Shift of bias in learning from drug compounds: The fleming project

1991 ◽  
pp. 482-493
Author(s):  
L. Di Pace ◽  
F. Fabrocini ◽  
G. Bolis
Keyword(s):  
Drug Compounds ◽  
Shift Of Bias

Benzyl and phenethyl isothiocyanates as promising epigenetic drug compounds by modulating histone acetylation and methylation marks in malignant melanoma

2021 ◽  
Author(s):  
Melina Mitsiogianni ◽  
Ioannis Anestopoulos ◽  
Sotiris Kyriakou ◽  
Dimitrios T. Trafalis ◽  
Rodrigo Franco ◽  
...  
Keyword(s):  
Malignant Melanoma ◽  
Histone Acetylation ◽  
Epigenetic Drug ◽  
Drug Compounds

scholarly journals DMSO-Related Effects in Protein Characterization

2005 ◽  
Vol 11 (2) ◽  
pp. 131-137 ◽  
Author(s):  
Agneta Tjernberg ◽  
Natalia Markova ◽  
William J. Griffiths ◽  
Dan Hallén
Keyword(s):  
Drug Discovery ◽  
Growth Hormone Receptor ◽  
Human Growth ◽  
Protein Characterization ◽  
Binding Property ◽  
Ionization Mass ◽  
Phosphatase Domain ◽  
Drug Compounds ◽  
Stock Solutions ◽  
Human Growth Hormone Receptor

DMSO is the standard solvent for preparing stock solutions of compounds for drug discovery. The assay concentration of DMSO is normally 0.1% to 5% (v/v) or 14 to 715 mM. Thus, DMSO is often one of the principal additives in assay buffers. This standardization of stock solutions does not eliminate possible pitfalls associated with the effects of the DMSO-containing solutions on individual proteins. In this article, the authors want to emphasize the importance of detailed studies of these effects in the early stages of drug discovery. Two protein systems, the extracellular soluble domain of the human growth hormone receptor (hGHbp) and the phosphatase domain of PFKFB1 (BPase), were used for the study on effects of DMSO on protein stability, protein aggregation, and binding of drug compounds. The study revealed significant differences in the proteins’ behavior in the presence and absence of low amounts of DMSO. The addition of DMSO resulted in destabilization of the proteins investigated and also changed the apparent binding property of 1 protein. The authors have also shown that low DMSO concentrations influence the ionization process in electrospray ionization mass spectrometry (ESI-MS).

Important issues in the cytotoxicity screening of nano-sized materials

2010 ◽  
Vol 2 (1) ◽  
pp. 1-5 ◽  
Author(s):  
Fröhlich E. ◽  
Claudia Meindl ◽  
Thomas R. Pieber
Keyword(s):  
Adverse Effect ◽  
Chemical Reactivity ◽  
False Negative ◽  
Medical Applications ◽  
Toxicological Assessment ◽  
Cellular Effects ◽  
Negative Results ◽  
False Negative Results ◽  
Drug Compounds ◽  
Screening Assays

Abstract Due to their extraordinary properties nano-sized materials (NMs) are increasingly used in industrial, pharmaceutical and medical applications. An even broader use is currently limited by concern about their potential adverse effect on health. Screening for toxic effects of all engineered NMs therefore, is needed to demonstrate biocompatibility. The identification of adverse cellular effects is one of the first steps in the toxicological assessment of drug compounds before they get to the market. A panel of cytotoxicity screening assays is available and can be used also for the assessment of NMs. The use of these established and validated assays for the testing of NMs, however, is complicated by the fact that NMs may interfere by color, chemical reactivity and light scattering leading to false positive or false negative results. The paper illustrates the principles of conventional cytotoxicity screening assays and discusses their suitability for the assessment of NMs. Adequate controls to identify interference and alternatives, if interference with the used assay is seen, are suggested.

scholarly journals Neurological disorder drug discovery from gene expression with tensor decomposition

2019 ◽  
Author(s):  
Y-h. Taguchi ◽  
Turki Turki
Keyword(s):  
Gene Expression ◽  
Neurological Disorder ◽  
Clinical Stage ◽  
Animal Experiments ◽  
Tensor Decomposition ◽  
Drug Candidate ◽  
Data Set ◽  
Candidate Drug ◽  
Model Animal ◽  
Drug Compounds

AbstractBackgroundIdentifying effective candidate drug compounds in patients with neurological disorders based on gene expression data is of great importance to the neurology field. By identifying effective candidate drugs to a given neurological disorder, neurologists would (1) reduce the time searching for effective treatments; and (2) gain additional useful information that leads to a better treatment outcome. Although there are many strategies to screen drug candidate in pre-clinical stage, it is not easy to check if candidate drug compounds can be also effective to human.ObjectiveWe tried to propose a strategy to screen genes whose expression is altered in model animal experiments to be compared with gene expressed differentically with drug treatment to human cell lines.MethodsRecently proposed tensor decomposition (TD) based unsupervised feature extraction (FE) is applied to single cell (sc) RNA-seq experiments of Alzheimer’s disease model animal mouse brain.ResultsFour hundreds and one genes are screened as those differentially expressed during Aβ accumulation as age progresses. These genes are significantly overlapped with those expressed differentially with the known drug treatments for three independent data sets: LINCS, DrugMatrix and GEO.ConclusionOur strategy, application of TD based unsupervised FE, is useful one to screen drug candidate compounds using scRNA-seq data set.

DC-Voltage-Induced Thermal Shift of Bias Point in<tex>$hboxLiNbO_3$</tex>Optical Modulators

2004 ◽  
Vol 16 (11) ◽  
pp. 2460-2462 ◽  
Author(s):  
H. Nagata ◽  
N.F. O'Brien ◽  
W.R. Bosenberg ◽  
G.L. Reiff ◽  
K.R. Voisine
Keyword(s):  
Optical Modulators ◽  
Dc Voltage ◽  
Bias Point ◽  
Shift Of Bias ◽  
Thermal Shift

scholarly journals Novel 4,6-Disubstituted s-Triazin-2-yl Amino Acid Derivatives as Promising Antifungal Agents

2020 ◽  
Vol 6 (4) ◽  
pp. 237
Author(s):  
Rakia Abd Alhameed ◽  
Zainab Almarhoon ◽  
Essam N. Sholkamy ◽  
Salman Ali Khan ◽  
Zaheer Ul-Haq ◽  
...  
Keyword(s):  
Amino Acid ◽  
Antifungal Activity ◽  
Active Site ◽  
Antifungal Agents ◽  
Docking Studies ◽  
Amino Acid Derivatives ◽  
Active Site Residues ◽  
Standard Drug ◽  
Drug Compounds ◽  
Inhibition Zones

A novel series of 4,6-disubstituted s-triazin-2-yl amino acid derivatives was prepared and characterized. Most of them showed antifungal activity against Candida albicans compared to clotrimazole (standard drug). Compounds bearing aniline derivatives, piperidine and glycine on the triazine core showed the highest inhibition zones at concentrations of 50, 100, 200, and 300 μg per disc. In addition, docking studies revealed that all the compounds accommodated well in the active site residues of N-myristoltransferase (NMT) and exhibited complementarity, which explains the observed antifungal activity. Interestingly, none of these compounds showed antibacterial activity.

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