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Assay and Drug Development Technologies

Norazwana Samat, Mei Fong Ng, Nur Faizah Ruslan, Kazuhide Shaun Okuda, Pei Jean Tan, Vyomesh Patel
Natural products are prolific producers of diverse chemical scaffolds, which have yielded several clinically useful drugs. However, the complex features of natural products present challenges for identifying bioactive molecules using high-throughput screens. For most assays, measured endpoints are either colorimetric or luminescence based. Thus, the presence of the major metabolites, tannins, and chlorophylls, in natural products could potentially interfere with these measurements to give either false-positive or false-negative hits...
July 9, 2018: Assay and Drug Development Technologies
Rehmat Zaman, Ghazanfar Ali, Zeeshan Anjum, Muhammad Sajid, Muhammad Mumtaz Khan, Aziz Ahmad, Syed Rizwan Abbas, Wajid Rehman
The presence of P-glycoprotein in the human intestine represents a significant barrier to effective drug therapy. These proteins form a multidrug-resistant barrier to most drugs, especially those administered orally. Thus, strategies are needed to prepare molecules to combat these resistant proteins and enable an increase in drug efficacy. We developed a novel tin-Schiff base complex using an ultrasonic bath, a new technique in small molecule synthesis. New bond formation was confirmed using ultraviolet and Fourier transform spectroscopies...
June 7, 2018: Assay and Drug Development Technologies
Ryokichi Koyama, Yasunori Fukuda, Yusuke Kamada, Hideyuki Nakagawa, Darbi Witmer, Geza Ambrus-Aikelin, Bi-Ching Sang, Masaharu Nakayama, Hidehisa Iwata
The retinoic acid-related orphan receptor gamma T (RORγt) plays an important role in Th17 cell proliferation and functionality. Thus, RORγt inverse agonists are thought to be potent therapeutic agents for Th17-mediated autoimmune diseases, such as rheumatoid arthritis, asthma, inflammatory bowel disease, and psoriasis. Although RORγt has constitutive activity, it is recognized that the receptor is physiologically regulated by various cholesterol derivatives. In this study, we sought to identify RORγt inverse agonists through a high-throughput screening campaign...
May 2018: Assay and Drug Development Technologies
Rachana Bhatt, Maxim Chudaev, Wlodek Mandecki, Emanuel Goldman
Antibiotic-resistant infections that do not respond to available drugs are becoming more common. Methicillin-resistant Staphylococcus aureus, carbapenem-resistant enterobacteria ("superbugs"), and many others pose a continuous threat to public health. To provide tools to combat such deadly infections, we present in this study a homogeneous assay focused on an insufficiently addressed molecular interaction linked to ribosomal translation. We show that a fluorescence resonance energy transfer (FRET) based screening assay can identify antibiotic molecules that inhibit ternary complex (EF-Tu:tRNA:GTP complex) formation, and therefore, protein synthesis in bacteria...
May 2018: Assay and Drug Development Technologies
Bruce J Melancon, Hermann A M Mucke
No abstract text is available yet for this article.
May 2018: Assay and Drug Development Technologies
Yankun Yu, Feng Liu, Liuming He, Seeram Ramakrishna, Monica Zheng, Lei Bu, Ying Xu
Co-administration of sofosbuvir, an anti-hepatitis C virus medication, and antiarrhythmic amiodarone causes symptomatic severe bradycardia in patients and animal models. However, in a few in vitro studies, the combination of sofosbuvir and amiodarone resulted in tachycardiac effects in human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs). This discrepancy may be attributable to the use of immature hiPSC-CMs in the in vitro studies. To address this, we evaluated the ability of our in-house hiPSC-CMs to assess the interactions between sofosbuvir and amiodarone in vitro...
May 2018: Assay and Drug Development Technologies
Hans De Wolf, Laure Cougnaud, Kirsten Van Hoorde, An De Bondt, Joerg K Wegner, Hugo Ceulemans, Hinrich Göhlmann
By adding biological information, beyond the chemical properties and desired effect of a compound, uncharted compound areas and connections can be explored. In this study, we add transcriptional information for 31K compounds of Janssen's primary screening deck, using the HT L1000 platform and assess (a) the transcriptional connection score for generating compound similarities, (b) machine learning algorithms for generating target activity predictions, and (c) the scaffold hopping potential of the resulting hits...
April 2018: Assay and Drug Development Technologies
Brian S Muntean, Dipak N Patil, Franck Madoux, James Fossetta, Louis Scampavia, Timothy P Spicer, Kirill A Martemyanov
G protein-coupled receptors (GPCRs) are excellent drug targets exploited by majority of the Food and Drug Administration-approved medications, but when modulated, are often accompanied by significant adverse effects. Targeting of other elements in GPCR pathways for improved safety and efficacy is thus an unmet need. The strength of GPCR signaling is tightly regulated by regulators of G protein signaling (RGS) proteins, making them attractive drug targets. We focused on a prominent RGS complex in the brain consisting of RGS7 and its binding partners Gβ5 and R7BP...
April 2018: Assay and Drug Development Technologies
Niloufar Majdabadi, Mehraban Falahati, Fariba Heidarie-Kohan, Shirin Farahyar, Parvaneh Rahimi-Moghaddam, Mahtab Ashrafi-Khozani, Tandis Razavi, Sina Mohammadnejad
The antifungal effects of 2-phenylethanol are clearly visible through its intervention in Candida morphogenesis. Chronic and recurrent vulvovaginitis, however, does not respond to this standard experimental therapy; therefore, the study presented in this article investigated the effect of common antifungal drugs (amphotericin B [AMB], fluconazole [FLU], and itraconazole [ITC]), in combination with 2-phenylethanol, on the Candida species isolated from cases of chronic and recurrent vulvovaginitis, thereby allowing the recommendation of a more appropriate treatment option...
April 2018: Assay and Drug Development Technologies
Anton Simeonov, Aaron Wilson, Doug Auld
No abstract text is available yet for this article.
April 2018: Assay and Drug Development Technologies
Matthew Tarnowski, Amélie Barozet, Carina Johansson, Per-Olof Eriksson, Ola Engkvist, Jarrod Walsh, J Willem M Nissink
Discerning false positives from true actives in high-throughput screening (HTS) output is fraught with difficulty as the reason of anomalous activity seen for compounds is often not clear-cut. In this study, we introduce a novel medium-throughput NMR assay for the identification of redox-cycling compounds (RCCs), which is based on detection of oxidation of a reducing agent. We compare its outcomes to those from horseradish peroxidase (HRP)/phenol red and resazurin (RZ)-based assays that are more commonly used for triaging HTS outputs...
April 2018: Assay and Drug Development Technologies
Archana Anandrao Wakharde, Shivkrupa Devrao Halbandge, Datta Baburao Phule, Sankunny Mohan Karuppayil
The human pathogen Candida albicans can grow as a biofilm on host tissues and on the surfaces of different prosthetic devices in a patient's body. Various studies have reported that biofilms formed by C. albicans are resistant to most of the currently used antibiotics including the widely prescribed drug, fluconazole. As such, novel strategies for the treatment of drug-resistant biofilms are required. Drug repositioning or the use of drugs outside their unique indication has the potential to radically change drug development...
February 15, 2018: Assay and Drug Development Technologies
Jinglin Xiong, Valentina Gonzalez Pecchi, Min Qui, Andrey A Ivanov, Xiulei Mo, Qiankun Niu, Xiang Chen, Haian Fu, Yuhong Du
Epigenetic modulators play critical roles in reprogramming of cellular functions, emerging as a new class of promising therapeutic targets. Nuclear receptor binding SET domain protein 3 (NSD3) is a member of the lysine methyltransferase family. Interestingly, the short isoform of NSD3 without the methyltransferase fragment, NSD3S, exhibits oncogenic activity in a wide range of cancers. We recently showed that NSD3S interacts with MYC, a central regulator of tumorigenesis, suggesting a mechanism by which NSD3S regulates cell proliferation through engaging MYC...
February 2018: Assay and Drug Development Technologies
Jannie M B Sand, Patricia Lamy, Pernille Juhl, Anne Sofie Siebuhr, Line V Iversen, Arkadiusz Nawrocki, Martin R Larsen, Robyn T Domsic, Nathalie Franchimont, Juan Chavez, Morten A Karsdal, Diana J Leeming
Type VII collagen is the main component of the anchoring fibrils connecting the basement membrane to the underlying interstitial matrix. Mutations in the type VII collagen gene cause dystrophic epidermolysis bullosa. Increased levels of type VII collagen in the skin have been reported in patients with systemic sclerosis (SSc), whereas reduced levels in the airways have been related to asthma. This indicates that type VII collagen plays an important part in upholding tissue integrity and that its remodeling may lead to pathological states...
February 2018: Assay and Drug Development Technologies
Yanhong Jin, Di Li, Shiying Lu, Han Zhao, Zhao Chen, Wei Hou, Benfang Helen Ruan
Human glutamate dehydrogenase (GDH) plays an important role in neurological diseases, tumor metabolism, and hyperinsulinism-hyperammonemia syndrome (HHS). However, there are very few inhibitors known for human GDH. Recently, Ebselen was reported to crosslink with Escherichia coli GDH at the active site cysteine residue (Cys321), but the sequence alignment showed that the corresponding residue is Ala329 in human GDH. To investigate whether Ebselen could be an inhibitor for human GDH, we cloned and expressed an N-terminal His-tagged human GDH in E...
February 2018: Assay and Drug Development Technologies
Manman Su, Dingding Wang, Weiqin Chang, Lixian Liu, Manhua Cui, Tianmin Xu
Atherosclerosis is a major cause for cardiovascular diseases. High-density lipoprotein (HDL) may reduce atherosclerosis through several different mechanisms. HDL is composed of lipids, cholesterol, cholesteryl esters, triglycerides, and phospholipids, mainly phosphatidylcholine plus specialized proteins called apolipoproteins (apos). In this study, we prepared vitamin E containing HDL (VE -HDL) that contains egg phosphatidylcholine, cholesterol, vitamin E, and two kinds of recombinant human apolipoproteins (rhapo)-rhapoA-I and rhapoE in vitro by the facilitation of cholate...
February 2018: Assay and Drug Development Technologies
Anton Simeonov, Aaron Wilson, Doug Auld
No abstract text is available yet for this article.
February 2018: Assay and Drug Development Technologies
Wei Huang, Kelly Whittaker, Huihua Zhang, Jian Wu, Si-Wei Zhu, Ruo-Pan Huang
Antibody arrays represent a high-throughput technique that enables the parallel detection of multiple proteins with minimal sample volume requirements. In recent years, antibody arrays have been widely used to identify new biomarkers for disease diagnosis or prognosis. Moreover, many academic research laboratories and commercial biotechnology companies are starting to apply antibody arrays in the field of drug discovery. In this review, some technical aspects of antibody array development and the various platforms currently available will be addressed; however, the main focus will be on the discussion of antibody array technologies and their applications in drug discovery...
February 2018: Assay and Drug Development Technologies
(no author information available yet)
No abstract text is available yet for this article.
February 2018: Assay and Drug Development Technologies
Ann F Hoffman, John Nolan, David F Gebhard, Debra Nickischer, Wienand Omta, Sam Cooper, Sharon Presnell, Judi Wardwell-Swanson, Myles Fennell
No abstract text is available yet for this article.
January 2018: Assay and Drug Development Technologies
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