A5054755565- Analytical Chemistry and Chromatography
- Microfluidic and Capillary Electrophoresis Applications
- Chemical Synthesis and Analysis
- Mass Spectrometry Techniques and Applications
- Inflammatory mediators and NSAID effects
- Innovative Microfluidic and Catalytic Techniques Innovation
- Biochemical and Molecular Research
- Surfactants and Colloidal Systems
- Supramolecular Chemistry and Complexes
- Microencapsulation and Drying Processes
- Biotin and Related Studies
- Orthopaedic implants and arthroplasty
- Cancer-related Molecular Pathways
- Folate and B Vitamins Research
- Lipid metabolism and biosynthesis
- Advancements in Transdermal Drug Delivery
- Matrix Theory and Algorithms
- Orthopedic Infections and Treatments
- Catalytic C–H Functionalization Methods
- bioluminescence and chemiluminescence research
- Analytical Chemistry and Sensors
- Amino Acid Enzymes and Metabolism
- Pharmacogenetics and Drug Metabolism
- Advancements in Photolithography Techniques
- Receptor Mechanisms and Signaling
The University of Texas at Austin
2024
Novartis (United States)
2019
Eli Lilly (United States)
2003-2018
Louisiana State University
1996-2002
Southeastern Louisiana University
1997
AGPAT6 is a member of the 1-acylglycerol-3-phosphate O-acyltransferase (AGPAT) family that appears to be important in triglyceride biosynthesis several tissues, but precise biochemical function enzyme unknown. In current study, we show microsomal glycerol-3-phosphate acyltransferase (GPAT). Membranes from HEK293 cells overexpressing human had higher levels GPAT activity. Substrate specificity studies suggested was active against both saturated and unsaturated long-chain fatty acyl-CoAs. Both...
As part of a program aimed at the discovery antinociceptive therapy for inflammatory conditions, screening hit was found to inhibit microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 17.4 μM. Structural information used improve enzyme potency by over 1000-fold. Addition appropriate substituent alleviated time-dependent cytochrome P450 3A4 (CYP3A4) inhibition. Further structure-activity relationship (SAR) studies led 8, which had desirable (IC50 = 12 nM in ex vivo human whole blood...
Chiral separations using various polymerized dipeptide surfactants in electrokinetic capillary chromatography (EKC) are investigated. The two main used this study were sodium N-undecylenyl-L-valine-L-leucine (L-SUVL), and N-undecylenyl-L-leucine-L-valine (L-SULV). These studies performed order to determine if the of amino acids is important terms chiral recognition separations. Both monomer polymer these compared for separation model atropisomers, (+/-)-1,1-bi-2-naphtol (BOH)...
A hallmark of cancer is unbridled proliferation that can result in increased demand for de novo synthesis purine and pyrimidine bases required DNA RNA biosynthesis. These synthetic pathways are frequently upregulated involve various folate-dependent enzymes. Antifolates have a proven record as clinically used oncolytic agents. Our recent research efforts produced LSN 3213128 (compound 28a), novel, selective, nonclassical, orally bioavailable antifolate with potent specific inhibitory...
Prostaglandin (PG) E<sub>2</sub> plays a critical role in eliciting inflammation. Nonsteroidal anti-inflammatory drugs and selective inhibitors of cyclooxygenase, which block PGE<sub>2</sub> production, have been used as key agents treating inflammation pain associated with arthritis other conditions. However, these significant side effects such gastrointestinal bleeding myocardial infarction, since they also the production prostanoids that are for normal physiologic functions. Microsomal...
Poly sodium N-undecyl leucine-leucine (poly SULL) is used as a diagnostic tool to investigate chiral molecular interactions via electrokinetic chromatography (EKC). SULL has two centers which are defined by asymmetric carbons. Each center of poly can have possible configurations (d or l). Consequently, four different optical within the surfactant molecule (l-l, d-d, l-d, and d-l). In this study, five analytes various charge states hydrophobicities were role electrostatic hydrophobicity on...
The effect of amino acid order on chiral selectivity in polymeric dipeptide surfactants, as well the physical properties is investigated. An understanding enantioselectivity such surfactants crucial to design more efficient and has implications other areas research enantioselective interactions based compounds (i.e., enzymes, hemoglobin, antibodies, etc.). It should be noted that are not easily crystallized. Therefore, a manner similar study proteins, fluorescence spectroscopy powerful tool...
A quantitative method for the determination of a partially modified, 2′-ribose alkoxy 18-mer phosphorothioate oligonucleotide in liver tissue has been developed. liquid:liquid extraction, ion-pair reverse phase chromatographic separation and tandem mass spectrometry were used to achieve quantitation range 125 10,000 ng g −1 mouse tissue. total cycle time 5 min was obtained while maintaining three potential impurities. Separations performed using Discovery RP-Amide C16, 100 × 2 mm column...
AICARFT is a folate dependent catalytic site within the ATIC gene, part of purine biosynthetic pathway, pathway frequently upregulated in cancers. LSN3213128 potent (16 nM) anti-folate inhibitor and selective relative to TS, SHMT1, MTHFD1, MTHFD2 MTHFD2L. Increases ZMP, accompanied by activation AMPK cell growth inhibition, were observed with treatment LY3213128. These effects on ZMP proliferation levels. In human breast MDA-MB-231met2 lung NCI-H460 lines, inhibition was rescued...
Abstract This study examines the role of steric hindrance near stereogenic centers four glutamic acid based polymeric surfactants. The single amino surfactants acid, methyl ester, ethyl and tert ‐butyl ester were investigated. micellar electrokinetic chromatography (MEKC) separation three binaphthyl derivatives benzodiazepines used to these factors. In addition, hydrophobicity polymers as a function pH was investigated by use fluorescence measurements.
We report the intramolecular 1,n-aminoboration for simultaneous synthesis of aza-heterocycles with distal carbon–boron bonds. Pd-catalyzed remote occurs 1,2-disubstituted alkenes; upon aminopalladation olefin, chain walking generates terminal Pd-alkyl intermediate, which selectively undergoes Fe-catalyzed borylation. Terminal bishomoallylic amines, amides, carbamates, and ureas afford borylated pyrrolidines lactams through 1,2-aminoboration. Forty-one examples 1,n-borylated heterocycles are...
Abstract The effects of acetate (Ac) concentration on the separation lanthanides from hydronium ion (H3O+) in capillary zone electrophoresis is investigated. sample acidity and buffers H3O+ peak have been studied. A mixture 14 rare earth metals, along with H3O+, can be baseline separated less than nine minutes by use a ternary buffer system [sodium (NaAc) /α-hydroxyisobutyric acid (HIBA) / UV CAT-1]. In contrast, replacing NaAc equal molar sodium chloride (NaCl) decreases electroosmotic flow...