Search Results - "SMITH, Jacqueline A. M"

Combining RAS(ON) G12C-selective inhibitor with SHP2 inhibition sensitises lung tumours to immune checkpoint blockade by Anastasiou, Panayiotis, Moore, Christopher, Rana, Sareena, Tomaschko, Mona, Pillsbury, Claire E., de Castro, Andrea, Boumelha, Jesse, Mugarza, Edurne, de Carné Trécesson, Sophie, Mikolajczak, Ania, Blaj, Cristina, Goldstone, Robert, Smith, Jacqueline A. M., Quintana, Elsa, Molina-Arcas, Miriam, Downward, Julian

“…Mutant selective drugs targeting the inactive, GDP-bound form of KRAS G12C have been approved for use in lung cancer, but resistance develops rapidly. Here we…”
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Combined inhibition of KRASG12C and mTORC1 kinase is synergistic in non-small cell lung cancer by Kitai, Hidenori, Choi, Philip H., Yang, Yu C., Boyer, Jacob A., Whaley, Adele, Pancholi, Priya, Thant, Claire, Reiter, Jason, Chen, Kevin, Markov, Vladimir, Taniguchi, Hirokazu, Yamaguchi, Rui, Ebi, Hiromichi, Evans, James, Jiang, Jingjing, Lee, Bianca, Wildes, David, de Stanchina, Elisa, Smith, Jacqueline A. M., Singh, Mallika, Rosen, Neal

“…Current KRAS G12C (OFF) inhibitors that target inactive GDP-bound KRAS G12C cause responses in less than half of patients and these responses are not durable…”
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RAS nucleotide cycling underlies the SHP2 phosphatase dependence of mutant BRAF-, NF1- and RAS-driven cancers by Nichols, Robert J., Haderk, Franziska, Stahlhut, Carlos, Schulze, Christopher J., Hemmati, Golzar, Wildes, David, Tzitzilonis, Christos, Mordec, Kasia, Marquez, Abby, Romero, Jason, Hsieh, Tientien, Zaman, Aubhishek, Olivas, Victor, McCoach, Caroline, Blakely, Collin M., Wang, Zhengping, Kiss, Gert, Koltun, Elena S., Gill, Adrian L., Singh, Mallika, Goldsmith, Mark A., Smith, Jacqueline A. M., Bivona, Trever G.

“…Oncogenic alterations in the RAS/RAF/MEK/ERK pathway drive the growth of a wide spectrum of cancers. While BRAF and MEK inhibitors are efficacious against BRAF…”
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Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth by Lee, Bianca J., Boyer, Jacob A., Burnett, G. Leslie, Thottumkara, Arun P., Tibrewal, Nidhi, Wilson, Stacy L., Hsieh, Tientien, Marquez, Abby, Lorenzana, Edward G., Evans, James W., Hulea, Laura, Kiss, Gert, Liu, Hui, Lee, Dong, Larsson, Ola, McLaughlan, Shannon, Topisirovic, Ivan, Wang, Zhengping, Wang, Zhican, Zhao, Yongyuan, Wildes, David, Aggen, James B., Singh, Mallika, Gill, Adrian L., Smith, Jacqueline A. M., Rosen, Neal

“…The clinical benefits of pan-mTOR active-site inhibitors are limited by toxicity and relief of feedback inhibition of receptor expression. To address these…”
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Shp1 Loss Enhances Macrophage Effector Function and Promotes Anti-Tumor Immunity by Myers, Darienne R, Abram, Clare L, Wildes, David, Belwafa, Amira, Welsh, Alia M N, Schulze, Christopher J, Choy, Tiffany J, Nguyen, Tram, Omaque, Neil, Hu, Yongmei, Singh, Mallika, Hansen, Rich, Goldsmith, Mark A, Quintana, Elsa, Smith, Jacqueline A M, Lowell, Clifford A

“…Shp1, encoded by the gene , is a protein tyrosine phosphatase that transduces inhibitory signals downstream of immunoreceptors in many immune cell types…”
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Author Correction: Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth by Lee, Bianca J., Boyer, Jacob A., Burnett, G. Leslie, Thottumkara, Arun P., Tibrewal, Nidhi, Wilson, Stacy L., Hsieh, Tientien, Marquez, Abby, Lorenzana, Edward G., Evans, James W., Hulea, Laura, Kiss, Gert, Liu, Hui, Lee, Dong, Larsson, Ola, McLaughlan, Shannon, Topisirovic, Ivan, Wang, Zhengping, Wang, Zhican, Zhao, Yongyuan, Wildes, David, Aggen, James B., Singh, Mallika, Gill, Adrian L., Smith, Jacqueline A. M., Rosen, Neal

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Efficacy of a Novel Bi-Steric mTORC1 Inhibitor in Models of B-Cell Acute Lymphoblastic Leukemia by Lee, Bianca J., Mallya, Sharmila, Dinglasan, Nuntana, Fung, Amos, Nguyen, Tram, Herzog, Lee-or, Thao, Joshua, Lorenzana, Edward G., Wildes, David, Singh, Mallika, Smith, Jacqueline A. M., Fruman, David A.

“…The mechanistic target of rapamycin (mTOR) is a kinase whose activity is elevated in hematological malignancies. mTOR-complex-1 (mTORC1) phosphorylates…”
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Author Correction: Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth by Lee, Bianca J., Boyer, Jacob A., Burnett, G. Leslie, Thottumkara, Arun P., Tibrewal, Nidhi, Wilson, Stacy L., Hsieh, Tientien, Marquez, Abby, Lorenzana, Edward G., Evans, James W., Hulea, Laura, Kiss, Gert, Liu, Hui, Lee, Dong, Larsson, Ola, McLaughlan, Shannon, Topisirovic, Ivan, Wang, Zhengping, Wang, Zhican, Zhao, Yongyuan, Wildes, David, Aggen, James B., Singh, Mallika, Gill, Adrian L., Smith, Jacqueline A. M., Rosen, Neal

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Relative contributions of norepinephrine and serotonin transporters to antinociceptive synergy between monoamine reuptake inhibitors and morphine in the rat formalin model by Shen, Fei, Tsuruda, Pamela R, Smith, Jacqueline A M, Obedencio, Glenmar P, Martin, William J

“…Multimodal analgesia is designed to optimize pain relief by coadministering drugs with distinct mechanisms of action or by combining multiple pharmacologies…”
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Prediction of human serotonin and norepinephrine transporter occupancy of duloxetine by pharmacokinetic/pharmacodynamic modeling in the rat by Bourdet, David L, Tsuruda, Pamela R, Obedencio, Glenmar P, Smith, Jacqueline A M

“…Translation of central nervous system occupancy and clinical effect from animal models to humans has remained elusive for many pharmacological targets. The…”
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Allosteric Inhibition of SHP2 Stimulates Antitumor Immunity by Transforming the Immunosuppressive Environment by Quintana, Elsa, Schulze, Christopher J., Myers, Darienne R., Choy, Tiffany J., Mordec, Kasia, Wildes, David, Shifrin, Nataliya Tobvis, Belwafa, Amira, Koltun, Elena S., Gill, Adrian L., Singh, Mallika, Kelsey, Stephen, Goldsmith, Mark A., Nichols, Robert, Smith, Jacqueline A.M.

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Preclinical to clinical translation of CNS transporter occupancy of TD-9855, a novel norepinephrine and serotonin reuptake inhibitor by Smith, Jacqueline A M, Bourdet, D L, Patil, D L, Daniels, O T, Ding, Y-S, Gallezot, J-D, Henry, S, Kim, K H S, Kshirsagar, S, Martin, W J, Obedencio, G P, Stangeland, E, Tsuruda, P R, Williams, W, Carson, R E, Patil, S T

“…Monoamine reuptake inhibitors exhibit unique clinical profiles that reflect distinct engagement of the central nervous system (CNS) transporters. We used a…”
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Chemical remodeling of a cellular chaperone to target the active state of mutant KRAS by Schulze, Christopher J., Seamon, Kyle J., Zhao, Yulei, Yang, Yu C., Cregg, Jim, Kim, Dongsung, Tomlinson, Aidan, Choy, Tiffany J., Wang, Zhican, Sang, Ben, Pourfarjam, Yasin, Lucas, Jessica, Cuevas-Navarro, Antonio, Ayala-Santos, Carlos, Vides, Alberto, Li, Chuanchuan, Marquez, Abby, Zhong, Mengqi, Vemulapalli, Vidyasiri, Weller, Caroline, Gould, Andrea, Whalen, Daniel M., Salvador, Anthony, Milin, Anthony, Saldajeno-Concar, Mae, Dinglasan, Nuntana, Chen, Anqi, Evans, Jim, Knox, John E., Koltun, Elena S., Singh, Mallika, Nichols, Robert, Wildes, David, Gill, Adrian L., Smith, Jacqueline A. M., Lito, Piro

“…The discovery of small-molecule inhibitors requires suitable binding pockets on protein surfaces. Proteins that lack this feature are considered undruggable…”
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Discovery, oral pharmacokinetics and in vivo efficacy of a highly selective 5-HT4 receptor agonist: Clinical compound TD-2749 by Long, Daniel D., Armstrong, Scott R., Beattie, David T., Choi, Seok-Ki, Fatheree, Paul R., Gendron, Roland A.L., Goldblum, Adam A., Humphrey, Patrick P., Marquess, Daniel G., Shaw, Jeng-Pyng, Smith, Jacqueline A.M., Derek Turner, S., Vickery, Ross G.

“…Further application of our multivalent approach to drug discovery directed to 5-HT4 receptor agonists is described. Optimization of the linker and secondary…”
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Concurrent inhibition of oncogenic and wild-type RAS-GTP for cancer therapy by Holderfield, Matthew, Lee, Bianca J., Jiang, Jingjing, Tomlinson, Aidan, Seamon, Kyle J., Mira, Alessia, Patrucco, Enrico, Goodhart, Grace, Dilly, Julien, Gindin, Yevgeniy, Dinglasan, Nuntana, Wang, Yingyun, Lai, Lick Pui, Cai, Shurui, Jiang, Lingyan, Nasholm, Nicole, Shifrin, Nataliya, Blaj, Cristina, Shah, Harshit, Evans, James W., Montazer, Nilufar, Lai, Oliver, Shi, Jade, Ahler, Ethan, Quintana, Elsa, Chang, Stephanie, Salvador, Anthony, Marquez, Abby, Cregg, Jim, Liu, Yang, Milin, Anthony, Chen, Anqi, Ziv, Tamar Bar, Parsons, Dylan, Knox, John E., Klomp, Jennifer E., Roth, Jennifer, Rees, Matthew, Ronan, Melissa, Cuevas-Navarro, Antonio, Hu, Feng, Lito, Piro, Santamaria, David, Aguirre, Andrew J., Waters, Andrew M., Der, Channing J., Ambrogio, Chiara, Wang, Zhengping, Gill, Adrian L., Koltun, Elena S., Smith, Jacqueline A. M., Wildes, David, Singh, Mallika

“…RAS oncogenes (collectively NRAS , HRAS and especially KRAS ) are among the most frequently mutated genes in cancer, with common driver mutations occurring at…”
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Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT4 receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation by Long, Daniel D., Armstrong, Scott R., Beattie, David T., Choi, Seok-Ki, Fatheree, Paul R., Gendron, Roland A.L., Genov, Daniel, Goldblum, Adam A., Humphrey, Patrick P., Jiang, Lan, Marquess, Daniel G., Shaw, Jeng-Pyng, Smith, Jacqueline A.M., Turner, S. Derek, Vickery, Ross G.

“…Utilization of Theravance’s multivalent approach to drug discovery towards 5-HT4 receptor agonists with a focus on identification of neutral (non-charged at…”
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A Multivalent Approach to the Design and Discovery of Orally Efficacious 5-HT4 Receptor Agonists by McKinnell, R. Murray, Armstrong, Scott R, Beattie, David T, Choi, Seok-Ki, Fatheree, Paul R, Gendron, Roland A. L, Goldblum, Adam, Humphrey, Patrick P, Long, Daniel D, Marquess, Daniel G, Shaw, J. P, Smith, Jacqueline A. M, Turner, S. Derek, Vickery, Ross G

“…5-HT4 receptor agonists such as tegaserod have demonstrated efficacy in the treatment of constipation predominant irritable bowel syndrome (IBS-C), a highly…”
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Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors by Burnett, G. Leslie, Yang, Yu C., Aggen, James B., Pitzen, Jennifer, Gliedt, Micah K., Semko, Chris M., Marquez, Abby, Evans, James W., Wang, Gang, Won, Walter S., Tomlinson, Aidan C. A., Kiss, Gert, Tzitzilonis, Christos, Thottumkara, Arun P., Cregg, James, Mellem, Kevin T., Choi, Jong S., Lee, Julie C., Zhao, Yongyuan, Lee, Bianca J., Meyerowitz, Justin G., Knox, John E., Jiang, Jingjing, Wang, Zhican, Wildes, David, Wang, Zhengping, Singh, Mallika, Smith, Jacqueline A. M., Gill, Adrian L.

“…Hyperactivation of mTOR kinase by mutations in the PI3K/mTOR pathway or by crosstalk with other mutant cancer drivers, such as RAS, is a feature of many…”
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Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer by Wasko, Urszula N., Jiang, Jingjing, Dalton, Tanner C., Curiel-Garcia, Alvaro, Edwards, A. Cole, Wang, Yingyun, Lee, Bianca, Orlen, Margo, Tian, Sha, Stalnecker, Clint A., Drizyte-Miller, Kristina, Menard, Marie, Dilly, Julien, Sastra, Stephen A., Palermo, Carmine F., Hasselluhn, Marie C., Decker-Farrell, Amanda R., Chang, Stephanie, Jiang, Lingyan, Wei, Xing, Yang, Yu C., Helland, Ciara, Courtney, Haley, Gindin, Yevgeniy, Muonio, Karl, Zhao, Ruiping, Kemp, Samantha B., Clendenin, Cynthia, Sor, Rina, Vostrejs, William P., Hibshman, Priya S., Amparo, Amber M., Hennessey, Connor, Rees, Matthew G., Ronan, Melissa M., Roth, Jennifer A., Brodbeck, Jens, Tomassoni, Lorenzo, Bakir, Basil, Socci, Nicholas D., Herring, Laura E., Barker, Natalie K., Wang, Junning, Cleary, James M., Wolpin, Brian M., Chabot, John A., Kluger, Michael D., Manji, Gulam A., Tsai, Kenneth Y., Sekulic, Miroslav, Lagana, Stephen M., Califano, Andrea, Quintana, Elsa, Wang, Zhengping, Smith, Jacqueline A. M., Holderfield, Matthew, Wildes, David, Lowe, Scott W., Badgley, Michael A., Aguirre, Andrew J., Vonderheide, Robert H., Stanger, Ben Z., Baslan, Timour, Der, Channing J., Singh, Mallika, Olive, Kenneth P.

“…Broad-spectrum RAS inhibition has the potential to benefit roughly a quarter of human patients with cancer whose tumours are driven by RAS mutations 1 , 2 …”
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Influence of ligand binding kinetics on functional inhibition of human recombinant serotonin and norepinephrine transporters by Tsuruda, Pamela R., Yung, Joey, Martin, William J., Chang, Ray, Mai, Ngoc, Smith, Jacqueline A.M.

“…Monoamine reuptake inhibitors treat a wide range of CNS disorders, including depression, obesity, and pain. The in vitro pharmacological properties of these…”
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