A5050473857- Sphingolipid Metabolism and Signaling
- Protein Degradation and Inhibitors
- Multiple Myeloma Research and Treatments
- Peptidase Inhibition and Analysis
- Cellular transport and secretion
- Lipid Membrane Structure and Behavior
- PI3K/AKT/mTOR signaling in cancer
- Bioactive Compounds and Antitumor Agents
- Nausea and vomiting management
- Click Chemistry and Applications
- ATP Synthase and ATPases Research
- Pathogenesis and Treatment of Hiccups
- Synthesis and Characterization of Heterocyclic Compounds
- Carbohydrate Chemistry and Synthesis
- Glycosylation and Glycoproteins Research
- Chemical Synthesis and Analysis
- Hepatitis B Virus Studies
- Protein Tyrosine Phosphatases
- Polyamine Metabolism and Applications
- Mast cells and histamine
- Viral Infections and Outbreaks Research
- Enzyme function and inhibition
- Cytokine Signaling Pathways and Interactions
- SARS-CoV-2 and COVID-19 Research
- Ubiquitin and proteasome pathways
Rosalind Franklin University of Medicine and Science
2022
University of Maryland, Baltimore
2015-2021
University of Maryland, Baltimore County
2017
University of Baltimore
2015
Virginia Tech
2011-2015
Johns Hopkins University
2013
Johns Hopkins Medicine
2013
S1P (sphingosine 1-phosphate) is a pleiotropic lipid mediator involved in numerous cellular and physiological functions. Of note among these are cell survival migration, as well lymphocyte trafficking. S1P, which exerts its effects via five GPCRs (G-protein-coupled receptors) (S1P1–S1P5), formed by the action of two SphKs kinases). Although SphK1 more intensively studied isotype, SphK2 unique it nuclear localization has been reported to oppose some actions ascribed SphK1. several scaffolds...
A focused library of analogues the dual PLK1 kinase/BRD4 bromodomain inhibitor BI-2536 was prepared and then analyzed for BRD4 inhibitory activities. Particularly, replacement cyclopentyl group with a 3-bromobenzyl moiety afforded most potent series (39j) K i = 8.7 nM, which equipotent against PLK1. The superior affinity 39j over parental compound to possibly derives from improved interactions WPF shelf. Meanwhile, substitution pyrimidine NH an oxygen atom reversed PLK1/BRD4 selectivity...
Sphingosine 1-phosphate (S1P) is a pleiotropic signaling molecule that acts as ligand for five G-protein coupled receptors (S1P1–5) whose downstream effects are implicated in variety of important pathologies including sickle cell disease, cancer, inflammation, and fibrosis. The synthesis S1P catalyzed by sphingosine kinase (SphK) isoforms 1 2, hence, inhibitors this phosphorylation step pivotal understanding the physiological functions SphKs. To date, SphK1 2 with potency, selectivity, vivo...
Key residues on opposing faces of the Bak-BH3 α-helix were recapitulated by 2,6,9-tri-substitution a purine scaffold.