Search Results - "Maduskuie, Thomas"

Species-Specific Metabolism of SGX523 by Aldehyde Oxidase and the Toxicological Implications by DIAMOND, Sharon, BOER, Jason, MADUSKUIE, Thomas P, FALAHATPISHEH, Nikoo, YU LI, YELESWARAM, Swamy

“…An investigation was conducted to follow up on the apparent species-dependent toxicity reported for…”
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Role of P-Glycoprotein and the Intestine in the Excretion of DPC 333 [(2R)-2-{(3R)-3-Amino-3-[4-(2-methylquinolin-4-ylmethoxy)phenyl]-2-oxopyrrolidin-1-yl}-N-hydroxy-4-methylpentanamide] in Rodents by Garner, C Edwin, Solon, Eric, Lai, Chii-Ming, Lin, Jianrong, Luo, Gang, Jones, Kevin, Duan, Jingwu, Decicco, Carl P, Maduskuie, Thomas, Mercer, Stephen E, Gan, Lian-Shen, Qian, Mingxin, Prakash, Shimoga, Shen, Huey-Shin, Lee, Frank W

“…The role of the intestine in the elimination of (2 R )-2-{(3 R )-3-amino-3-[4-(2-methylquinolin-4-ylmethoxy)phenyl]-2-oxopyrrolidin-1-yl}- N…”
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Synthesis and evaluation of succinoyl-caprolactam γ-secretase inhibitors by Thompson, Lorin A., Liauw, Ann Y., Ramanjulu, Mercy M., Kasireddy-Polam, Padmaja, Mercer, Stephen E., Maduskuie, Thomas P., Glicksman, Marcie, Roach, Arthur H., Meredith, Jere E., Liu, Rui-Qin, Combs, Andrew P., Higaki, Jeffrey N., Cordell, Barbara, Seiffert, Dietmar, Zaczek, Robert C., Robertson, David W., Olson, Richard E.

“…The synthesis, evaluation, and structure–activity relationships of a series of succinoyl lactam inhibitors of the Alzheimer’s disease γ-secretase are…”
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Rational Design and Synthesis of Novel, Potent Bis-phenylamidine Carboxylate Factor Xa Inhibitors by Maduskuie, Thomas P, McNamara, Kevin J, Ru, Yu, Knabb, Robert M, Stouten, Pieter F. W

“…The molecular modeling studies, rational design, and synthesis of a novel series of bis-phenylamidine carboxylate compounds which are inhibitors of factor Xa…”
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The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies by Stubbs, Matthew C, Burn, Timothy C, Sparks, Richard, Maduskuie, Thomas, Diamond, Sharon, Rupar, Mark, Wen, Xiaoming, Volgina, Alla, Zolotarjova, Nina, Waeltz, Paul, Favata, Margaret, Jalluri, Ravi, Liu, Huiqing, Liu, Xuesong Mike, Li, Jun, Collins, Robert, Falahatpisheh, Nikoo, Polam, Padmaja, DiMatteo, Darlise, Feldman, Patricia, Dostalik, Valerie, Thekkat, Pramod, Gardiner, Christine, He, Xin, Li, Yanlong, Covington, Maryanne, Wynn, Richard, Ruggeri, Bruce, Yeleswaram, Swamy, Xue, Chu-Biao, Yao, Wenqing, Combs, Andrew P, Huber, Reid, Hollis, Gregory, Scherle, Peggy, Liu, Phillip C C

“…Bromodomain and extraterminal domain (BET) proteins regulate the expression of many cancer-associated genes and pathways; BET inhibitors have demonstrated…”
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INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3‑Kinase Delta (PI3Kδ) by Yue, Eddy W, Li, Yun-Long, Douty, Brent, He, Chunhong, Mei, Song, Wayland, Brian, Maduskuie, Thomas, Falahatpisheh, Nikoo, Sparks, Richard B, Polam, Padmaja, Zhu, Wenyu, Glenn, Joseph, Feng, Hao, Zhang, Ke, Li, Yanlong, He, Xin, Katiyar, Kamna, Covington, Maryanne, Feldman, Patricia, Shin, Niu, Wang, Kathy He, Diamond, Sharon, Li, Yu, Koblish, Holly K, Hall, Leslie, Scherle, Peggy, Yeleswaram, Swamy, Xue, Chu-Biao, Metcalf, Brian, Combs, Andrew P, Yao, Wenqing

“…A medicinal chemistry effort focused on identifying a structurally diverse candidate for phosphoinositide 3-kinase delta (PI3Kδ) led to the discovery of…”
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Evolution of a series of peptidoleukotriene antagonists: synthesis and structure/activity relationships of 1,3,5-substituted indoles and indazoles by Matassa, Victor G, Maduskuie, Thomas P, Shapiro, Howard S, Hesp, Barrie, Snyder, David W, Aharony, David, Krell, Robert D, Keith, Richard A

“…1,3,5-Substituted indoles and indazoles have been studied as receptor antagonists of the peptidoleukotrienes. The best of these compounds generally had a…”
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Abstract 5071: Preclinical characterization of the potent and selective BET inhibitor INCB057643 in models of hematologic malignancies by Stubbs, Matthew C., Maduskuie, Thomas, Burn, Timothy, Diamond-Fosbenner, Sharon, Falahatpisheh, Nikoo, Volgina, Alla, Zolotarjova, Nina, Wen, Xiaoming, Feldman, Patricia, Rupar, Mark, Collins, Robert, Marando, Cindy, Ruggeri, Bruce, Covington, Maryanne, Liu, Xuesong Mike, Wynn, Richard, Yeleswaram, Swamy, Yao, Wenqing, Huber, Reid, Hollis, Gregory, Scherle, Peggy, Combs, Andrew P., Liu, Phillip C.

“…Inhibitors of the Bromodomain and Extra-Terminal (BET) family of bromodomain containing proteins regulate expression of key cell fate, cell cycle, and survival…”
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Acyl CoA:Cholesterol Acyltransferase (ACAT) Inhibitors: Synthesis and Structure-Activity Relationship Studies of a New Series of Trisubstituted Imidazoles by Higley, C. Anne, Wilde, Richard G, Maduskuie, Thomas P, Johnson, Alexander L, Pennev, Pennio, Billheimer, Jeffrey T, Robinson, Candy S, Gillies, Peter J, Wexler, Ruth R

“…A series of 4,5-diaryl-2-(substituted thio)-1H-imidazoles has been synthesized and demonstrated to be potent inhibitors of acyl-CoA:cholesterol acyltransferase…”
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Design, Synthesis, and Structure-Activity Relationship Studies for a New Imidazole Series of J774 Macrophage Specific Acyl-CoA:Cholesterol Acyltransferase (ACAT) Inhibitors by Maduskuie, Thomas P, Wilde, Richard G, Billheimer, Jeffrey T, Cromley, Debra A, Germain, Sandra, Gillies, Peter J, Higley, C. Anne, Johnson, Alex L, Pennev, Penio, Shimshick, Edward J, Wexler, Ruth R

“…Acyl-CoA:cholesterol acyltransferase (ACAT) is the primary enzyme involved in intracellular cholesterol esterification. Arterial wall infiltration by…”
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Abstract 3525: The BET inhibitor INCB054329 is efficacious as a single agent or in combination with targeted agents in colorectal cancer models by Liu, Xuesong, Li, Jun, He, Xin, Stubbs, Matthew, Favata, Margaret, Wen, Xiaoming, Chang, Hong, Rumberger, Beth R., Li, Yanlong, Maduskuie, Thomas, Sparks, Richard, Falahatpisheh, Nikoo, Polam, Padmaja, Combs, Andrew P., Huber, Reid, Hollis, Gregory, Scherle, Peggy, Liu, Phillip C.

“…The Bromodomain and extra-terminal (BET) family of proteins consists of BRD2, BRD3, BRD4 and BRDT. Each BET protein contains two bromodomains (BD1 and BD2)…”
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Abstract C103: The combination of PI3kδ-selective inhibition and immunomodulation shows efficacy in solid tumor models by Koblish, Holly K., Wang, Liang-Chuan, Hansbury, Michael, Zhang, Yue, Yang, Gengjie, Burn, Timothy, Waeltz, Paul, Rupar, Mark, Yue, Eddy, Douty, Brent, Maduskuie, Thomas, Falahatpisheh, Nikoo, Li, Yun-long, Combs, Andrew, Hollis, Gregory, Huber, Reid, Scherle, Peggy

“…Understanding the in vivo responses to immunoregulatory agents provides a basis for building more efficacious combination regimens. Pharmacologic inhibition of…”
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Abstract 4904: The BET inhibitor INCB054329 enhances the activity of checkpoint modulation in syngeneic tumor models by Koblish, Holly K., Hansbury, Michael, Hall, Leslie, Wang, Liang-Chuan, Zhang, Yue, Covington, Maryanne, Burn, Timothy, Rupar, Mark, Gardiner, Christine, Condamine, Thomas, Lasky, Kerri, Stubbs, Matthew C., Yue, Eddy, Sparks, Richard, Maduskuie, Thomas, Combs, Andrew P., Hollis, Gregory, Huber, Reid, Liu, Phillip CC, Scherle, Peggy

“…Inhibitors of the BET family of bromodomain proteins have been shown to be growth inhibitory across a spectrum of tumor types due to their ability to regulate…”
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Abstract 3780: Activity of the BET inhibitor INCB054329 in models of lymphoma by Stubbs, Matthew, Collins, Robert, Volgina, Alla, Liu, Mike, Favata, Margaret, Rupar, Mark, Wen, Xiaomng, Sparks, Richard, Maduskuie, Thomas, Covington, Maryanne, Burn, Timothy, Ruggeri, Bruce, Combs, Andrew P., Yao, Wenqing, Huber, Reid, Hollis, Gregory, Scherle, Peggy, Liu, Phillip CC

“…Inhibitors of the BET family of Bromodomain proteins have been shown to be growth inhibitory across a spectrum of tumor types due to their ability to regulate…”
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Abstract 692: The BET inhibitor INCB054329 is synergistic with JAK1 inhibition in models of multiple myeloma by Stubbs, Matthew C., Liu, Xuesong M., Wen, Xiaoming, Li, Jun, Dostalik, Valerie, O'Connor, Sybil, Caulder, Eian, Favata, Margaret, Rupar, Mark, Li, Yu, Rumberger, Beth, Maduskuie, Thomas, Sparks, Richard, Falahatpisheh, Nikoo, Polam, Padmaja, Vaddi, Kris, Burn, Timothy, Combs, Andrew P., Yao, Wenqing, Huber, Reid, Hollis, Gregory, Scherle, Peggy, Liu, Phillip CC

“…Bromodomain and Extra Terminal (BET) protein inhibitors have emerged as a potentially effective therapeutic option for multiple tumor types, through their…”
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Abstract 691: Activity of the BET inhibitor INCB054329 in models of multiple myeloma by Stubbs, Matthew, Wen, Xiaoming, Dostalik, Valerie, O'Connor, Sybil, Caulder, Eian, Vogina, Alla, Maduskuie, Thomas, Sparks, Richard, Huang, Taisheng, Falahatpisheh, Nikoo, Polam, Padmaja, Xue, Chu-Biao, Liu, Xuesong M., Burn, Timothy, Vaddi, Kris, Combs, Andrew P., Huber, Reid, Hollis, Gregory, Scherle, Peggy, Liu, Phillip CC

“…Multiple myeloma (MM) is a disease of plasma cell transformation. Current therapy for MM is initially effective, but nearly all tumors relapse, making new…”
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Abstract 3523: Discovery of a novel BET inhibitor INCB054329 by Liu, Phillip CC, Liu, Xuesong Mike, Stubbs, Matthew C., Maduskuie, Thomas, Sparks, Richard, Zolotarjova, Nina, Li, Jun, Wen, Xiaoming, Favata, Margaret, Feldman, Patricia, Volgina, Alla, DiMatteo, Darlise, Collins, Robert, Falahatpisheh, Nikoo, Polam, Padmaja, Li, Yu, Covington, Maryanne, Diamond-Fosbenner, Sharon, Wynn, Richard, Burn, Timothy, Vaddi, Kris, Yeleswaram, Swamy, Combs, Andrew P., Yao, Wenqing, Huber, Reid, Scherle, Peggy, Hollis, Gregory

“…Bromodomains (BD) are protein modules that bind acetylated lysine residues and are components of many epigenetic modifiers and transcription factors. The BET…”
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Abstract 2671: INCB050465, a novel PI3Kδ inhibitor, synergizes with PIM protein kinase inhibition to cause tumor regression in a model of DLBCL by Shin, Niu, Koblish, Holly, Covington, Maryanne, Li, Yanlong, Wang, Kathy, Wang, Qian, Feldman, Patricia, Hall, Leslie, O'Connor, Sybil, He, Xin, Katiyar, Kamna, Li, Yu, Yue, Eddy W., Maduskuie, Thomas P., Douty, Brent, Mei, Song, Li, Yun-Long, Xue, Chu-Biao, Combs, Andrew, Yao, Wenqing, Diamond-Fosbenner, Sharon, Yeleswaram, Swamy, Newton, Robert, Vaddi, Kris, Huber, Reid, Scherle, Peggy

“…Phosphatidylinositol 3-kinases (PI3Ks) belong to a family of lipid signaling kinases that phosphorylate phosphatidylinositol-4,5-bisphosphate (PIP2), giving…”
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Pharmacokinetics and pharmacodynamics of DPC 333 (2R)-2-((3R)-3 -amino -3{4 -[2 -methyl -4 -quinolinyl) methoxy] phenyl}-2-oxopyrrolidinyl -n -hydroxy -4 -methylpentanamide , a potent and selective inhibitor of tumor necrosis factor α-Converting enzyme in rodents, dogs, chimpanzees, and humans by MINGXIN QIAN, BAI, Stephen A, YUZHONG DENG, MADUSKUIE, Thomas, TRZASKOS, James, DUAN, James J.-W, DECICCO, Carl P, CHRIST, David D, BROGDON, Bernice, WU, Jing-Tao, LIU, Rui-Qin, COVINGTON, Maryanne B, VADDI, Kris, NEWTON, Robert C, FOSSLER, Michael J, GARNER, C. Edwin

“…DPC 333 ((2R)-2-((3R)-3-amino-3{4-[2-methyl-4-quinolinyl) methoxy] phenyl}-2-oxopyrrolidinyl)-N-hydroxy-4-methylpentanamide)) is a potent and selective…”
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Synthesis and in vitro LTD4 antagonist activity of bicyclic and monocyclic cyclopentylurethane and cyclopentylacetamide N-arylsulfonyl amides by Matassa, Victor G, Brown, Frederick J, Bernstein, Peter R, Shapiro, Howard S, Maduskuie, Thomas P, Cronk, Laura A, Vacek, Edward P, Yee, Ying K, Snyder, David W

“…The dissociation constants (KB) at the LTD4 receptor on guinea pig trachea of a series of monocyclic and bicyclic cyclopentylurethane and cyclopentylacetamide…”
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