A method for rapid protease substrate evaluation and optimization.

abstract：BACKGROUND:ADAMTS (A disintegrin-like metalloproteinase with thrombospondin motifs) is a group of 19 zinc-dependent metalloproteases known to function in many pathological and physiological processes, such as adhesion, cell fusion, signaling, proteolysis and ECM degradation. OBJECTIVES:The aim of this study was to dem...

journal_title：Combinatorial chemistry & high throughput screening

authors： Tayman MA,Koyuncu İ,Köklü NÖ

更新日期：2020-01-01 00:00:00

abstract：:Sequential injection analysis (SIA) has been employed as the platform for the development of a high throughput automated assay for glutathione (GSH) in nutrition supplements. The proposed assay is based on the on-line formation of a UV-absorbing thioacrylate derivative (lambda(max) = 285 nm) upon reaction of thiol wit...

journal_title：Combinatorial chemistry & high throughput screening

authors： Zacharis CK,Tzanavaras PD

更新日期：2010-07-01 00:00:00

abstract：OBJECTIVE:Osteopontin (OPN), a phosphorylated sialoprotein, has been shown to overexpress in a variety of cancers and to contribute tumor progression and metastasis by increasing cell migration and adhesion. In the current study, we aimed to investigate the prognostic and predictive role of OPN in patients with advance...

journal_title：Combinatorial chemistry & high throughput screening

authors： Yazici O,Dogan M,Ozal G,Aktas SH,Demirkazik A,Utkan G,Senler FC,Icli F,Akbulut H

更新日期：2020-09-02 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：:Most essential functions are associated with various protein-protein interactions, particularly the cytokine-receptor interaction. Knowledge of the heterogeneous network of cytokine- receptor interactions provides insights into various human physiological functions. However, only a few studies are focused on the compu...

journal_title：Combinatorial chemistry & high throughput screening

authors： Wei L,Zou Q,Liao M,Lu H,Zhao Y

更新日期：2016-01-01 00:00:00

abstract：Aims & Objective:Corona Virus Disease 2019 (COVID-19) caused by the human coronavirus 2019 (HCoV-19, also known as SARS-CoV-2) infection is currently in a global outbreak. COVID-19 has posed a huge threat to public health and economic stability worldwide. CR3022, a human monoclonal neutralizing antibody isolated from a...

journal_title：Combinatorial chemistry & high throughput screening

authors： Yu W,Wu X,Ren J,Zhang X,Wang Y,Li C,Xu W,Li J,Li G,Zheng W,Liao H,Yuan X

更新日期：2020-10-26 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：:Structural genomics, structure-based analysis of gene products, has so far mainly concentrated on soluble proteins because of their less demanding requirements for overexpression, purification and crystallisation compared to membrane proteins. This so-called "low-hanging fruit" approach has generated more than 25,000 ...

journal_title：Combinatorial chemistry & high throughput screening

authors： Lundstrom K

更新日期：2004-08-01 00:00:00

abstract：:This paper aims to review recent developments in the synthesis of quinazolines and quinazolinone derivatives under conditions that include the application of microwave heating in the ring forming step. Recently, two reviews on the synthesis and chemistry of natural and synthetic quinazolines and quinazolinones have be...

journal_title：Combinatorial chemistry & high throughput screening

authors： Besson T,Chosson E

更新日期：2007-12-01 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：: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：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：: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：: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

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：:Direct renin inhibitors (DRIs) have increasingly shown a significant advantage in the treatment of hypertension and protection of target organs. In this paper, a series of azaindole class renin inhibitors were subjected to 3D-QSAR study using Topomer CoMFA. Five kinds of splitting mode for different fragment cutting a...

journal_title：Combinatorial chemistry & high throughput screening

authors： Xiang Y,Song J,Zhang Z

更新日期：2014-01-01 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：OBJECTIVE:The aim of this study areto screen MicroRNAs (miRNAs) related to the prognosis of lung adenocarcinoma (LUAD) and to explore the possible molecular mechanisms. METHODS:The data for a total of 535 patients with LUAD data were downloaded from The Cancer Genome Atlas (TCGA) database. The miRNAs for LUAD prognosi...

journal_title：Combinatorial chemistry & high throughput screening

authors： Wang W,Liu B,Duan X,Feng X,Wang T,Wang P,Ding M,Zhang Q,Feng F,Wu Y,Yao W,Wang Q,Yang Y

更新日期：2020-01-01 00:00:00

abstract：BACKGROUND:Clinical outcomes after rotator cuff repair associated with diabetes mellitus(DM) are generally favorable, but no study has attempted to establish the influence of DM on outcomes after rotator cuff repair. PURPOSE:To conduct a meta-analysis of clinical studies evaluating patient outcomes between people with...

journal_title：Combinatorial chemistry & high throughput screening

authors： Lu X,Sun H,Xu Y,Cao X

更新日期：2020-10-20 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：AIM AND OBJECTIVE:In ancient China, rice bran was used to treat diabetes and hyperlipidemia. The aim of this paper is to explore the active compounds and underlying mechanism of rice bran petroleum ether extracts (RBPE) against diabetes using network pharmacology. MATERIALS AND METHODS:Gas chromatography-mass spectrom...

journal_title：Combinatorial chemistry & high throughput screening

authors： Huang X,Zhang M,Wu H,Wang X,Xu F

更新日期：2020-08-21 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：:In recent years, combinatorial libraries have become a major tool for drug discovery and drug development. Along the way, one potential use of combinatorial chemistry libraries almost been neglected: the basic study of intermolecular interactions. Especially "one-bead-one-structure" libraries can be a powerful means f...

journal_title：Combinatorial chemistry & high throughput screening

authors： Nestler HP,Liu R

更新日期：1998-10-01 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：BACKGROUND:Corona Virus Disease 2019 (COVID-19) pandemic threatens patients, societies and healthcare systems around the world. There is an emergent need to search for possible medications. OBJECTIVE:This article intends to use virtual screening and molecular docking methods to find potential inhibitors that can respo...

journal_title：Combinatorial chemistry & high throughput screening

authors： Chtita S,Belhassan A,Aouidate A,Belaidi S,Bouachrine M,Lakhlifi T

更新日期：2020-07-30 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：: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：AIM AND OBJECTIVE:In the last decades, cancer has become a major problem in public health all around the globe. Chimeric chemical structures have been established as an important trend on medicinal chemistry in the last years. Thiazacridines are hybrid molecules composed of a thiazolidine and acridine nucleus, both pha...

journal_title：Combinatorial chemistry & high throughput screening

authors： Almeida ML,Viana DCF,da Costa VCM,Dos Santos FA,Pereira MC,Pitta MGR,de Melo Rêgo MJB,Pitta IR,Pitta MGR

更新日期：2020-01-01 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：: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