Search Results - "Dutra, Jason K"

Structural basis of lipid-droplet localization of 17-beta-hydroxysteroid dehydrogenase 13 by Liu, Shenping, Sommese, Ruth F., Nedoma, Nicole L., Stevens, Lucy Mae, Dutra, Jason K., Zhang, Liying, Edmonds, David J., Wang, Yang, Garnsey, Michelle, Clasquin, Michelle F.

“…Hydroxysteroid 17-beta-dehydrogenase 13 (HSD17B13) is a hepatic lipid droplet-associated enzyme that is upregulated in patients with non-alcoholic fatty liver…”
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SuFEx Activation with Ca(NTf 2 ) 2 : A Unified Strategy to Access Sulfamides, Sulfamates, and Sulfonamides from S(VI) Fluorides by Mahapatra, Subham, Woroch, Cristian P, Butler, Todd W, Carneiro, Sabrina N, Kwan, Sabrina C, Khasnavis, Samuel R, Gu, Junha, Dutra, Jason K, Vetelino, Beth C, Bellenger, Justin, Am Ende, Christopher W, Ball, Nicholas D

“…A method to activate sulfamoyl fluorides, fluorosulfates, and sulfonyl fluorides with calcium triflimide and DABCO for SuFEx with amines is described. The…”
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Application of the Bicyclo[1.1.1]pentane Motif as a Nonclassical Phenyl Ring Bioisostere in the Design of a Potent and Orally Active γ-Secretase Inhibitor by Stepan, Antonia F, Subramanyam, Chakrapani, Efremov, Ivan V, Dutra, Jason K, O’Sullivan, Theresa J, DiRico, Kenneth J, McDonald, W. Scott, Won, Annie, Dorff, Peter H, Nolan, Charles E, Becker, Stacey L, Pustilnik, Leslie R, Riddell, David R, Kauffman, Gregory W, Kormos, Bethany L, Zhang, Liming, Lu, Yasong, Capetta, Steven H, Green, Michael E, Karki, Kapil, Sibley, Evelyn, Atchison, Kevin P, Hallgren, Andrew J, Oborski, Christine E, Robshaw, Ashley E, Sneed, Blossom, O’Donnell, Christopher J

“…Replacement of the central, para-substituted fluorophenyl ring in the γ-secretase inhibitor 1 (BMS-708,163) with the bicyclo[1.1.1]­pentane motif led to the…”
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Pharmacological evaluation of clinically relevant concentrations of (2R,6R)-hydroxynorketamine by Shaffer, Christopher L., Dutra, Jason K., Tseng, Wei Chou, Weber, Mark L., Bogart, Luke J., Hales, Katherine, Pang, Jincheng, Volfson, Dmitri, am Ende, Christopher W., Green, Michael E., Buhl, Derek L.

“…Ketamine is a rapid-onset antidepressant whose efficacy long outlasts its pharmacokinetics. Multiple studies suggest ketamine's antidepressant effects require…”
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Mechanistic differences between linear vs. spirocyclic dialkyldiazirine probes for photoaffinity labeling by O'Brien, Jessica G K, Conway, Louis P, Ramaraj, Paramesh K, Jadhav, Appaso M, Jin, Jun, Dutra, Jason K, Evers, Parrish, Masoud, Shadi S, Schupp, Manuel, Saridakis, Iakovos, Chen, Yong, Maulide, Nuno, Pezacki, John P, Am Ende, Christopher W, Parker, Christopher G, Fox, Joseph M

“…Dialkyldiazirines have emerged as a photo-reactive group of choice for interactome mapping in live cell experiments. Upon irradiation, 'linear'…”
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Fluorophosphonates on‐Demand: A General and Simplified Approach toward Fluorophosphonate Synthesis by Dutra, Jason K., Foley, Timothy L., Huang, Zhen, Fisher, Ethan L., Lachapelle, Erik A., Mahapatra, Subham, Ogilvie, Kevin, Butler, Todd W., Bellenger, Justin, Devraj Majmudar, Jaimeen, am Ende, Christopher W.

“…Herein, we report a general and simplified synthesis of fluorophosphonates directly from p‐nitrophenylphosphonates. This FP on‐demand reaction is mediated by a…”
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Structural basis of the acyl-transfer mechanism of human GPAT1 by Johnson, Zachary Lee, Ammirati, Mark, Wasilko, David Jonathan, Chang, Jeanne S., Noell, Stephen, Foley, Timothy L., Yoon, Hyejin, Smith, Kathleen, Asano, Shoh, Hales, Katherine, Wan, Min, Yang, Qingyi, Piotrowski, Mary A., Farley, Kathleen A., Gilbert, Tamara, Aschenbrenner, Lisa M., Fennell, Kimberly F., Dutra, Jason K., Xu, Mary, Guo, Chunyang, Varghese, Alison E., Bellenger, Justin, Quinn, Alandra, am Ende, Christopher W., West, Graham M., Griffor, Matthew C., Bennett, Donald, Calabrese, Matthew, Steppan, Claire M., Han, Seungil, Wu, Huixian

“…Glycerol-3-phosphate acyltransferase (GPAT)1 is a mitochondrial outer membrane protein that catalyzes the first step of de novo glycerolipid biosynthesis…”
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Fluorophosphonate‐Based Degrader Identifies Degradable Serine Hydrolases by Quantitative Proteomics by Field, S. Denise, Lee, Wankyu, Dutra, Jason K., Serneo, Finley Scott F., Oyer, Jon, Xu, Hua, Johnson, Douglas S., am Ende, Christopher W., Seneviratne, Uthpala

“…Novel chemical biology probes linking a serine hydrolase‐directed fluorophosphonate warhead and cereblon‐binding pomalidomide were assessed for the degradation…”
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Trifluoromethyl Oxetanes: Synthesis and Evaluation as a tert‐Butyl Isostere by Mukherjee, Paramita, Pettersson, Martin, Dutra, Jason K., Xie, Longfei, am Ende, Christopher W.

“…The synthesis of a new trifluoromethyl oxetane was developed using a Corey–Chaykovsky epoxidation/ring‐expansion reaction of trifluoromethyl ketones. The…”
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Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation by O’Neill, Brian T, Beck, Elizabeth M, Butler, Christopher R, Nolan, Charles E, Gonzales, Cathleen, Zhang, Lei, Doran, Shawn D, Lapham, Kimberly, Buzon, Leanne M, Dutra, Jason K, Barreiro, Gabriela, Hou, Xinjun, Martinez-Alsina, Luis A, Rogers, Bruce N, Villalobos, Anabella, Murray, John C, Ogilvie, Kevin, LaChapelle, Erik A, Chang, Cheng, Lanyon, Lorraine F, Steppan, Claire M, Robshaw, Ashley, Hales, Katherine, Boucher, Germaine G, Pandher, Karamjeet, Houle, Christopher, Ambroise, Claude W, Karanian, David, Riddell, David, Bales, Kelly R, Brodney, Michael A

“…A major challenge in the development of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors for the treatment of Alzheimer’s disease is the…”
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Metabolism-Directed Design of Oxetane-Containing Arylsulfonamide Derivatives as γ-Secretase Inhibitors by Stepan, Antonia F, Karki, Kapil, McDonald, W. Scott, Dorff, Peter H, Dutra, Jason K, DiRico, Kenneth J, Won, Annie, Subramanyam, Chakrapani, Efremov, Ivan V, O’Donnell, Christopher J, Nolan, Charles E, Becker, Stacey L, Pustilnik, Leslie R, Sneed, Blossom, Sun, Hao, Lu, Yasong, Robshaw, Ashley E, Riddell, David, O'Sullivan, Theresa J, Sibley, Evelyn, Capetta, Steven, Atchison, Kevin, Hallgren, Andrew J, Miller, Emily, Wood, Anthony, Obach, R. Scott

“…A metabolism-based approach toward the optimization of a series of N-arylsulfonamide-based γ-secretase inhibitors is reported. The lead cyclohexyl analogue 6…”
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Discovery of a Series of Efficient, Centrally Efficacious BACE1 Inhibitors through Structure-Based Drug Design by Butler, Christopher R, Brodney, Michael A, Beck, Elizabeth M, Barreiro, Gabriela, Nolan, Charles E, Pan, Feng, Vajdos, Felix, Parris, Kevin, Varghese, Alison H, Helal, Christopher J, Lira, Ricardo, Doran, Shawn D, Riddell, David R, Buzon, Leanne M, Dutra, Jason K, Martinez-Alsina, Luis A, Ogilvie, Kevin, Murray, John C, Young, Joseph M, Atchison, Kevin, Robshaw, Ashley, Gonzales, Cathleen, Wang, Jinlong, Zhang, Yong, O’Neill, Brian T

“…The identification of centrally efficacious β-secretase (BACE1) inhibitors for the treatment of Alzheimer’s disease (AD) has historically been thwarted by an…”
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Identification of a Novel Positron Emission Tomography (PET) Ligand for Imaging β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE-1) in Brain by Zhang, Lei, Chen, Laigao, Dutra, Jason K, Beck, Elizabeth M, Nag, Sangram, Takano, Akihiro, Amini, Nahid, Arakawa, Ryosuke, Brodney, Michael A, Buzon, Leanne M, Doran, Shawn D, Lanyon, Lorraine F, McCarthy, Timothy J, Bales, Kelly R, Nolan, Charles E, O’Neill, Brian T, Schildknegt, Klaas, Halldin, Christer, Villalobos, Anabella

“…Alzheimer’s disease (AD) is characterized by accumulation of β-amyloid (Aβ) plaques and neurofibrillary tau tangles in the brain. β-Site amyloid precursor…”
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Discovery and Optimization of a Novel Spiropyrrolidine Inhibitor of β-Secretase (BACE1) through Fragment-Based Drug Design by Efremov, Ivan V, Vajdos, Felix F, Borzilleri, Kris A, Capetta, Steven, Chen, Hou, Dorff, Peter H, Dutra, Jason K, Goldstein, Steven W, Mansour, Mahmoud, McColl, Alexander, Noell, Stephen, Oborski, Christine E, O’Connell, Thomas N, O’Sullivan, Theresa J, Pandit, Jayvardhan, Wang, Hong, Wei, BinQing, Withka, Jane M

“…The aspartyl protease β-secretase, or BACE, has been demonstrated to be a key factor in the proteolytic formation of Aβ-peptide, a major component of plaques…”
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Quantitative Analysis of 18 F-PF-06684511, a Novel PET Radioligand for Selective β-Secretase 1 Imaging, in Nonhuman Primate Brain by Takano, Akihiro, Chen, Laigao, Nag, Sangram, Brodney, Michael A, Arakawa, Ryosuke, Chang, Cheng, Amini, Nahid, Doran, Shawn D, Dutra, Jason K, McCarthy, Timothy J, Nolan, Charles E, O'Neill, Brian T, Villalobos, Anabella, Zhang, Lei, Halldin, Christer

“…β-secretase 1 (BACE1) is a key enzyme in the generation of β-amyloid, which is accumulated in the brain of Alzheimer disease patients. PF-06684511 was…”
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Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine by Li, Jin, DeMello, Kristin M.Lundy, Cheng, Henry, Sakya, Subas M., Bronk, Brian S., Rafka, Robert J., Jaynes, Burton H., Ziegler, Carl B., Kilroy, Carolyn, Mann, Donald W., Nimz, Eric L., Lynch, Michael P., Haven, Michelle L., Kolosko, Nicole L., Minich, Martha L., Li, Chao, Dutra, Jason K., Rast, Bryson, Crosson, Rhonda M., Morton, Barry J., Kirk, Glen W., Callaghan, Kathleen M., Koss, David A., Shavnya, Andrei, Lund, Lisa A., Seibel, Scott B., Petras, Carol F., Silvia, Annette

“…Structure–activity relationship (SAR) studies of 2-[3-di(and tri)fluoromethyl-5-arylpyrazol-1-yl]-5-methanesulfonylpyridine derivatives for canine COX enzymes…”
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Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors by Cheng, Hengmiao, Lundy DeMello, Kristin M., Li, Jin, Sakya, Subas M., Ando, Kazuo, Kawamura, K., Kato, Tomoki, Rafka, Robert J., Jaynes, Burton H., Ziegler, Carl B., Stevens, Rod, Lund, Lisa A., Mann, Donald W., Kilroy, Carolyn, Haven, Michelle L., Nimz, Erik L., Dutra, Jason K., Li, Chao, Minich, Martha L., Kolosko, Nicole L., Petras, Carol, Silvia, Annette M., Seibel, Scott B.

“…The discovery of heteroaryl-phenyl-substituted pyrazole derivatives as canine selective COX-2 inhibitors is described. Structure–activity relationship (SAR)…”
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Synthesis and SAR of azalide 3,6-ketal aromatic derivatives as potent gram-positive and gram-negative antibacterial agents by Cheng, Hengmiao, Dirlam, John P., Ziegler, Carl B., Lundy, Kristin M., Hayashi, Shigeru F., Kamicker, Barbara J., Dutra, Jason K., Daniel, Kirsten L., Santoro, Sheryl L., George, David M., Bertsche, Camilla D., Sakya, Subas M., Suarez-Contreras, Melani

“…3,6-Ketals of 15-membered azalide pseudoaglycones are a novel series of macrolide antibiotics. The aromatic derivatives of the azalide 3,6-ketals demonstrated…”
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Quantitative Analysis of 18F-PF-06684511, a Novel PET Radioligand for Selective β-Secretase 1 Imaging, in Nonhuman Primate Brain by Takano, Akihiro, Chen, Laigao, Nag, Sangram, Brodney, Michael A, Arakawa, Ryosuke, Chang, Cheng, Amini, Nahid, Doran, Shawn D, Dutra, Jason K, McCarthy, Timothy J, Nolan, Charles E, O'Neill, Brian T, Villalobos, Anabella, Zhang, Lei, Halldin, Christer

“…β-secretase 1 (BACE1) is a key enzyme in the generation of β-amyloid, which is accumulated in the brain of Alzheimer disease patients. PF-06684511 was…”
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Model systems for flavoenzyme activity. A versatile synthesis of N(3)-alkylated flavins by Dutra, Jason K., Cuello, Alejandro O., Rotello, Vincent M.

“…Reaction of isoalloxazines (flavins) with primary and secondary alcohols using Mitsunobu conditions provides flavins alkylated at the N(3) position. This…”
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