Search Results - "Ghebreselasie, Kebreab"

Oxicams Bind in a Novel Mode to the Cyclooxygenase Active Site via a Two-water-mediated H-bonding Network by Xu, Shu, Hermanson, Daniel J., Banerjee, Surajit, Ghebreselasie, Kebreab, Clayton, Gina M., Garavito, R. Michael, Marnett, Lawrence J.

“…Oxicams are widely used nonsteroidal anti-inflammatory drugs (NSAIDs), but little is known about the molecular basis of the interaction with their target…”
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Design, Synthesis, and Structure–Activity Relationship Studies of Fluorescent Inhibitors of Cycloxygenase‑2 as Targeted Optical Imaging Agents by Uddin, Md. Jashim, Crews, Brenda C, Ghebreselasie, Kebreab, Marnett, Lawrence J

“…Cycloxygenase-2 (COX-2) is an attractive target for molecular imaging because it is an inducible enzyme that is expressed in response to inflammatory and…”
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Cyclooxygenase-1-Selective Inhibitors Based on the (E)-2′-Des-methyl-sulindac Sulfide Scaffold by Liedtke, Andy J, Crews, Brenda C, Daniel, Cristina M, Blobaum, Anna L, Kingsley, Philip J, Ghebreselasie, Kebreab, Marnett, Lawrence J

“…Prostaglandins (PGs) are powerful lipid mediators in many physiological and pathophysiological responses. They are produced by oxidation of arachidonic acid…”
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nido-Dicarbaborate Induces Potent and Selective Inhibition of Cyclooxygenase-2 by Neumann, Wilma, Xu, Shu, Sárosi, Menyhárt B., Scholz, Matthias S., Crews, Brenda C., Ghebreselasie, Kebreab, Banerjee, Surajit, Marnett, Lawrence J., Hey-Hawkins, Evamarie

“…Carbaboranes are increasingly studied as pharmacophores, particularly as replacements for aromatic systems. However, especially ortho‐carbaborane is prone to…”
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Trifluoromethyl Fluorocoxib A Detects Cyclooxygenase‑2 Expression in Inflammatory Tissues and Human Tumor Xenografts by Uddin, Md. Jashim, Crews, Brenda C, Huda, Imran, Ghebreselasie, Kebreab, Daniel, Cristina K, Marnett, Lawrence J

“…Fluorocoxib A is an effective COX-2-targeted optical imaging agent, used for in vivo detection of inflammatory tissues and premalignant and malignant tumors…”
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Discovery of Furanone-Based Radiopharmaceuticals for Diagnostic Targeting of COX‑1 in Ovarian Cancer by Uddin, Md. Jashim, Wilson, Andrew J, Crews, Brenda C, Malerba, Paola, Uddin, Md. Imam, Kingsley, Philip J, Ghebreselasie, Kebreab, Daniel, Cristina K, Nickels, Michael L, Tantawy, Mohammed N, Jashim, Elma, Manning, H. Charles, Khabele, Dineo, Marnett, Lawrence J

“…In vivo targeting and visualization of cyclooxygenase-1 (COX-1) using multimodal positron emission tomography/computed tomography imaging represents a unique…”
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Chemical stability of 2-arachidonylglycerol under biological conditions by Rouzer, Carol A, Ghebreselasie, Kebreab, Marnett, Lawrence J

“…Recent evidence indicates that 2-arachidonylglycerol (2-AG) is a potent and specific ligand for the central and peripheral cannabinoid receptors. Therefore,…”
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Synthesis and evaluation of [123I]-indomethacin derivatives as COX-2 targeted imaging agents by Uddin, Md. Jashim, Crews, Brenda C., Blobaum, Anna L., Kingsley, Philip J., Ghebreselasie, Kebreab, Saleh, Sam S., Clanton, Jeffrey A., Baldwin, Ronald M., Marnett, Lawrence J.

“…A novel series of iodinated indomethacin derivatives was synthesized, and evaluated as selective inhibitors of COX‐2. Two candidate compounds…”
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Fluorescent indomethacin-dansyl conjugates utilize the membrane-binding domain of cyclooxygenase-2 to block the opening to the active site by Xu, Shu, Uddin, Md. Jashim, Banerjee, Surajit, Duggan, Kelsey, Musee, Joel, Kiefer, James R., Ghebreselasie, Kebreab, Rouzer, Carol A., Marnett, Lawrence J.

“…Many indomethacin amides and esters are cyclooxygenase-2 (COX-2)–selective inhibitors, providing a framework for the design of COX-2–targeted imaging and…”
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Dual cyclooxygenase–fatty acid amide hydrolase inhibitor exploits novel binding interactions in the cyclooxygenase active site by Goodman, Michael C., Xu, Shu, Rouzer, Carol A., Banerjee, Surajit, Ghebreselasie, Kebreab, Migliore, Marco, Piomelli, Daniele, Marnett, Lawrence J.

“…The cyclooxygenases COX-1 and COX-2 oxygenate arachidonic acid (AA) to prostaglandin H2 (PGH2). COX-2 also oxygenates the endocannabinoids…”
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Conjugation of Cisplatin Analogues and Cyclooxygenase Inhibitors to Overcome Cisplatin Resistance by Neumann, Wilma, Crews, Brenda C., Sárosi, Menyhárt B., Daniel, Cristina M., Ghebreselasie, Kebreab, Scholz, Matthias S., Marnett, Lawrence J., Hey-Hawkins, Evamarie

“…Cyclooxygenase (COX) is an enzyme involved in tumorigenesis and is associated with tumor cell resistance against platinum‐based antitumor drugs. Cisplatin…”
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Dual cyclooxygenase–fatty acid amide hydrolase inhibitor exploits novel binding interactions in the cyclooxygenase active site by Goodman, Michael C., Xu, Shu, Rouzer, Carol A., Banerjee, Surajit, Ghebreselasie, Kebreab, Migliore, Marco, Piomelli, Daniele, Marnett, Lawrence J.

“…The cyclooxygenases COX-1 and COX-2 oxygenate arachidonic acid (AA) to prostaglandin H2 (PGH2). COX-2 also oxygenates the endocannabinoids…”
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Harmaline Analogs as Substrate-Selective Cyclooxygenase‑2 Inhibitors by Uddin, Md. Jashim, Xu, Shu, Crews, Brenda C, Aleem, Ansari M, Ghebreselasie, Kebreab, Banerjee, Surajit, Marnett, Lawrence J

“…We report the design, synthesis, and evaluation of a series of harmaline analogs as selective inhibitors of 2-arachidonylglycerol (2-AG) oxygenation over…”
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Activatable COX‐2 Probes in Optical Imaging of Cancer by Uddin, Md. Jashim, Crews, Brenda C, Ghebreselasie, Kebreab, Daniel, Cristina K, Marnett, Lawrence J.

“…Abstract only Conventional imaging methods, such as angiography, computed tomography, magnetic resonance imaging and radionuclide imaging, rely on contrast…”
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The Structural Basis of Cyclooxygenase‐2 Inhibition by Fenamates by Xu, Shu, Banerjee, Surajit, Kudalkar, Shalley N, Perry, Evan T, Ghebreselasie, Kebreab, Marnett, Lawrence J

“…Abstract only Two cyclooxygenase (COX) isoforms, COX‐1 and COX‐2, catalyze the first two steps of prostaglandin biosynthesis from arachidonic acid (AA) and are…”
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Action at a distance: mutations of peripheral residues transform rapid reversible inhibitors to slow, tight binders of cyclooxygenase-2 by Blobaum, Anna L, Xu, Shu, Rowlinson, Scott W, Duggan, Kelsey C, Banerjee, Surajit, Kudalkar, Shalley N, Birmingham, William R, Ghebreselasie, Kebreab, Marnett, Lawrence J

“…Cyclooxygenase enzymes (COX-1 and COX-2) catalyze the conversion of arachidonic acid to prostaglandin G2. The inhibitory activity of rapid, reversible COX…”
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Targeted Detection of Cyclooxygenase‑1 in Ovarian Cancer by Malerba, Paola, Crews, Brenda C, Ghebreselasie, Kebreab, Daniel, Cristina K, Jashim, Elma, Aleem, Ansari M, Salam, Redoan A, Marnett, Lawrence J, Uddin, Md. Jashim

“…Overexpression of cyclooxygenase-1 (COX-1) is associated with the initiation and progression of ovarian cancer, and targeted imaging of COX-1 is a promising…”
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Antitumor Activity of Cytotoxic Cyclooxygenase‑2 Inhibitors by Uddin, Md. Jashim, Crews, Brenda C, Xu, Shu, Ghebreselasie, Kebreab, Daniel, Cristina K, Kingsley, Philip J, Banerjee, Surajit, Marnett, Lawrence J

“…Targeted delivery of chemotherapeutic agents to tumors has been explored as a means to increase the selectivity and potency of cytotoxicity. Most efforts in…”
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Fluorinated COX-2 inhibitors as agents in PET imaging of inflammation and cancer by Uddin, Md Jashim, Crews, Brenda C, Ghebreselasie, Kebreab, Huda, Imran, Kingsley, Philip J, Ansari, Mohammad Sib, Tantawy, Mohammed N, Reese, Jeffery, Marnett, Lawrence J

“…COX-2 is a major contributor to the inflammatory response and cancer progression so it is an important target for prevention and therapy. COX-2 is absent or…”
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PET radiotracer [18F]-P6 selectively targeting COX-1 as a novel biomarker in ovarian cancer: Preliminary investigation by Perrone, Maria Grazia, Malerba, Paola, Uddin, Md. Jashim, Vitale, Paola, Panella, Andrea, Crews, Brenda C., Daniel, Cristina K., Ghebreselasie, Kebreab, Nickels, Mike, Tantawy, Mohammed N., Manning, H. Charles, Marnett, Lawrence J., Scilimati, Antonio

“…Cyclooxygenase-1 (COX-1), but not COX-2, is expressed at high levels in the early stages of human epithelial ovarian cancer where it seems to play a key role…”
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