Search Results - "Speers, Anna E"

Activity-Based Protein Profiling in Vivo Using a Copper(I)-Catalyzed Azide-Alkyne [3 + 2] Cycloaddition by Speers, Anna E, Adam, Gregory C, Cravatt, Benjamin F

“…Toward the goal of assigning function to the tens of thousands of protein products encoded by eukaryotic and prokaryotic genomes, the field of proteomics…”
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A Tandem Orthogonal Proteolysis Strategy for High-Content Chemical Proteomics by Speers, Anna E, Cravatt, Benjamin F

“…The field of proteomics aims to assign functions to the numerous protein products encoded by eukaryotic and prokaryotic genomes. Toward this end, chemical…”
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Development and Optimization of Piperidyl-1,2,3-Triazole Ureas as Selective Chemical Probes of Endocannabinoid Biosynthesis by Hsu, Ku-Lung, Tsuboi, Katsunori, Whitby, Landon R, Speers, Anna E, Pugh, Holly, Inloes, Jordon, Cravatt, Benjamin F

“…We have previously shown that 1,2,3-triazole ureas (1,2,3-TUs) act as versatile class of irreversible serine hydrolase inhibitors that can be tuned to create…”
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Discovery and Optimization of Sulfonyl Acrylonitriles as Selective, Covalent Inhibitors of Protein Phosphatase Methylesterase-1 by Bachovchin, Daniel A, Zuhl, Andrea M, Speers, Anna E, Wolfe, Monique R, Weerapana, Eranthie, Brown, Steven J, Rosen, Hugh, Cravatt, Benjamin F

“…The serine hydrolase protein phosphatase methylesterase-1 (PME-1) regulates the methylesterification state of protein phosphatase 2A (PP2A) and has been…”
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Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors by Bachovchin, Daniel A, Mohr, Justin T, Speers, Anna E, Wang, Chu, Berlin, Jacob M, Spicer, Timothy P, Fernandez-Vega, Virneliz, Chase, Peter, Hodder, Peter S, Schürer, Stephan C, Nomura, Daniel K, Rosen, Hugh, Fu, Gregory C, Cravatt, Benjamin F

“…National Institutes of Health (NIH)-sponsored screening centers provide academic researchers with a special opportunity to pursue small-molecule probes for…”
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Chemical Strategies for Activity-Based Proteomics by Speers, Anna E, Cravatt, Benjamin F

“…The assignment of molecular and cellular functions to the numerous protein products encoded by prokaryotic and eukaryotic genomes presents a major challenge…”
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Phosphatidylinositol 3,4,5-Trisphosphate Activity Probes for the Labeling and Proteomic Characterization of Protein Binding Partners by Rowland, Meng M, Bostic, Heidi E, Gong, Denghuang, Speers, Anna E, Lucas, Nathan, Cho, Wonhwa, Cravatt, Benjamin F, Best, Michael D

“…Phosphatidylinositol polyphosphate lipids, such as phosphatidylinositol 3,4,5-trisphosphate [PI­(3,4,5)­P3], regulate critical biological processes, many of…”
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Shotgun Analysis of Integral Membrane Proteins Facilitated by Elevated Temperature by Speers, Anna E, Blackler, Adele R, Wu, Christine C

“…The beneficial effects on peak selectivity and resolution of conducting liquid chromatography (LC) at elevated temperature (e.g., 30−80 °C) are generally…”
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Proteomics of Integral Membrane ProteinsTheory and Application by Speers, Anna E, Wu, Christine C

“…The hydrophobic core of the phopholipid bilayers are the driving force behind the integral membrane proteins (IMP) structure. The theory and application of…”
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Rapid Development of a Potent Photo-triggered Inhibitor of the Serine Hydrolase RBBP9 by Liu, Xiaodan, Dix, Melissa, Speers, Anna E., Bachovchin, Daniel A., Zuhl, Andrea M., Cravatt, Benjamin F., Kodadek, Thomas J.

“…The serine hydrolases constitute a large class of enzymes that play important roles in physiology. There is great interest in the development of potent and…”
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Tandem orthogonal proteolysis-activity-based protein profiling (TOP-ABPP)-a general method for mapping sites of probe modification in proteomes by Cravatt, Benjamin F, Weerapana, Eranthie, Speers, Anna E

“…Activity-based protein profiling (ABPP) utilizes active site-directed chemical probes to monitor the functional state of enzymes directly in native biological…”
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Discovery and Optimization of Piperidyl-1,2,3-Triazole Ureas as Potent, Selective, and in Vivo-Active Inhibitors of α/β-Hydrolase Domain Containing 6 (ABHD6) by Hsu, Ku-Lung, Tsuboi, Katsunori, Chang, Jae Won, Whitby, Landon R, Speers, Anna E, Pugh, Holly, Cravatt, Benjamin F

“…α/β-Hydrolase domain containing 6 (ABHD6) is a transmembrane serine hydrolase that hydrolyzes the endogenous cannabinoid 2-arachidonoylglycerol (2-AG) to…”
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Potent and Selective Inhibitors of Glutathione S-Transferase Omega 1 That Impair Cancer Drug Resistance by Tsuboi, Katsunori, Bachovchin, Daniel A, Speers, Anna E, Spicer, Timothy P, Fernandez-Vega, Virneliz, Hodder, Peter, Rosen, Hugh, Cravatt, Benjamin F

“…Glutathione S-transferases (GSTs) are a superfamily of enzymes that conjugate glutathione to a wide variety of both exogenous and endogenous compounds for…”
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Mechanistic Characterization of a 2‑Thioxanthine Myeloperoxidase Inhibitor and Selectivity Assessment Utilizing Click Chemistry–Activity-Based Protein Profiling by Ward, Jessica, Spath, Samantha N, Pabst, Brandon, Carpino, Philip A, Ruggeri, Roger B, Xing, Gang, Speers, Anna E, Cravatt, Benjamin F, Ahn, Kay

“…Myeloperoxidase (MPO) is a heme peroxidase that catalyzes the production of hypochlorous acid. Despite a high level of interest in MPO as a therapeutic target,…”
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Profiling Enzyme Activities In Vivo Using Click Chemistry Methods by Speers, Anna E, Cravatt, Benjamin F

“…Methods for profiling the activity of enzymes in vivo are needed to understand the role that these proteins and their endogenous regulators play in…”
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Selective Inhibitor of Platelet-Activating Factor Acetylhydrolases 1b2 and 1b3 That Impairs Cancer Cell Survival by Chang, Jae Won, Zuhl, Andrea M, Speers, Anna E, Niessen, Sherry, Brown, Steven J, Mulvihill, Melinda M, Fan, Yi Chiao, Spicer, Timothy P, Southern, Mark, Scampavia, Louis, Fernandez-Vega, Virneliz, Dix, Melissa M, Cameron, Michael D, Hodder, Peter S, Rosen, Hugh, Nomura, Daniel K, Kwon, Ohyun, Hsu, Ku-Lung, Cravatt, Benjamin F

“…Platelet-activating factor acetylhydrolases (PAFAHs) 1b2 and 1b3 are poorly characterized serine hydrolases that form a complex with a noncatalytic protein…”
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Target-Based Screen Against a Periplasmic Serine Protease That Regulates Intrabacterial pH Homeostasis in Mycobacterium tuberculosis by Zhao, Nan, Darby, Crystal M, Small, Jennifer, Bachovchin, Daniel A, Jiang, Xiuju, Burns-Huang, Kristin E, Botella, Helene, Ehrt, Sabine, Boger, Dale L, Anderson, Erin D, Cravatt, Benjamin F, Speers, Anna E, Fernandez-Vega, Virneliz, Hodder, Peter S, Eberhart, Christina, Rosen, Hugh, Spicer, Timothy P, Nathan, Carl F

“…Mycobacterium tuberculosis (Mtb) maintains its intrabacterial pH (pHIB) near neutrality in the acidic environment of phagosomes within activated macrophages. A…”
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Confirming Target Engagement for Reversible Inhibitors in Vivo by Kinetically Tuned Activity-Based Probes by Adibekian, Alexander, Martin, Brent R, Chang, Jae Won, Hsu, Ku-Lung, Tsuboi, Katsunori, Bachovchin, Daniel A, Speers, Anna E, Brown, Steven J, Spicer, Timothy, Fernandez-Vega, Virneliz, Ferguson, Jill, Hodder, Peter S, Rosen, Hugh, Cravatt, Benjamin F

“…The development of small-molecule inhibitors for perturbing enzyme function requires assays to confirm that the inhibitors interact with their enzymatic…”
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Selective inhibitors and tailored activity probes for lipoprotein-associated phospholipase A by Nagano, Joseph M.G, Hsu, Ku-Lung, Whitby, Landon R, Niphakis, Micah J, Speers, Anna E, Brown, Steven J, Spicer, Timothy, Fernandez-Vega, Virneliz, Ferguson, Jill, Hodder, Peter, Srinivasan, Prabhavathi, Gonzalez, Tara D, Rosen, Hugh, Bahnson, Brian J, Cravatt, Benjamin F

“…Lipoprotein-associated phospholipase A₂ (Lp-PLA₂ or PLA₂G7) binds to low-density lipoprotein (LDL) particles, where it is thought to hydrolyze oxidatively…”
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Selective inhibitors and tailored activity probes for lipoprotein-associated phospholipase A2 by Nagano, Joseph M.G., Hsu, Ku-Lung, Whitby, Landon R., Niphakis, Micah J., Speers, Anna E., Brown, Steven J., Spicer, Timothy, Fernandez-Vega, Virneliz, Ferguson, Jill, Hodder, Peter, Srinivasan, Prabhavathi, Gonzalez, Tara D., Rosen, Hugh, Bahnson, Brian J., Cravatt, Benjamin F.

“…Lipoprotein-associated phospholipase A2 (Lp-PLA2 or PLA2G7) binds to low-density lipoprotein (LDL) particles, where it is thought to hydrolyze oxidatively…”
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