Assay and drug development technologies最新文献_第10页

Correction to: A New Spectral Shift-Based Method to Characterize Molecular Interactions, by Langer, et al. Assay Drug Dev Technol. 2022;20(2):83-94; doi: 10.1089/adt.2021.133. 修正:一种新的基于光谱位移的方法来表征分子相互作用，由Langer等人。检测药物开发技术，2022;20(2):83-94;doi: 10.1089 / adt.2021.133。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-04-07 DOI: 10.1089/adt.2021.133.correx

引用次数: 0

Call for Special Issue Papers: New Modalities in Chemical Probes and Pharmacological Tools in Drug Discovery. 特刊论文征集：药物发现中化学探针和药理学工具的新模式。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-04-01 DOI: 10.1089/adt.2022.29098.cfp

M. Kostic, B. Melancon

引用次数: 0

Developmental Cardiotoxicity and Hepatotoxicity of Flurbiprofen Axetil to Zebrafish Embryo. 氟比洛芬酯对斑马鱼胚胎的发育性心脏毒性和肝毒性。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-04-01 DOI: 10.1089/adt.2021.127

Yuping Wang, Min Zhou, Jing Wang, Chu-Fang Lin, Xiang-li Gao, Li Zhang, Wenshui Yao, Longxin Zhang

{"title":"Developmental Cardiotoxicity and Hepatotoxicity of Flurbiprofen Axetil to Zebrafish Embryo.","authors":"Yuping Wang, Min Zhou, Jing Wang, Chu-Fang Lin, Xiang-li Gao, Li Zhang, Wenshui Yao, Longxin Zhang","doi":"10.1089/adt.2021.127","DOIUrl":"https://doi.org/10.1089/adt.2021.127","url":null,"abstract":"Flurbiprofen axetil (FA) is a nonsteroidal targeted analgesic and widely used for postoperative analgesia and cancer analgesia. Extensive works have been done in the evaluation of FA's clinical analgesic effect on adults. Along with the increase of FA usage, the potential toxicity and molecular mechanism in embryo development need to be better understood. In this article, multiple embryonic development indexes of zebrafish were introduced to evaluate the FA toxicity to provide clinical guidance for gravidas medicine. We performed a zebrafish embryo toxicity (ZFET) test by exposing embryos to a series of concentration gradients of FA medium starting from 24 hours postfertilization (hpf). The mortality rate, hatching rate, and malformation rate of drug-treated zebrafish were assessed at 72, 96, and 120 hpf. Effects of ≤10% lethal concentration (LC10) of FA on embryogenesis were evaluated by eye area, body length, and yolk sac area. A 0.5 μg/mL or fewer FA treatment did not show any adverse effects, but the LC10 FA significantly caused zebrafish malformation. Organ disorders, including slow heart rate, enlarged pericardium, and liver atrophy, were found in the dysplasia individuals when compared with control. TUNEL assay suggested that apoptotic cells in malformation embryos were produced by FA and the increasing dosage exacerbated apoptosis. Quantitative real-time polymerase chain reaction revealed that expressions of cardiac development-associated transcription factors, liver development-related genes, and apoptosis regulating genes were aberrant. These results indicate that the ZFET can be applied in the FA toxicity test, and a low lethal dose of FA is harmful to zebrafish embryogenesis, especially in embryo carcinogenesis and hepatogenesis.","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2022-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42987879","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

Development of a High-Throughput Screening Assay for Small-Molecule Inhibitors of Androgen Receptor Splice Variants. 雄激素受体剪接变异体小分子抑制剂高通量筛选试验的建立。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-04-01 Epub Date: 2022-03-23 DOI: 10.1089/adt.2021.128

Amy E Monaghan, Alison Porter, Irene Hunter, Angus Morrison, Stuart P McElroy, Iain J McEwan

{"title":"Development of a High-Throughput Screening Assay for Small-Molecule Inhibitors of Androgen Receptor Splice Variants.","authors":"Amy E Monaghan, Alison Porter, Irene Hunter, Angus Morrison, Stuart P McElroy, Iain J McEwan","doi":"10.1089/adt.2021.128","DOIUrl":"https://doi.org/10.1089/adt.2021.128","url":null,"abstract":"<p><p>The role of the androgen receptor (AR) in the progression of prostate cancer (PCa) is well established and competitive inhibition of AR ligand binding domain (LBD) has been the mainstay of antiandrogen therapies for advanced and metastatic disease. However, the efficacy of such drugs is often limited by the emergence of resistance, mediated through point mutations and receptor splice variants lacking the AR-LBD. As a result, the prognosis for patients with malignant, castrate-resistant disease remains poor. The amino terminal domain (NTD) of the AR has been shown to be critical for AR function. Its modular activation function (AF-1) is important for both gene regulation and participation in protein-protein interactions. However, due to the intrinsically disordered structure of the domain, its potential as a candidate for therapeutic intervention has been generally overlooked. In this article, we describe the design and development of a functional cell-based assay aimed at identifying small-molecule inhibitors of the AR-NTD. We demonstrate the suitability of the assay for high-throughput screening platforms and validate two initial hits emerging from a small, targeted, library screen in PCa cells.</p>","PeriodicalId":8586,"journal":{"name":"Assay and drug development technologies","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2022-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/cb/b5/adt.2021.128.PMC9057896.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40328156","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 2

Call for Special Issue Papers: Chemical Probes and Pharmacological Tools for Imaging Applications. 特刊论文征集：用于成像应用的化学探针和药理学工具。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-04-01 DOI: 10.1089/adt.2022.29099.cfp

M. Kostic, B. Melancon

引用次数: 0

Interview with Craig W. Lindsley, PhD. Craig W. Lindsley博士访谈

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-03-31 DOI: 10.1089/adt.2022.29097.bjm

B. Melancon

引用次数: 0

Forging Ahead with ASSAY. 与化验携手前行。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-03-30 DOI: 10.1089/adt.2022.29100.bjm

B. Melancon

引用次数: 0

Drug Repurposing Patent Applications October: December 2021. 药物再利用专利申请10月:2021年12月

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-02-09 DOI: 10.1089/adt.2022.002

H. Mucke

引用次数: 0

Call for Special Issue Papers: Chemical Probes and Pharmacological Tools for Kinase Signaling. 特刊论文征集：激酶信号传导的化学探针和药理学工具。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-02-03 DOI: 10.1089/adt.2020.29096.cfp5

Milka Kostic, Bruce J Melancon

引用次数: 0

Call for Special Issue Papers: Special Issue on High-throughput Technologies for the Discovery and Development of Chemical Probes and Pharmacological Tools. 特刊论文征集:化学探针和药理学工具的高通量发现和开发技术特刊。

IF 1.8 4区医学

Assay and drug development technologies Pub Date : 2022-02-03 DOI: 10.1089/adt.2020.29095.cfp5

Milka Kostic, Bruce J Melancon

引用次数: 0