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37 results on '"Johnson, Douglas S."'

1. Photoaffinity Labeling and Quantitative Chemical Proteomics Identify LXRβ as the Functional Target of Enhancers of Astrocytic apoE

Author

Seneviratne, Uthpala, Huang, Zhen, am Ende, Christopher W., Butler, Todd W., Cleary, Leah, Dresselhaus, Erica, Evrard, Edelweiss, Fisher, Ethan L., Green, Michael E., Helal, Christopher J., Humphrey, John M., Lanyon, Lorraine F., Marconi, Michael, Mukherjee, Paramita, Sciabola, Simone, Steppan, Claire M., Sylvain, Emily K., Tuttle, Jamison B., Verhoest, Patrick R., Wager, Travis T., Xie, Longfei, Ramaswamy, Gayathri, Johnson, Douglas S., and Pettersson, Martin

Published
2021
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2. The innate immunity protein IFITM3 modulates γ-secretase in Alzheimer’s disease

Author

Hur, Ji-Yeun, Frost, Georgia R., Wu, Xianzhong, Crump, Christina, Pan, Si Jia, Wong, Eitan, Barros, Marilia, Li, Thomas, Nie, Pengju, Zhai, Yujia, Wang, Jen Chyong, TCW, Julia, Guo, Lei, McKenzie, Andrew, Ming, Chen, Zhou, Xianxiao, Wang, Minghui, Sagi, Yotam, Renton, Alan E., Esposito, Bianca T., Kim, Yong, Sadleir, Katherine R., Trinh, Ivy, Rissman, Robert A., Vassar, Robert, Zhang, Bin, Johnson, Douglas S., Masliah, Eliezer, Greengard, Paul, Goate, Alison, and Li, Yue-Ming

Published
2020
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3. Molecular medicine and neurodegenerative diseases.

Author

Chang, Christopher J, Cravatt, Benjamin F, Johnson, Douglas S, and Lim, Mi Hee

Subjects
Humans, Neurodegenerative Diseases, Cell Death, Amyloid beta-Peptides, Molecular Medicine, General Chemistry, Chemical Sciences
Published
2014

4. Photobiomodulation therapy combined with static magnetic field is better than placebo in patients with fibromyalgia: a randomized placebo-controlled trial

Author

RIBEIRO, Neide F., primary, LEAL-JUNIOR, Ernesto C. P., additional, JOHNSON, Douglas S., additional, DEMCHAK, Timothy, additional, MACHADO, Caroline M., additional, DIAS, Luana B., additional, DE OLIVEIRA, Marcelo F., additional, LINO, Matheus M., additional, RODRIGUES, Wesley D., additional, SANTO, Jonathan, additional, DE BARROS, Carolina N., additional, CASALECHI, Heliodora L., additional, and TOMAZONI, Shaiane S., additional

Published
2023
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10. Discovery and Characterization of a Highly Selective FAAH Inhibitor that Reduces Inflammatory Pain

Author

Ahn, Kay, Johnson, Douglas S., Mileni, Mauro, Beidler, David, Long, Jonathan Z., McKinney, Michele K., Weerapana, Eranthie, Sadagopan, Nalini, Liimatta, Marya, Smith, Sarah E., Lazerwith, Scott, Stiff, Cory, Kamtekar, Satwik, Bhattacharya, Keshab, Zhang, Yanhua, Swaney, Stephen, Van Becelaere, Keri, Stevens, Raymond C., and Cravatt, Benjamin F.

Published
2009
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17. Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy

Author

Pettersson, Martin, primary, Johnson, Douglas S., additional, Rankic, Danica A., additional, Kauffman, Gregory W., additional, am Ende, Christopher W., additional, Butler, Todd W., additional, Boscoe, Brian, additional, Evrard, Edelweiss, additional, Helal, Christopher J., additional, Humphrey, John M., additional, Stepan, Antonia F., additional, Stiff, Cory M., additional, Yang, Eddie, additional, Xie, Longfei, additional, Bales, Kelly R., additional, Hajos-Korcsok, Eva, additional, Jenkinson, Stephen, additional, Pettersen, Betty, additional, Pustilnik, Leslie R., additional, Ramirez, David S., additional, Steyn, Stefanus J., additional, Wood, Kathleen M., additional, and Verhoest, Patrick R., additional

Published
2017
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19. Chemoproteomic profiling reveals that cathepsin D off-target activity drives ocular toxicity of β-secretase inhibitors

Author

Zuhl, Andrea M., primary, Nolan, Charles E., additional, Brodney, Michael A., additional, Niessen, Sherry, additional, Atchison, Kevin, additional, Houle, Christopher, additional, Karanian, David A., additional, Ambroise, Claude, additional, Brulet, Jeffrey W., additional, Beck, Elizabeth M., additional, Doran, Shawn D., additional, O’Neill, Brian T., additional, am Ende, Christopher W., additional, Chang, Cheng, additional, Geoghegan, Kieran F., additional, West, Graham M., additional, Judkins, Joshua C., additional, Hou, Xinjun, additional, Riddell, David R., additional, and Johnson, Douglas S., additional

Published
2016
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22. Design of Pyridopyrazine-1,6-dione γ-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability

Author

Pettersson, Martin, primary, Johnson, Douglas S., additional, Humphrey, John M., additional, Butler, Todd W., additional, am Ende, Christopher W., additional, Fish, Benjamin A., additional, Green, Michael E., additional, Kauffman, Gregory W., additional, Mullins, Patrick B., additional, O’Donnell, Christopher J., additional, Stepan, Antonia F., additional, Stiff, Cory M., additional, Subramanyam, Chakrapani, additional, Tran, Tuan P., additional, Vetelino, Beth Cooper, additional, Yang, Eddie, additional, Xie, Longfei, additional, Bales, Kelly R., additional, Pustilnik, Leslie R., additional, Steyn, Stefanus J., additional, Wood, Kathleen M., additional, and Verhoest, Patrick R., additional

Published
2015
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26. Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor

Author

Johnson, Douglas S., primary, Stiff, Cory, additional, Lazerwith, Scott E., additional, Kesten, Suzanne R., additional, Fay, Lorraine K., additional, Morris, Mark, additional, Beidler, David, additional, Liimatta, Marya B., additional, Smith, Sarah E., additional, Dudley, David T., additional, Sadagopan, Nalini, additional, Bhattachar, Shobha N., additional, Kesten, Stephen J., additional, Nomanbhoy, Tyzoon K., additional, Cravatt, Benjamin F., additional, and Ahn, Kay, additional

Published
2010
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29. Blocking of fatty acid amide hydrolase activity with PF-04457845 in human brain: a positron emission tomography study with the novel radioligand [11C]CURB.

Author

Boileau, Isabelle, Rusjan, Pablo M, Williams, Belinda, Mansouri, Esmaeil, Mizrahi, Romina, De Luca, Vincenzo, Johnson, Douglas S, Wilson, Alan A, Houle, Sylvain, Kish, Stephen J, and Tong, Junchao

Subjects
FATTY acid synthases, POSITRON emission tomography, RADIOLIGAND assay, HYDROLASES, ENZYMES
Abstract

Positron emission tomography with [11C]CURB was recently developed to quantify fatty acid amide hydrolase (FAAH), the enzyme responsible for hydrolyzing the endocannabinoid anandamide. This study investigated the test-retest reliability of [11C]CURB as well as its in vivo specificity and the validity of the kinetic model by using the highly specific FAAH inhibitor, PF-04457845. Five healthy volunteers completed test-retest [11C]CURB scans 1 to 2 months apart and six subjects completed baseline and blocking scans on the same day after PF-04457845 (p.o.) administration (1, 4, or 20 mg; n=2 each). The composite parameter λk3 (an index of FAAH activity, λ=K1/k2) was estimated using an irreversible two-tissue compartment model with plasma input function. There were no clinically observable responses to oral PF-04457845 or [11C]CURB injection. Oral administration of PF-04457845 reduced [11C]CURB binding to a homogeneous level at all three doses, with λk3 values decreased by ⩾91%. Excellent reproducibility and good reliability (test-retest variability=9%; intraclass correlation coefficient=0.79) were observed across all regions of interest investigated. Our findings suggest that λk3/[11C]CURB is a reliable, highly sensitive, and selective tool to measure FAAH activity in human brain in vivo. Moreover, PF-04457845 is a highly potent FAAH inhibitor (>95% inhibition at 1 mg) in living human brain. [ABSTRACT FROM AUTHOR]

Published
2015
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31. I. Design and application of piezoceramic transducers to transient pressure measurements. II. Some measurements of curvature and thickness of reflecting normal shocks at low initial pressures

Author

Johnson, Douglas S., Johnson, Douglas S., Johnson, Douglas S., and Johnson, Douglas S.

Abstract

A small pressure transducer, using the piezoelectric properties of a manufactured ceramic, was designed, constructed and installed in the end plate of the GALCIT 17-inch shock tube to obtain high-speed measurements of the pressure field behind a reflecting shock. The design problem for piezoceramic pressure transducers and some possible solutions are discussed in detail. Results of transducer calibration and recommendations for improvement of the instrument are presented. An initial program to determine the curvature of a shock at low initial pressures was run concurrently with calibration of five of the above pressure transducers. The results of this program are described in as much detail as the data obtained to date will permit. At an initial pressure of 30 microns in the GALCIT 17-inch tube, the shock obtained at a Mach number of about 7.5 in argon is observed to have a total curvature of approximately 10 millimeters, or approximately two per cent of the tube diameter. The shock thickness observed under these conditions is approximately 5 millimeters. These results indicate that it may be entirely possible to obtain good optical measurements inside the shock, but that it may be necessary to resort to special techniques to avoid optical distortion caused by curvature.

Published
1962

33. DESIGN, CONSTRUCTION, AND CALIBRATION OF THE FJSRL 17-INCH LOW DENSITY SHOCK TUBE.

Author

FRANK J SEILER RESEARCH LAB AIR FORCE ACADEMY COLO, Stebbins, Charles F., Johnson,Douglas S., FRANK J SEILER RESEARCH LAB AIR FORCE ACADEMY COLO, Stebbins, Charles F., and Johnson,Douglas S.

Abstract

The tube is to be used for studying real gas phenomena in a real shock tube. The FJSRL shock tube can be fired at test pressures ranging from 1/2 micron Hg up to atmospheric pressure, with multi-test and multi-driver gas capabilities. Diaphragm pressure ratios range between 100,000 and 10 to the 8th power giving a practical range of Mach numbers, in argon, of 2

Published
1966

36. O-hydroxyacetamide carbamates as a highly potent and selective class of endocannabinoid hydrolase inhibitors.

Author

Niphakis MJ, Johnson DS, Ballard TE, Stiff C, and Cravatt BF

Subjects
Acetamides chemistry, Acetamides classification, Amidohydrolases antagonists & inhibitors, Amidohydrolases metabolism, Animals, Carbamates chemistry, Carbamates classification, Endocannabinoids metabolism, Enzyme Inhibitors chemistry, Enzyme Inhibitors classification, Enzyme Inhibitors pharmacology, HEK293 Cells, Humans, Mice, Mice, Inbred C57BL, Protease Inhibitors chemistry, Protease Inhibitors classification, Acetamides pharmacology, Carbamates pharmacology, Endocannabinoids antagonists & inhibitors, Protease Inhibitors pharmacology
Abstract

The two major endocannabinoid transmitters, anandamide (AEA) and 2-arachidonoylglycerol (2-AG), are degraded by distinct enzymes in the nervous system, fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL), respectively. FAAH and MAGL inhibitors cause elevations in brain AEA and 2-AG levels, respectively, and reduce pain, anxiety, and depression in rodents without causing the full spectrum of psychotropic behavioral effects observed with direct cannabinoid receptor-1 (CB1) agonists. These findings have inspired the development of several classes of endocannabinoid hydrolase inhibitors, most of which have been optimized to show specificity for either FAAH or MAGL or, in certain cases, equipotent activity for both enzymes. Here, we investigate an unusual class of O-hydroxyacetamide carbamate inhibitors and find that individual compounds from this class can serve as selective FAAH or dual FAAH/MAGL inhibitors in vivo across a dose range (0.125-12.5 mg kg(-1)) suitable for behavioral studies. Competitive and click chemistry activity-based protein profiling confirmed that the O-hydroxyacetamide carbamate SA-57 is remarkably selective for FAAH and MAGL in vivo, targeting only one other enzyme in brain, the additional 2-AG hydrolase ABHD6. These data designate O-hydroxyacetamide carbamates as a versatile chemotype for creating endocannabinoid hydrolase inhibitors that display excellent in vivo activity and tunable selectivity for FAAH-anandamide versus MAGL (and ABHD6)-2-AG pathways.

Published
2012
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37. Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor.

Author

Johnson DS, Stiff C, Lazerwith SE, Kesten SR, Fay LK, Morris M, Beidler D, Liimatta MB, Smith SE, Dudley DT, Sadagopan N, Bhattachar SN, Kesten SJ, Nomanbhoy TK, Cravatt BF, and Ahn K

Abstract

Fatty acid amide hydrolase (FAAH) is an integral membrane serine hydrolase that degrades the fatty acid amide family of signaling lipids, including the endocannabinoid anandamide. Genetic or pharmacological inactivation of FAAH leads to analgesic and anti-inflammatory phenotypes in rodents without showing the undesirable side effects observed with direct cannabinoid receptor agonists, indicating that FAAH may represent an attractive therapeutic target for the treatment of inflammatory pain and other nervous system disorders. Herein, we report the discovery and characterization of a highly efficacious and selective FAAH inhibitor PF-04457845 (23). Compound 23 inhibits FAAH by a covalent, irreversible mechanism involving carbamylation of the active-site serine nucleophile of FAAH with high in vitro potency (k(inact)/K(i) and IC(50) values of 40300 M(-1) s(-1) and 7.2 nM, respectively, for human FAAH). Compound 23 has exquisite selectivity for FAAH relative to other members of the serine hydrolase superfamily as demonstrated by competitive activity-based protein profiling. Oral administration of 23 at 0.1 mg/kg results in efficacy comparable to that of naproxen at 10 mg/kg in a rat model of inflammatory pain. Compound 23 is being evaluated in human clinical trials.

Published
2011
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