Search Results - "Niphakis, Micah J"

Enzyme Inhibitor Discovery by Activity-Based Protein Profiling by Niphakis, Micah J, Cravatt, Benjamin F

“…Eukaryotic and prokaryotic organisms possess huge numbers of uncharacterized enzymes. Selective inhibitors offer powerful probes for assigning functions to…”
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Proteome-wide mapping of cholesterol-interacting proteins in mammalian cells by Hulce, Jonathan J, Cognetta, Armand B, Niphakis, Micah J, Tully, Sarah E, Cravatt, Benjamin F

“…A combination of clickable, photoreactive sterol probes and mass spectrometry yields a chemoproteomic strategy for profiling protein-cholesterol interaction in…”
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A Global Map of Lipid-Binding Proteins and Their Ligandability in Cells by Niphakis, Micah J., Lum, Kenneth M., Cognetta, Armand B., Correia, Bruno E., Ichu, Taka-Aki, Olucha, Jose, Brown, Steven J., Kundu, Soumajit, Piscitelli, Fabiana, Rosen, Hugh, Cravatt, Benjamin F.

“…Lipids play central roles in physiology and disease, where their structural, metabolic, and signaling functions often arise from interactions with proteins…”
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Mapping the Protein Interaction Landscape for Fully Functionalized Small-Molecule Probes in Human Cells by Kambe, Tohru, Correia, Bruno E, Niphakis, Micah J, Cravatt, Benjamin F

“…Phenotypic screening provides a means to discover small molecules that perturb cell biological processes. Discerning the proteins and biochemical pathways…”
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ABHD17 regulation of plasma membrane palmitoylation and N-Ras-dependent cancer growth by Remsberg, Jarrett R., Suciu, Radu M., Zambetti, Noemi A., Hanigan, Thomas W., Firestone, Ari J., Inguva, Anagha, Long, Amanda, Ngo, Nhi, Lum, Kenneth M., Henry, Cassandra L., Richardson, Stewart K., Predovic, Marina, Huang, Ben, Dix, Melissa M., Howell, Amy R., Niphakis, Micah J., Shannon, Kevin, Cravatt, Benjamin F.

“…Multiple Ras proteins, including N-Ras, depend on a palmitoylation/depalmitoylation cycle to regulate their subcellular trafficking and oncogenicity. General…”
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Monoacylglycerol Lipase Inhibitors Reverse Paclitaxel-Induced Nociceptive Behavior and Proinflammatory Markers in a Mouse Model of Chemotherapy-Induced Neuropathy by Curry, Zachary A, Wilkerson, Jenny L, Bagdas, Deniz, Kyte, S Lauren, Patel, Nipa, Donvito, Giulia, Mustafa, Mohammed A, Poklis, Justin L, Niphakis, Micah J, Hsu, Ku-Lung, Cravatt, Benjamin F, Gewirtz, David A, Damaj, M Imad, Lichtman, Aron H

“…Although paclitaxel effectively treats various cancers, its debilitating peripheral neuropathic pain side effects often persist long after treatment has ended…”
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Palladium(II)-Catalyzed Direct Arylation of Enaminones Using Organotrifluoroborates by Ge, Haibo, Niphakis, Micah J, Georg, Gunda I

“…A Pd(II)-catalyzed reaction for the direct arylation of cyclic enaminones is reported. The reactivity of electron-rich, electron-poor, and sterically…”
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Proteome-Wide Reactivity Profiling Identifies Diverse Carbamate Chemotypes Tuned for Serine Hydrolase Inhibition by Chang, Jae Won, Cognetta, Armand B, Niphakis, Micah J, Cravatt, Benjamin F

“…Serine hydrolases are one of the largest and most diverse enzyme classes in Nature. Inhibitors of serine hydrolases are used to treat many diseases, including…”
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Synthesis of Tylocrebrine and Related Phenanthroindolizidines by VOF3-Mediated Oxidative Aryl-Alkene Coupling by Niphakis, Micah J, Georg, Gunda I

“…A highly convergent strategy to prepare phenanthroindolizidines is reported involving three consecutive C−C coupling reactions. This sequence features a novel…”
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The endocannabinoid hydrolysis inhibitor SA-57: Intrinsic antinociceptive effects, augmented morphine-induced antinociception, and attenuated heroin seeking behavior in mice by Wilkerson, Jenny L., Ghosh, Sudeshna, Mustafa, Mohammed, Abdullah, Rehab A., Niphakis, Micah J., Cabrera, Roberto, Maldonado, Rafael L., Cravatt, Benjamin F., Lichtman, Aron H.

“…Although opioids are highly efficacious analgesics, their abuse potential and other untoward side effects diminish their therapeutic utility. The addition of…”
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Inflammation causes insulin resistance in mice via interferon regulatory factor 3 (IRF3)-mediated reduction in FAHFA levels by Yan, Shuai, Santoro, Anna, Niphakis, Micah J., Pinto, Antonio M., Jacobs, Christopher L., Ahmad, Rasheed, Suciu, Radu M., Fonslow, Bryan R., Herbst-Graham, Rachel A., Ngo, Nhi, Henry, Cassandra L., Herbst, Dylan M., Saghatelian, Alan, Kahn, Barbara B., Rosen, Evan D.

“…Obesity-induced inflammation causes metabolic dysfunction, but the mechanisms remain elusive. Here we show that the innate immune transcription factor…”
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Neuroprotective effects of fatty acid amide hydrolase catabolic enzyme inhibition in a HIV-1 Tat model of neuroAIDS by Hermes, Douglas J., Xu, Changqing, Poklis, Justin L., Niphakis, Micah J., Cravatt, Benjamin F., Mackie, Ken, Lichtman, Aron H., Ignatowska-Jankowska, Bogna M., Fitting, Sylvia

“…The HIV-1 transactivator of transcription (Tat) is a neurotoxin involved in the pathogenesis of HIV-1 associated neurocognitive disorders (HAND). The…”
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A helping HAND: therapeutic potential of MAGL inhibition against HIV-1-associated neuroinflammation by League, Alexis F, Yadav-Samudrala, Barkha J, Kolagani, Ramya, Cline, Calista A, Jacobs, Ian R, Manke, Jonathan, Niphakis, Micah J, Cravatt, Benjamin F, Lichtman, Aron H, Ignatowska-Jankowska, Bogna M, Fitting, Sylvia

“…Human immunodeficiency virus (HIV) affects nearly 40 million people globally, with roughly 80% of all people living with HIV receiving antiretroviral therapy…”
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Evaluation of NHS Carbamates as a Potent and Selective Class of Endocannabinoid Hydrolase Inhibitors by Niphakis, Micah J, Cognetta, Armand B, Chang, Jae Won, Buczynski, Matthew W, Parsons, Loren H, Byrne, Frederika, Burston, James J, Chapman, Victoria, Cravatt, Benjamin F

“…Monoacylglycerol lipase (MAGL) is a principal metabolic enzyme responsible for hydrolyzing the endogenous cannabinoid (endocannabinoid) 2-arachidonoylglycerol…”
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Monoacylglycerol Lipase Inhibitor MJN110 Reduces Neuronal Hyperexcitability, Restores Dendritic Arborization Complexity, and Regulates Reward-Related Behavior in Presence of HIV-1 Tat by League, Alexis F, Gorman, Benjamin L, Hermes, Douglas J, Johnson, Clare T, Jacobs, Ian R, Yadav-Samudrala, Barkha J, Poklis, Justin L, Niphakis, Micah J, Cravatt, Benjamin F, Lichtman, Aron H, Ignatowska-Jankowska, Bogna M, Fitting, Sylvia

“…While current therapeutic strategies for people living with human immunodeficiency virus type 1 (HIV-1) suppress virus replication peripherally, viral proteins…”
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Synthesis of 6- and 7-Membered Cyclic Enaminones: Scope and Mechanism by Niphakis, Micah J, Turunen, Brandon J, Georg, Gunda I

“…Six- and seven-membered cyclic enaminones can be prepared using common, environmentally benign reagents. Amino acids are used as synthetic precursors allowing…”
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Diacylglycerol lipase disinhibits VTA dopamine neurons during chronic nicotine exposure by Buczynski, Matthew W., Herman, Melissa A., Hsu, Ku-Lung, Natividad, Luis A., Irimia, Cristina, Polis, Ilham Y., Pugh, Holly, Chang, Jae Won, Niphakis, Micah J., Cravatt, Benjamin F., Roberto, Marisa, Parsons, Loren H.

“…Chronic nicotine exposure (CNE) alters synaptic transmission in the ventral tegmental area (VTA) in a manner that enhances dopaminergic signaling and promotes…”
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Inhibitory Control Deficits Associated with Upregulation of CB1R in the HIV-1 Tat Transgenic Mouse Model of Hand by Jacobs, Ian R., Xu, Changqing, Hermes, Douglas J., League, Alexis F., Xu, Callie, Nath, Bhupendra, Jiang, Wei, Niphakis, Micah J., Cravatt, Benjamin F., Mackie, Ken, Mukhopadhyay, Somnath, Lichtman, Aron H., Ignatowska-Jankowska, Bogna M., Fitting, Sylvia

“…In the era of combined antiretroviral therapy, HIV-1 infected individuals are living longer lives; however, longevity is met with an increasing number of HIV-1…”
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Inhibitory Neurotransmission Is Sex-Dependently Affected by Tat Expression in Transgenic Mice and Suppressed by the Fatty Acid Amide Hydrolase Enzyme Inhibitor PF3845 via Cannabinoid Type-1 Receptor Mechanisms by Xu, Changqing, Yadav-Samudrala, Barkha J, Xu, Callie, Nath, Bhupendra, Mistry, Twisha, Jiang, Wei, Niphakis, Micah J, Cravatt, Benjamin F, Mukhopadhyay, Somnath, Lichtman, Aron H, Ignatowska-Jankowska, Bogna M, Fitting, Sylvia

“…(1) Background. The endocannabinoid (eCB) system, which regulates physiological and cognitive processes, presents a promising therapeutic target for treating…”
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Determining target engagement in living systems by Simon, Gabriel M, Niphakis, Micah J, Cravatt, Benjamin F

“…Chemical probes are critical tools for elucidating the biological functions of proteins and can lead to new medicines for treating disease. The pharmacological…”
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