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Your search keyword '"Harris, Christopher M."' showing total 6 results
Start Over Author "Harris, Christopher M." Journal journal of medicinal chemistry
6 results on '"Harris, Christopher M."'

1. Identification of Selective Dual ROCK1 and ROCK2 Inhibitors Using Structure-Based Drug Design

Author

Hobson, Adrian D., primary, Judge, Russell A., additional, Aguirre, Ana L., additional, Brown, Brian S., additional, Cui, Yifang, additional, Ding, Ping, additional, Dominguez, Eric, additional, DiGiammarino, Enrico, additional, Egan, David A., additional, Freiberg, Gail M., additional, Gopalakrishnan, Sujatha M., additional, Harris, Christopher M., additional, Honore, Marie P., additional, Kage, Karen L., additional, Kapecki, Nicolas J., additional, Ling, Christopher, additional, Ma, Junli, additional, Mack, Helmut, additional, Mamo, Mulugeta, additional, Maurus, Stefan, additional, McRae, Bradford, additional, Moore, Nigel S., additional, Mueller, Bernhard K., additional, Mueller, Reinhold, additional, Namovic, Marian T., additional, Patel, Kaushal, additional, Pratt, Steve D., additional, Putman, C. Brent, additional, Queeney, Kara L., additional, Sarris, Kathy K., additional, Schaffter, Lisa M., additional, Stoll, Vincent, additional, Vasudevan, Anil, additional, Wang, Lei, additional, Wang, Lu, additional, Wirthl, William, additional, and Yach, Kimberly, additional

Published
2018
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2. Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders

Author

Hobson, Adrian D., primary, Harris, Christopher M., additional, van der Kam, Elizabeth L., additional, Turner, Sean C., additional, Abibi, Ayome, additional, Aguirre, Ana L., additional, Bousquet, Peter, additional, Kebede, Tegest, additional, Konopacki, Donald B., additional, Gintant, Gary, additional, Kim, Youngjae, additional, Larson, Kelly, additional, Maull, John W., additional, Moore, Nigel S., additional, Shi, Dan, additional, Shrestha, Anurupa, additional, Tang, Xiubo, additional, Zhang, Peng, additional, and Sarris, Kathy K., additional

Published
2015
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3. Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.

Author

Hobson, Adrian D., Harris, Christopher M., van der Kam, Elizabeth L., Turner, Sean C., Abibi, Ayome, Aguirre, Ana L., Bousquet, Peter, Kebede, Tegest, Konopacki, Donald B., Gintant, Gary, Youngjae Kim, Larson, Kelly, Maull, John W., Moore, Nigel S., Dan Shi, Shrestha, Anurupa, Xiubo Tang, Peng Zhang, and Sarris, Kathy K.

Subjects
*BIOAVAILABILITY, *ORAL medication, *TREATMENT of neurodegeneration, *SPHINGOSINE-1-phosphate, *CHEMICAL agonists, *BLOOD-brain barrier
Abstract

S1P5 is one of 5 receptors for sphingosine-1-phosphate and is highly expressed on endothelial cells within the blood-brain barrier, where it maintains barrier integrity in in vitro models (J. Neuroinflamm. 2012, 9, 133). Little more is known about the effects of S1P5 modulation due to the absence of tool molecules with suitable selectivity and drug-like properties. We recently reported that molecule A-971432 (Harris, 2010) (29 in this paper) is highly efficacious in reversing lipid accumulation and age-related cognitive decline in rats (Van der Kam, AAIC 2014). Herein we describe the development of a series of selective S1P5 agonists that led to the identification of compound 29, which is highly selective for S1P5 and has excellent plasma and CNS exposure after oral dosing in preclinical species. To further support its suitability for in vivo studies of S1P5 biology, we extensively characterized 29, including confirmation of its selectivity in pharmacodynamic assays of S1P1 and S1P3 function in rats. In addition, we found that 29improves blood-brain barrier integrity in an in vitro model and reverses age-related cognitive decline in mice. These results suggest that S1P5 agonism is an innovative approach with potential benefit in neurodegenerative disorders involving lipid imbalance and/or compromised blood-brain barrier such as Alzheimer's disease or multiple sclerosis. [ABSTRACT FROM AUTHOR]

Published
2015
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4. 3-Amino-benzo[d]isoxazoles as Novel Multitargeted Inhibitors of Receptor Tyrosine Kinases

Author

Ji, Zhiqin, primary, Ahmed, Asma A., additional, Albert, Daniel H., additional, Bouska, Jennifer J., additional, Bousquet, Peter F., additional, Cunha, George, A., additional, Diaz, Gilbert, additional, Glaser, Keith B., additional, Guo, Jun, additional, Harris, Christopher M., additional, Li, Junling, additional, Marcotte, Patrick A., additional, Moskey, Maria D., additional, Oie, Tetsuro, additional, Pease, Lori, additional, Soni, Nirupama B., additional, Stewart, Kent D., additional, Davidsen, Steven K., additional, and Michaelides, Michael R., additional

Published
2008
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5. 1,4-Dihydroindeno[1,2-c]pyrazoles with Acetylenic Side Chains as Novel and Potent Multitargeted Receptor Tyrosine Kinase Inhibitors with Low Affinity for the hERG Ion Channel

Author

Dinges, Jürgen, primary, Albert, Daniel H., additional, Arnold, Lee D., additional, Ashworth, Kimba L., additional, Akritopoulou-Zanze, Irini, additional, Bousquet, Peter F., additional, Bouska, Jennifer J., additional, Cunha, George A., additional, Davidsen, Steven K., additional, Diaz, Gilbert J., additional, Djuric, Stevan W., additional, Gasiecki, Alan F., additional, Gintant, Gary A., additional, Gracias, Vijaya J., additional, Harris, Christopher M., additional, Houseman, Kathryn A., additional, Hutchins, Charles W., additional, Johnson, Eric F., additional, Li, Hu, additional, Marcotte, Patrick A., additional, Martin, Ruth L., additional, Michaelides, Michael R., additional, Nyein, Michelle, additional, Sowin, Thomas J., additional, Su, Zhi, additional, Tapang, Paul H., additional, Xia, Zhiren, additional, and Zhang, Henry Q., additional

Published
2007
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6. Discovery of N-(4-(3-Amino-1H-indazol-4-yl)phenyl)-N‘-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-Aminoindazole-Based Orally Active Multitargeted Receptor Tyrosine Kinase Inhibitor

Author

Dai, Yujia, primary, Hartandi, Kresna, additional, Ji, Zhiqin, additional, Ahmed, Asma A., additional, Albert, Daniel H., additional, Bauch, Joy L., additional, Bouska, Jennifer J., additional, Bousquet, Peter F., additional, Cunha, George A., additional, Glaser, Keith B., additional, Harris, Christopher M., additional, Hickman, Dean, additional, Guo, Jun, additional, Li, Junling, additional, Marcotte, Patrick A., additional, Marsh, Kennan C., additional, Moskey, Maria D., additional, Martin, Ruth L., additional, Olson, Amanda M., additional, Osterling, Donald J., additional, Pease, Lori J., additional, Soni, Niru B., additional, Stewart, Kent D., additional, Stoll, Vincent S., additional, Tapang, Paul, additional, Reuter, David R., additional, Davidsen, Steven K., additional, and Michaelides, Michael R., additional

Published
2007
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