Search Results - "Gordon, W. Perry"

Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5‑Chloro‑N2‑(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)‑N4‑(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials by Marsilje, Thomas H, Pei, Wei, Chen, Bei, Lu, Wenshuo, Uno, Tetsuo, Jin, Yunho, Jiang, Tao, Kim, Sungjoon, Li, Nanxin, Warmuth, Markus, Sarkisova, Yelena, Sun, Frank, Steffy, Auzon, Pferdekamper, AnneMarie C, Li, Allen G, Joseph, Sean B, Kim, Young, Liu, Bo, Tuntland, Tove, Cui, Xiaoming, Gray, Nathanael S, Steensma, Ruo, Wan, Yongqin, Jiang, Jiqing, Chopiuk, Greg, Li, Jie, Gordon, W. Perry, Richmond, Wendy, Johnson, Kevin, Chang, Jonathan, Groessl, Todd, He, You-Qun, Phimister, Andrew, Aycinena, Alex, Lee, Christian C, Bursulaya, Badry, Karanewsky, Donald S, Seidel, H. Martin, Harris, Jennifer L, Michellys, Pierre-Yves

“…The synthesis, preclinical profile, and in vivo efficacy in rat xenograft models of the novel and selective anaplastic lymphoma kinase inhibitor 15b (LDK378)…”
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Discovery of Trifluoromethyl(pyrimidin-2-yl)azetidine-2-carboxamides as Potent, Orally Bioavailable TGR5 (GPBAR1) Agonists: Structure–Activity Relationships, Lead Optimization, and Chronic In Vivo Efficacy by Phillips, Dean P, Gao, Wenqi, Yang, Yang, Zhang, Guobao, Lerario, Isabelle K, Lau, Thomas L, Jiang, Jiqing, Wang, Xia, Nguyen, Deborah G, Bhat, B. Ganesh, Trotter, Carol, Sullivan, Heather, Welzel, Gustav, Landry, Jannine, Chen, Yali, Joseph, Sean B, Li, Chun, Gordon, W. Perry, Richmond, Wendy, Johnson, Kevin, Bretz, Angela, Bursulaya, Badry, Pan, Shifeng, McNamara, Peter, Seidel, H. Martin

“…Activation of the G-protein coupled receptor (GPCR) Takeda G-protein receptor 5 (TGR5), also known as G-protein bile acid receptor 1 (GPBAR1), has been shown…”
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Interstrain differences of in vitro metabolic stability and impact on early drug discovery by Richmond, Wendy, Wogan, Megan, Isbell, John, Gordon, W Perry

“…With the extensive use of different strains of mice and rats in in vivo efficacy models, lack of relevant metabolic clearance data among strains has been a…”
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Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6‑Azaindole Derivative GNF2133 by Liu, Yahu A, Jin, Qihui, Zou, Yefen, Ding, Qiang, Yan, Shanshan, Wang, Zhicheng, Hao, Xueshi, Nguyen, Bao, Zhang, Xiaoyue, Pan, Jianfeng, Mo, Tingting, Jacobsen, Kate, Lam, Thanh, Wu, Tom Y.-H, Petrassi, H. Michael, Bursulaya, Badry, DiDonato, Michael, Gordon, W. Perry, Liu, Bo, Baaten, Janine, Hill, Robert, Nguyen-Tran, Vân, Qiu, Minhua, Zhang, You-Qing, Kamireddy, Anwesh, Espinola, Sheryll, Deaton, Lisa, Ha, Sukwon, Harb, George, Jia, Yong, Li, Jing, Shen, Weijun, Schumacher, Andrew M, Colman, Karyn, Glynne, Richard, Pan, Shifeng, McNamara, Peter, Laffitte, Bryan, Meeusen, Shelly, Molteni, Valentina, Loren, Jon

“…Autoimmune deficiency and destruction in either β-cell mass or function can cause insufficient insulin levels and, as a result, hyperglycemia and diabetes…”
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TrkB inhibition by GNF-4256 slows growth and enhances chemotherapeutic efficacy in neuroblastoma xenografts by Croucher, Jamie L., Iyer, Radhika, Li, Nanxin, Molteni, Valentina, Loren, Jon, Gordon, W. Perry, Tuntland, Tove, Liu, Bo, Brodeur, Garrett M.

“…Purpose Neuroblastoma (NB) is one of the most common and deadly pediatric solid tumors. NB is characterized by clinical heterogeneity, from spontaneous…”
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Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5-Chloro- N 2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)- N 4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials by Marsilje, Thomas H., Pei, Wei, Chen, Bei, Lu, Wenshuo, Uno, Tetsuo, Jin, Yunho, Jiang, Tao, Kim, Sungjoon, Li, Nanxin, Warmuth, Markus, Sarkisova, Yelena, Sun, Frank, Steffy, Auzon, Pferdekamper, AnneMarie C., Li, Allen G., Joseph, Sean B., Kim, Young, Liu, Bo, Tuntland, Tove, Cui, Xiaoming, Gray, Nathanael S., Steensma, Ruo, Wan, Yongqin, Jiang, Jiqing, Chopiuk, Greg, Li, Jie, Gordon, W. Perry, Richmond, Wendy, Johnson, Kevin, Chang, Jonathan, Groessl, Todd, He, You-Qun, Phimister, Andrew, Aycinena, Alex, Lee, Christian C., Bursulaya, Badry, Karanewsky, Donald S., Seidel, H. Martin, Harris, Jennifer L., Michellys, Pierre-Yves

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Investigations of mechanisms of reactive metabolite formation from (R)-(+)-pulegone by Nelson, S D, McClanahan, R H, Thomassen, D, Gordon, W P, Knebel, N

“…1. (R)-(+)-Pulegone is a monoterpene that is oxidized by cytochromes P-450 to reactive metabolites that initiate events in the pathogenesis of hepatotoxicity…”
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The genotoxicity of 2-bromoacrolein and 2,3-dibromopropanal by Gordon, W P, Søderlund, E J, Holme, J A, Nelson, S D, Iyer, L, Rivedal, E, Dybing, E

“…2-Bromoacrolein (2-BA) and 2,3-dibromopropanal (2,3-DBPA), an identified and a postulated reactive metabolite of tris(2,3-dibromopropyl)phosphate (Tris-BP),…”
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Studies on the mechanism of acetamide hepatocarcinogenicity by Dybing, E, Søderlund, E J, Gordon, W P, Holme, J A, Christensen, T, Becher, G, Rivedal, E, Thorgeirsson, S S

“…The hepatocarcinogen acetamide, in single doses of 100 and 400 mg/kg b.wt., was shown to act as an initiator in a dose-dependent fashion in rat liver using the…”
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Hepatotoxicity and pulmonary toxicity of pennyroyal oil and its constituent terpenes in the mouse by Gordon, W P, Forte, A J, McMurtry, R J, Gal, J, Nelson, S D

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Disposition of 8-methyl-8-azabicyclo[3,2,1]octan-3-yl 3,5-dichlorobenzoate, a potent 5-hydroxytryptamine antagonist, and two metabolites in dogs and monkeys by Cheng, H, Larsen, D L, Ragner, J A, Sproles, G D, Gordon, W P

“…The disposition of 8-methyl-8-azabicyclo[3,2,1]octan-3-yl 3,5-dichlorobenzoate (MDL 72,222; 1), a potent 5-hydroxytryptamine antagonist, and its N-demethylated…”
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Identification of urinary metabolites of 8-methyl-8-azabicyclo-[3,2,1] octan-3-yl 3,5-dichlorobenzoate (MDL 72,222) in the dog and monkey by Gordon, W P, Cheng, H, Larsen, D L, Ragner, J A, Landmesser, N G

“…The metabolism of 8-methyl-8-azabicyclo- 3,2,1]octan-3-yl 3,5-dichlorobenzoate (MDL 72,222) was studied in the dog and monkey. Four urinary metabolites were…”
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Metabolism in vitro of tris(2,3-dibromopropyl)-phosphate: oxidative debromination and bis(2,3-dibromopropyl)phosphate formation as correlates of mutagenicity and covalent protein binding by Søderlund, E J, Gordon, W P, Nelson, S D, Omichinski, J G, Dybing, E

“…Tris(2,3-dibromopropyl)phosphate (Tris-BP) was found to be metabolized by liver microsomes obtained from untreated and phenobarbital-pretreated rats…”
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Activation mechanism of tris(2,3-dibromopropyl)phosphate to the potent mutagen, 2-bromoacrolein by Nelson, S D, Omichinski, J G, Iyer, L, Gordon, W P, Soderlund, E J, Dybing, E

“…The potent mutagen 2- bromoacrolein is formed from the carcinogenic flame retardant tris(2,3-dibromopropyl)phosphate (Tris-BP) on incubation with hepatic…”
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Preparation of (+)- and (-)-2,3-dibromo-1-propanol by Huitric, Alain C, Gordon, W. Perry, Nelson, Sidney D

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Metabolism of 2-(2-thienyl)allylamine hydrochloride in the rat: identification of a novel metabolite by Gordon, W P, McCarthy, J R, Chang, S Y

“…A novel metabolite, 2-(2-thienyl)propionic acid, is formed in vivo from 2-(2-thienyl)allylamine hydrochloride. Mass spectral analysis suggested…”
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Mammalian Drug Metabolism by Nelson, Sidney D, Gordon, W. Perry

“…Drugs and other chemicals that do not occur in mammalian systems are metabolized by a wide variety of enzymes. Reactions catalyzed by these enzymes have been…”
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Carcinogenicity of deuterium-labeled 1,2-dimethylhydrazine in mice by TURUSOV, V. S, LANKO, N. S, PARFENOV, Y. D, GORDON, W. P, NELSON, S. D, HILLERY, P. S, KEEFER, L. K

“…To study the effect of deuterium substitution on the carcinogenicity of 1,2-dimethylhydrazine (DMH) in mice, two comparisons were made between DMH and its…”
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Procarbazine spermatogenesis toxicity: deuterium isotope effects point to regioselective metabolism in mice by Yost, G S, Horstman, M G, el Walily, A F, Gordon, W P, Nelson, S D

“…Procarbazine was shown to decrease spermatogenesis in male mice in a dose-dependent manner. Significant decreases (44% of controls) in spermatogenesis were…”
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Variability in the determination of fraction metabolized in a triangular metabolic problem and its resolution with stable isotope methodology by Lin, H, Levy, R H, Lane, E A, Gordon, W P

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