Structural Exploration of Synthetic Chromones as Selective MAO-B Inhibitors: A Mini Review.

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：: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：: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 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：: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：: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：BACKGROUND:Topological indices have numerous implementations in chemistry, biology and in lot of other areas. It is a real number associated to a graph, which provides information about its physical and chemical properties and their correlations. For a connected graph H, the degree distance defined as DD(H)=∑_(\{h_1,h_...

journal_title：Combinatorial chemistry & high throughput screening

authors： Imran M,Akhtar S,Ahmad U,Ahmad S,Bilal A

更新日期：2020-12-24 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：: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：INTRODUCTION:Enzymatic degradation of peptidoglycan, a structural cell wall component of Gram-positive bacteria, has attracted considerable attention being a specific target for many known antibiotics. METHODS:Peptidoglycan hydrolases are involved in bacterial lysis through peptidoglycan degradation. β-N-acetylglucosa...

journal_title：Combinatorial chemistry & high throughput screening

authors： Rathee A,Panwar A,Kumari S,Chhibber S,Kumar A

更新日期：2020-11-03 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：:In pursuit of utilizing combinatorial peptide libraries on beads, rapid and robust screening is one of the key steps for the success of high-throughput process. We have introduced improved structural features that greatly facilitate a MALDI-MS/MS-based sequencing, associated with easy and fast synthesis and analysis o...

journal_title：Combinatorial chemistry & high throughput screening

authors： Jee JE,Ang YL,Cha J,Ang MW,Ling J,Lim J,Lee SS

更新日期：2014-01-01 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：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：: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：:As HTS technologies come of age, pharmaceutical companies are focusing increasingly on the quality of their screening collections. Storage conditions and their influence on compound stability and solubility are debated intensely. At Novartis, a strategy was developed that is different to most other companies: (1) comp...

journal_title：Combinatorial chemistry & high throughput screening

authors： Schopfer U,Engeloch C,Stanek J,Girod M,Schuffenhauer A,Jacoby E,Acklin P

更新日期：2005-09-01 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：:Mitochondria are the center of metabolism and the critical role of aberrant mitochondrial fission in the onset and progression of a wide range of human diseases such as neurodegenerative disorders, cardiovascular disease, ischemic stroke and diabetes, is slowly becoming recognized. Under physiological conditions, mito...

journal_title：Combinatorial chemistry & high throughput screening

authors： Hanumanthappa P,Rajanikant GK

更新日期：2014-01-01 00:00:00

abstract：:Virtual screening encompasses a wide range of computational approaches aimed at the high-throughput, cost-efficient exploration of chemical libraries or databases to discover new bioactive compounds or novel medical indications of known drugs. Here, we have performed a systematic comparison of the performance of a lar...

journal_title：Combinatorial chemistry & high throughput screening

authors： Di Ianni ME,Gantner ME,Ruiz ME,Castro EA,Bruno-Blanch LE,Talevi A

更新日期：2015-01-01 00:00:00

abstract：:Over the last years microarray technology has become one of the principal platform technologies for the high-throughput analysis of biological systems. Starting with the construction of first DNA microarrays in the 1990s, microarray technology has flourished in the last years and many different new formats have been d...

journal_title：Combinatorial chemistry & high throughput screening

authors： Sobek J,Bartscherer K,Jacob A,Hoheisel JD,Angenendt P

更新日期：2006-06-01 00:00:00

abstract：:A new multicomponent domino reaction for rapid and regioselective synthesis of highly functionalized benzo[h]naphtho[2,3-a]acridine-15,16(5H,14H)-diones has been established. The reaction can be conducted by using readily available and inexpensive substrates under microwave irradiation. The procedures are facile, avoi...

journal_title：Combinatorial chemistry & high throughput screening

authors： Wang SL,Zhang G,Jie D,Jiang B,Wang XH,Tu SJ

更新日期：2012-06-01 00:00:00

abstract：:Building accurate quantitative structure-activity relationships (QSAR) is important in drug design, environmental modeling, toxicology, and chemical property prediction. QSAR methods can be utilized to solve mainly two types of problems viz., pattern recognition, (or classification) where output is discrete (i.e. clas...

journal_title：Combinatorial chemistry & high throughput screening

authors： Kulkarni AJ,Jayaraman VK,Kulkarni BD

更新日期：2009-05-01 00:00:00

abstract：AIM AND OBJECTIVE:In the past decade, the drug design technologies have been improved enormously. The computer-aided drug design (CADD) has played an important role in analysis and prediction in drug development, which makes the procedure more economical and efficient. However, computation with big data, such as ZINC c...

journal_title：Combinatorial chemistry & high throughput screening

authors： Hua GJ,Hung CL,Tang CY

更新日期：2018-01-01 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：: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：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：: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：: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：:Clinical application of viral vectors is often hampered by the lack of selectivity of viral particles for the targeted tissue. This drawback decreases the efficiency of gene delivery and raises safety concerns. We successfully established a novel in vitro evolution protocol to engineer adeno-associated virus vectors w...

journal_title：Combinatorial chemistry & high throughput screening

authors： Märsch S,Huber A,Hallek M,Büning H,Perabo L

更新日期：2010-11-01 00:00:00

abstract：:Protein methyltransferases (PMTs) orchestrate epigenetic modifications through post-translational methylation of various protein substrates including histones. Since dysregulation of this process is widely implicated in many cancers, it is of pertinent interest to screen inhibitors of PMTs, as they offer novel target-...

journal_title：Combinatorial chemistry & high throughput screening

authors： Ibanez G,Shum D,Blum G,Bhinder B,Radu C,Antczak C,Luo M,Djaballah H

更新日期：2012-06-01 00:00:00