A5064506209- Radiopharmaceutical Chemistry and Applications
- Medical Imaging Techniques and Applications
- Cancer, Hypoxia, and Metabolism
- Cancer Treatment and Pharmacology
- Urinary Bladder and Prostate Research
- ATP Synthase and ATPases Research
- Microtubule and mitosis dynamics
- Peptidase Inhibition and Analysis
- Prostate Cancer Treatment and Research
- Sphingolipid Metabolism and Signaling
- Medical Imaging and Pathology Studies
- Estrogen and related hormone effects
- Metabolism, Diabetes, and Cancer
- Inflammatory mediators and NSAID effects
- Click Chemistry and Applications
- Nanoplatforms for cancer theranostics
- Lanthanide and Transition Metal Complexes
- Urinary Tract Infections Management
- Lung Cancer Treatments and Mutations
- Hormonal and reproductive studies
- Monoclonal and Polyclonal Antibodies Research
- Endoplasmic Reticulum Stress and Disease
- Synthetic Organic Chemistry Methods
- Ion Channels and Receptors
- Eicosanoids and Hypertension Pharmacology
University of Alberta
2016-2025
Centre for Addiction and Mental Health
2022
McGill University
2022
Health Net
2022
University Health Network
2022
Alberta Hospital Edmonton
2015-2021
Northern Alberta Institute of Technology
2019
Cancer Institute (WIA)
2010-2014
TU Dresden
2001-2013
Lantheus Medical Imaging (United States)
2010
Cyclooxygenase-2 isozyme is a promising anti-inflammatory drug target, and overexpression of this enzyme also associated with several cancers neurodegenerative diseases. The amino-acid sequence structural similarity between inducible cyclooxygenase-2 housekeeping cyclooxygenase-1 isoforms present significant challenge to design selective inhibitors. Herein, we describe the use active site as reaction vessel for in situ generation its own highly specific Multi-component competitive-binding...
Macrocyclic chelators and their metal complexes have widespread applications in the biomedical sciences, including radiopharmaceutical chemistry. The use of copper radionuclides radiopharmaceuticals is increasing. been found to enhanced vivo stability over acyclic such as ethylenediaminetetraacetic acid (EDTA) diethylenetriaminepentaacetic (DTPA). currently used choice for labeling biological molecules are analogues TETA (1,4,8,11-tetraazacyclotetradecane-1,4,8,11-tetraacetic acid); however,...
Prostate-specific membrane antigen (PSMA) is frequently overexpressed and upregulated in prostate cancer. To date, various (18)F- (68)Ga-labeled urea-based radiotracers for PET imaging of PSMA have been developed entered clinical trials. Here, we describe an automated synthesis [(18)F]DCFPyL via direct radiofluorination validation preclinical models cancer.[(18)F]DCFPyL was synthesized nucleophilic heteroaromatic substitution reaction a single reactor TRACERlab FXFN unit....
Elevated growth in breast cancer (BC) activates hypoxia-inducible factor (HIF1a) and downstream, facilitative glucose transporter 1 (GLUT1), which can be visualized with 2-deoxy-2-[18F]fluoro-D-glucose ([18F]FDG). GLUT5 (fructose) GLUT2 (glucose/fructose) might provide alternative targets for BC imaging as to why effects of hypoxia on GLUT1/2/5 levels function were examined human models. HIF1a mRNA was analyzed patient biopsies. In MCF10A, MCF7, MDA-MB231 cells, [18F]FDG,...
The copper-free strain-promoted click chemistry between 18F-labeled aza-dibenzocyclooctyne [18F]FB-DBCO and various azides is described. was prepared in 85% isolated radiochemical yield (decay-corrected) through acylation of amino 1 with N-succinimidyl 4-[18F]fluorobenzoate ([18F]SFB). showed promising radiopharmacological profil fast blood clearance as assessed dynamic small animal PET studies. Metabolic stability 60% intact compound after 60 min post injection normal Balb/C mice half-life...
Abstract Autotaxin catalyzes the formation of lysophosphatidic acid, which stimulates tumor growth and metastasis decreases effectiveness cancer therapies. In breast cancer, autotaxin is secreted mainly by adipocytes, especially when stimulated inflammatory cytokines produced tumors. this work, we studied effects an ATX inhibitor, GLPG1690, in phase III clinical trials for idiopathic pulmonary fibrosis, on responses to radiotherapy chemotherapy a syngeneic orthotopic mouse model cancer....
Target modules (TMs), intermediate molecules required for UniCAR T-cell therapy, are promising immunotheranostic approaches. In the current work, we developed TMs containing a monomeric or dimeric form of antagonist bombesin peptide (BBN2) and assessed their potential diagnostic imaging using positron emission tomography (PET) as well immunotherapy in combination with T-cells to target image GRPR expression prostate cancer. Synthesized BBN2 retained binding vitro. Both specifically activated...
(-)-Isoproterenol [4-[1-hydroxy-2-[(1-methylethyl)amino]ethyl]-1,2-benzene diol hydrochloride] relaxes murine detrusor through beta-adrenoceptors (ARs); however, the beta-AR subtypes involved are unknown. beta(2)-ARs have been associated with caveolae, plasma-lemmal scaffolding domains that absent in caveolin-1 (cav-1) knockout (KO) mice. Here, we studied responses absence and presence of subtype-selective antagonists wild-type (WT) cav-1 KO To inquire whether model is relevant to man,...
<sup>18</sup>F-3′-Deoxy-3′-fluorothymidine (<sup>18</sup>F-FLT) is a PET tracer that accumulates in proliferating tissues. The current study was undertaken to determine whether equilibrative nucleoside transporter 1 (ENT1) important for <sup>18</sup>F-FLT uptake normal tissues and tumors. <b>Methods:</b> ENT1-knockout (ENT1<sup>−/−</sup>) mice were generated compared with wild-type (ENT1<sup>+/+</sup>) using small-animal PET. In addition, ENT1<sup>+/+</sup> also injected the ENT1 inhibitor...
Polymeric micellar nanoparticles represent versatile and biocompatible platforms for targeted drug delivery. However, tracking their biodistribution, stability, clearance profile in vivo is challenging. The goal of this study was to prepare surface-modified micelles with peptide GE11 targeting the epidermal growth factor receptor (EGFR). In vitro fluorescence studies demonstrated significantly higher internalization into EGFR-expressing HCT116 colon cancer cells versus EGFR-negative SW620...
Use of [<sup>18</sup>F]FDG-positron emission tomography (PET) in clinical breast cancer (BC) imaging is limited mainly by insufficient expression levels facilitative glucose transporter (GLUT)1 up to 50% all patients. Fructose-specific hexose GLUT5 represents an alternative biomarker for PET metabolism BC. The goal the present study was compare uptake characteristics selected hexose-based radiotracers murine BC model EMT6. Uptake 1-deoxy-1-[<sup>18</sup>F]fluoro-d-fructose...
Current translational cancer research is directed to the development of high affinity peptide ligands for targeting neuropeptide receptors overexpressed in different types cancer. Besides their desired binding receptor, suitability radiolabeled peptides as vectors molecular imaging and therapy depends on additional aspects such tumor-to-background ratio, favorable clearance pattern from nontarget tissue, sufficient metabolic stability vivo. This study reports how a switch prosthetic group,...
Lysyl oxidase (LOX; ExPASy ENZYME entry: EC 1.4.3.13) and members of the LOX-like family, LOXL1-LOXL4, are copper-dependent enzymes that can modify proteins extracellular matrix. Expression LOX is elevated in many human cancers, including breast cancer. expression correlates with level tissue hypoxia, it known to play a critical role cancer metastasis. The goal present study was target (1) molecular probe fluorescent labeling visualize vitro (2) radiolabeled peptide vivo three different...
Cyclooxygenase-2 (COX-2) is the inducible isoform of cyclooxygenase enzyme family. COX-2 involved in tumor development and progression, frequent overexpression a variety human cancers has made an important drug target for cancer treatment. Non-invasive imaging expression would be useful assessing COX-2-mediated effects on chemoprevention radiosensitization using inhibitors as emerging class anti-cancer drugs, especially colorectal cancer. Herein, we describe radiopharmacological analysis...
Theranostic isotope pairs have gained recent clinical interest as they can be labeled to the same tracer and applied for diagnostic therapeutic purposes. The goals of this study were A) investigate cyclotron production clinically relevant <sup>133</sup>La activities using natural isotopically enriched barium target material, B) compare fundamental positron emission tomography (PET) phantom imaging characteristics with common PET radionuclides, C) demonstrate in vivo preclinical tumor...
Multiple sclerosis (MS) is a progressive and inflammatory demyelinating disease of the CNS. Peroxisomes perform critical functions that contribute to CNS homeostasis. We investigated peroxisome injury mitigating effects peroxisome-restorative therapy on demyelination in models MS. Human autopsied tissues (male female), human cell cultures, cuprizone-mediated mice (female) were examined by RT-PCR, Western blotting, immunolabeling. The therapeutic proliferator, 4-phenylbutyrate (4-PBA) was...
Transition-metal-mediated bioconjugation chemistry has been used extensively to design and synthesize molecular probes visualize, characterize, quantify biological processes within intact living organisms at the cellular subcellular levels. We demonstrate development validation of chemoselective [18F]fluoro-arylation cysteine residues using Pd-mediated S-arylation with 4-[18F]fluoroiodobenzene ([18F]FIB) as an aryl electrophile. The novel technique proceeded in excellent radiochemical yields...