Search Results - "McGee, Lawrence R."

PI3Kδ and PI3Kγ as Targets for Autoimmune and Inflammatory Diseases by Cushing, Timothy D, Metz, Daniela P, Whittington, Douglas A, McGee, Lawrence R

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Discovery of AMG 232, a Potent, Selective, and Orally Bioavailable MDM2–p53 Inhibitor in Clinical Development by Sun, Daqing, Li, Zhihong, Rew, Yosup, Gribble, Michael, Bartberger, Michael D, Beck, Hilary P, Canon, Jude, Chen, Ada, Chen, Xiaoqi, Chow, David, Deignan, Jeffrey, Duquette, Jason, Eksterowicz, John, Fisher, Benjamin, Fox, Brian M, Fu, Jiasheng, Gonzalez, Ana Z, Gonzalez-Lopez De Turiso, Felix, Houze, Jonathan B, Huang, Xin, Jiang, Min, Jin, Lixia, Kayser, Frank, Liu, Jiwen (Jim), Lo, Mei-Chu, Long, Alexander M, Lucas, Brian, McGee, Lawrence R, McIntosh, Joel, Mihalic, Jeff, Oliner, Jonathan D, Osgood, Tao, Peterson, Matthew L, Roveto, Philip, Saiki, Anne Y, Shaffer, Paul, Toteva, Maria, Wang, Yingcai, Wang, Yu Chung, Wortman, Sarah, Yakowec, Peter, Yan, Xuelei, Ye, Qiuping, Yu, Dongyin, Yu, Ming, Zhao, Xiaoning, Zhou, Jing, Zhu, Jiang, Olson, Steven H, Medina, Julio C

“…We recently reported the discovery of AM-8553 (1), a potent and selective piperidinone inhibitor of the MDM2–p53 interaction. Continued research investigation…”
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Practical Total Synthesis of the Anti-Influenza Drug GS-4104 by Rohloff, John C, Kent, Kenneth M, Postich, Michael J, Becker, Mark W, Chapman, Harlan H, Kelly, Daphne E, Lew, Willard, Louie, Michael S, McGee, Lawrence R, Prisbe, Ernest J, Schultze, Lisa M, Yu, Richard H, Zhang, Lijun

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Novel series of tunable µOR modulators with enhanced brain penetration for the treatment of opioid use disorder, pain and neuropsychiatric indications by Nerurkar, Alok, Nguyen, Thomas, Wang, Sheldon, Bhatt, Ulhas, Li, Kevin, Li, Yihong, Ding, Pingyu, Seidl, Frederick J., Holan, Martin, Lee, John, Widjaja, Tien, Wei, Zhi-Liang, Sadlowski, Corinne, Sperandio, David, McGee, Lawrence R., Youngblood, Beth, Schwartz, Neil, Gehlert, Donald, Medina, Julio C.

“…Structural optimization of a previously reported agonist of µOR, PZM21 is described resulting in the discovery of a novel series of amides with at least…”
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Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101) by Rew, Yosup, Du, Xiaohui, Eksterowicz, John, Zhou, Haiying, Jahchan, Nadine, Zhu, Liusheng, Yan, Xuelei, Kawai, Hiroyuki, McGee, Lawrence R, Medina, Julio C, Huang, Tom, Chen, Chelsea, Zavorotinskaya, Tatiana, Sutimantanapi, Dena, Waszczuk, Joanna, Jackson, Erica, Huang, Elizabeth, Ye, Qiuping, Fantin, Valeria R, Sun, Daqing

“…The glucocorticoid receptor (GR) has been linked to therapy resistance across a wide range of cancer types. Preclinical data suggest that antagonists of this…”
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AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia by Li, Cong, Liu, Liqin, Liang, Lingming, Xia, Zhen, Li, Zhihong, Wang, Xianghong, McGee, Lawrence R, Newhall, Katie, Sinclair, Angus, Kamb, Alexander, Wickramasinghe, Dineli, Dai, Kang

“…Resistance to FLT3 inhibitors is a serious clinical issue in treating acute myelogenous leukemia (AML). AMG 925, a dual FLT3/CDK4 inhibitor, has been developed…”
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Discovery and in Vivo Evaluation of (S)‑N‑(1-(7-Fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)‑9H‑purin-6-amine (AMG319) and Related PI3Kδ Inhibitors for Inflammation and Autoimmune Disease by Cushing, Timothy D., Hao, Xiaolin, Shin, Youngsook, Andrews, Kristin, Brown, Matthew, Cardozo, Mario, Chen, Yi, Duquette, Jason, Fisher, Ben, Gonzalez-Lopez de Turiso, Felix, He, Xiao, Henne, Kirk R., Hu, Yi-Ling, Hungate, Randall, Johnson, Michael G., Kelly, Ron C., Lucas, Brian, McCarter, John D., McGee, Lawrence R., Medina, Julio C., San Miguel, Tisha, Mohn, Deanna, Pattaropong, Vatee, Pettus, Liping H., Reichelt, Andreas, Rzasa, Robert M., Seganish, Jennifer, Tasker, Andrew S., Wahl, Robert C., Wannberg, Sharon, Whittington, Douglas A., Whoriskey, John, Yu, Gang, Zalameda, Leeanne, Zhang, Dawei, Metz, Daniela P.

“…The development and optimization of a series of quinolinylpurines as potent and selective PI3Kδ kinase inhibitors with excellent physicochemical properties are…”
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An Expeditious Synthesis of the MDM2–p53 Inhibitor AM-8553 by Lucas, Brian S, Fisher, Benjamin, McGee, Lawrence R, Olson, Steven H, Medina, Julio C, Cheung, Eugene

“…The development of the structurally complex MDM2/p53 inhibitor AM-8553 was impeded by the low yield of the initial synthesis. A second generation synthesis is…”
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Selective and Potent Morpholinone Inhibitors of the MDM2–p53 Protein–Protein Interaction by Gonzalez, Ana Z, Eksterowicz, John, Bartberger, Michael D, Beck, Hilary P, Canon, Jude, Chen, Ada, Chow, David, Duquette, Jason, Fox, Brian M, Fu, Jiasheng, Huang, Xin, Houze, Jonathan B, Jin, Lixia, Li, Yihong, Li, Zhihong, Ling, Yun, Lo, Mei-Chu, Long, Alexander M, McGee, Lawrence R, McIntosh, Joel, McMinn, Dustin L, Oliner, Jonathan D, Osgood, Tao, Rew, Yosup, Saiki, Anne Y, Shaffer, Paul, Wortman, Sarah, Yakowec, Peter, Yan, Xuelei, Ye, Qiuping, Yu, Dongyin, Zhao, Xiaoning, Zhou, Jing, Olson, Steven H, Medina, Julio C, Sun, Daqing

“…We previously reported the discovery of AMG 232, a highly potent and selective piperidinone inhibitor of the MDM2–p53 interaction. Our continued search for…”
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Novel inhibitors are cytotoxic for myeloma cells with NFkB inducing kinase-dependent activation of NFkB by Demchenko, Yulia N, Brents, Leslie A, Li, Zhihong, Bergsagel, Leif P, McGee, Lawrence R, Kuehl, Michael W

“…NFkB activity is critical for survival and proliferation of normal lymphoid cells and many kinds of B-cell tumors, including multiple myeloma (MM). NFkB…”
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Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors by Shin, Youngsook, Suchomel, Julia, Cardozo, Mario, Duquette, Jason, He, Xiao, Henne, Kirk, Hu, Yi-Ling, Kelly, Ron C, McCarter, John, McGee, Lawrence R, Medina, Julio C, Metz, Daniela, San Miguel, Tisha, Mohn, Deanna, Tran, Thuy, Vissinga, Christine, Wong, Simon, Wannberg, Sharon, Whittington, Douglas A, Whoriskey, John, Yu, Gang, Zalameda, Leeanne, Zhang, Xuxia, Cushing, Timothy D

“…Lead optimization efforts resulted in the discovery of two potent, selective, and orally bioavailable PI3Kδ inhibitors, 1 (AM-8508) and 2 (AM-9635), with good…”
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Discovery of AM-7209, a Potent and Selective 4‑Amidobenzoic Acid Inhibitor of the MDM2–p53 Interaction by Rew, Yosup, Sun, Daqing, Yan, Xuelei, Beck, Hilary P, Canon, Jude, Chen, Ada, Duquette, Jason, Eksterowicz, John, Fox, Brian M, Fu, Jiasheng, Gonzalez, Ana Z, Houze, Jonathan, Huang, Xin, Jiang, Min, Jin, Lixia, Li, Yihong, Li, Zhihong, Ling, Yun, Lo, Mei-Chu, Long, Alexander M, McGee, Lawrence R, McIntosh, Joel, Oliner, Jonathan D, Osgood, Tao, Saiki, Anne Y, Shaffer, Paul, Wang, Yu Chung, Wortman, Sarah, Yakowec, Peter, Ye, Qiuping, Yu, Dongyin, Zhao, Xiaoning, Zhou, Jing, Medina, Julio C, Olson, Steven H

“…Structure-based rational design and extensive structure–activity relationship studies led to the discovery of AMG 232 (1), a potent piperidinone inhibitor of…”
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Discovery of AMG 925, a FLT3 and CDK4 Dual Kinase Inhibitor with Preferential Affinity for the Activated State of FLT3 by Li, Zhihong, Wang, Xianghong, Eksterowicz, John, Gribble, Michael W, Alba, Grace Q, Ayres, Merrill, Carlson, Timothy J, Chen, Ada, Chen, Xiaoqi, Cho, Robert, Connors, Richard V, DeGraffenreid, Michael, Deignan, Jeffrey T, Duquette, Jason, Fan, Pingchen, Fisher, Benjamin, Fu, Jiasheng, Huard, Justin N, Kaizerman, Jacob, Keegan, Kathleen S, Li, Cong, Li, Kexue, Li, Yunxiao, Liang, Lingming, Liu, Wen, Lively, Sarah E, Lo, Mei-Chu, Ma, Ji, McMinn, Dustin L, Mihalic, Jeffrey T, Modi, Kriti, Ngo, Rachel, Pattabiraman, Kanaka, Piper, Derek E, Queva, Christophe, Ragains, Mark L, Suchomel, Julia, Thibault, Steve, Walker, Nigel, Wang, Xiaodong, Wang, Zhulun, Wanska, Malgorzata, Wehn, Paul M, Weidner, Margaret F, Zhang, Alex J, Zhao, Xiaoning, Kamb, Alexander, Wickramasinghe, Dineli, Dai, Kang, McGee, Lawrence R, Medina, Julio C

“…We describe the structural optimization of a lead compound 1 that exhibits dual inhibitory activities against FLT3 and CDK4. A series of…”
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INT131: A Selective Modulator of PPARγ by Motani, Alykhan, Wang, Zhulun, Weiszmann, Jennifer, McGee, Lawrence R., Lee, Gary, Liu, Qingxiang, Staunton, Jocelyn, Fang, Zexu, Fuentes, Helen, Lindstrom, Michelle, Liu, Jinsong, Biermann, Donna H.T., Jaen, Juan, Walker, Nigel P.C., Learned, R. Marc, Chen, Jin-Long, Li, Yang

“…The nuclear hormone receptor peroxisome proliferator-activated receptor γ (PPARγ; NR1C3) plays a central role in adipogenesis and is the molecular target of…”
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Novel Inhibitors of the MDM2-p53 Interaction Featuring Hydrogen Bond Acceptors as Carboxylic Acid Isosteres by Gonzalez, Ana Z, Li, Zhihong, Beck, Hilary P, Canon, Jude, Chen, Ada, Chow, David, Duquette, Jason, Eksterowicz, John, Fox, Brian M, Fu, Jiasheng, Huang, Xin, Houze, Jonathan, Jin, Lixia, Li, Yihong, Ling, Yun, Lo, Mei-Chu, Long, Alexander M, McGee, Lawrence R, McIntosh, Joel, Oliner, Jonathan D, Osgood, Tao, Rew, Yosup, Saiki, Anne Y, Shaffer, Paul, Wortman, Sarah, Yakowec, Peter, Yan, Xuelei, Ye, Qiuping, Yu, Dongyin, Zhao, Xiaoning, Zhou, Jing, Olson, Steven H, Sun, Daqing, Medina, Julio C

“…We previously reported the discovery of potent and selective morpholinone and piperidinone inhibitors of the MDM2-p53 interaction. These inhibitors have in…”
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Inhibiting NF-κB-inducing kinase (NIK): Discovery, structure-based design, synthesis, structure–activity relationship, and co-crystal structures by Li, Kexue, McGee, Lawrence R., Fisher, Ben, Sudom, Athena, Liu, Jinsong, Rubenstein, Steven M., Anwer, Mohmed K., Cushing, Timothy D., Shin, Youngsook, Ayres, Merrill, Lee, Fei, Eksterowicz, John, Faulder, Paul, Waszkowycz, Bohdan, Plotnikova, Olga, Farrelly, Ellyn, Xiao, Shou-Hua, Chen, Guoqing, Wang, Zhulun

“…The discovery, structure-based design, synthesis, and optimization of NIK inhibitors are described. Our work began with an HTS hit, imidazopyridinyl…”
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Preclinical evaluation of AMG 925, a FLT3/CDK4 dual kinase inhibitor for treating acute myeloid leukemia by Keegan, Kathleen, Li, Cong, Li, Zhihong, Ma, Ji, Ragains, Mark, Coberly, Suzanne, Hollenback, David, Eksterowicz, John, Liang, Lingming, Weidner, Margaret, Huard, Justin, Wang, Xianghong, Alba, Grace, Orf, Jessica, Lo, Mei-Chu, Zhao, Sharon, Ngo, Rachel, Chen, Ada, Liu, Lily, Carlson, Timothy, Quéva, Christophe, McGee, Lawrence R, Medina, Julio, Kamb, Alexander, Wickramasinghe, Dineli, Dai, Kang

“…Acute myeloid leukemia (AML) remains a serious unmet medical need. Despite high remission rates with chemotherapy standard-of-care treatment, the disease…”
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Synthesis and SAR study of potent and selective PI3Kδ inhibitors by Bui, Minna, Hao, Xiaolin, Shin, Youngsook, Cardozo, Mario, He, Xiao, Henne, Kirk, Suchomel, Julia, McCarter, John, McGee, Lawrence R., San Miguel, Tisha, Medina, Julio C., Mohn, Deanna, Tran, Thuy, Wannberg, Sharon, Wong, Jamie, Wong, Simon, Zalameda, Leeanne, Metz, Daniela, Cushing, Timothy D.

“…[Display omitted] 2,3,4-Substituted quinolines such as (10a) were found to be potent inhibitors of PI3Kδ in both biochemical and cellular assays with good…”
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Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2‑((1S)‑1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro‑N‑methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2‑((1S)‑1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro‑N‑methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-1430) by Gonzalez-Lopez de Turiso, Felix, Hao, Xiaolin, Shin, Youngsook, Bui, Minna, Campuzano, Iain D. G, Cardozo, Mario, Dunn, Michelle C, Duquette, Jason, Fisher, Benjamin, Foti, Robert S, Henne, Kirk, He, Xiao, Hu, Yi-Ling, Kelly, Ron C, Johnson, Michael G, Lucas, Brian S, McCarter, John, McGee, Lawrence R, Medina, Julio C, Metz, Daniela, San Miguel, Tisha, Mohn, Deanna, Tran, Thuy, Vissinga, Christine, Wannberg, Sharon, Whittington, Douglas A, Whoriskey, John, Yu, Gang, Zalameda, Leeanne, Zhang, Xuxia, Cushing, Timothy D

“…Optimization of the potency and pharmacokinetic profile of 2,3,4-trisubstituted quinoline, 4, led to the discovery of two potent, selective, and orally…”
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Discovery and in Vivo Evaluation of Dual PI3Kβ/δ Inhibitors by Gonzalez-Lopez de Turiso, Felix, Shin, Youngsook, Brown, Matthew, Cardozo, Mario, Chen, Yi, Fong, David, Hao, Xiaolin, He, Xiao, Henne, Kirk, Hu, Yi-Ling, Johnson, Michael G, Kohn, Todd, Lohman, Julia, McBride, Helen J, McGee, Lawrence R, Medina, Julio C, Metz, Daniela, Miner, Kent, Mohn, Deanna, Pattaropong, Vatee, Seganish, Jennifer, Simard, Jillian L, Wannberg, Sharon, Whittington, Douglas A, Yu, Gang, Cushing, Timothy D

“…Structure-based rational design led to the synthesis of a novel series of potent PI3K inhibitors. The optimized pyrrolopyridine analogue 63 was a potent and…”
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