Search Results - "ROECKER, Anthony J"

Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia by Roecker, Anthony J, Cox, Christopher D, Coleman, Paul J

“…Since its discovery in 1998, the orexin system, composed of two G-protein coupled receptors, orexins 1 and 2, and two neuropeptide agonists, orexins A and B,…”
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Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors by Yin, Jie, Babaoglu, Kerim, Brautigam, Chad A, Clark, Lindsay, Shao, Zhenhua, Scheuermann, Thomas H, Harrell, Charles M, Gotter, Anthony L, Roecker, Anthony J, Winrow, Christopher J, Renger, John J, Coleman, Paul J, Rosenbaum, Daniel M

“…Human orexin receptors (hOX 1 R and hOX 2 R) are GPCRs involved in sleep regulation. Structures of hOX 1 R bound to a selective antagonist or to a dual…”
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Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man by Gotter, Anthony L., Forman, Mark S., Harrell, Charles M., Stevens, Joanne, Svetnik, Vladimir, Yee, Ka Lai, Li, Xiaodong, Roecker, Anthony J., Fox, Steven V., Tannenbaum, Pamela L., Garson, Susan L., Lepeleire, Inge De, Calder, Nicole, Rosen, Laura, Struyk, Arie, Coleman, Paul J., Herring, W. Joseph, Renger, John J., Winrow, Christopher J.

“…Orexin neuropeptides regulate sleep/wake through orexin receptors (OX 1 R, OX 2 R); OX 2 R is the predominant mediator of arousal promotion. The potential for…”
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Orexin receptors as therapeutic drug targets by Gotter, Anthony L, Roecker, Anthony J, Hargreaves, Richard, Coleman, Paul J, Winrow, Christopher J, Renger, John J

“…Orexin (hypocretin) receptor antagonists stand as a model for the development of targeted CNS small-molecule therapeutics. The identification of mutations in…”
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Discovery of dual orexin receptor antagonists (DORAs) for the treatment of insomnia by Coleman, Paul J, Cox, Christopher D, Roecker, Anthony J

“…Orexins are excitatory neuropeptides that have a critical role in maintaining wakefulness. Orexin receptor antagonists promote sleep in animals and humans…”
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The dual orexin receptor antagonist, DORA‐22, lowers histamine levels in the lateral hypothalamus and prefrontal cortex without lowering hippocampal acetylcholine by Yao, Lihang, Ramirez, Andres D., Roecker, Anthony J., Fox, Steven V., Uslaner, Jason M., Smith, Sean M., Hodgson, Robert, Coleman, Paul J., Renger, John J., Winrow, Christopher J., Gotter, Anthony L.

“…Chronic insomnia is defined as a persistent difficulty with sleep initiation maintenance or non‐restorative sleep. The therapeutic standard of care for this…”
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Association of respiratory failure with inhibition of NaV1.6 in the phrenic nerve by Klein, Rebecca M., Layton, Mark E., Regan, Hillary, Regan, Christopher P., Li, Yuxing, Filzen, Tracey, Cato, Matt, Clements, Michelle K., Wang, Jixin, Sanoja, Raul, Greshock, Thomas J., Roecker, Anthony J., Pero, Joseph E., Kim, Ron, Burgey, Christopher, John, Christopher T., Wang, Ying-Hong, Bhandari, Neetesh, Struyk, Arie, Kraus, Richard L., Henze, Darrell A., Houghton, Andrea K.

“…As part of a drug discovery effort to identify potent inhibitors of NaV1.7 for the treatment of pain, we observed that inhibitors produced unexpected…”
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Discovery of 5′′-Chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2′:5′,3′′-terpyridine-3′-carboxamide (MK-1064): A Selective Orexin 2 Receptor Antagonist (2-SORA) for the Treatment of Insomnia by Roecker, Anthony J., Mercer, Swati P., Schreier, John D., Cox, Christopher D., Fraley, Mark E., Steen, Justin T., Lemaire, Wei, Bruno, Joseph G., Harrell, C. Meacham, Garson, Susan L., Gotter, Anthony L., Fox, Steven V., Stevens, Joanne, Tannenbaum, Pamela L., Prueksaritanont, Thomayant, Cabalu, Tamara D., Cui, Donghui, Stellabott, Joyce, Hartman, George D., Young, Steven D., Winrow, Christopher J., Renger, John J., Coleman, Paul J.

“…The field of small‐molecule orexin antagonist research has evolved rapidly in the last 15 years from the discovery of the orexin peptides to clinical…”
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Identification of a novel small-molecule inhibitor of the hypoxia-inducible factor 1 pathway by TAN, Chalet, DE NORONHA, Rita G, WEI ZHOU, OLSON, Jeffrey J, PEREIRA, M. Manuela, NICOLAOU, K. C, VAN MEIR, Erwin G, ROECKER, Anthony J, PYRZYNSKA, Beata, KHWAJA, Fatima, ZHAOBIN ZHANG, HUANCHUN ZHANG, QUINCY TENG, NICHOLSON, Ainsley C, GIANNAKAKOU, Paraskevi

“…Hypoxia-inducible factor 1 (HIF-1) is the central mediator of cellular responses to low oxygen and has recently become an important therapeutic target for…”
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Investigation of orexin-2 selective receptor antagonists: Structural modifications resulting in dual orexin receptor antagonists by Skudlarek, Jason W., DiMarco, Christina N., Babaoglu, Kerim, Roecker, Anthony J., Bruno, Joseph G., Pausch, Mark A., O'Brien, Julie A., Cabalu, Tamara D., Stevens, Joanne, Brunner, Joseph, Tannenbaum, Pamela L., Wuelfing, W. Peter, Garson, Susan L., Fox, Steven V., Savitz, Alan T., Harrell, Charles M., Gotter, Anthony L., Winrow, Christopher J., Renger, John J., Kuduk, Scott D., Coleman, Paul J.

“…[Display omitted] In an ongoing effort to explore the use of orexin receptor antagonists for the treatment of insomnia, dual orexin receptor antagonists…”
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Orexin receptor antagonism prevents transcriptional and behavioral plasticity resulting from stimulant exposure by Winrow, Christopher J., Tanis, Keith Q., Reiss, Duane R., Rigby, Alison M., Uslaner, Jason M., Uebele, Victor N., Doran, Scott M., Fox, Steven V., Garson, Susan L., Gotter, Anthony L., Levine, David M., Roecker, Anthony J., Coleman, Paul J., Koblan, Kenneth S., Renger, John J.

“…Orexin is a key neurotransmitter of central arousal and reward circuits in the CNS. Two receptors respond to orexin signaling, Orexin 1 Receptor (OX1R) and…”
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Discovery of 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs) by Mercer, Swati P., Roecker, Anthony J., Garson, Susan, Reiss, Duane R., Meacham Harrell, C., Murphy, Kathy L., Bruno, Joseph G., Bednar, Rodney A., Lemaire, Wei, Cui, Donghui, Cabalu, Tamara D., Tang, Cuyue, Prueksaritanont, Thomayant, Hartman, George D., Young, Steven D., Winrow, Christopher J., Renger, John J., Coleman, Paul J.

“…The orexin (or hypocretin) system has been identified as a novel target for the treatment of insomnia due to the wealth of biological and genetic data…”
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Continuous Flow-Enabled Synthesis of Bench-Stable Bicyclo[1.1.1]pentane Trifluoroborate Salts and Their Utilization in Metallaphotoredox Cross-Couplings by VanHeyst, Michael D, Qi, Ji, Roecker, Anthony J, Hughes, Jonathan M. E, Cheng, Lili, Zhao, Zheyu, Yin, Jingjun

“…Bicyclo­[1.1.1]­pentane motifs have gained increasing popularity in medicinal chemistry as bioisosteres because of their ability to impact key physicochemical…”
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Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP by Roecker, Anthony J., Coleman, Paul J., Mercer, Swati P., Schreier, John D., Buser, Carolyn A., Walsh, Eileen S., Hamilton, Kelly, Lobell, Robert B., Tao, Weikang, Diehl, Ronald E., South, Vicki J., Davide, Joseph P., Kohl, Nancy E., Yan, Youwei, Kuo, Lawrence C., Li, Chunze, Fernandez-Metzler, Carmen, Mahan, Elizabeth A., Prueksaritanont, Thomayant, Hartman, George D.

“…1,4-Diaryl-4,5-dihydropyrazoles (i.e., 25) are reported as potent inhibitors of the mitotic kinesin KSP. Inspired by previous efforts in the…”
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Building a Culture of Medicinal Chemistry Knowledge Sharing by Beshore, Douglas C, Haidle, Andrew M, Arasappan, Ashok, Lim, Yeon-Hee, Raheem, Izzat, Roecker, Anthony J, Shockley, Samantha E, Simov, Vladimir

“…Increasing the efficiency of the drug discovery process is a challenge faced by drug hunters everywhere. One strategy medicinal chemists employ to meet this…”
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Discovery of the Dual Orexin Receptor Antagonist [(7R)-4-(5-Chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the Treatment of Insomnia by Cox, Christopher D, Breslin, Michael J, Whitman, David B, Schreier, John D, McGaughey, Georgia B, Bogusky, Michael J, Roecker, Anthony J, Mercer, Swati P, Bednar, Rodney A, Lemaire, Wei, Bruno, Joseph G, Reiss, Duane R, Harrell, C. Meacham, Murphy, Kathy L, Garson, Susan L, Doran, Scott M, Prueksaritanont, Thomayant, Anderson, Wayne B, Tang, Cuyue, Roller, Shane, Cabalu, Tamara D, Cui, Donghui, Hartman, George D, Young, Steven D, Koblan, Ken S, Winrow, Christopher J, Renger, John J, Coleman, Paul J

“…Despite increased understanding of the biological basis for sleep control in the brain, few novel mechanisms for the treatment of insomnia have been identified…”
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Discovery of selective, orally bioavailable, N-linked arylsulfonamide Nav1.7 inhibitors with pain efficacy in mice by Roecker, Anthony J., Egbertson, Melissa, Jones, Kristen L.G., Gomez, Robert, Kraus, Richard L., Li, Yuxing, Koser, Amy Jo, Urban, Mark O., Klein, Rebecca, Clements, Michelle, Panigel, Jacqueline, Daley, Christopher, Wang, Jixin, Finger, Eleftheria N., Majercak, John, Santarelli, Vincent, Gregan, Irene, Cato, Matthew, Filzen, Tracey, Jovanovska, Aneta, Wang, Ying-Hong, Wang, Deping, Joyce, Leo A., Sherer, Edward C., Peng, Xuanjia, Wang, Xiu, Sun, Haiyan, Coleman, Paul J., Houghton, Andrea K., Layton, Mark E.

“…[Display omitted] The voltage-gated sodium channel Nav1.7 is a genetically validated target for the treatment of pain with gain-of-function mutations in man…”
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Orexin receptor antagonists: medicinal chemistry and therapeutic potential by Roecker, Anthony J, Coleman, Paul J

“…Actelion Pharmaceuticals achieved clinical proof-of-concept for the treatment of insomnia in 2007 with the release of Phase II data on Almorexant, a potent…”
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Fluorinated Isoindolinone-Based Glucosylceramide Synthase Inhibitors with Low Human Dose Projections by Loughran, H. Marie, Schirripa, Kathy M., Roecker, Anthony J., Breslin, Michael J., Tong, Ling, Fillgrove, Kerry L., Kuo, Yuhsin, Bleasby, Kelly, Collier, Hannah, Altman, Michael D., Ford, Melissa C., Newman, Justin A., Drolet, Robert E., Cosden, Mali, Jinn, Sarah, Flick, Rosemarie B., Liu, Xiaomei, Minnick, Christina, Watt, Marla L., Lemaire, Wei, Burlein, Christine, Adam, Gregory C., Austin, Lauren A., Marcus, Jacob N., Smith, Sean M., Fraley, Mark E.

“…Inhibition of glucosylceramide synthase (GCS) has been proposed as a therapeutic strategy for the treatment of Parkinson’s Disease (PD), particularly in…”
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Selective orexin 2 receptor antagonism blocks cue-induced reinstatement, but not nicotine self-administration or nicotine-induced reinstatement by Uslaner, Jason M., Winrow, Christopher J., Gotter, Anthony L., Roecker, Anthony J., Coleman, Paul J., Hutson, Pete H., Le, Anh D., Renger, John J.

“…•Several orexin 1 receptor antagonists impact behaviors associated with drug abuse.•The role of the orexin 2 receptor in these behaviors is unclear.•We…”
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