A5044632824- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- NF-κB Signaling Pathways
- Synthesis and Catalytic Reactions
- Galectins and Cancer Biology
- Synthesis of Indole Derivatives
- Protein Tyrosine Phosphatases
- Natural product bioactivities and synthesis
- Synthesis and biological activity
- Eicosanoids and Hypertension Pharmacology
- Neuroinflammation and Neurodegeneration Mechanisms
- Cytokine Signaling Pathways and Interactions
- Catalytic C–H Functionalization Methods
- Computational Drug Discovery Methods
- Hormonal Regulation and Hypertension
- Immune Response and Inflammation
- Crystal structures of chemical compounds
- Asthma and respiratory diseases
- Synthesis and Biological Activity
- T-cell and Retrovirus Studies
- Pesticide Exposure and Toxicity
- Respiratory and Cough-Related Research
- Phenothiazines and Benzothiazines Synthesis and Activities
- Muscle Physiology and Disorders
- Lymphoma Diagnosis and Treatment
Columbia University Irving Medical Center
2015-2025
Columbia University
2008-2024
Dartmouth College
2007-2020
Albert Einstein College of Medicine
2015
Abstract While efforts to identify microglial subtypes have recently accelerated, the relation of transcriptomically defined states function has been largely limited in silico annotations. Here, we characterize a set pharmacological compounds that proposed polarize human microglia towards two distinct – one enriched for AD and MS genes another characterized by increased expression antigen presentation genes. Using different model systems including HMC3 cells, iPSC-derived cerebral organoids,...
The covalent inhibition of acetylcholinesterase (AChE) by organophosphate compounds (OPCs) prevents the hydrolysis neurotransmitter, acetylcholine, and results in overstimulation muscarinic nicotinic receptors leading to severe cholinergic crisis. To treat toxic exposure OPCs, focus has been on using reactivator (e.g., oximes) reverse adduct formation enzyme’s active site, release regenerated, form AChE. However, interaction between OPC inhibitor enzyme is usually followed a secondary...
The lymphoid tyrosine phosphatase (Lyp, PTPN22) is a critical negative regulator of T cell antigen receptor (TCR) signaling. A single-nucleotide polymorphism (SNP) in the ptpn22 gene correlates with incidence various autoimmune diseases, including type 1 diabetes, rheumatoid arthritis, and systemic lupus erythematosus. Since disease-associated allele more potent inhibitor TCR signaling, specific Lyp inhibitors may become valuable treating autoimmunity. Using structure-based approach, we...
Equilibrative transporters are potential drug targets; however, most functional assays involve radioactive substrate uptake that is unsuitable for high-throughput screens (HTS). We developed a robust yeast-based growth assay potentially applicable to many equilibrative transporters. As proof of principle, we applied our approach Nucleoside Transporter 1 the malarial parasite Plasmodium falciparum (PfENT1). PfENT1 inhibitors might serve as novel antimalarial drugs since PfENT1-mediated purine...
Severe bronchospasm refractory to β-agonists continues cause significant morbidity and mortality in asthmatic patients. We questioned whether chloride channels/transporters are novel targets for the relaxation of airway smooth muscle (ASM). have screened a library compounds, derivatives anthranilic indanyloxyacetic acid, that were originally developed antagonize channels kidney. hypothesized members this would be calcium-activated channel blockers airway. The initial screen compound...
A novel generation of indole-2,3-quinodimethanes via the deamination 1,2,3,4-tetrahydropyrrolo[s3,4-b]indoles is reported.
While efforts to identify microglial subtypes have recently accelerated, the relation of transcriptomically defined states function has been largely limited in silico annotations. Here, we characterize a set pharmacological compounds that proposed polarize human microglia towards two distinct – one enriched for AD and MS genes another characterized by increased expression antigen presentation genes. Using different model systems including HMC3 cells, iPSC-derived cerebral organoids, effect...
In the title compound, C14H9I2NO2S, two I atoms lie essentially in plane of indole ring and there is some iodine–iodine repulsion.
We previously identified the
Elevation and accumulation of amyloid b-peptide (Ab) are hallmark pathological characteristics Alzheimer’s disease (AD) in animal models patients. The production Ab is mediated by cleavage precursor protein (APP) two proteolytic enzymes, b-site cleaving enzyme (BACE1) γ-secretase. Recent work has identified a mutation close proximity to the BACE1 site APP rendering those who bear resistant AD age-associated cognitive decline. This indicates seminal for risk progression, validates promise...
Abstract Review: data on syntheses, reactions and applications of pyridazines, pyrimidines, pyrzines, their benzo‐fused derivatives published in 2012; 103 refs.