Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity
Schenkel, Laurie B, Olivieri, Philip R, Boezio, Alessandro A, Deak, Holly L, Emkey, Renee, Graceffa, Russell F, Gunaydin, Hakan, Guzman-Perez, Angel, Lee, Josie H, Teffera, Yohannes, Wang, Weiya, Youngblood, Beth D, Yu, Violeta L, Zhang, Maosheng, Gavva, Narender R, Lehto, Sonya G, Geuns-Meyer, Stephanie
Published in Journal of medicinal chemistry (24.03.2016)
Published in Journal of medicinal chemistry (24.03.2016)
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Pharmacological characterization of potent and selective NaV1.7 inhibitors engineered from Chilobrachys jingzhao tarantula venom peptide JzTx-V
Moyer, Bryan D, Murray, Justin K, Ligutti, Joseph, Andrews, Kristin, Favreau, Philippe, Jordan, John B, Lee, Josie H, Liu, Dong, Long, Jason, Sham, Kelvin, Shi, Licheng, Stöcklin, Reto, Wu, Bin, Yin, Ruoyuan, Yu, Violeta, Zou, Anruo, Biswas, Kaustav, Miranda, Les P
Published in PloS one (01.05.2018)
Published in PloS one (01.05.2018)
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Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors
DiMauro, Erin F, Altmann, Stephen, Berry, Loren M, Bregman, Howard, Chakka, Nagasree, Chu-Moyer, Margaret, Bojic, Elma Feric, Foti, Robert S, Fremeau, Robert, Gao, Hua, Gunaydin, Hakan, Guzman-Perez, Angel, Hall, Brian E, Huang, Hongbing, Jarosh, Michael, Kornecook, Thomas, Lee, Josie, Ligutti, Joseph, Liu, Dong, Moyer, Bryan D, Ortuno, Daniel, Rose, Paul E, Schenkel, Laurie B, Taborn, Kristin, Wang, Jean, Wang, Yan, Yu, Violeta, Weiss, Matthew M
Published in Journal of medicinal chemistry (08.09.2016)
Published in Journal of medicinal chemistry (08.09.2016)
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Discovery of a biarylamide series of potent, state-dependent NaV1.7 inhibitors
Schenkel, Laurie B., DiMauro, Erin F., Nguyen, Hanh N., Chakka, Nagasree, Du, Bingfan, Foti, Robert S., Guzman-Perez, Angel, Jarosh, Michael, La, Daniel S., Ligutti, Joseph, Milgram, Benjamin C., Moyer, Bryan D., Peterson, Emily A., Roberts, John, Yu, Violeta L., Weiss, Matthew M.
Published in Bioorganic & medicinal chemistry letters (15.08.2017)
Published in Bioorganic & medicinal chemistry letters (15.08.2017)
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The Discovery and Optimization of a Novel Class of Potent, Selective, and Orally Bioavailable Anaplastic Lymphoma Kinase (ALK) Inhibitors with Potential Utility for the Treatment of Cancer
Lewis, Richard T, Bode, Christiane M, Choquette, Deborah M, Potashman, Michele, Romero, Karina, Stellwagen, John C, Teffera, Yohannes, Moore, Earl, Whittington, Douglas A, Chen, Hao, Epstein, Linda F, Emkey, Renee, Andrews, Paul S, Yu, Violeta L, Saffran, Douglas C, Xu, Man, Drew, Allison, Merkel, Patricia, Szilvassy, Steven, Brake, Rachael L
Published in Journal of medicinal chemistry (26.07.2012)
Published in Journal of medicinal chemistry (26.07.2012)
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Kinetic characterization and identification of a novel inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 using a time-resolved fluorescence resonance energy transfer-based assay technology
Dao, Jennifer H., Kurzeja, Robert J.M., Morachis, Jose M., Veith, Henrike, Lewis, Jeffery, Yu, Violeta, Tegley, Christopher M., Tagari, Philip
Published in Analytical biochemistry (15.01.2009)
Published in Analytical biochemistry (15.01.2009)
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Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement
Marx, Isaac E, Dineen, Thomas A, Able, Jessica, Bode, Christiane, Bregman, Howard, Chu-Moyer, Margaret, DiMauro, Erin F, Du, Bingfan, Foti, Robert S, Fremeau, Robert T, Gao, Hua, Gunaydin, Hakan, Hall, Brian E, Huang, Liyue, Kornecook, Thomas, Kreiman, Charles R, La, Daniel S, Ligutti, Joseph, Lin, Min-Hwa Jasmine, Liu, Dong, McDermott, Jeff S, Moyer, Bryan D, Peterson, Emily A, Roberts, Jonathan T, Rose, Paul, Wang, Jean, Youngblood, Beth D, Yu, Violeta, Weiss, Matthew M
Published in ACS medicinal chemistry letters (08.12.2016)
Published in ACS medicinal chemistry letters (08.12.2016)
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Identification and inhibition of the ICE/CED-3 protease necessary for mammalian apoptosis
Nicholson, Donald W, Ali, Ambereen, Thornberry, Nancy A, Vaillancourt, John P, Ding, Connie K, Gallant, Michel, Gareau, Yves, Griffin, Patrick R, Labelle, Marc, Lazebnik, Yuri A, Munday, Neil A, Raju, Sayyaparaju M, Smulson, Mark E, Yamin, Ting-Ting, Yu, Violeta L, Miller, Douglas K
Published in Nature (London) (06.07.1995)
Published in Nature (London) (06.07.1995)
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Molecular Cloning and Pro-apoptotic Activity of ICErelII and ICErelIII, Members of the ICE/CED-3 Family of Cysteine Proteases (∗)
Munday, Neil A., Vaillancourt, John P., Ali, Ambereen, Casano, Francesca J., Miller, Douglas K., Molineaux, Susan M., Yamin, Ting-Ting, Yu, Violeta L., Nicholson, Donald W.
Published in The Journal of biological chemistry (30.06.1995)
Published in The Journal of biological chemistry (30.06.1995)
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Discovery of Aryl Aminoquinazoline Pyridones as Potent, Selective, and Orally Efficacious Inhibitors of Receptor Tyrosine Kinase c-Kit
Hu, Essa, Tasker, Andrew, White, Ryan D, Kunz, Roxanne K, Human, Jason, Chen, Ning, Bürli, Roland, Hungate, Randall, Novak, Perry, Itano, Andrea, Zhang, Xuxia, Yu, Violeta, Nguyen, Yen, Tudor, Yanyan, Plant, Matthew, Flynn, Shaun, Xu, Yang, Meagher, Kristin L, Whittington, Douglas A, Ng, Gordon Y
Published in Journal of medicinal chemistry (12.06.2008)
Published in Journal of medicinal chemistry (12.06.2008)
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KCNJ2 inhibition mitigates mechanical injury in a human brain organoid model of traumatic brain injury
Lai, Jesse D., Berlind, Joshua E., Fricklas, Gabriella, Lie, Cecilia, Urenda, Jean-Paul, Lam, Kelsey, Sta Maria, Naomi, Jacobs, Russell, Yu, Violeta, Zhao, Zhen, Ichida, Justin K.
Published in Cell stem cell (04.04.2024)
Published in Cell stem cell (04.04.2024)
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Sulfonamides as Selective Na(V)1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities
Weiss, Matthew M., Dineen, Thomas A., Marx, Isaac E., Altmann, Steven, Boezio, Alessandro, Bregman, Howard, Chu-Moyer, Margaret, DiMauro, Erin F., Bojic, Elma Feric, Foti, Robert S., Gao, Hua, Graceffa, Russell, Gunaydin, Hakan, Guzman-Perez, Angel, Huang, Hongbing, Huang, Liyue, Jarosh, Michael, Kornecook, Thomas, Kreiman, Charles R., Ligutti, Joseph, La, Daniel S., Lin, Min-Hwa Jasmine, Liu, Dong, Moyer, Bryan D., Nguyen, Hanh N., Peterson, Emily A., Rose, Paul E., Taborn, Kristin, Youngblood, Beth D., Yu, Violeta, Fremeau, Robert T.
Published in Journal of medicinal chemistry (27.07.2017)
Published in Journal of medicinal chemistry (27.07.2017)
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Journal Article
Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective Na(V)1.7 Inhibitors
DiMauro, Erin F., Altmann, Stephen, Berry, Loren M., Bregman, Howard, Chakka, Nagasree, Chu-Moyer, Margaret, Bojic, Elma Feric, Foti, Robert S., Fremeau, Robert, Gao, Hua, Gunaydin, Hakan, Guzman-Perez, Angel, Hall, Brian E., Huang, Hongbing, Jarosh, Michael, Korneook, Thomas, Lee, Josie, Ligutti, Joseph, Liu, Dong, Moyer, Bryan D., Ortuno, Daniel, Rose, Paul E., Schenkel, Laurie B., Taborn, Kristin, Wang, Jean, Wang, Yan, Yu, Violeta, Weiss, Matthew M.
Published in Journal of medicinal chemistry (08.09.2016)
Published in Journal of medicinal chemistry (08.09.2016)
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Journal Article
Discovery of pyridyl urea sulfonamide inhibitors of NaV1.7
Butler, John R., Rescourio, Gwenaella, Milgram, Benjamin C., Foti, Robert S., Kornecook, Thomas, Ligutti, Joseph, Moyer, Bryan D., Taborn, Kristin, Youngblood, Beth D., Yu, Violeta, Shimanovich, Roman, Boezio, Alessandro, Weiss, Matthew
Published in Bioorganic & medicinal chemistry letters (01.10.2022)
Published in Bioorganic & medicinal chemistry letters (01.10.2022)
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Journal Article
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity
Graceffa, Russell F, Boezio, Alessandro A, Able, Jessica, Altmann, Steven, Berry, Loren M, Boezio, Christiane, Butler, John R, Chu-Moyer, Margaret, Cooke, Melanie, DiMauro, Erin F, Dineen, Thomas A, Feric Bojic, Elma, Foti, Robert S, Fremeau, Robert T, Guzman-Perez, Angel, Gao, Hua, Gunaydin, Hakan, Huang, Hongbing, Huang, Liyue, Ilch, Christopher, Jarosh, Michael, Kornecook, Thomas, Kreiman, Charles R, La, Daniel S, Ligutti, Joseph, Milgram, Benjamin C, Lin, Min-Hwa Jasmine, Marx, Isaac E, Nguyen, Hanh N, Peterson, Emily A, Rescourio, Gwen, Roberts, John, Schenkel, Laurie, Shimanovich, Roman, Sparling, Brian A, Stellwagen, John, Taborn, Kristin, Vaida, Karina R, Wang, Jean, Yeoman, John, Yu, Violeta, Zhu, Dawn, Moyer, Bryan D, Weiss, Matthew M
Published in Journal of medicinal chemistry (27.07.2017)
Published in Journal of medicinal chemistry (27.07.2017)
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Journal Article
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities
Weiss, Matthew M, Dineen, Thomas A, Marx, Isaac E, Altmann, Steven, Boezio, Alessandro, Bregman, Howard, Chu-Moyer, Margaret, DiMauro, Erin F, Feric Bojic, Elma, Foti, Robert S, Gao, Hua, Graceffa, Russell, Gunaydin, Hakan, Guzman-Perez, Angel, Huang, Hongbing, Huang, Liyue, Jarosh, Michael, Kornecook, Thomas, Kreiman, Charles R, Ligutti, Joseph, La, Daniel S, Lin, Min-Hwa Jasmine, Liu, Dong, Moyer, Bryan D, Nguyen, Hanh N, Peterson, Emily A, Rose, Paul E, Taborn, Kristin, Youngblood, Beth D, Yu, Violeta, Fremeau, Robert T
Published in Journal of medicinal chemistry (27.07.2017)
Published in Journal of medicinal chemistry (27.07.2017)
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Journal Article
Pharmacological characterization of potent and selective Na.sub.V1.7 inhibitors engineered from Chilobrachys jingzhao tarantula venom peptide JzTx-V
Moyer, Bryan D, Murray, Justin K, Ligutti, Joseph, Andrews, Kristin, Favreau, Philippe, Jordan, John B, Lee, Josie H, Liu, Dong, Long, Jason, Sham, Kelvin, Shi, Licheng, Stöcklin, Reto, Wu, Bin, Yin, Ruoyuan, Yu, Violeta, Zou, Anruo, Biswas, Kaustav, Miranda, Les P
Published in PloS one (03.05.2018)
Published in PloS one (03.05.2018)
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1,2,4-Triazolsulfone: A novel isosteric replacement of acylsulfonamides in the context of Na(v)1.7 inhibition
Boezio, Alessandro A., Andrews, Kristin, Boezio, Christiane, Chu-Moyer, Margaret, Copeland, Katrina W., DiMauro, Erin F., Foti, Robert S., Fremeau, Robert T., Gao, Hua, Geuns-Meyer, Stephanie, Graceffa, Russell F., Gunaydin, Hakan, Huang, Hongbing, La, Daniel S., Ligutti, Joseph, Moyer, Bryan D., Peterson, Emily A., Yu, Violeta, Weiss, Matthew M.
Published in Bioorganic & medicinal chemistry letters (15.06.2018)
Published in Bioorganic & medicinal chemistry letters (15.06.2018)
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Journal Article
The discovery of benzoxazine sulfonamide inhibitors of NaV1.7: Tools that bridge efficacy and target engagement
La, Daniel S., Peterson, Emily A., Bode, Christiane, Boezio, Alessandro A., Bregman, Howard, Chu-Moyer, Margaret Y., Coats, James, DiMauro, Erin F., Dineen, Thomas A., Du, Bingfan, Gao, Hua, Graceffa, Russell, Gunaydin, Hakan, Guzman-Perez, Angel, Fremeau, Robert, Huang, Xin, Ilch, Christopher, Kornecook, Thomas J., Kreiman, Charles, Ligutti, Joseph, Jasmine Lin, Min-Hwa, McDermott, Jeff S., Marx, Isaac, Matson, David J., McDonough, Stefan I., Moyer, Bryan D., Nho Nguyen, Hanh, Taborn, Kristin, Yu, Violeta, Weiss, Matthew M.
Published in Bioorganic & medicinal chemistry letters (01.08.2017)
Published in Bioorganic & medicinal chemistry letters (01.08.2017)
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