Search Results - "Johnstone, Shawn"

Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective by Johnstone, Shawn, Albert, Jeffrey S.

“…[Display omitted] New strategies to potentially improve drug safety and efficacy emerge with allosteric programs. Biased allosteric modulators can be designed…”
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Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition by Kennedy, Amanda J., Sundström, Linda, Geschwindner, Stefan, Poon, Eunice K. Y., Jiang, Yuhong, Chen, Rongfeng, Cooke, Rob, Johnstone, Shawn, Madin, Andrew, Lim, Junxian, Liu, Qingqi, Lohman, Rink-Jan, Nordqvist, Anneli, Fridén-Saxin, Maria, Yang, Wenzhen, Brown, Dean G., Fairlie, David P., Dekker, Niek

“…Protease-activated receptor-2 (PAR2) has been implicated in multiple pathophysiologies but drug discovery is challenging due to low small molecule tractability…”
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The Power of Visual Imagery in Synthesis Planning. Stereocontrolled Approaches to CGP-60536B, a Potent Renin Inhibitor by Hanessian, Stephen, Claridge, Stephen, Johnstone, Shawn

“…Two strategies were developed toward the stereocontrolled synthesis of 8-aryl-3-hydroxy-4-amino-2,7-diisopropyloctanoic acids with predetermined stereogenic…”
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Rational Design of Macrocyclic Noncovalent Inhibitors of SARS-CoV-2 M pro from a DNA-Encoded Chemical Library Screening Hit That Demonstrate Potent Inhibition against Pan-Coronavirus Homologues and Nirmatrelvir-Resistant Variants by Wang, Xu, Gotchev, Dimitar, Fan, Kristi Yi, Vega, Marvin M, Mani, Nagraj, McGovern-Gooch, Kayleigh, Cuconati, Andrea, Tercero, Breanna, Wang, Xiaohe, Carpino, Philip, Maskos, Klaus, Centrella, Paolo A, Schmitt, Andreas, Preuss, Franziska, Prasad, Archna, Chen, Chia-Yi, Clark, Matthew A, Guilinger, John P, Johnstone, Shawn, von König, Konstanze, Keefe, Anthony D, Liu, Jenny, Turcotte, Stéphane, Zhang, Ying, Konz Makino, Debora L, Lam, Angela M, Cole, Andrew G, Sofia, Michael J

“…The recent global COVID-19 pandemic has highlighted treatments for coronavirus infection as an unmet medical need. The main protease (M ) has been an important…”
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Rational Design of Macrocyclic Noncovalent Inhibitors of SARS-CoV‑2 Mpro from a DNA-Encoded Chemical Library Screening Hit That Demonstrate Potent Inhibition against Pan-Coronavirus Homologues and Nirmatrelvir-Resistant Variants by Wang, Xu, Gotchev, Dimitar, Fan, Kristi Yi, Vega, Marvin M., Mani, Nagraj, McGovern-Gooch, Kayleigh, Cuconati, Andrea, Tercero, Breanna, Wang, Xiaohe, Carpino, Philip, Maskos, Klaus, Centrella, Paolo A., Schmitt, Andreas, Preuss, Franziska, Prasad, Archna, Chen, Chia-yi, Clark, Matthew A., Guilinger, John P., Johnstone, Shawn, von König, Konstanze, Keefe, Anthony D., Liu, Jenny, Turcotte, Stéphane, Zhang, Ying, Konz Makino, Debora L., Lam, Angela M., Cole, Andrew G., Sofia, Michael J.

“…The recent global COVID-19 pandemic has highlighted treatments for coronavirus infection as an unmet medical need. The main protease (Mpro) has been an…”
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The BET Bromodomain Inhibitors EP11313 and EP11336 Have Potent Anti-Leukemic Activity in Acute Myeloid Leukemia (AML) and Augment the Effects of All-Trans-Retinoic Acid (AtRA) in Vitro by Swords, Ronan T., Brothers, Shaun, Ayad, Nagi, Perez, Aymee, Watts, Justin M., Vargas, Fernando, Elias, Roy, Rodriguez, Ana, Johnstone, Shawn, Albert, Jeffrey, Collard, Joseph, Zelent, Arthur, Wahlestedt, Claes

“…Introduction - The Myc proteins are transcription factors that have essential roles in cell growth and proliferation by both positively and negatively…”
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EG-04DEVELOPMENT OF HIGHLY POTENT, SELECTIVE BET BROMODOMAIN INHIBITORS THAT ARE CNS PENETRANT AND EFFECTIVE IN RODENT MODELS OF BRAIN CANCER by Johnstone, Shawn, Johhnsone, Andrea, Penas, Clara, Stathias, Vasileios, Brothers, Shaun, Ayad, Nagi, Wahlestedt, Claes, Albert, Jeffrey

“…BRD2, BRD3, and BRD4 are members of the BET family of bromodomain inhibitors that have received intense current interest as novel treatments for cancer. The…”
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Total Synthesis and Structural Confirmation of the Marine Natural Product Dysinosin A:  A Novel Inhibitor of Thrombin and Factor VIIa by Hanessian, Stephen, Margarita, Roberto, Hall, Adrian, Johnstone, Shawn, Tremblay, Martin, Parlanti, Luca

“…The structure and absolute configuration of the marine antithrombotic product dysinosin A was confirmed by total synthesis. The strategy involved…”
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EG-04 DEVELOPMENT OF HIGHLY POTENT, SELECTIVE BET BROMODOMAIN INHIBITORS THAT ARE CNS PENETRANT AND EFFECTIVE IN RODENT MODELS OF BRAIN CANCER by Johnstone, S., Johhnsone, A., Penas, C., Stathias, V., Brothers, S., Ayad, N., Wahlestedt, C., Albert, J.

“…BRD2, BRD3, and BRD4 are members of the BET family of bromodomain inhibitors that have received intense current interest as novel treatments for cancer. The…”
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N-Methyl-3-(tetrahydro-2H-pyran-4-yl)-2,3,4,9-tetrahydro-1H-carbaz ole- 6-carboxamides as a novel class of cannabinoid receptors agonists with low CNS penetration by Wei, Zhongyong, Yang, Hua, Liu, Ziping, Tremblay, Maxime, Johnstone, Shawn, Beha, Sara, Yue, Shi Yi, Srivastava, Sanjay, Tomaszewski, Miroslaw J, Brown, William, Walpole, Christopher, St-Onge, Stephane, Lessard, Etienne, Archambault, Anne-Julie, Groblewski, Thierry, Page, Daniel

“…Cannabinoid CB1 receptor agonists exhibit potent analgesic effects in rodents and humans, but their clinical utility as analgesic drugs is often limited by…”
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N-Methyl-3-(tetrahydro-2H-pyran-4-yl)-2,3,4,9-tetrahydro-1H-carbazole-6-carboxamides as a novel class of cannabinoid receptors agonists with low CNS penetration by Wei, Zhongyong, Yang, Hua, Liu, Ziping, Tremblay, Maxime, Johnstone, Shawn, Béha, Sara, Yue, Shi Yi, Srivastava, Sanjay, Tomaszewski, Miroslaw J., Brown, William, Walpole, Christopher, St-Onge, Stéphane, Lessard, Etienne, Archambault, Anne-Julie, Groblewski, Thierry, Pagé, Daniel

“…Cannabinoid CB1 receptor agonists exhibit potent analgesic effects in rodents and humans, but their clinical utility as analgesic drugs is often limited by…”
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Synthesis of Hydroxamic Esters via Alkoxyaminocarbonylation of β-Dicarbonyl Compounds by Hanessian, Stephen, Johnstone, Shawn

“…N-t-Butoxycarbonyl-O-sulfonyl-substituted hydroxylamines react with soft enolates to yield O - t-butoxycarbonylamino derivatives rather than the expected…”
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Potent and orally efficacious benzothiazole amides as TRPV1 antagonists by Besidski, Yevgeni, Brown, William, Bylund, Johan, Dabrowski, Michael, Dautrey, Sophie, Harter, Magali, Horoszok, Lucy, Hu, Yin, Johnson, Dean, Johnstone, Shawn, Jones, Paul, Leclerc, Sandrine, Kolmodin, Karin, Kers, Inger, Labarre, Maryse, Labrecque, Denis, Laird, Jennifer, Lundström, Therese, Martino, John, Maudet, Mickaël, Munro, Alexander, Nylöf, Martin, Penwell, Andrea, Rotticci, Didier, Slaitas, Andis, Sundgren-Andersson, Anna, Svensson, Mats, Terp, Gitte, Villanueva, Huascar, Walpole, Christopher, Zemribo, Ronald, Griffin, Andrew M.

“…Benzothiazole amides were identified as TRPV1 antagonists from high throughput screening. Compound 37 maintained potent antagonism with improved metabolic…”
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Total synthesis and structural confirmation of the marine natural product dvsinosin A: A novel inhibitor of thrombin and factor VIIa by HANESSIAN, Stephen, MARGARITA, Roberto, HALL, Adrian, JOHNSTONE, Shawn, TREMBLAY, Martin, PARLANTI, Luca

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New and old challenges in total synthesis. From concept to practice by Hanessian, S., Margarita, Roberto, Hall, Adrian, Johnstone, Shawn, Tremblay, M., Parlanti, L.

“…The total synthesis of dysinosin A, a novel member of the aeruginosin group of marine natural products is discussed. The stereocontrolled synthesis also…”
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