The Emory Chemical Biology Discovery Center: leveraging academic innovation to advance novel targets through HTS and beyond.

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：:Organic reactions performed in the absence of solvent in domestic ovens without appropriate temperature control are generally considered as not reproducible, particularly when different instruments are used. For this reason, reproducibility has historically been one of the major issues associated with Microwave-Assist...

journal_title：Combinatorial chemistry & high throughput screening

authors： Díaz-Ortiz A,de la Hoz A,Alcázar J,Carrillo JR,Herrero MA,Fontana A,Muñoz Jde M,Prieto P,de Cózar A

更新日期：2011-02-01 00:00:00

abstract：:The National Institute of Mental Health (NIMH) Psychoactive Drug Screening Program (PDSP) is a resource that provides free screening of novel compounds to academic investigators. This program differs from other public-sector screening programs in that compounds are screened against a large panel of transmembrane recep...

journal_title：Combinatorial chemistry & high throughput screening

authors： Jensen NH,Roth BL

更新日期：2008-07-01 00:00:00

abstract：:A three-component 3+2 cycloaddition reaction followed by Suzuki coupling reaction was carried out to synthesize a library of compounds using automation (parallel synthesizer). Scaffolds that are unexplored in literature were used for the synthesis of library. The iodo-triazoles formed by 3+2 cycloaddition reaction wer...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kavitha M,Mahipal B,Mainkar PS,Chandrasekhar S

更新日期：2013-09-01 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：:Whole Cell-matrix-assisted laser desorption/ionization-time-of-flight mass spectrometry (MALDI-TOF-MS) is an emerging sensitive technique for rapid typing of microorganisms, efficient screening of biocombinatorial libraries of natural compounds and the analysis of complex biological samples, as whole cells, subcellula...

journal_title：Combinatorial chemistry & high throughput screening

authors： Vater J,Gao X,Hitzeroth G,Wilde C,Franke P

更新日期：2003-09-01 00:00:00

abstract：:A method for producing tri- and tetrasubstituted ureas from carbamoyl imidazolium salts is presented. Carbamoyl imidazolium salts are prepared from the reaction of N,N carbonyldiimidazole (CDI) with secondary amines, followed by alkylation with iodomethane. These stable salts can be stored for extended periods and ar...

journal_title：Combinatorial chemistry & high throughput screening

authors： Batey RA,Shen M,Santhakumar V,Yoshina-Ishii C

更新日期：2002-05-01 00:00:00

abstract：:High Throughput experimentation has been well established as a tool in early stage catalyst development and catalyst and process scale-up today. One of the more challenging areas of catalytic research is polymer catalysis. The main difference with most non-polymer catalytic conversions is the fact that the product is ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Gruter GJ,Sipos L,Adrianus Dam M

更新日期：2012-02-01 00:00:00

abstract：:The aim of this study was to examine the anticancer activities and phytochemical profiles of Dicranum scoparium against HeLa cell lines. The bio-guided fractionation studies of dichloromethane extract have high antiproliferative activities. Fractions 7, 9, 19, 20 are rich source of unsaturated fatty acids, and- in the...

journal_title：Combinatorial chemistry & high throughput screening

authors： Abay G,Altun M,Koldaş S,Tüfekçi AR,Demirtas I

更新日期：2015-01-01 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：BACKGROUND:Thiazolidine compounds are known to show interesting pharmacological activity. In particular, they are used as antiseizure, fungicidal, anti-bacterial, antitubercular, antiinflammatory, antiamoebic, anti-diabetic and local anesthetic agents. Some of these compounds have also shown antiparkinsonism, antioxida...

journal_title：Combinatorial chemistry & high throughput screening

authors： Taherkhorsand H,Nikpassand M

更新日期：2018-01-01 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：:In the post-human genome-sequencing era, the availability of recombinant proteins has become crucial for the identification of proteins with therapeutic potential. Based upon bioinformatic coding predictions of the genes for putative secreted proteins, we established a high-throughput protein pipeline (HTPP) for the p...

journal_title：Combinatorial chemistry & high throughput screening

authors： Battle T,Antonsson B,Feger G,Besson D

更新日期：2006-11-01 00:00:00

abstract：:The Nobel Prize in Chemistry 1902 was given to Hermann Emil Fischer "in recognition of the extraordinary services he had rendered by his work on sugar and purine synthesis". This truly great chemist of all time named a group of bicyclic nitrogenous structures as purines, discovered the synthesis of glucose, fructose a...

journal_title：Combinatorial chemistry & high throughput screening

authors： Franzén R,Tois J

更新日期：2003-08-01 00:00:00

abstract：:The article describes the development of a robust pharmacophore model and the investigation of structure activity relationship analysis of 46 xanthine derivatives reported for DPP-IV inhibition using PHASE module of Schrodinger software. The present works also encompasses molecular interaction of 46 xanthine ligand th...

journal_title：Combinatorial chemistry & high throughput screening

authors： Agrawal R,Jain P,Dikshit SN,Bahare RS

更新日期：2013-05-01 00:00:00

abstract：AIM AND OBJECTIVE:This study was designed to explore the active compounds and significant pathways of Guizhi-Shaoyao-Zhimu decoction (GSZD) for treating diabetes mellitus using molecular docking combined with network pharmacology. MATERIALS AND METHODS:Chemical constituents of GSZD and diabetes-related target proteins...

journal_title：Combinatorial chemistry & high throughput screening

authors： Zhang Q,Li R,Peng W,Zhang M,Liu J,Wei S,Wang J,Wu C,Gao Y,Pu X

更新日期：2019-01-01 00:00:00

abstract：BACKGROUND:In recent years, Staphylococcus aureus have developed resistance to medicines used for the treatment of human infections. Therefore, the search for antibacterial agents of high potency against Staphylococcus aureus is of great concern. Peptide deformylase (PDF), a metalloprotease catalyzing the removal of a ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Liang L,Zhou Q,Hao Z,Wang F,Zhu Y,Lin Q,Gao J

更新日期：2018-01-01 00:00:00

abstract：AIMS AND OBJECTIVES:Secondary metabolism in marine organisms produces a diversity of biologically important natural compounds that are not present in terrestrial species. Sea cucumbers belong to the invertebrate Echinodermata and are famous for their nutraceutical, medical and food values. They are known for possession...

journal_title：Combinatorial chemistry & high throughput screening

authors： Khattab RA,Elbandy M,Lawrence A,Paget T,Rae-Rho J,Binnaser YS,Ali I

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

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：:Microwave-assisted Suzuki-Miyaura and Stille cross-coupling reactions for the synthesis of highly electron-rich and diversely functionalized biaryl intermediates are presented. Microwave-irradiation has been demonstrated to be a very powerful tool for performing difficult transition metal-catalyzed cross-coupling reac...

journal_title：Combinatorial chemistry & high throughput screening

authors： Appukkuttan P,Dehaen W,Van der Eycken E

更新日期：2007-11-01 00:00:00

abstract：:In the life cycle of hepatitis C virus (HCV), NS3/NS4A protease has been proved to play a vital role in the replication of the HCV virus. Narlaprevir and its derivatives, the inhibitors of NS3/NS4A, would be potentially developed as important anti-HCV drugs in the future. In this study, quantitative structure-activity...

journal_title：Combinatorial chemistry & high throughput screening

authors： Zhu J,Li Y,Yu H,Zhang L,Mao X,Hou T

更新日期：2012-07-01 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：:Combinatorial phage peptide libraries have been used to identify the ligands for specific target molecules. These libraries are also useful for identification of the specific substrates of various proteases. A substrate phage library has a random peptide sequence at the N-terminus of the phage coat protein and an addi...

journal_title：Combinatorial chemistry & high throughput screening

authors： Ohkubo S,Miyadera K,Sugimoto Y,Matsuo K,Wierzba K,Yamada Y

更新日期：2001-11-01 00:00:00

abstract：:Screening of phage display libraries allows rapid identification of peptides binding to a target. However, functional analysis of the phage sequences and their reproduction as soluble and stable peptides are often the most time-consuming part in the screening. We have used here intein-based peptide biosynthesis to pro...

journal_title：Combinatorial chemistry & high throughput screening

authors： Björklund M,Valtanen H,Savilahti H,Koivunen E

更新日期：2003-02-01 00:00:00

abstract：AIM AND OBJECTIVE:For the development of new class of anticancer agents, a series of novel 2-amino-3-cyanopyridine derivatives were designed from virtual screening with Glide program by setting Topoisomerase II as the target. MATERIALS AND METHODS:The top ranked ten molecules from the virtual screening were synthesize...

journal_title：Combinatorial chemistry & high throughput screening

authors： Dev S,Dhaneshwar SR,Mathew B

更新日期：2018-01-01 00:00:00

abstract：:Approximately 5-10% of all colorectal carcinomas arise from cancer predisposition syndromes caused by heterozygote germline mutations in post-replicative DNA mismatch repair (MMR) genes. In contrast to gastrointestinal polyposis syndromes, carcinomas in these patients do not occur on the background of increased number...

journal_title：Combinatorial chemistry & high throughput screening

authors： Merkelbach-Bruse S,Köse S,Losen I,Bosserhoff AK,Buettner R

更新日期：2000-12-01 00:00:00

abstract：:Embryonic stem cells, due to their self-renewal and pluripotency properties, can be used to repair damaged tissues and as an unlimited source of differentiated cells. Although stem cells represent an important opportunity for cell based therapy and small molecules screening (in the context of drug or target discovery)...

journal_title：Combinatorial chemistry & high throughput screening

authors： Jee J,Jeon H,Hwang D,Sommer P,Park Z,Cechetto J,Dorval T

更新日期：2012-09-01 00:00:00

abstract：:Genetic mutations/polymorphisms analyses play a great role in genetic and medical research, and clinical diagnosis. Most conventional methods for genetic assay are based on slab gel electrophoresis that is both labor-intensive and time-consuming. Recently, capillary electrophoresis (CE) has been used for genetic analy...

journal_title：Combinatorial chemistry & high throughput screening

authors： Ren J

更新日期：2000-02-01 00:00:00

abstract：:Polo-like kinase 1 (Plk1) is a decisive enzyme with its multifunctional activity in cell cycle progression especially mitosis. The over expression of Plk1 in broad spectrum of cancer types turns into a promising therapeutic target against cancer. In the present study, several ligand based pharmacophore models and atom...

journal_title：Combinatorial chemistry & high throughput screening

authors： Chekkara R,Gorla VR,Susithra E,Tenkayala SR

更新日期：2014-01-01 00:00:00