealth of information. Nevertheless, an abundance of the proteome contains hypothetical proteins or proteins of unknown function, where high throughput ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Powers R

更新日期：2007-09-01 00:00:00

abstract：:Two approaches were utilized to increase the throughput of pulsed ultrafiltration assays of ligand binding to human serum albumin, reducing the volume of the ultrafiltration chamber and combining pulsed ultrafiltration with high performance liquid chromatography-atmospheric pressure chemical ionization mass spectromet...

journal_title：Combinatorial chemistry & high throughput screening

authors： Gu C,Nikolic D,Lai J,Xu X,van Breemen RB

更新日期：1999-12-01 00:00:00

abstract：:We have developed high throughput fluorescence cell imaging methods to screen chemical libraries for compounds with effects on diverse aspects of cell physiology. We describe screens for compounds that arrest cells in mitosis, that block cell migration, and that block the secretory pathway. Each of these screens yield...

journal_title：Combinatorial chemistry & high throughput screening

authors： Yarrow JC,Feng Y,Perlman ZE,Kirchhausen T,Mitchison TJ

更新日期：2003-06-01 00:00:00