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Articles 241 - 270 of 397
Full-Text Articles in Chemistry
Novel Thermal Analytical Techniques To Characterize Drugs And Drug Delivery, Lakshmi Swetha Kaza
Novel Thermal Analytical Techniques To Characterize Drugs And Drug Delivery, Lakshmi Swetha Kaza
ETD Archive
This thesis encompasses three significant projects. The study includes the characterization and evaluation of the properties of a commercial contraceptive transdermal patch, Ortho Evra® by Dielectric Analysis and Differential Scanning Calorimetry (DSC). This study helps in monitoring the mobility of the drug and transport properties by Isothermal and Scanning Dielectric Analysis as a function of temperature and frequency. The drugs in this product are norelgestromin and ethinyl estradiol. DSC was used to detect any crystalline character of the drugs by their fusion properties. Having no melting endotherm and detecting a glass transition temperature suggested that the drugs in the patches …
Development Of Bioanalytical Methods For Clinical Applications And Drug Screening, Xiaohan Cai
Development Of Bioanalytical Methods For Clinical Applications And Drug Screening, Xiaohan Cai
ETD Archive
In the past decade, bioanalytical method development has become an integral part of clinical diagnosis, biomarker discovery, and drug discovery and development. The new and emerged bioanalytical technologies allow the quantitative and qualitative analysis of small molecules and biomolecules with high sensitivity and specificity. Specifically, the bioanalytical methods based on LC-MS and methylation-specific PCR are well suited for detecting low-abundance metabolites, proteins, and DNA in biofluids and tissues for biomarker investigation. They offer great clinical promises for early diseases diagnosis and therapeutic interventions. Besides, the LC-MS/MS quantitative method is essential for the estimation of pharmacokinetic and toxicological properties in drug …
Capillary Gradient Chromatofocusing-Mass Spectrometry;A Sensitive Approach For Protein Analysis, James Anthony Hribar
Capillary Gradient Chromatofocusing-Mass Spectrometry;A Sensitive Approach For Protein Analysis, James Anthony Hribar
ETD Archive
Gradient chromatofocusing-mass spectrometry is a new technique for protein analysis recently introduced by our research group. Capable of separating and identifying proteins according to pI values and molecular weight, gradient chromatofocusing-mass spectrometry has been achieved by integrating a new ion-exchange chromatography technique called gradient chromatofocusing with a newly discovered buffer system that promotes mass spectrometry detection. Differing from traditional ion-exchange chromatography techniques, gradient chromatofocusing employs specific low molecular weight, volatile buffer components that are introduced onto an ion-exchange HPLC column by programming a binary gradient pumping system to deliver the correct proportions of acidic mobile phase to overcome buffering of …
Development Of Quantitative Lc-Ms/Ms Methods For The Pharmacological Studies Of Anti-Cancer Drugs, Lan Li
Development Of Quantitative Lc-Ms/Ms Methods For The Pharmacological Studies Of Anti-Cancer Drugs, Lan Li
ETD Archive
In the development of anti-cancer drugs, it is essential to study the pharmacological profiles of the drugs. Among the analytical tools utilized in the pharmacological studies, LC-MS/MS has gained increased popularity due to its unequivocal sensitivity and specificity, as well as the ability of handling a wide variety of compounds with relatively simple sample preparation procedures. In this work, a brief review on the method rational, instrumentations, analytical method validation, and work flow of the method development was included. The processes of LC-MS/MS method development for the pharmacological studies of three anti-cancer drugs (i.e., methoxyamine, fludarabine, and 6-benzylthioinosine) were illustrated. …
Thermal Analysis As An Important Research Tool For Colleges And Universities, Jeffrey Allen Fruscella
Thermal Analysis As An Important Research Tool For Colleges And Universities, Jeffrey Allen Fruscella
ETD Archive
Three experiments were performed to demonstrate that thermal analysis is an important tool for use in colleges and universities for conducting scientific research. The first experiment used thermogravimetry, differential scanning calorimetry and thermal mechanical analysis to compare polymer resins from two ResinKits®, one from 1994 and the other from 2010. Analysis was done to determine if resins from the 1994 kit were viable standards. The experiments showed significant thermal differences between select resins and it was concluded that resins form the 1994 ResinKit® are no longer acceptable as standards.The second experiment used thermogravimetry and differential scanning calorimetry to determine the …
Factors Affecting Heme Transfer From "Gapdh": A Possible Heme Carrier Protein, Rajesh Vempati
Factors Affecting Heme Transfer From "Gapdh": A Possible Heme Carrier Protein, Rajesh Vempati
ETD Archive
The aim of my research is to understand the mechanism of heme transfer by carrier proteins into heme proteins. The mechanism of heme insertion into proteins is poorly understood. Previous experiments reported from our lab identified GAPDH as a possible heme carrier protein involved in heme transfer (Ritu Chakravarti et al PNAS). This work focuses on 2 aspects of heme transfer. a.) Rate of transfer of heme from GAPDH to apomyoglobin. We examined the rate of transfer of native proto-heme and the analogue meso-heme. The results showed that the rate of heme transfer was twice as fast for meso-heme compared …
Introduction To Pharmaceutical Thermal Analysis: A Teaching Tool, Shravan Singh Thakur
Introduction To Pharmaceutical Thermal Analysis: A Teaching Tool, Shravan Singh Thakur
ETD Archive
Significant Thermal Analysis-physical chemical data needs to be acquired by the new analyst whether an entry level chemist or a new function for the experienced pharmaceutical scientist. This teaching tool describes the introductory use of Differential Scanning Calorimetry (DSC), Thermogravimetric Analysis (TGA) and Thermomechanical Analysis (TMA) for characterizing pharmaceuticals. Optimum Experimental conditions for DSC, TGA and TMA will focus on collecting the best results and interpretations. Does the sample contain volatiles? Evaporation creates endothermic peaks, 2 water or solvent can lower the glass transition temperature (Tg) by up to 100°C and affect the crystallization temperature on cooling. The decomposition temperature …
[Fe-Fe]-Hydrogenase Reactivated By Residue Mutations As Bridging Carbonyl Rearranges: A Qm/Mm Study, Stefan Motiu, Valentin Gogonea
[Fe-Fe]-Hydrogenase Reactivated By Residue Mutations As Bridging Carbonyl Rearranges: A Qm/Mm Study, Stefan Motiu, Valentin Gogonea
Chemistry Faculty Publications
In this work, we found aqueous enzyme phase reaction pathways for the reactivation of the exogenously inhibited [Fe-Fe]-hydrogenases by O2, or OH−, which metabolizes to H2O (Dogaru et al., Int J Quantum Chem 2008, 108; Motiu et al., Int J Quantum Chem 2007, 107, 1248). We used the hybrid quantum mechanics/molecular mechanics (QM/MM) method to study the reactivation pathways of the exogenously inhibited enzyme matrix. The ONIOM calculations performed on the enzyme agree with experimental results (Liu et al., J Am Chem Soc 2002, 124, 5175), that is, wild-type [Fe-Fe]-hydrogenase H-cluster is inhibited by oxygen metabolites. An enzyme spherical region …
Dnmt1 Stability Is Regulated By Proteins Coordinating Deubiquitination And Acetylation-Driven Ubiquitination, Zhanwen Du, Jing Song, Yong Wang, Yiqing Zhao, Kishore Guda, Shuming Yang, Hung Ying Kao, Yan Xu, Joseph Willis, Sanford D. Markowitz, David Sedwick, Robert M. Ewing, Zhenghe Wang
Dnmt1 Stability Is Regulated By Proteins Coordinating Deubiquitination And Acetylation-Driven Ubiquitination, Zhanwen Du, Jing Song, Yong Wang, Yiqing Zhao, Kishore Guda, Shuming Yang, Hung Ying Kao, Yan Xu, Joseph Willis, Sanford D. Markowitz, David Sedwick, Robert M. Ewing, Zhenghe Wang
Chemistry Faculty Publications
DNA methyltransferase 1 (DNMT1) is the primary enzyme that maintains DNA methylation. We describe a previously unknown mode of regulation of DNMT1 protein stability through the coordinated action of an array of DNMT1-associated proteins. DNMT1 was destabilized by acetylation by the acetyltransferase Tip60, which triggered ubiquitination by the E3 ligase UHRF1, thereby targeting DNMT1 for proteasomal degradation. In contrast, DNMT1 was stabilized by histone deacetylase 1 (HDAC1) and the deubiquitinase HAUSP (herpes virus–associated ubiquitin-specific protease). Analysis of the abundance of DNMT1 and Tip60, as well as the association between HAUSP and DNMT1, suggested that during the cell cycle the initiation …
Cox-2 Inhibitor Nimesulide Analogs Are Aromatase Suppressors In Breast Cancer Cells, Bin Su, Xiaohan Cai, Yanyan Hong, Shiuan Chen
Cox-2 Inhibitor Nimesulide Analogs Are Aromatase Suppressors In Breast Cancer Cells, Bin Su, Xiaohan Cai, Yanyan Hong, Shiuan Chen
Chemistry Faculty Publications
Cyclooxygenase-2 (COX-2) inhibitor nimesulide derivatives compounds A and B decreased aromatase activity in breast cancer cells via a novel mechanism different to aromatase inhibitors (AIs), and were defined as “aromatase suppressors”. Breast carcinoma cells (MCF-7aro and T47Daro) transfected with aromatase full gene were used to explore the mechanisms of the two compounds. They dose and time-dependently suppressed aromatase activity in MCF-7aro and T47Daro cells in the nanomole range. However, they neither directly inhibited aromatase, nor improved aromatase degradation even at much higher concentrations. They could also suppress androgen stimulated cell growth, but did not affect estrogen enhanced cell proliferation. These …
Residue Mutations In [Fe-Fe]-Hydrogenase Impedes O 2 Binding: A Qm/Mm Investigation, Daniela Dogaru, Stefan Motiu, Valentin Gogonea
Residue Mutations In [Fe-Fe]-Hydrogenase Impedes O 2 Binding: A Qm/Mm Investigation, Daniela Dogaru, Stefan Motiu, Valentin Gogonea
Chemistry Faculty Publications
[Fe-Fe]-hydrogenases are enzymes that reversibly catalyze the reaction of protons and electrons to molecular hydrogen, which occurs in anaerobic media. In living systems, [Fe-Fe]-hydrogenases are mostly used for H(2) production. The [Fe-Fe]-hydrogenase H-cluster is the active site, which contains two iron atoms. The latest theoretical investigations1,2 advocate that the structure of di-iron air inhibited species are either Fe(p) (II)-Fe(d) (II)-O-H(-), or Fe(p) (II)-Fe(d) (II)-O-O-H, thus O(2) has to be prevented from binding to Fe(d) in all di-iron subcluster oxidation states in order to retain a catalytically active enzyme. By performing residue mutations on [Fe-Fe]-hydrogenases, we were able to weaken O(2) …
An Antimicrobial Peptide Regulates Tumor-Associated Macrophage Trafficking Via The Chemokine Receptor Ccr2, A Model For Tumorigenesis, Ge Jin, Hameem I. Kawsar, Stanley A. Hirsch, Chun Zeng, Xun Jia, Zhimin Feng, Santosh K. Ghosh, Qing Yin Zheng, Aimin Zhou, Thomas M. Mcintyre, Aaron Weinberg
An Antimicrobial Peptide Regulates Tumor-Associated Macrophage Trafficking Via The Chemokine Receptor Ccr2, A Model For Tumorigenesis, Ge Jin, Hameem I. Kawsar, Stanley A. Hirsch, Chun Zeng, Xun Jia, Zhimin Feng, Santosh K. Ghosh, Qing Yin Zheng, Aimin Zhou, Thomas M. Mcintyre, Aaron Weinberg
Chemistry Faculty Publications
Background: Tumor-associated macrophages (TAMs) constitute a significant part of infiltrating inflammatory cells that are frequently correlated with progression and poor prognosis of a variety of cancers. Tumor cell-produced human β-defensin-3 (hBD-3) has been associated with TAM trafficking in oral cancer; however, its involvement in tumor-related inflammatory processes remains largely unknown. Methodology: The relationship between hBD-3, monocyte chemoattractant protein-1 (MCP-1), TAMs, and CCR2 was examined using immunofluorescence microscopy in normal and oral carcinoma in situ biopsy specimens. The ability of hBD-3 to chemoattract host macrophages in vivo using a nude mouse model and analysis of hBD-3 on monocytic cell migration in …
Terminal Deoxynucleotidyl Transferase: The Story Of A Misguided Dna Polymerase, Edward A. Motea, Anthony J. Berdis
Terminal Deoxynucleotidyl Transferase: The Story Of A Misguided Dna Polymerase, Edward A. Motea, Anthony J. Berdis
Chemistry Faculty Publications
Nearly every DNA polymerase characterized to date exclusively catalyzes the incorporation of mononucleotides into a growing primer using a DNA or RNA template as a guide to direct each incorporation event. There is, however, one unique DNA polymerase designated terminal deoxynucleotidyl transferase that performs DNA synthesis using only single-stranded DNA as the nucleic acid substrate. In this chapter, we review the biological role of this enigmatic DNA polymerase and the biochemical mechanism for its ability to perform DNA synthesis in the absence of a templating strand. We compare and contrast the molecular events for template-independent DNA synthesis catalyzed by terminal …
Non-Natural Nucleotides As Probes For The Mechanism And Fidelity Of Dna Polymerases, Irene Lee, Anthony J. Berdis
Non-Natural Nucleotides As Probes For The Mechanism And Fidelity Of Dna Polymerases, Irene Lee, Anthony J. Berdis
Chemistry Faculty Publications
DNA is a remarkable macromolecule that functions primarily as the carrier of the genetic information of organisms ranging from viruses to bacteria to eukaryotes. The ability of DNA polymerases to efficiently and accurately replicate genetic material represents one of the most fundamental yet complex biological processes found in nature. The central dogma of DNA polymerization is that the efficiency and fidelity of this biological process is dependent upon proper hydrogen-bonding interactions between an incoming nucleotide and its templating partner. However, the foundation of this dogma has been recently challenged by the demonstration that DNA polymerases can effectively and, in some …
Dna Polymerases: Perfect Enzymes For An Imperfect World, Anthony J. Berdis
Dna Polymerases: Perfect Enzymes For An Imperfect World, Anthony J. Berdis
Chemistry Faculty Publications
This Special Thematic Issue explores the molecular properties of DNA polymerases as extraordinary biological catalysts. In this short introductory chapter, I briefly highlight some of the most important concepts from the articles contained within this Special Issue. The contents of this Special Issue are arranged into distinct sub-categories corresponding to mechanistic studies of faithful DNA polymerization, studies of "specialized" DNA polymerases that function on damaged DNA, and DNA polymerases that are of therapeutic importance against various diseases. Emphasis is placed on understanding the dynamic cellular roles and biochemical functions of DNA polymerases, and how their structure and mechanism impact their …
Nanostructured Poly(3,4-Ethylenedioxythiophene)–Metalloporphyrin Films: Improved Catalytic Detection Of Peroxynitrite, Serban Peteu, Pubudu Peiris, Ermias Gebermichael, Mekki Bayachou
Nanostructured Poly(3,4-Ethylenedioxythiophene)–Metalloporphyrin Films: Improved Catalytic Detection Of Peroxynitrite, Serban Peteu, Pubudu Peiris, Ermias Gebermichael, Mekki Bayachou
Chemistry Faculty Publications
We investigated in this paper the sensing performance of inherently conductive polymer, poly(3,4-ethylenedioxythiophene) (PEDOT), functionalized with hemin (iron protoporphyrin) as an electrocatalytic reporter. The sensing platform is prepared by electrodeposition of a composite film of hemin–PEDOT on a 30-μm diameter carbon fiber electrode (CFE). The polymerized films were characterized by field emission scanning electron microscopy (FESEM), which pointed to nanostructured films with tortuous pores. The electrocatalytic oxidation of peroxynitrite was characterized by cyclic voltammetry as well as other electrochemical methods. The catalytic current is proportional to the analyte's concentration. Optimized hemin–PEDOT modified CFEs were utilized for the first time to …
Selective Regulation Of Aromatase Expression For Drug Discovery, Robert W. Brueggemeier, Bin Su, Michael V. Darby, Yasuro Sugimoto
Selective Regulation Of Aromatase Expression For Drug Discovery, Robert W. Brueggemeier, Bin Su, Michael V. Darby, Yasuro Sugimoto
Chemistry Faculty Publications
Aromatase is a particularly attractive drug target in the treatment of hormone-responsive breast cancer, and aromatase activity in breast cancer patients is greater in or near the tumor tissue compared with the normal breast tissue. Complex regulation of aromatase expression in human tissues involves alternative promoter sites that provide tissue-specific control. Previous studies in our laboratories suggested a strong association between aromatase (CYP19) gene expression and the expression of cyclooxygenase (COX) genes. Additionally, COX selective inhibitors can suppress CYP19 gene expression and decrease aromatase activity. Our current hypothesis is that pharmacological regulation of aromatase can act locally to decrease the …
Homozygous Frameshift Mutation In Tmco1 Causes A Syndrome With Craniofacial Dysmorphism, Skeletal Anomalies, And Mental Retardation, Baozhong Xin, Erik G. Puffenberger, Susan Turben, Haiyan Tan, Aimin Zhou, Heng Wang
Homozygous Frameshift Mutation In Tmco1 Causes A Syndrome With Craniofacial Dysmorphism, Skeletal Anomalies, And Mental Retardation, Baozhong Xin, Erik G. Puffenberger, Susan Turben, Haiyan Tan, Aimin Zhou, Heng Wang
Chemistry Faculty Publications
We identified an autosomal recessive condition in 11 individuals in the Old Order Amish of northeastern Ohio. The syndrome was characterized by distinctive craniofacial dysmorphism, skeletal anomalies, and mental retardation. The typical craniofacial dysmorphism included brachycephaly, highly arched bushy eyebrows, synophrys, long eyelashes, low-set ears, microdontism of primary teeth, and generalized gingival hyperplasia, whereas Sprengel deformity of scapula, fusion of spine, rib abnormities, pectus excavatum, and pes planus represented skeletal anomalies. The genome-wide homozygosity mapping using six affected individuals localized the disease gene to a 3.3-Mb region on chromosome 1q23.3-q24.1. Candidate gene sequencing identified a homozygous frameshift mutation, c.139_140delAG, in …
Design, Synthesis And Characterization Of Oriented Glyco-Affinity Macroligands For Glyco-Capturing, Glycomics And Glycoproteomics Applications, Srinivas Chalagalla
Design, Synthesis And Characterization Of Oriented Glyco-Affinity Macroligands For Glyco-Capturing, Glycomics And Glycoproteomics Applications, Srinivas Chalagalla
ETD Archive
Cell surface carbohydrates existing as parts of glycoproteins, glycolipids, and other conjugates present the first information about cell to the outside world and are intimately involved in various biological events such as intercellular communication, and molecular and cellular targeting. However, mechanisms of most processes at the molecular level are still unclear. Therefore, it is very important to develop carbohydrate-specific binding molecules for rapid, efficient, sensitive purification and accurate analysis of complex carbohydrate structures as well as their functions. Furthermore, carbohydrate-specific binding molecules can be expected to be used in medical diagnostic applications for carbohydrate biomarkers. In this thesis study, oriented …
Dna Mutation/Methylation Screening Method For Colon Cancer Screening, Wei Meng
Dna Mutation/Methylation Screening Method For Colon Cancer Screening, Wei Meng
ETD Archive
Cancer is a result of unregulated cell growth. For all types of cancer currently studied, the transition from a healthy cell to a malignant tumor cell is a step-by-step process which requires mutation in at least several oncogenes and tumor suppressor genes together. Another cancer early event is DNA methylation. Cancer-related DNA methylation focuses on promoter hypermethylation of the certain genes. The DNA mutation and methylation profile can serve as biomarkers for diagnosing early stage of cancer. Colorectal cancer is the third most common cancer type in the United States and has been well studied. The essential mechanism of cancer …
Molecular Basis Of The Role Of Kindlin 2 In Cell Adhesion, Hettiarachchige Dhanuja Deepamalee Perera
Molecular Basis Of The Role Of Kindlin 2 In Cell Adhesion, Hettiarachchige Dhanuja Deepamalee Perera
ETD Archive
Kindlins are a novel family of cytoskeleton proteins that plays an important role in the activation of heterodimeric integrin transmembrane receptors. These receptors play a vital role in cell adhesion, cell migration and other cellular processes. The Kindlin protein family consists of three homologous proteins, Kindlin 1, 2 and 3 with differential tissue distribution and varying expression levels in human. Mutations of Kindlin 1 protein are clinically linked to Kindler Syndrome. Kindlin 2 knockdown studies have shown embryonic lethality in mouse, but no diseases have been clinically testified. Kindlin 3 mutations are associated with bleeding disorders, e.g. LADIII. Talin is …
Human Prostate Cancer Cell Apoptosis Induced By Interferon-Y And Double-Stranded Rna And Studies On The Biological Roles Of Transmembrane And Coiled-Coil Domains 1, Haiyan Tan
ETD Archive
No abstract provided.
Study Of Drug Delivery Behavior Through Biomembranes Using Thermal And Bioanalytical Techniques, Hareesha Reddy Venumuddala
Study Of Drug Delivery Behavior Through Biomembranes Using Thermal And Bioanalytical Techniques, Hareesha Reddy Venumuddala
ETD Archive
This Master of Science thesis encompasses two projects in chemical pharmaceuticals. The first is a study of excipients and the added new information collected beyond Thermal Gravimetric Analysis and Differential Scanning Calorimetry from Dielectric Analysis. These new properties enhance our global knowledge of excipients by thermal analytical methods. Excipients, the inactive ingredients in formulated drugs, aid different functions of the active pharmacy ingredient, the drugs. Low temperature transitions, by DEA including melting of frozen solvents, e.g. water, are more definitive than observed by low temperature DSC. Millions of dollars are expended annually on pharmaceutical testing to qualify excipients for fully …
Disintegration Of Tablets And Capsules Measured By Isothermal Thermal Mechanical Analysis And Macrophotography, Visweswararao Badipatla
Disintegration Of Tablets And Capsules Measured By Isothermal Thermal Mechanical Analysis And Macrophotography, Visweswararao Badipatla
ETD Archive
The current United States Pharmacopoeia (USP) test for tablet and encapsulated drug disintegration does not specify the initial disintegration time and provides limited information on the disintegration process itself. An isothermal Thermal Mechanical Analysis (IsoTMA) method is presented to measure the rate and initial time of drug disintegration, that is, the mechanical collapse of the gelatin capsule or the solid tablet. This method monitors changes in the dimensions of the formulated drugs during their disintegration in a liquid. Dimensional changes can be followed as a function of time, temperature, applied stress and pH. Some of the drugs studied were Olanzapine®, …
Targeting Base Excision Repair Suggests A New Therapeutic Strategy Of Fludarabine For The Treatment Of Chronic Lymphocytic Leukemia, A. D. Bulgar, M. Snell, J. R. Donze, E. B. Kirkland, Lan Li, Shuming Yang, Yan Xu, S. L. Gerson, Lili Liu
Targeting Base Excision Repair Suggests A New Therapeutic Strategy Of Fludarabine For The Treatment Of Chronic Lymphocytic Leukemia, A. D. Bulgar, M. Snell, J. R. Donze, E. B. Kirkland, Lan Li, Shuming Yang, Yan Xu, S. L. Gerson, Lili Liu
Chemistry Faculty Publications
No abstract provided.
Highly Nitrated Cyclopropanes As New High Energy Materials: Dft Calculations On The Properties Of C3H6−N(No2)N (N=3–6), Aloysus K. Lawong, David W. Ball
Highly Nitrated Cyclopropanes As New High Energy Materials: Dft Calculations On The Properties Of C3H6−N(No2)N (N=3–6), Aloysus K. Lawong, David W. Ball
Chemistry Faculty Publications
As part of a continuing study of new potential high energy materials, here we present results of calculations on cyclopropane molecules with three or more nitro groups. DFT calculations suggest that all molecules can exist as minimum-energy stationary states. Energy calculations indicate that some nitrocyclopropanes have a specific enthalpy of decomposition in excess of 8kJg−1, suggesting that they be explored as new potential high energy materials.
Double Superhelix Model Of High Density Lipoprotein, Zhiping Wu, Valentin Gogonea, Xavier Lee, Mathew A. Wagner
Double Superhelix Model Of High Density Lipoprotein, Zhiping Wu, Valentin Gogonea, Xavier Lee, Mathew A. Wagner
Chemistry Faculty Publications
High density lipoprotein (HDL), the carrier of so-called “good” cholesterol, serves as the major athero-protective lipoprotein and has emerged as a key therapeutic target for cardiovascular disease. We applied small angle neutron scattering (SANS) with contrast variation and selective isotopic deuteration to the study of nascent HDL to obtain the low resolution structure in solution of the overall time-averaged conformation of apolipoprotein AI (apoA-I) versus the lipid (acyl chain) core of the particle. Remarkably, apoA-I is observed to possess an open helical shape that wraps around a central ellipsoidal lipid phase. Using the low resolution SANS shapes of the protein …
Synthesis And Cytotoxic Analysis Of Some Disodium 3Β,6Β-Dihydroxysterol Disulfates, Jianguo Cui, Hui Wang, Yi Xin, Aimin Zhou
Synthesis And Cytotoxic Analysis Of Some Disodium 3Β,6Β-Dihydroxysterol Disulfates, Jianguo Cui, Hui Wang, Yi Xin, Aimin Zhou
Chemistry Faculty Publications
Disodium 3β,6β-dihydroxy-5α-cholestane disulfate (1) was synthesized in 4 steps with a high overall yield from cholesterol. First, cholesterol (4a) was converted to cholest-4-en-3,6-dione (5a) via oxidation with pyridinium chlorochromate (PCC) and then 5a was reduced by NaBH4 in the presence of NiCl2 to produce cholest-3β,6β-diol (6a). The reaction of 6a with the triethylamine-sulfur trioxide complex generated diammonium 3β,6β-dihydroxy-5α-cholestane disulfate (7a) and the treatment of 7a by cation exchange resin 732 (sodium form)(Na+) yielded the target steroid 1. Disodium 24-ethyl-3β,6β-dihydroxycholest-22-ene disulfate (2) and disodium 24-ethyl-3β,6β-dihydroxycholestane disulfate (3) were synthesized using a similar method. The cytotoxicity of these compounds against Sk-Hep-1 (human …
Lead Optimization Of Cox-2 Inhibitor Nimesulide Analogs To Overcome Aromatase Inhibitor Resistance In Breast Cancer Cells, Bin Su, Shiuan Chen
Lead Optimization Of Cox-2 Inhibitor Nimesulide Analogs To Overcome Aromatase Inhibitor Resistance In Breast Cancer Cells, Bin Su, Shiuan Chen
Chemistry Faculty Publications
A series of COX-2 selective inhibitor nimesulide derivatives were synthesized. Their anti-cell proliferation activities were evaluated with a long-term estrogen deprived MCF-7aro (LTEDaro) breast cancer cell line, which is the biological model of aromatase inhibitor resistance for hormone-dependent breast cancer. Compared to nimesulide which inhibited LTEDaro cell proliferation with an IC50 at 170.30 μM, several new compounds showed IC50 close to 1.0 μM.
Determination Of 6-Benzylthioinosine In Mouse And Human Plasma By Liquid Chromatography–Tandem Mass Spectrometry, Lan Li, Yan Xu, David N. Wald, William Tse
Determination Of 6-Benzylthioinosine In Mouse And Human Plasma By Liquid Chromatography–Tandem Mass Spectrometry, Lan Li, Yan Xu, David N. Wald, William Tse
Chemistry Faculty Publications
This paper described the development and validation of a liquid chromatography–tandem mass spectrometry (LC–MS/MS) method for the quantitative determination of 6-benzylthioinosine (6BT), a novel myeloid leukemia differentiation-inducing agent, in mouse and human plasma. In this method, 2-amino-6-benzylthioinosine (2A6BT) was used as internal standard and ethyl acetate was used as organic solvent for the extraction of 6BT and internal standard from plasma samples. The extracted samples were separated on YMC ODS-AQ® column (2.0 mm × 50 mm), and the eluates from the column were monitored by the positive-electrospray-ionization tandem mass spectrometer (ESI+-MS/MS). Quantification of 6BT by internal calibration with 2A6BT was …