Target identification strategies in chemical genetics.

abstract：:A general procedure for the synthesis of a large variety of compounds comprising an alpha, beta,-unsaturated carbonyl functionality was developed. The use of one-pot cascade synthesis with (triphenylphosphora-nylidene)ethenone as a versatile reagent for various formations including heterocycles of different ring sizes...

journal_title：Combinatorial chemistry & high throughput screening

authors： Westmana J,Orrling K

更新日期：2002-11-01 00:00:00

abstract：AIM AND OBJECTIVE:Thiazol-2-imine derivatives are interested for their pharmaceutical and biologic activities. A literature survey reveals that there have been no any reports on the synthesis of thiazol-2-imine derivatives without substituents in position C-4 and C-5 via one-pot reaction. Herein we report an efficient ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Nasiri F,Sabahi-Agabager L

更新日期：2017-01-01 00:00:00

abstract：:Unfavorable oral bioavailability is an important reason accounting for the failure of the drug candidates. Considering the lack of in vitro high-throughput screening assay for oral bioavailability, it is critical to develop in silico models for early predictions of oral bioavailability. In this review, we summarize pr...

journal_title：Combinatorial chemistry & high throughput screening

authors： Zhu J,Wang J,Yu H,Li Y,Hou T

更新日期：2011-06-01 00:00:00

abstract：:Phage display is a biological system which facilitates the cloning and rapid selection of peptides from large combinatorial libraries. In compa-rison to the chemical combinatorial approach, the advantages of phage display lie in its simplicity and replicability. While phage display has many diverse applications, this ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Andres CJ,Denhart DJ,Deshpande MS,Gillman KW

更新日期：1999-08-01 00:00:00

abstract：:The breast cancer resistant protein (BCRP) is an important transporter and its inhibitors play an important role in cancer treatment by improving the oral bioavailability as well as blood brain barrier (BBB) permeability of anticancer drugs. In this work, a computational model was developed to predict the compounds as...

journal_title：Combinatorial chemistry & high throughput screening

authors： Belekar V,Lingineni K,Garg P

更新日期：2015-01-01 00:00:00

abstract：AIM AND OBJECTIVE:In this work, we synthesized and characterized a novel Brönsted acidic ionic liquid from the reaction of N, N, N', N'-tetramethylethylenediamine with chlorosulfonic acid and explored its catalytic activity in 1, 8-dioxo-octahydroxanthenes synthesis. MATERIALS AND METHODS:Dimedone, aryl aldehydes, and...

journal_title：Combinatorial chemistry & high throughput screening

authors： Piralghar ZA,Hashemi MM,Ezabadi A

更新日期：2018-01-01 00:00:00

abstract：:Bacteriophage (phage) display has been exploited for the purpose of discovering new cancer specific targeting peptides. However, this approach has resulted in only a small number of tumor targeting peptides useful as in vivo imaging agents. We hypothesize that in vivo screening for tumor uptake of fluorescently tagged...

journal_title：Combinatorial chemistry & high throughput screening

authors： Newton-Northup JR,Figueroa SD,Deutscher SL

更新日期：2011-01-01 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：:In the present work, an analytical methodology based on molecularly imprinted solid-phase extraction (MISPE) has been developed for the determination of bisphenol A (BPA) in environmental and food samples. In order to select the optimum material, a combinatorial library of molecularly imprinted polymers in small-scale...

journal_title：Combinatorial chemistry & high throughput screening

authors： Martin-Esteban A,Tadeo JL

更新日期：2006-12-01 00:00:00

abstract：:Recently, we established a robust method for the detection of hybridization events using a DNA microarray deposited on a nanoporous membrane. Here, in a follow-up study, we demonstrate the performance of this approach on a larger set of LNA-modified oligoprobes and genomic DNA sequences. Twenty-six different LNA-modif...

journal_title：Combinatorial chemistry & high throughput screening

authors： Liu JP,Drungowski M,Nyársik L,Schwartz R,Lehrach H,Herwig R,Janitz M

更新日期：2007-05-01 00:00:00

abstract：BACKGROUND:The Rab family proteins are involved in membrane trafficking, cell growth and differentiation. Rab38 is implicated in the biogenesis of melanosomes that help in the synthesis, storage and transport of melanin pigments. The Rab38 protein is overexpressed at the RNA level in melanoma cancer. AIM AND OBJECTIVE...

journal_title：Combinatorial chemistry & high throughput screening

authors： Abdelmonsef AH,Dulapalli R,Dasari T,Padmarao LS,Mukkera T,Vuruputuri U

更新日期：2016-01-01 00:00:00

abstract：BACKGROUND:A set of antibiotic fluoroquinolones with confirmed antimicrobial activity were analyzed with the use of two types of quantum chemical calculation methods and quantitative structure-activity relationships (QSAR). OBJECTIVE:The purpose of this study was to demonstrate the common and differentiating character...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kawczak P,Bober L,Bączek T

更新日期：2018-01-01 00:00:00

abstract：:Centaurea solstitialis L. ssp. solstitialis (CSS) has been used as medicine for various diseases. In this work, root, stem and flower parts of the plant were separately extracted with methanol to execute bioassay-guided isolation. Antiproliferative activities of each extracts on C6 cells (Rat Brain tumor cells) and He...

journal_title：Combinatorial chemistry & high throughput screening

authors： Erenler R,Sen O,Yaglioglu AS,Demirtas I

更新日期：2016-01-01 00:00:00

abstract：:To meet growing needs for high throughput gene expression profiling, we established a new automated high throughput TaqMan RT-PCR method for quantitative mRNA expression analysis. In this method, the Allegro( trade mark ) (Zymark) system conducts all sample tracking and liquid handling steps, and ABI PRISM 7900 HT (Ap...

journal_title：Combinatorial chemistry & high throughput screening

authors： Pinhasov A,Mei J,Amaratunga D,Amato FA,Lu H,Kauffman J,Xin H,Brenneman DE,Johnson DL,Andrade-Gordon P,Ilyin SE

更新日期：2004-03-01 00:00:00

abstract：OBJECTIVE:Lung cancer is the most prevalent cancer in the world, and lung adenocarcinoma is the most common lung cancer subtype. Identification and determination of relevant prognostic markers are the key steps to personalized cancer management. METHODS:We collected the gene expression profiles from 265 tumor tissues ...

journal_title：Combinatorial chemistry & high throughput screening

authors： He ZH,Lv W,Wang LM,Wang YQ,Hu J

更新日期：2019-01-01 00:00:00

abstract：:Calcium (Ca(2+)) fluoroionophores are useful in cell-based functional assays of G-protein coupled receptor (GPCR) activation or ion channel modulation. In this paper we describe new calcium probes that improve or overcome certain deficiencies in existing probes. These new fluoroionophores are based on acylation of ami...

journal_title：Combinatorial chemistry & high throughput screening

authors： Gee KR,Rukavishnikov A,Rothe A

更新日期：2003-06-01 00:00:00

abstract：AIM AND OBJECTIVE:Avicularin has been found to inhibit the proliferation of HepG-2 cells in vitro in the screening of our laboratory. We intended to explain the molecular mechanism of this effect. Therefore, the combined methods of reverse molecular docking and network pharmacology were used in order to illuminate the ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Duan C,Li Y,Dong X,Xu W,Ma Y

更新日期：2019-01-01 00:00:00

abstract：AIM AND OBJECTIVE:MMP-13 belongs to a large family of proteases called matrix metalloproteinases (MMPs) that degrades type II collagen, the main structural protein of articular cartilage. The main pathologic role of MMP-13 over expression is to contribute to the development of osteoarthritis. METHODS:To find new inhib...

journal_title：Combinatorial chemistry & high throughput screening

authors： Ramezani M,Shamsara J

更新日期：2017-01-01 00:00:00

abstract：:A convenient one-pot, three-component reaction of aromatic aldehydes, 6-amino-1,3-dimethyluracil and active methylene compounds in the presence of Zr(HSO4)4 as a heterogeneous catalyst, under solvent-free conditions brings a very simple and highly efficient method for the preparation of pyrimido[4,5-b]quinolines, pyri...

journal_title：Combinatorial chemistry & high throughput screening

authors： Abdolmohammadi S,Balalaie S,Barari M,Rominger F

更新日期：2013-02-01 00:00:00

abstract：:The section on patent review will be focused in the areas of interest to the readers of CCHTS. The search was conducted using the following key words: combinatorial chemistry, high throughput screening, drug repurposing, chemical library, high content screening, drug discovery and natural products. All patents highlig...

journal_title：Combinatorial chemistry & high throughput screening

authors： Roy A

更新日期：2011-05-01 00:00:00

abstract：AIM AND OBJECTIVE:The importance of Chromeno[4,3-b]pyridines in bioactive compounds, highlighted the ongoing research on developing novel methods for the construction of this heterocyclic scaffold. Regarding the advantageous features of multi-component reactions in organic synthesis, we will try to synthesize pyridocou...

journal_title：Combinatorial chemistry & high throughput screening

authors： Nikookar H,Moghimi S,Sayahi MH,Mahdavi M,Ranjbar PR,Firoozpour L,Foroumadi A

更新日期：2018-01-01 00:00:00

abstract：:Gelatinase B/MMP-9 fulfills crucial regulator or effector functions in disease states and may be pharmacologically targeted by specific inhibitors. The characteristics of cleavages of a natural gelatinase B substrate were simulated and amino acids with zinc-ion chelating side-groups were employed to design a library o...

journal_title：Combinatorial chemistry & high throughput screening

authors： Hu J,Dubois V,Chaltin P,Fiten P,Dillen C,Van den Steen PE,Opdenakker G

更新日期：2006-09-01 00:00:00

abstract：:The appropriate selection of initial receptor structure has been the 'cornerstone' or foundation of successful structure-based virtual screening (SBVS), and plagued the structure-based design with a significantly practical problem to determine the major physiological states or important transition states of receptors ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Zhao Y,Wang H,Zang Y,Zhu X,Zhang S,Zhang L

更新日期：2020-11-10 00:00:00

abstract：:Recent studies have suggested that both constitutive androstane receptor (CAR) and pregnane X-receptor (PXR) are involved in the induction of rat liver microsomal cytochrome P-450 (CYP) 2B and 3A through a mechanism called cross-talk. In this study we intend to determine if a PXR-reporter gene assay could be used for ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Cui X,Thomas A,Montgomery D,Gu C,Morrison RA,White RE,Cheng KC

更新日期：2005-06-01 00:00:00

abstract：:Accurate classification of instances depends on identification and removal of redundant features. Classification of data having high dimensionality is usually performed in conjunction with an appropriate feature selection method. Feature selection enables identification of the most informative feature subset from the ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Patil D,Raj R,Shingade P,Kulkarni B,Jayaraman VK

更新日期：2009-06-01 00:00:00

abstract：:A pulsed ultrafiltration-mass spectrometric screening assay has been developed to generate and identify electrophilic metabolites of xenobiotic compounds formed by hepatic cytochrome P450 enzymes. This assay would be suitable for the early identification of potentially toxic compounds during the initial phase of drug ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Nikolic D,Fan PW,Bolton JL,van Breemen RB

更新日期：1999-06-01 00:00:00

abstract：:EGFR (ErbB-1/HER1) kinase plays an important role in cancer therapy. Two classification models were established to predict whether a compound is an inhibitor or a decoy of human EGFR (ErbR-1) by using Kohonen's self-organizing map (SOM) and support vector machine (SVM). A dataset containing 1248 ATP binding site inhib...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kong Y,Qu D,Chen X,Gong YN,Yan A

更新日期：2016-01-01 00:00:00

abstract：:As technologies for high throughput and high content screening continue to evolve, new platforms for quantitative cellular imaging will play an increasingly important role in identifying and profiling lead compounds. To gain insight into the effects of a compound on cell morphology or intracellular events, it is neces...

journal_title：Combinatorial chemistry & high throughput screening

authors： Elliott GS

更新日期：2009-11-01 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：: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