Novel small-molecule inhibitors of arylamine N-acetyltransferases: drug discovery by high-throughput screening.

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：: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：BACKGROUND:Considering the low ocular bioavailability of conventional formulations used for ocular bacterial infection treatment, there's a need for designing efficient novel drug delivery systems that may enhance of precorneal retention time and corneal permeability. AIM AND OBJECTIVE:The current research focuses on ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kırımlıoğlu GY,Özer S,Büyükköroğlu G,Yazan Y

更新日期：2020-04-27 00:00:00

abstract：:A comparative structure-affinity study of anthraquinone dyes adsorption on cellulose fibre is presented in this paper. We used receptor-dependent 4D-QSAR methods based on grid and neural (SOM) methodology coupled with IVEPLS procedure. The applied RD 4D-QSAR approach focuses mainly on the ability of mapping dye proper...

journal_title：Combinatorial chemistry & high throughput screening

authors： Bak A,Wyszomirski M,Magdziarz T,Smolinski A,Polanski J

更新日期：2014-01-01 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：: ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Huang T

更新日期：2019-01-01 00:00:00

abstract：:Fingerprint representations of molecular structure and properties were among the first computational tools for similarity searching and are widely applied to this date, which is in part due to their computational efficiency and ease-of-use. Moreover, despite their simplicity, 2D molecular fingerprints have been surpri...

journal_title：Combinatorial chemistry & high throughput screening

authors： Wang Y,Bajorath J

更新日期：2010-03-01 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：: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：AIMS AND OBJECTIVE:The infectious disease treatment remains a challenging concern owing to the increasing number of pathogenic microorganisms associated with resistance to multiple drugs. A promising approach for combating microbial infection is to combine two or more known bioactive heterocyclic pharmacophores in one ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Tratrat C

更新日期：2020-01-01 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：: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 review is to describe and to analyze the ingredients that are necessary in order to develop a robust and effective experimental approach for the high-throughput characterization of protein-nanostructured surface interaction. In the first part of this paper we review the nanostructured surface synthesis...

journal_title：Combinatorial chemistry & high throughput screening

authors： Scopelliti PE,Bongiorno G,Milani P

更新日期：2011-03-01 00:00:00

abstract：:4-Benzothiazol-2-ylamino-4-oxo-2-butenoic acid, prepared from reaction of 2-aminobenzothiazole and maleic anhydride, are used as an acid component in Passerini three-component reaction, under solvent-free media, to produce unsaturated α-benzothiazole acyloxyamides in good yields. ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Sheikholeslami-Farahani F,Shahvelayati AS

更新日期：2013-11-01 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：:We have developed a high throughput assay for the measurement of protease activity in solution. This technology will accelerate research in functional proteomics and enable biologists to streamline protease substrate evaluation and optimization. The peptide sequences that serve as protease substrates in this assay are...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kozlov IA,Melnyk PC,Zhao C,Hachmann JP,Shevchenko V,Srinivasan A,Barker DL,Lebl M

更新日期：2006-07-01 00:00:00

abstract：AIM AND OBJECTIVE:Antibiotic resistance is a serious constraint to the development of new effective antibacterials. Therefore, the discovery of the new antibacterials remains one of the main challenges in modern medicinal chemistry. This study was undertaken to identify novel molecules with antibacterial activity. MAT...

journal_title：Combinatorial chemistry & high throughput screening

authors： Ivanenkov YA,Yamidanov RS,Osterman IA,Sergiev PV,Aladinskiy VA,Aladinskaya AV,Terentiev VA,Veselov MS,Ayginin AA,Skvortsov DA,Komarova KS,Chemeris AV,Baimiev AK,Sofronova AA,Malyshev AS,Machulkin AE,Petrov RA,Bezrukov D

更新日期：2019-08-08 00:00:00

abstract：:Chromosome analysis has been a cornerstone both for the identification of genetic defects that predispose to a variety of genetic syndromes as well as for the analysis of cancer progression. The relatively low resolution of metaphase chromosomes, however, only allows characterization of major genetic events which are ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Cowell JK

更新日期：2004-09-01 00:00:00

abstract：BACKGROUND:Increasing the resistance issue has become the reason for the development of new antibacterial in crucial condition. Many ways are tracked to determine the most effective antibacterial agent. Some proteins that are a key role in bacteria metabolism are targeted, including MurA in cell wall biosynthesis and g...

journal_title：Combinatorial chemistry & high throughput screening

authors： Apriyanti E,Satari MH,Kurnia D

更新日期：2021-01-01 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：AIMS AND OBJECTIVE:Alzheimer's disease is now a most prevalent neuro degenerative disease of central nervous system leading to dementia in elderly aged population. Numerous pathological changes have been associated in the progression of Alzheimer's disease. One of such pathological hypothesis is declined cholinergic ac...

journal_title：Combinatorial chemistry & high throughput screening

authors： Macha B,Kulkarni R,Garige AK,Palabindala R,Akkinepally R,Garlapati A

更新日期：2020-12-10 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：AIM AND OBJECTIVE:Calculus Bovis (CB) has been employed to treat diseases for a long time. It has been identified to play significant anti-inflammatory and anti-tumor roles. However, the mechanism of treating primary liver cancer (PLC) remains to be revealed. This study aims to clarify the molecules and mechanisms of C...

journal_title：Combinatorial chemistry & high throughput screening

authors： Zhang Z,Zeng P,Gao W,Wu R,Deng T,Chen S,Tian X

更新日期：2021-01-01 00:00:00

abstract：:Shotgun phage display cloning is a useful tool for studying interactions between bacterial and host proteins. Libraries are constructed by cloning randomly fragmented prokaryotic DNA into phage mid-vectors. Theoretically, these libraries will consist of phages that together display all proteins encoded by the bacteria...

journal_title：Combinatorial chemistry & high throughput screening

authors： Jacobsson K,Frykberg L

更新日期：2001-04-01 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：:A biomimetic sensor is proposed as a promising new analytical method for determination of captopril in different classes of samples. The sensor was prepared by modifying a carbon paste electrode with iron (II) phthalocyanine bis(pyridine) [FePc(dipy)] complex. Amperometric measurements in a batch analytical mode were ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Wong A,Lanza MR,Sotomayor MD

更新日期：2010-09-01 00:00:00

abstract：:Chemical inhibitors have had a profound impact on many diverse fields of biology. The goal of chemical genetics is to use small molecules to perturb biological systems in a manner conceptually similar to traditional genetics. Key to the advancement of the chemical genetic paradigm is the further development of tools a...

journal_title：Combinatorial chemistry & high throughput screening

authors： Tochtrop GP,King RW

更新日期：2004-11-01 00:00:00

abstract：AIM AND OBJECTIVE:4-Hydroxyphenylpyruvate dioxygenase (HPPD), converting phydroxyphenylpyruvate (HPPA) to homogentisate (HGA), is an important target for treating type I tyrosinemia and synthesizing novel herbicides due to its significant role in tyrosine catabolism. Hence, it is imperative to design novel HPPD inhibit...

journal_title：Combinatorial chemistry & high throughput screening

authors： Fu Y,Sun YN,Cao HF,Yi KH,Zhao LX,Li JZ,Ye F

更新日期：2017-01-01 00:00:00

abstract：:The important factor which differentiates gemini surfactants from conventional monomeric surfactants is the spacer group. The molecular connectivity method was used to study the effect of the spacer group on critical micelle concentration of cationic gemini surfactants. Two models were derived employing only Kier and ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Mozrzymas A

更新日期：2016-01-01 00:00:00

abstract：:Recyclable ZnO nano-rods catalyst as a most efficient and straightforward protocol for one-pot, three-component synthesis of spirooxindole derivatives at room temperature under solvent-free conditions in both reaction media and work-up procedure is described. This method is of great value because of its environmentall...

journal_title：Combinatorial chemistry & high throughput screening

authors： Hosseini-Sarvari M,Tavakolian M

更新日期：2012-12-01 00:00:00