Journal of Biomolecular Screening最新文献

Long Noncoding RNAs CAT2064 and CAT2042 may Function as Diagnostic Biomarkers for Prostate Cancer by Affecting Target MicrorRNAs. 长非编码 RNA CAT2064 和 CAT2042 可通过影响目标微小 RNA 发挥前列腺癌诊断生物标志物的作用。

IF 1.5

Journal of Biomolecular Screening Pub Date : 2024-07-01 Epub Date: 2021-08-24 DOI: 10.1007/s12291-021-00999-6

Farzane Amirmahani, Nasim Ebrahimi, Rafee Habib Askandar, Marzieh Rasouli Eshkaftaki, Katayoun Fazeli, Michael R Hamblin

{"title":"Long Noncoding RNAs CAT2064 and CAT2042 may Function as Diagnostic Biomarkers for Prostate Cancer by Affecting Target MicrorRNAs.","authors":"Farzane Amirmahani, Nasim Ebrahimi, Rafee Habib Askandar, Marzieh Rasouli Eshkaftaki, Katayoun Fazeli, Michael R Hamblin","doi":"10.1007/s12291-021-00999-6","DOIUrl":"10.1007/s12291-021-00999-6","url":null,"abstract":"Prostate cancer (PCa) is the second most common cancer in men throughout the world, and the main cause of cancer death. Long noncoding RNAs (lncRNAs) act as crucial regulators in many human cancers. In this research, we measured the expression level of novel lncRNAs and their associated micro-RNAs (miRNAs) in PCa. In the present research, three lncRNAs were selected using the Mitranscriptome projec (CAT2064, CAT2042, and CAT2164.2). Samples of prostate tissue (20 PCa, and 20 BPH) and blood (14 PCa, and 14 BPH) were collected and the Real-time Quantitative Polymerase Chain Reaction (RT-qPCR) was used to measure the expression levels of the lncRNAs and their associated miRNAs. Based on our results, CAT2064 was significantly increased and CAT2042 was significantly decreased in human PCa tissue in comparison with BPH tissue. To discriminate PCa from BPH, CAT2064 (P < 0.05; 0.8750 AUC-ROC) showed a better potential as a diagnostic molecular biomarker compared to CAT2042 (P < 0.05; 0.8454 AUC-ROC). Furthermore, RT-qPCR results measured in blood samples from PCa patients showed a higher expression level of CAT2064 (P < 0.0001; AUC-ROC value of 0.8914) in comparison to CAT2042. CAT2064 and CAT2042 showed a positive correlation with the expression of miR-5095 and miR-1273a (r = 0.02885, 0.3202; P = 0.9413, 0.2266, respectively). CAT2064 and CAT2042 also had a negative correlation with miR-1304-3p and miR-1285-5p (r = - 0.3877, - 0.09330; P = 0.15, 0.7311, respectively). Collectively, CAT2064 and CAT2042 and their miRNA targets may constitute a regulatory network in PCa, and could serve as novel biomarkers.Supplementary information: The online version contains supplementary material available at 10.1007/s12291-021-00999-6.","PeriodicalId":15087,"journal":{"name":"Journal of Biomolecular Screening","volume":"6 1","pages":"322-330"},"PeriodicalIF":1.5,"publicationDate":"2024-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11239640/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87379283","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Novel Chemical Scaffolds for Inhibition of Rifamycin-Resistant RNA Polymerase Discovered from High-Throughput Screening. 高通量筛选发现抑制利福霉素耐药RNA聚合酶的新型化学支架。

Journal of Biomolecular Screening Pub Date : 2016-12-01 DOI: 10.1177/1087057116679994

N. Scharf, V. Molodtsov, A. Kontos, K. Murakami, G. Garcia

{"title":"Novel Chemical Scaffolds for Inhibition of Rifamycin-Resistant RNA Polymerase Discovered from High-Throughput Screening.","authors":"N. Scharf, V. Molodtsov, A. Kontos, K. Murakami, G. Garcia","doi":"10.1177/1087057116679994","DOIUrl":"https://doi.org/10.1177/1087057116679994","url":null,"abstract":"Rifampin has been a cornerstone of tuberculosis (TB) treatment since its introduction. The rise of multidrug-resistant and extensively drug-resistant TB makes the development of novel therapeutics effective against these strains an urgent need. Site-specific mutations in the target enzyme of rifampin, RNA polymerase (RNAP) comprises the majority (~97%) of rifamycin-resistant (RifR) strains of Mycobacterium tuberculosis (MTB). To identify novel inhibitors of bacterial RNAP, an in vitro plasmid-based transcription assay that uses malachite green (MG) to detect transcribed RNA containing MG aptamers was developed. This assay was optimized in a 384-well plate format and used to screen 150,000 compounds against an Escherichia coli homolog of the most clinically relevant RifR RNAP (βS531L) containing a mutation (β'V408G) that compensates for the fitness defect of this RifR mutant. Following confirmation and concentration-response studies, 10 compounds were identified with similar in vitro inhibition values across a panel of wild-type and RifR E. coli and MTB RNAPs. Four compounds identified from the screen are active against MTB in culture at concentrations below 200 µM. Initial follow-up has resulted in the elimination of one scaffold due to potential pan-assay interference.","PeriodicalId":15087,"journal":{"name":"Journal of Biomolecular Screening","volume":"1 1","pages":"1087057116679994"},"PeriodicalIF":0.0,"publicationDate":"2016-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1177/1087057116679994","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"65313127","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 5

Product Focus: Screening Robotics and Automation 产品重点:筛选机器人及自动化

Journal of Biomolecular Screening Pub Date : 2010-07-01 DOI: 10.1177/1087057110373266

P. Taylor

引用次数: 0

Product Focus: High-Content Screening and Imaging 产品重点:高含量筛选和成像

Journal of Biomolecular Screening Pub Date : 2010-05-28 DOI: 10.1177/1087057110368517

C. Hart

引用次数: 0

Optimizing the expression of recombinant alphabetagamma GABAA receptors in HEK293 cells for high-throughput screening. 优化重组alphabetagamma GABAA受体在HEK293细胞中的表达，进行高通量筛选。

Journal of Biomolecular Screening Pub Date : 2009-01-01 DOI: 10.1177/1087057108328017

Daniel Gilbert, Abolghasem Esmaeili, Joseph W Lynch

{"title":"Optimizing the expression of recombinant alphabetagamma GABAA receptors in HEK293 cells for high-throughput screening.","authors":"Daniel Gilbert, Abolghasem Esmaeili, Joseph W Lynch","doi":"10.1177/1087057108328017","DOIUrl":"https://doi.org/10.1177/1087057108328017","url":null,"abstract":"Despite being important clinical targets, it is not straightforward to reliably express recombinant trimeric alphabetagamma GABA-A receptors (GABA(A)Rs) for high-throughput screening. This study therefore sought to devise a simple and reliable means of transiently expressing alpha1beta1gamma1 and alpha1beta1gamma2 GABA(A)Rs in HEK293 cells. Expression efficiencies resulting from 5 different transfection strategies were assessed by flow cytometry and pharmacological analysis using an anion-sensitive yellow fluorescent protein-based assay. PolyFect and Effectene, employed according to the manufacturers' instructions, conferred the strongest and most reliable expression of trimeric alphabetagamma GABA(A)Rs. Functional analysis via the yellow fluorescent protein assay revealed dramatic differences in the pharmacological properties of gamma1- and gamma2-containing receptors, consistent with previous electrophysiological characterizations. The authors conclude that this method of expressing and screening recombinant GABA(A)Rs provides an effective means of discovering novel GABA(A)R modulators for use as therapeutic lead compounds and pharmacological probes.","PeriodicalId":15087,"journal":{"name":"Journal of Biomolecular Screening","volume":"14 1","pages":"86-91"},"PeriodicalIF":0.0,"publicationDate":"2009-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1177/1087057108328017","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"27948554","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 17

A high-throughput ligand competition binding assay for the androgen receptor and other nuclear receptors. 雄激素受体和其他核受体的高通量配体竞争结合测定。

Journal of Biomolecular Screening Pub Date : 2009-01-01 DOI: 10.1177/1087057108326662

Clémentine Féau, Leggy A Arnold, Aaron Kosinski, R Kiplin Guy

引用次数: 23

Genome-wide linkage analysis with clustered SNP markers. 聚类SNP标记的全基因组连锁分析。

Journal of Biomolecular Screening Pub Date : 2009-01-01 DOI: 10.1177/1087057108327327

Kaja K Selmer, Kristin Brandal, Ole K Olstad, Bård Birkenes, Dag E Undlien, Thore Egeland

{"title":"Genome-wide linkage analysis with clustered SNP markers.","authors":"Kaja K Selmer, Kristin Brandal, Ole K Olstad, Bård Birkenes, Dag E Undlien, Thore Egeland","doi":"10.1177/1087057108327327","DOIUrl":"https://doi.org/10.1177/1087057108327327","url":null,"abstract":"Single nucleotide polymorphisms (SNPs) have recently replaced microsatellites as the genetic markers of choice in linkage analysis, primarily because they are more abundant and the genotypes more amenable for automatic calling. One of the most recently launched linkage mapping sets (LMS) is the Applied Biosystems Human LMS 4K, which is a genome-wide linkage set based on the SNPlex technology and the use of clustered SNPs. In this article the authors report on their experience with this set and the associated genotyping software GeneMapper version 4.0, which they have used for linkage analyses in 17 moderate to large families with assumed monogenic disease. For comparison of methods, they also performed a genome-wide linkage analysis in 1 of the 17 families using the Affymetrix GeneChip Human Mapping 10K 2.0 array. The conclusion is that both methods performed technically well, with high call rates and comparable and low rates of Mendelian inconsistencies. However, genotyping is less automated in GeneMapper version 4.0 than in the Affymetrix software and thus more time consuming.","PeriodicalId":15087,"journal":{"name":"Journal of Biomolecular Screening","volume":"14 1","pages":"92-6"},"PeriodicalIF":0.0,"publicationDate":"2009-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1177/1087057108327327","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"27949028","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 12

High-throughput biochemical kinase selectivity assays: panel development and screening applications. 高通量生化激酶选择性测定:面板开发和筛选应用。

Journal of Biomolecular Screening Pub Date : 2009-01-01 Epub Date: 2008-12-10 DOI: 10.1177/1087057108326663

Amy Card, Chris Caldwell, Hyunsuk Min, Bina Lokchander, Hualin Xi, Simone Sciabola, Ajith V Kamath, Susan L Clugston, William R Tschantz, Leyu Wang, Deborah J Moshinsky

{"title":"High-throughput biochemical kinase selectivity assays: panel development and screening applications.","authors":"Amy Card, Chris Caldwell, Hyunsuk Min, Bina Lokchander, Hualin Xi, Simone Sciabola, Ajith V Kamath, Susan L Clugston, William R Tschantz, Leyu Wang, Deborah J Moshinsky","doi":"10.1177/1087057108326663","DOIUrl":"https://doi.org/10.1177/1087057108326663","url":null,"abstract":"Kinases represent attractive targets for drug discovery. Eight small-molecule kinase inhibitors are currently marketed in the area of oncology, and numerous others are in clinical trials. Characterization of the selectivity profiles of these compounds is important to target appropriate patient populations and to reduce the potential of toxicity due to off-target effects. The authors describe the development, validation, and utilization of a biochemical kinase assay panel for the selectivity profiling of inhibitors. The panel was developed as 29 radiometric Flashplate assays, and then an initial 13 were transitioned to a nonradiometric Caliper mobility shift assay format. Generation of high-quality data from the panel is detailed along with a comparison of the assay formats. Both assay technologies were found to be suitable for panel screening, but mobility shift assays yielded higher data quality. The selectivity data generated here should be useful in computational modeling and help facilitate, in conjunction with sequence and structural information, the rational design of inhibitors with well-defined selectivity profiles.","PeriodicalId":15087,"journal":{"name":"Journal of Biomolecular Screening","volume":"14 1","pages":"31-42"},"PeriodicalIF":0.0,"publicationDate":"2009-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1177/1087057108326663","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"27892502","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 41

Isolation of novel EGFR-specific VHH domains. 新的egfr特异性VHH结构域的分离。

Journal of Biomolecular Screening Pub Date : 2009-01-01 DOI: 10.1177/1087057108327064

Elizabeth B Gottlin, Xiangrong Guan, Charles Pegram, Allen Cannedy, Michael J Campa, Edward F Patz

{"title":"Isolation of novel EGFR-specific VHH domains.","authors":"Elizabeth B Gottlin, Xiangrong Guan, Charles Pegram, Allen Cannedy, Michael J Campa, Edward F Patz","doi":"10.1177/1087057108327064","DOIUrl":"https://doi.org/10.1177/1087057108327064","url":null,"abstract":"Epidermal growth factor receptor (EGFR) is overexpressed or mutated in a high percentage of tumors. EGFR has long been considered a promising target for cancer diagnostic and therapeutic applications. However, monoclonal antibodies and other large antibody constructs diffuse into tumors slowly, limiting their efficacy. To develop lower molecular weight probes for EGFR and other tumor cell receptors, the authors immunized a llama with the extracellular domains (ECDs) of EGFR and an oncogenic mutant receptor, EGFRvIII, and with extracts of tumor cell lines. From the immune repertoire of the llama, the authors constructed a heavy chain variable domain (VHH domain)-phage library. At approximately 16 kDa, the VHH domain is a tenth of the size of a monoclonal antibody and is the smallest antibody fragment that retains specificity. By affinity selection from this library, the authors isolated many VHH domains with specificity for EGFR. The VHH domains bind to whole cells expressing the receptor but not to control cells lacking the receptor and can immunoprecipitate EGFR from cell lysates. Some VHH domains have cross-specificity with existing anti-EGFR monoclonal antibodies and have reasonably high (nM) affinities. The llama-VHH domain library is also potentially a rich source of targeting agents directed toward other tumor cell receptors.","PeriodicalId":15087,"journal":{"name":"Journal of Biomolecular Screening","volume":"14 1","pages":"77-85"},"PeriodicalIF":0.0,"publicationDate":"2009-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1177/1087057108327064","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"27948553","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 19

Characterizing cannabinoid CB2 receptor ligands using DiscoveRx PathHunter beta-arrestin assay. 使用DiscoveRx PathHunter β -阻滞蛋白测定表征大麻素CB2受体配体。

Journal of Biomolecular Screening Pub Date : 2009-01-01 DOI: 10.1177/1087057108327329

Debra McGuinness, Asra Malikzay, Richard Visconti, Karen Lin, Marvin Bayne, Frederick Monsma, Charles A Lunn

{"title":"Characterizing cannabinoid CB2 receptor ligands using DiscoveRx PathHunter beta-arrestin assay.","authors":"Debra McGuinness, Asra Malikzay, Richard Visconti, Karen Lin, Marvin Bayne, Frederick Monsma, Charles A Lunn","doi":"10.1177/1087057108327329","DOIUrl":"https://doi.org/10.1177/1087057108327329","url":null,"abstract":"The authors have characterized a set of cannabinoid CB(2) receptor ligands, including triaryl bis sulfone inverse agonists, in a cell-based receptor/beta-arrestin interaction assay (DiscoveRx PathHunter). The results were compared with results using a competitive ligand binding assay, and with effects on forskolin-stimulated cAMP levels (PerkinElmer LANCE). The authors show good correlation between the 3 assay systems tested, with the beta-arrestin protein complementation assay exhibiting a more robust signal than the cAMP assay for cannabinoid CB(2) agonists. Further assay validation shows that DiscoveRx PathHunter HEK293 CB(2) beta-arrestin assay can be carried out from cryopreserved cell suspensions, eliminating variations caused by the need for multiple cell pools during live cell screening campaigns. These results, and the authors' results evaluating a test set of random library compounds, validate the use of ligand-induced interaction between the human cannabinoid CB(2) receptor and beta-arrestin as an appropriate and valuable screening platform for compounds specific for the cannabinoid CB(2) receptor.","PeriodicalId":15087,"journal":{"name":"Journal of Biomolecular Screening","volume":"14 1","pages":"49-58"},"PeriodicalIF":0.0,"publicationDate":"2009-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1177/1087057108327329","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"27948549","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 56