Search results for: Frank Wuest

Items from 1 to 20 out of 61 results

article

Synthesis and Biological Evaluation of 1,3,5‐Trisubstituted 2‐Pyrazolines as Novel Cyclooxygenase‐2 Inhibitors with Antiproliferative Activity

Teymour Vahedpour, Jatinder Kaur, Salar Hemmati, Maryam Hamzeh‐Mivehroud, more

Chemistry & Biodiversity > 18 > 3 > n/a - n/a

A new series of 1,3,5‐trisubstituted 2‐pyrazolines for the inhibition of cyclooxygenase‐2 (COX‐2) were synthesized. The designed structures include a COX‐2 pharmacophore SO₂CH₃ at the para‐position of the phenyl ring located at C‐5 of a pyrazoline scaffold. The synthesized compounds were tested for in vitro COX‐1/COX‐2 inhibition and cell toxicity against human colorectal adenocarcinoma cell lines...

article

In Cellulo Generation of Fluorescent Probes for Live‐Cell Imaging of Cylooxygenase‐2

Jatinder Kaur, Atul Bhardwaj, Frank Wuest

Chemistry – A European Journal > 27 > 10 > 3326 - 3337

Live‐cell imaging with fluorescent probes is an essential tool in chemical biology to visualize the dynamics of biological processes in real‐time. Intracellular disease biomarker imaging remains a formidable challenge due to the intrinsic limitations of conventional fluorescent probes and the complex nature of cells. This work reports the in cellulo assembly of a fluorescent probe to image cyclooxygenase‐2...

article

Cover Feature: In Cellulo Generation of Fluorescent Probes for Live‐Cell Imaging of Cylooxygenase‐2 (Chem. Eur. J. 10/2021)

Jatinder Kaur, Atul Bhardwaj, Frank Wuest

Chemistry – A European Journal > 27 > 10 > 3189 - 3189

In cellulo generation of fluorescent probes is an essential tool in chemical biology to visualize the dynamics of biological processes in real‐time. A highly flexible in cellulo fluorogenic click chemistry strategy was developed and tested for the precise detection and tracking of inflammation and cancer biomarker cyclooxygenase‐2 (COX‐2) in live cells with superior sensitivity in the visible range...

article

Intranasal anti‐caspase‐1 therapy preserves myelin and glucose metabolism in a model of progressive multiple sclerosis

Leina B. Saito, Jason P. Fernandes, Mackenzie J. Smith, Matthew A. L. Doan, more

Glia > 69 > 1 > 216 - 229

Inflammatory demyelination and axonal injury in the central nervous system (CNS) are cardinal features of progressive multiple sclerosis (MS), and linked to activated brain macrophage‐like cells (BMCs) including resident microglia and trafficking macrophages. Caspase‐1 is a pivotal mediator of inflammation and cell death in the CNS. We investigated the effects of caspase‐1 activation and its regulation...

article

Targeting phosphatidylserine for radionuclide-based molecular imaging of apoptosis

Melinda Wuest, Amanda Perreault, Susan Richter, James C. Knight, more

Apoptosis > 2019 > 24 > 3-4 > 221-244

One major characteristic of programmed cell death (apoptosis) results in the increased expression of phosphatidylserine (PS) on the outer membrane of dying cells. Consequently, PS represents an excellent target for non-invasive imaging of apoptosis by single-photon emission computed tomography (SPECT) and positron emission tomography (PET). Annexin V is a 36 kDa protein which binds with high affinity...

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Impact of structural alterations on the radiopharmacological profile of 18F-labeled pyrimidines as cyclooxygenase-2 (COX-2) imaging agents

Ole Tietz, Alison Marshall, Cody Bergman, Melinda Wuest, more

Nuclear Medicine and Biology > 2018 > 62-63 > C > 9-17

Non-invasive imaging of COX-2 in cancer represents a powerful tool for assessing COX-2-mediated effects on chemoprevention and radiosensitization using potent and selective COX-2 inhibitors as an emerging class of anticancer drugs. Careful assessment of the pharmacokinetic profile of radiolabeled COX-2 inhibitors is of crucial importance for the development of suitable radiotracers for COX-2 imaging...

article

Targeting Prostate-Specific Membrane Antigen (PSMA) with F-18-Labeled Compounds: the Influence of Prosthetic Groups on Tumor Uptake and Clearance Profile

Vincent Bouvet, Melinda Wuest, Justin J. Bailey, Cody Bergman, more

Molecular Imaging and Biology > 2017 > 19 > 6 > 923-932

Purpose Prostate-specific membrane antigen (PSMA) is an important biomarker expressed in the majority of prostate cancers. The favorable positron emission tomography (PET) imaging profile of the PSMA imaging agent 2-(3-(1-carboxy-5-[(6-[¹⁸F]fluoro-pyridine-3-carbonyl)-amino]-pentyl)-ureido)-pentane-dioic acid [¹⁸F]DCFPyL in preclinical prostate cancer models and in prostate cancer patients stimulated...

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Structure–activity relationship of novel series of 1,5-disubstituted tetrazoles as cyclooxygenase-2 inhibitors: Design, synthesis, bioassay screening and molecular docking studies

Baker Jawabrah Al-Hourani, Wajdy Al-Awaida, Khalid Z. Matalka, Musa I. El-Barghouthi, more

Bioorganic & Medicinal Chemistry Letters > 2016 > 26 > 19 > 4757-4762

A novel class of modified 1,5-disubstituted tetrazoles was designed and synthesized, their biological activity as cyclooxygenases inhibitors was screened, and their molecular docking studies were performed. The structural modifications of the first category included the 4-methylsulfonyl phenyl at C-1 of the central moiety and the linkers (–OH, –CH₂OH, –CH₂CH₂OH) with different lengths at the para...

article

Synthesis and crystal structure of N-[(dimethylamino)methylidene]-4-[1-(4-nitrophenyl)-1H-tetrazol-5-yl]-benzenesulfonamide: Molecular docking and bioassay studies as cyclooxygenase-2 inhibitor

Baker Jawabrah Al-Hourani, Musa I. El-Barghouthi, Robert McDonald, Wajdy Al-Awaida, more

Journal of Molecular Structure > 2016 > 1119 > C > 220-226

The synthesis of N-[(dimethylamino)methylidene]-4-[1-(4-nitrophenyl)-1H-tetrazol-5-yl]benzenesulfonamide (3) has been easily approached and the structure has been determined by X-ray crystallography. Tetrazole 3 crystallizes in the monoclinic space group C2/c, with the cell parameters determined as a = 35.5408 (18) Å, b = 7.6972 (4) Å, c = 13.0700 (7) Å³, β = 96.8598 (6)°, V = 3549.9 (3) Å³, and Z = 8...

article

Design and synthesis of [125I]Pyricoxib: A novel 125I-labeled cyclooxygenase-2 (COX-2) inhibitors

Ole Tietz, James Dzandzi, Atul Bhardwaj, John F. Valliant, more

Bioorganic & Medicinal Chemistry Letters > 2016 > 26 > 6 > 1516-1520

Cyclooxygenase-2 (COX-2) is the key enzyme in the prostaglandin synthesis pathway which is involved in various pathophysiological conditions. The enzyme is membrane bound and located inside of the endoplasmic reticulum and nuclear membrane. Effective perfusion of inhibitors to the active site requires lipophilic drugs, which consequently display high unspecific background accumulation, for example,...

article

¹⁸F-Labeled wild-type annexin V: comparison of random and site-selective radiolabeling methods

Amanda Perreault, James C. Knight, Monica Wang, Jenilee Way, more

Amino Acids > 2016 > 48 > 1 > 65-74

Early stage apoptosis is characterized by the externalization of phosphatidylserine (PS) from the inner leaflet of the plasma membrane to the outer periphery. Consequently, PS represents an excellent target for non-invasive imaging of apoptosis by positron emission tomography. Annexin V is a 36 kDa protein which binds with high affinity to PS. Radiolabeling of wild-type annexin V with fluorine-18...

article

Automated synthesis of [¹⁸F]DCFPyL via direct radiofluorination and validation in preclinical prostate cancer models

Vincent Bouvet, Melinda Wuest, Hans-Soenke Jans, Nancy Janzen, more

EJNMMI Research > 2016 > 6 > 1 > 1-15

Background Prostate-specific membrane antigen (PSMA) is frequently overexpressed and upregulated in prostate cancer. To date, various ¹⁸F- and ⁶⁸Ga-labeled urea-based radiotracers for PET imaging of PSMA have been developed and entered clinical trials. Here, we describe an automated synthesis of [¹⁸F]DCFPyL via direct radiofluorination and validation in preclinical models of prostate cancer. Methods...

article

PET imaging of cyclooxygenase-2 (COX-2) in a pre-clinical colorectal cancer model

Ole Tietz, Melinda Wuest, Alison Marshall, Darryl Glubrecht, more

EJNMMI Research > 2016 > 6 > 1 > 1-11

Background Cyclooxygenase-2 (COX-2) is the inducible isoform of the cyclooxygenase enzyme family. COX-2 is involved in tumor development and progression, and frequent overexpression of COX-2 in a variety of human cancers has made COX-2 an important drug target for cancer treatment. Non-invasive imaging of COX-2 expression in cancer would be useful for assessing COX-2-mediated effects on chemoprevention...

article

Docking studies and the crystal structure of two tetrazole derivatives: 5-(4-chlorophenyl)-1-{4-(methylsulfonyl)phenyl}-1H-tetrazole and 4-{5-(4-methoxyphenyl)-1H-tetrazol-1-yl}benzenesulfonamide

Baker Jawabrah Al-Hourani, Musa I. El-Barghouthi, Robert Mcdonald, Wajdy Al-Awaida, more

Journal of Molecular Structure > 2015 > 1101 > C > 21-27

The structures of 5-(4-chlorophenyl)-1-{4-(methylsulfonyl)phenyl}-1H-tetrazole (3) and 4-{5-(4-methoxyphenyl)-1H-tetrazol-1-yl}benzenesulfonamide (5) have been determined by X-ray crystallography. Tetrazoles 3 and 5 crystallize in the monoclinic space groups Ia and P2₁/c, respectively. The cell dimensions of azole 3 are a = 11.0413 (5) Å, b = 11.8428 (5) Å, c = 12.2483 (5) Å³, β = 111.7129 (4)°, V = 1487...

article

Synthesis and structural identification of fluorine‐18 labeled parathyroid hormone

Yang Yang, Susan Richter, Frank Wuest, Michael R. Doschak

Journal of Labelled Compounds and Radiopharmaceuticals > 58 > 11-12 > 453 - 457

Parathyroid hormone (PTH) is an 84 amino acid peptide hormone that plays a key role in bone and mineral metabolism. The biological actions of PTH are mediated via the N‐terminal PTH(1–34) fragment, serving as the PTH receptor‐binding sequence, and which is therefore used clinically to treat conditions of low bone mass such as osteoporosis. In this study, PTH(1–34) was conjugated with non‐radioactive...

article

Radiopharmacological evaluation of 18F-labeled phosphatidylserine-binding peptides for molecular imaging of apoptosis

Melinda Wuest, Amanda Perreault, Janice Kapty, Susan Richter, more

Nuclear Medicine and Biology > 2015 > 42 > 11 > 864-874

Radiolabeled phosphatidylserine (PS)-binding peptides represent an innovative strategy for molecular imaging of apoptosis with positron emission tomography (PET). The goal of this study was the radiopharmacological evaluation of radiolabeled peptides for their binding to PS on apoptotic cancer cells, involving metabolic stability, cellular uptake, biodistribution, and dynamic PET imaging experiments...

article

Targeting lysyl oxidase for molecular imaging in breast cancer

Melinda Wuest, Manuela Kuchar, Sai Kiran Sharma, Susan Richter, more

Breast Cancer Research > 2015 > 17 > 1 > 1-15

Introduction 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 of the extracellular matrix. Expression of LOX is elevated in many human cancers, including breast cancer. LOX expression correlates with the level of tissue hypoxia, and it is known to play a critical role in breast cancer metastasis...

article

Synthesis, bioassay studies, and molecular docking of novel 5-substituted 1H tetrazoles as cyclooxygenase-2 (COX-2) inhibitors

Baker Jawabrah Al-Hourani, Sai Kiran Sharma, Jatinder Kaur, Frank Wuest

Medicinal Chemistry Research > 2015 > 24 > 1 > 78-85

A series of 1,5-diaryl-substituted tetrazole derivatives were designed and synthesized by introducing the SO₂NH₂ COX-2 pharmacophore to position C-5 of the tetrazole moiety via the phenyl group, while a selection of different para substituents (H, CH₃, OCH₃, Cl, F, CF₃ ,or N(CH₃)₂) was attached to the other aryl substituent. An in vitro binding assay was carried out to determine COX-1 and COX-2 inhibitory...

article

Synthesis and evaluation of 2-amino-5-(4-[18F]fluorophenyl)pent-4-ynoic acid ([18F]FPhPA): A novel 18F-labeled amino acid for oncologic PET imaging

Jenilee D. Way, Monica Wang, Ingrit Hamann, Melinda Wuest, more

Nuclear Medicine and Biology > 2014 > 41 > 8 > 660-669

¹⁸ F-labeled amino acids are important PET radiotracers for molecular imaging of cancer. This study describes synthesis and radiopharmacological evaluation of 2-amino-5-(4-[ ¹⁸ F]fluorophenyl)pent-4-ynoic acid ([ ¹⁸ F]FPhPA) as a novel amino acid radiotracer for oncologic imaging. ¹⁸ F]FPhPA was prepared using Pd-mediated Sonogashira cross-coupling reaction between 4-[...

article

89Zr immuno-PET of epithelial ovarian cancer

Sai Kiran Sharma, Brian Zeglis, Kuntal Sevak, Jason Lewis, more

Nuclear Medicine and Biology > 2014 > 41 > 7 > 638-639

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Search results for: Frank Wuest

Synthesis and Biological Evaluation of 1,3,5‐Trisubstituted 2‐Pyrazolines as Novel Cyclooxygenase‐2 Inhibitors with Antiproliferative Activity

In Cellulo Generation of Fluorescent Probes for Live‐Cell Imaging of Cylooxygenase‐2

Cover Feature: In Cellulo Generation of Fluorescent Probes for Live‐Cell Imaging of Cylooxygenase‐2 (Chem. Eur. J. 10/2021)

Intranasal anti‐caspase‐1 therapy preserves myelin and glucose metabolism in a model of progressive multiple sclerosis

Targeting phosphatidylserine for radionuclide-based molecular imaging of apoptosis

Impact of structural alterations on the radiopharmacological profile of 18F-labeled pyrimidines as cyclooxygenase-2 (COX-2) imaging agents

Targeting Prostate-Specific Membrane Antigen (PSMA) with F-18-Labeled Compounds: the Influence of Prosthetic Groups on Tumor Uptake and Clearance Profile

Structure–activity relationship of novel series of 1,5-disubstituted tetrazoles as cyclooxygenase-2 inhibitors: Design, synthesis, bioassay screening and molecular docking studies

Synthesis and crystal structure of N-[(dimethylamino)methylidene]-4-[1-(4-nitrophenyl)-1H-tetrazol-5-yl]-benzenesulfonamide: Molecular docking and bioassay studies as cyclooxygenase-2 inhibitor

Design and synthesis of [125I]Pyricoxib: A novel 125I-labeled cyclooxygenase-2 (COX-2) inhibitors

¹⁸F-Labeled wild-type annexin V: comparison of random and site-selective radiolabeling methods

Automated synthesis of [¹⁸F]DCFPyL via direct radiofluorination and validation in preclinical prostate cancer models

PET imaging of cyclooxygenase-2 (COX-2) in a pre-clinical colorectal cancer model

Docking studies and the crystal structure of two tetrazole derivatives: 5-(4-chlorophenyl)-1-{4-(methylsulfonyl)phenyl}-1H-tetrazole and 4-{5-(4-methoxyphenyl)-1H-tetrazol-1-yl}benzenesulfonamide

Synthesis and structural identification of fluorine‐18 labeled parathyroid hormone

Radiopharmacological evaluation of 18F-labeled phosphatidylserine-binding peptides for molecular imaging of apoptosis

Targeting lysyl oxidase for molecular imaging in breast cancer

Synthesis, bioassay studies, and molecular docking of novel 5-substituted 1H tetrazoles as cyclooxygenase-2 (COX-2) inhibitors

Synthesis and evaluation of 2-amino-5-(4-[18F]fluorophenyl)pent-4-ynoic acid ([18F]FPhPA): A novel 18F-labeled amino acid for oncologic PET imaging

89Zr immuno-PET of epithelial ovarian cancer

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