Search Results - "Breslin, Michael J."

Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation by Hong, Chuan, Byrne, Noel J., Zamlynny, Beata, Tummala, Srivanya, Xiao, Li, Shipman, Jennifer M., Partridge, Andrea T., Minnick, Christina, Breslin, Michael J., Rudd, Michael T., Stachel, Shawn J., Rada, Vanessa L., Kern, Jeffrey C., Armacost, Kira A., Hollingsworth, Scott A., O’Brien, Julie A., Hall, Dawn L., McDonald, Terrence P., Strickland, Corey, Brooun, Alexei, Soisson, Stephen M., Hollenstein, Kaspar

“…Narcolepsy type 1 (NT1) is a chronic neurological disorder that impairs the brain’s ability to control sleep-wake cycles. Current therapies are limited to the…”
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Pharmacological characterization of MK-6096 – A dual orexin receptor antagonist for insomnia by Winrow, Christopher J., Gotter, Anthony L., Cox, Christopher D., Tannenbaum, Pamela L., Garson, Susan L., Doran, Scott M., Breslin, Michael J., Schreier, John D., Fox, Steven V., Harrell, Charles M., Stevens, Joanne, Reiss, Duane R., Cui, Donghui, Coleman, Paul J., Renger, John J.

“…Orexin (hypocretin) neuropeptides promote wakefulness by signaling through two G-protein coupled receptors, Orexin 1 Receptor (OX 1R) and Orexin 2 Receptor (OX…”
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Promotion of Sleep by Suvorexant-A Novel Dual Orexin Receptor Antagonist by Winrow, Christopher J., Gotter, Anthony L., Cox, Christopher D., Doran, Scott M., Tannenbaum, Pamela L., Breslin, Michael J., Garson, Susan L., Fox, Steven V., Harrell, Charles M., Stevens, Joanne, Reiss, Duane R., Cui, Donghui, Coleman, Paul J., Renger, John J.

“…Orexins/hypocretins are key neuropeptides responsible for regulating central arousal and reward circuits. Two receptors respond to orexin signaling, orexin 1…”
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Kinesin Spindle Protein (KSP) Inhibitors. 9. Discovery of (2S)-4-(2,5-Difluorophenyl)-N-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the Treatment of Taxane-Refractory Cancer by Cox, Christopher D, Coleman, Paul J, Breslin, Michael J, Whitman, David B, Garbaccio, Robert M, Fraley, Mark E, Buser, Carolyn A, Walsh, Eileen S, Hamilton, Kelly, Schaber, Michael D, Lobell, Robert B, Tao, Weikang, Davide, Joseph P, Diehl, Ronald E, Abrams, Marc T, South, Vicki J, Huber, Hans E, Torrent, Maricel, Prueksaritanont, Thomayant, Li, Chunze, Slaughter, Donald E, Mahan, Elizabeth, Fernandez-Metzler, Carmen, Yan, Youwei, Kuo, Lawrence C, Kohl, Nancy E, Hartman, George D

“…Inhibition of kinesin spindle protein (KSP) is a novel mechanism for treatment of cancer with the potential to overcome limitations associated with currently…”
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Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP by Cox, Christopher D., Breslin, Michael J., Mariano, Brenda J., Coleman, Paul J., Buser, Carolyn A., Walsh, Eileen S., Hamilton, Kelly, Huber, Hans E., Kohl, Nancy E., Torrent, Maricel, Yan, Youwei, Kuo, Laurence C., Hartman, George D.

“…Optimization of high-throughput screening (HTS) hits resulted in the discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of KSP…”
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Discovery of a Potent, CNS‐Penetrant Orexin Receptor Antagonist Based on an N,N‐Disubstituted‐1,4‐diazepane Scaffold that Promotes Sleep in Rats by Whitman, David B., Cox, Christopher D., Breslin, Michael J., Brashear, Karen M., Schreier, John D., Bogusky, Michael J., Bednar, Rodney A., Lemaire, Wei, Bruno, Joseph G., Hartman, George D., Reiss , Duane R., Harrell, C. Meacham, Kraus, Richard L., Li, Yuxing, Garson, Susan L., Doran, Scott M., Prueksaritanont, Thomayant, Li, Chunze, Winrow, Christopher J., Koblan, Kenneth S., Renger, John J., Coleman, Paul J.

“…Silent Night: Antagonism of the orexin (or hypocretin) system has recently been identified as a novel mechanism for the treatment of insomnia. Herein, we…”
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Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP by COX, Christopher D, TORRENT, Maricel, LOBELL, Robert B, WEIKANG TAO, SOUTH, Vicki J, KOHL, Nancy E, YOUWEI YAN, KUO, Lawrence C, PRUEKSARITANONT, Thomayant, SLAUGHTER, Donald E, CHUNZE LI, MAHAN, Elizabeth, BRESLIN, Michael J, BING LU, HARTMAN, George D, MARIANO, Brenda J, WHITMAN, David B, COLEMAN, Paul J, BUSER, Carolyn A, WALSH, Eileen S, HAMILTON, Kelly, SCHABER, Michael D

“…Molecular modeling in combination with X-ray crystallographic information was employed to identify a region of the kinesin spindle protein (KSP) binding site…”
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Analgesia and peripheral c-fiber modulation by selective Nav1.8 inhibition in rhesus by Vardigan, Joshua D, Pall, Parul S, McDevitt, Dillon S, Huang, ChienJung, Clements, Michelle K, Li, Yuxing, Kraus, Richard L, Breslin, Michael J, Bungard, Christopher J, Nemenov, Mikhail I, Klukinov, Mikhail, Burgey, Chritopher S, Layton, Mark E, Stachel, Shawn J, Lange, Henry S, Savitz, Alan T, Santarelli, Vincent P, Henze, Darrell A, Uslaner, Jason M

“…Voltage-gated sodium (Nav) channels present untapped therapeutic value for better and safer pain medications. The Nav1.8 channel isoform is of particular…”
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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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2‑Aminopyridines as Potent and Selective Nav1.8 Inhibitors Exhibiting Efficacy in a Nonhuman Primate Pain Model by Breslin, Michael J., Schubert, Jeffrey W., Wang, Deping, Huang, Chienjung, Clements, Michelle K., Li, Yuxing, Zhou, Xiaoping, Vardigan, Joshua D., Kraus, Richard L., Santarelli, Vincent P., Uslaner, Jason M., Coleman, Paul J., Stachel, Shawn J.

“…Herein we describe the discovery of a 2-aminopyridine scaffold as a potent and isoform selective inhibitor of the Nav1.8 sodium channel. Parallel library…”
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2-Aminopyridines as Potent and Selective Na v 1.8 Inhibitors Exhibiting Efficacy in a Nonhuman Primate Pain Model by Breslin, Michael J, Schubert, Jeffrey W, Wang, Deping, Huang, Chienjung, Clements, Michelle K, Li, Yuxing, Zhou, Xiaoping, Vardigan, Joshua D, Kraus, Richard L, Santarelli, Vincent P, Uslaner, Jason M, Coleman, Paul J, Stachel, Shawn J

“…Herein we describe the discovery of a 2-aminopyridine scaffold as a potent and isoform selective inhibitor of the Na 1.8 sodium channel. Parallel library…”
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Examining the relationship between schizotypy and religious experience among Irish adults by Breslin, Michael J., Lewis, Christopher Alan

“…The term schizotypy is used to describe a diverse range of characteristics symptomatic of schizotypal personality disorder and borderline personality disorder…”
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The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey by Smith, Sean M., Uslaner, Jason M., Cox, Christopher D., Huszar, Sarah L., Cannon, Christopher E., Vardigan, Joshua D., Eddins, Donnie, Toolan, Dawn M., Kandebo, Monika, Yao, Lihang, Raheem, Izzat T., Schreier, John D., Breslin, Michael J., Coleman, Paul J., Renger, John J.

“…Phosphodiesterase 10A (PDE10A) is a novel target for the treatment of schizophrenia that may address multiple symptomatic domains associated with this…”
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Psychometric Properties of Three Measures of “Facebook Engagement and/or Addiction” Among a Sample of English-Speaking Pakistani University Students by Turley, Joanne, Lewis, Christopher Alan, Musharraf, Sadia, Malik, Jamil A., Breslin, Michael J.

“…For researchers interested in measuring the construct of “Facebook engagement and/or addiction,” there are a number of existing measures including the Bergen…”
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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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Discovery of [(2R,5R)-5-{[(5-Fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): A Dual Orexin Receptor Antagonist with Potent Sleep-Promoting Properties by Coleman, Paul J., Schreier, John D., Cox, Christopher D., Breslin, Michael J., Whitman, David B., Bogusky, Michael J., McGaughey, Georgia B., Bednar, Rodney A., Lemaire, Wei, Doran, Scott M., Fox, Steven V., Garson, Susan L., Gotter, Anthony L., Harrell, C. Meacham, Reiss, Duane R., Cabalu, Tamara D., Cui, Donghui, Prueksaritanont, Thomayant, Stevens, Joanne, Tannenbaum, Pamela L., Ball, Richard G., Stellabott, Joyce, Young, Steven D., Hartman, George D., Winrow, Christopher J., Renger, John J.

“…Insomnia is a common disorder that can be comorbid with other physical and psychological illnesses. Traditional management of insomnia relies on general…”
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Eysenck's model of personality and prayer: the utility of a multidimensional approach by Breslin, Michael J., Lewis, Christopher Alan

“…Previous research has confirmed that psychoticism is the dimension of personality that is fundamental to individual differences in prayer. However,…”
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Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant by Raheem, Izzat T., Breslin, Michael J., Bruno, Joseph, Cabalu, Tamara D., Cooke, Andrew, Cox, Christopher D., Cui, Donghui, Garson, Susan, Gotter, Anthony L., Fox, Steven V., Harrell, C. Meacham, Kuduk, Scott D., Lemaire, Wei, Prueksaritanont, Thomayant, Renger, John J., Stump, Craig, Tannenbaum, Pamela L., Williams, Peter D., Winrow, Christopher J., Coleman, Paul J.

“…[Display omitted] Highly selective orexin receptor antagonists (SORAs) of the orexin 2 receptor (OX2R) have become attractive targets both as potential…”
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Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia by Raheem, Izzat T., Breslin, Michael J., Fandozzi, Christine, Fuerst, Joy, Hill, Nicole, Huszar, Sarah, Kandebo, Monika, Kim, Somang H., Ma, Bennett, McGaughey, Georgia, Renger, John J., Schreier, John D., Sharma, Sujata, Smith, Sean, Uslaner, Jason, Yan, Youwei, Coleman, Paul J., Cox, Christopher D.

“…We describe the discovery of potent and orally bioavailable tetrahydropyridopyrimidine inhibitors of phosphodiesterase 10A by systematic optimization of a…”
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Shaping suvorexant: application of experimental and theoretical methods for driving synthetic designs by McGaughey, Georgia, Bayly, Christopher I., Cox, Christopher D., Schreier, John D., Breslin, Michael J., Bogusky, Michael, Pitzenberger, Steve, Ball, Richard, Coleman, Paul J.

“…Dual Orexin Receptor Antagonists (DORA) bind to both the Orexin 1 and 2 receptors. High resolution crystal structures of the Orexin 1 and 2 receptors, both…”
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