AIMC Topic: Pyrimidines
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Label-Free Quantification of Pharmacokinetics in Skin with Stimulated Raman Scattering Microscopy and Deep Learning.
The Journal of investigative dermatology
Jul 22, 2020
The treatment of inflammatory skin conditions relies on a deep understanding of how drugs and tissue behave and interact. Although numerous methods have been developed that aim to follow and quantify topical drug pharmacokinetics, these tools can com...
Effect of congenital adrenal hyperplasia treated by glucocorticoids on plasma metabolome: a machine-learning-based analysis.
Scientific reports
Jun 1, 2020
BACKGROUND: Congenital adrenal hyperplasia (CAH) due to 21-hydroxylase deficiency leads to impaired cortisol biosynthesis. Treatment includes glucocorticoid supplementation. We studied the specific metabolomics signatures in CAH patients using two di...
Label-Free Tomographic Imaging of Lipid Droplets in Foam Cells for Machine-Learning-Assisted Therapeutic Evaluation of Targeted Nanodrugs.
ACS nano
Jan 10, 2020
Lipid droplet (LD) accumulation, a key feature of foam cells, constitutes an attractive target for therapeutic intervention in atherosclerosis. However, despite advances in cellular imaging techniques, current noninvasive and quantitative methods hav...
Robotic assisted generation of 2'-deoxy-2'-fluoro-modifed RNA aptamers - High performance enabling strategies in aptamer selection.
Methods (San Diego, Calif.)
May 30, 2019
Aptamer selection is a laborious procedure, requiring expertise and significant resources. These characteristics limit the accessibility of researchers to these molecular tools. We describe a selection procedure, making use of a robotic system that a...
Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as selective Btk inhibitors with improved pharmacokinetic properties for the treatment of rheumatoid arthritis.
European journal of medicinal chemistry
Dec 28, 2017
Bruton's tyrosine kinase (Btk) is a Tec family kinase with a well-defined role in the B cell receptor (BCR) and Fcγ receptor (FcR) signaling pathways, which makes it a uniquely attractive target for the treatment of autoimmune diseases, such as rheum...
Molecular Structure
Dogs
Microsomes, Liver
Protein Kinase Inhibitors
Humans
Cell Line
Pyrimidines
Animals
Protein-Tyrosine Kinases
Cell Proliferation
Agammaglobulinaemia Tyrosine Kinase
Drug Design
Structure-Activity Relationship
Haplorhini
Rats, Sprague-Dawley
Arthritis, Rheumatoid
Models, Molecular
Mice
Pyrroles
Dose-Response Relationship, Drug
Rats
Pharmacokinetic and safety profile of tofacitinib in children with polyarticular course juvenile idiopathic arthritis: results of a phase 1, open-label, multicenter study.
Pediatric rheumatology online journal
Dec 28, 2017
BACKGROUND: Juvenile idiopathic arthritis (JIA) is the most common pediatric rheumatic disease and a leading cause of childhood disability. The objective of this study was to characterize the PK, safety, and taste acceptability of tofacitinib in pati...
Surveillance of iclaprim activity: In vitro susceptibility of gram-positive pathogens collected from 2012 to 2014 from the United States, Asia Pacific, Latin American and Europe.
Diagnostic microbiology and infectious disease
Dec 7, 2017
Iclaprim is a diaminopyrimidine, which inhibits bacterial dihydrofolate reductase, and it is highly active against Gram-positive pathogens including emerging drug-resistant pathogens. In vitro activity of iclaprim and comparators against 2814 Gram-po...
Enhancement of Nucleoside Production in Based on Biosynthetic Pathway Analysis.
BioMed research international
Nov 29, 2017
To enhance nucleoside production in , the biosynthetic pathways of purine and pyrimidine nucleosides were constructed and verified. The differential expression analysis showed that , and genes involved in purine nucleotide biosynthesis were signifi...
Machine Learning of Global Phosphoproteomic Profiles Enables Discrimination of Direct versus Indirect Kinase Substrates.
Molecular & cellular proteomics : MCP
Mar 6, 2017
Mass spectrometry allows quantification of tens of thousands of phosphorylation sites from minute amounts of cellular material. Despite this wealth of information, our understanding of phosphorylation-based signaling is limited, in part because it is...
HPLC-UV method for simultaneous determination of MK-1775 and AZD-7762 in both acetonitrile-aqueous solution and mouse plasma.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences
Dec 30, 2016
A sensitive and precise method is described for the simultaneous determination of two small molecule kinase inhibitors: MK-1775 (MK) and AZD-7762 (AZD), in acetonitrile (ACN)-aqueous solution and in mouse plasma. A Nova-Pak C18 reversed phase column ...
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