Medicinal-Pharmaceutical Chemistry Commons^™

Identifying Medication Targets For Psychostimulant Addiction: Unraveling The Dopamine D3 Receptor Hypothesis, Thomas M. Keck, William S. John, Paul W. Czoty, Michael A. Nader, Amy Hauck Newman

College of Science & Mathematics Departmental Research

The dopamine D3 receptor (D3R) is a target for developing medications to treat substance use disorders. D3R-selective compounds with high affinity and varying efficacies have been discovered, providing critical research tools for cell-based studies that have been translated to in vivo models of drug abuse. D3R antagonists and partial agonists have shown especially promising results in rodent models of relapse-like behavior, including stress-, drug-, and cue-induced reinstatement of drug seeking. However, to date, translation to human studies has been limited. Herein, we present an overview and illustrate some of the pitfalls and challenges of developing novel D3R-selective compounds toward clinical …

Facile Methods For The Analysis Of Lysophosphatidic Acids In Human Plasma, Jialu Wang

Dissertations and Theses

Lysophosphatidic acid (LPA) influences many physiological processes, such as brain and vascular development. It is associated with several diseases including ovarian cancer, breast cancer, prostate cancer, colorectal cancer, hepatocellular carcinoma, multiple myeloma atherosclerotic diseases, cardiovascular diseases, pulmonary inflammatory diseases and renal diseases. LPA plasma and serum levels have been reported to be important values in diagnosing ovarian cancer and other diseases. However, the extraction and quantification of LPA in plasma are very challenging because of the low physiological concentration and similar structures of LPA to other phospholipids. Many previous studies have not described the separation of LPA from other phospholipids, …

Stability Of Lidocaine Tested By Forced Degradation And Its Interactions With Serum Albumin, Lindsay Nichols

STAR Program Research Presentations

A concern for future long-term manned space expeditions is the ability to treat illnesses with appropriate pharmaceuticals. However, pharmaceuticals degrade faster in space than on Earth presumably due to an abundance of space radiation. The stability of Lidocaine was investigated because it is a common pain reliever currently used on the International Space Station. One of the most common proteins in blood is serum albumin, which acts as a carrier to distribute drugs throughout the body. It is important to know how well the drug binds to serum albumin so that the rate of distribution of Lidocaine-bound protein in blood …

Stereocontrolled 1,2-Cis Glycosylation As The Driving Force Of Progress In Synthetic Carbohydrate Chemistry, Swati Nigudkar, Alexei Demchenko

Chemistry & Biochemistry Faculty Works

Recent developments in stereoselective 1,2-cis glycosylation that have emerged during the past decade are surveyed herein. For detailed coverage of the previous achievements in the field the reader is referred to our earlier reviews: A. V. Demchenko, Curr. Org. Chem., 2003, 7, 35–79 and Synlett, 2003, 1225–1240.

Energetics, Structure, And Rovibrational Spectroscopic Properties Of The Sulfurous Anions Sno− And Osn−, Ryan C. Fortenberry, Joseph S. Francisco

Department of Chemistry: Faculty Publications

The SNO⁻ and OSN⁻ anions are shown in this work to be very stable negatively charged species in line with other recent work [T. Trabelsi et al., J. Chem. Phys. 143, 164301 (2015)]. Utilizing established quartic force field techniques, the structural and rovibrational data for these anions are produced. The SNO⁻ anion is less linear and has weaker bonds than the corresponding neutral radical giving much smaller rotational constants.OSN⁻ is largely unchanged in these regards with inclusion of the additional electron.The S–N bond is actually stronger,and the rotational constants of OSN⁻ versus OSN are …

The Importance Of Context: An Exploration Of Factors Influencing The Adoption Of Student-Centered Teaching Among Chemistry, Biology, And Physics Faculty, Travis J. Lund, Marilyne Stains

Department of Chemistry: Faculty Publications

Background: Research at the secondary and postsecondary levels has clearly demonstrated the critical role that individual and contextual characteristics play in instructors’ decision to adopt educational innovations. Although recent research has shed light on factors influencing the teaching practices of science, technology, engineering, and mathematics (STEM) faculty, it is still not well understood how unique departmental environments impact faculty adoption of evidence-based instructional practices (EBIPs) within the context of a single institution. In this study, we sought to characterize the communication channels utilized by STEM faculty, as well as the contextual and individual factors that influence the teaching practices …

Hfq Regulates Antibacterial Antibiotic Biosynthesis And Extracellular Lytic-Enzyme Production In Lysobacter Enzymogenes Oh11, Gaoge Xu, Yuxin Zhao, Liangcheng Du, Guoliang Qian, Fengquan Liu

Department of Chemistry: Faculty Publications

Lysobacter enzymogenes is an important biocontrol agent with the ability to produce a variety of lytic enzymes and novel antibiotics. Little is known about their regulatory mechanisms. Understanding these will be helpful for improving biocontrol of crop diseases and potential medical application. In the present study, we generated an hfq (encoding a putative ribonucleic acid chaperone) deletion mutant, and then utilized a new genomic marker-free method to construct an hfq-complemented strain. We showed for the first time that Hfq played a pleiotropic role in regulating the antibacterial antibiotic bio- synthesis and extracellular lytic enzyme activity in L. enzymogenes. Mutation of …

Ketoconozole, Jeremy M. Wood

Natural Sciences Student Research Presentations

This is a poster presented at the Natural Sciences Poster Session at Parkland College, which provides the chemical makeup, dosage, and the body's response to Ketoconazole, or Nizoral, an antifungal medication used in the treatment of animals.

Lamictal, Jessica L. Sherman-Corbett

Natural Sciences Student Research Presentations

This is a poster presented at the Natural Sciences Poster Session at Parkland College, which provides the chemical makeup, dosage, and the body's response to Lamictal, a medication used as therapy for seizure disorders and bipolar disorders in adults.

Specific N-Glycans Of Hepatocellular Carcinoma Cell Surface And The Abnormal Increase Of Core-Α-1, 6-Fucosylated Triantennary Glycan Via N-Acetylglucosaminyltransferases-Iva Regulation, Huan Nie, Xia Liu, Yubao Zhang, Tingting Li, Chao Zhan, Wenjuan Huo, Anshun He, Yuanfei Yao, Yu Jin, Youpeng Qu, Xue-Long Sun, Yu Li

Chemistry Faculty Publications

Glycosylation alterations of cell surface proteins are often observed during the progression of malignancies. The specific cell surface N-glycans were profiled in hepatocellular carcinoma (HCC) with clinical tissues (88 tumor and adjacent normal tissues) and the corresponding serum samples of HCC patients. The level of core-α-1,6-fucosylated triantennary glycan (NA3Fb) increased both on the cell surface and in the serum samples of HCC patients (p < 0.01). Additionally, the change of NA3Fb was not influenced by Hepatitis B virus (HBV)and cirrhosis. Furthermore, the mRNA and protein expression of N-acetylglucosaminyltransferase IVa (GnT-IVa), which was related to the synthesis of the NA3Fb, was substantially increased in HCC tissues. Knockdown of GnT-IVa leads to a decreased level of NA3Fb and decreased ability of invasion and migration in HCC cells. NA3Fb can be regarded as a specific cell surface N-glycan of HCC. The high expression of GnT-IVa is the cause of the abnormal increase of NA3Fb on the HCC cell surface, which regulates cell migration. This study demonstrated the specific N-glycans of the cell surface and the mechanisms of altered glycoform related with HCC. These findings lead to better understanding of the function of glycan and glycosyltransferase in the tumorigenesis, progression and metastasis of HCC.

Development Of Non-Traditional Platinum Anticancer Agents: Trans-Platinum Planar Amine Compounds And Polynuclear Platinum Compounds, Daniel E. Lee

Theses and Dissertations

Development of Non-Traditional Platinum Anticancer Agents: trans-Platinum Planar Amine Compounds and Polynuclear Platinum Compounds

By Daniel E. Lee, Ph.D.

A dissertation submitted in partial fulfillment of the requirements for the degree of Doctor of Philosophy at Virginia Commonwealth University.

Virginia Commonwealth University, 2015

Major Director: Nicholas P Farrell, Ph.D., Professor, Department of Chemistry

Platinum anticancer compounds with cis geometry, similar to cisplatin, have been explored to circumvent the cisplatin resistance; however, they were not considered broadly active in cisplatin cells due to exhibiting similar or same cell death mechanism as cisplatin. Platinum compounds with trans geometry were less studied …

Peptide Drug Discovery: Innovative Technologies And Transformational Medicines, David J. Diller, Mark Jarosinski, Tomi K. Sawyer, Joseph Audie

Chemistry & Physics Faculty Publications

Interest in peptide drug discovery is surging. In the past several years,numerous pharmaceutical and biotech companies have committed considerable resources to peptide-based drug discovery. In part,this is being fueled by an increasing recognition that peptide drugs combine many of the virtues of small molecules and proteins, while minimizing several of their drawbacks, and that peptides can potentially expand the druggable space to include intracellular, extracellular and membrane associated protein–protein interactions. Moreover, powerful new in vitro and in silico technologies and breakthroughs in our understanding of natural peptides have emerged that provide peptide chemists with the toolsand insights they need to …

Zyban, Shawna R. Meadows

Natural Sciences Student Research Presentations

This is a poster presented at the Natural Sciences Poster Session at Parkland College, which provides the chemical makeup, dosage, and the body's response to Zyban, or bupropion hydrochloride, a medication used to treat depression and seasonal affective disorder.

Kapvay, Russell E. Anderson

Natural Sciences Student Research Presentations

This is a poster presented at the Natural Sciences Poster Session at Parkland College, which provides the chemical makeup, dosage, and the body's response to Kapvay, or Clonidine Hydrochloric, a medication used to manage hypertension and in the treatment of severe pain.

Cordarone, Miriana Mccombe

Natural Sciences Student Research Presentations

This is a poster presented at the Natural Sciences Poster Session at Parkland College, which provides the chemical makeup, dosage, and the body's response to Cordarone, or amiodarone hydrochloride, a medication used for the treatment of ventricular arrhythmias and supraventricular arrhythmias.

Paxil, Allyson M. Hadfield

Natural Sciences Student Research Presentations

This is a poster presented at the Natural Sciences Poster Session at Parkland College, which provides the chemical makeup, dosage, and the body's response to Paxil, a medication used to treat depression, obsessive-compulsive disorders, panic attacks and anxiety disorders.

Orap, Sophie A. Catlin

Natural Sciences Student Research Presentations

This is a poster presented at the Natural Sciences Poster Session at Parkland College, which provides the chemical makeup, dosage, and the body's response to Orap, a medication used in the treatment of Tourette's syndrome.

The Link Between Adhd And Chemical Exposures, Lily Rong

Natural Sciences Student Research Presentations

A part of the Natural Sciences Poster Session at Parkland College, this poster investigates the relationship of Attention Deficit Hyperactivity Disorder to exposures to perfluorinated compounds (PFCs) and polychlorinated biphenyls (PCBs).

Interesting Properties Of P-, D-, And F-Block Elements When Coordinated With Dipicolinic Acid And Its Derivatives As Ligands: Their Use As Inorganic Pharmaceuticals, Michael J. Celestine, Jimmie L. Bullock, Shivani Boodram, Varma H. Rambaran, Alvin A. Holder

Chemistry & Biochemistry Faculty Publications

This is a review of the literature concerning the interesting properties of p-, d-, and f-block elements when coordinated with 2,6-pyridinedicarboxylic acid (dipicolinic acid, H₂dipic) and its derivatives as ligands, with a focus on their use as inorganic pharmaceuticals. Some of the complexes reported were used as insulin-like, bioimaging contrasting agents, antimicrobial agents, and anticancer agents.

Design, Synthesis, And Pharmacological Evaluation Of Three Series Of Lobelane Analogs As Inhibitors Of The Vesicular Monoamine Transporter (Vmat2), John P. Culver

Theses and Dissertations--Pharmacy

Methamphetamine (METH) abuse is a serious problem in the United States and worldwide. The reward experienced by METH users is due to the increase in extracellular dopamine (DA) concentrations caused by an interaction between METH and the DA transporter (DAT) as well as the Vesicular Monoamine Transporter-2 (VMAT2). The reward felt by users of METH leads to further use of the drug and subsequent abuse. The current project examined the ability of three novel series of lobelane analogs to interact with a binding site on the Vesicular Monoamine Transporter-2 (VMAT2) in an attempt to inhibit the effects of METH. Lobelane …