Search Results - "Hosea, Natilie"

Prediction of Human Pharmacokinetics From Preclinical Information: Comparative Accuracy of Quantitative Prediction Approaches by Hosea, Natilie A., Collard, Wendy T., Cole, Susan, Maurer, Tristan S., Fang, Rick X., Jones, Hannah, Kakar, Shefali M., Nakai, Yasuhiro, Smith, Bill J., Webster, Rob, Beaumont, Kevin

“…Quantitative prediction of human pharmacokinetics is critical in assessing the viability of drug candidates and in determining first‐in‐human dosing. Numerous…”
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THE IMPACT OF P-GLYCOPROTEIN ON THE DISPOSITION OF DRUGS TARGETED FOR INDICATIONS OF THE CENTRAL NERVOUS SYSTEM: EVALUATION USING THE MDR1A/1B KNOCKOUT MOUSE MODEL by Doran, Angela, Obach, R Scott, Smith, Bill J, Hosea, Natilie A, Becker, Stacey, Callegari, Ernesto, Chen, Cuiping, Chen, Xi, Choo, Edna, Cianfrogna, Julie, Cox, Loretta M, Gibbs, John P, Gibbs, Megan A, Hatch, Heather, Hop, Cornelis E C A, Kasman, Ilana N, Laperle, Jennifer, Liu, Jianhua, Liu, Xingrong, Logman, Michael, Maclin, Debra, Nedza, Frank M, Nelson, Frederick, Olson, Emily, Rahematpura, Sandhya, Raunig, David, Rogers, Sabrinia, Schmidt, Kari, Spracklin, Douglas K, Szewc, Mark, Troutman, Matthew, Tseng, Elaine, Tu, Meihua, Van Deusen, Jeffrey W, Venkatakrishnan, Karthik, Walens, Gary, Wang, Ellen Q, Wong, Diane, Yasgar, Adam S, Zhang, Chenghong

“…Thirty-two structurally diverse drugs used for the treatment of various conditions of the central nervous system (CNS), along with two active metabolites, and…”
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Simulation of Human Intravenous and Oral Pharmacokinetics of 21 Diverse Compounds Using Physiologically Based Pharmacokinetic Modelling by Jones, Hannah M., Gardner, Iain B., Collard, Wendy T., Stanley, PhilJ, Oxley, Penny, Hosea, Natilie A., Plowchalk, David, Gernhardt, Steve, Lin, Jing, Dickins, Maurice, Rahavendran, S. Ravi, Jones, Barry C., Watson, Kenny J., Pertinez, Henry, Kumar, Vikas, Cole, Susan

“…Background: The importance of predicting human pharmacokinetics during compound selection has been recognized in the pharmaceutical industry. To this end there…”
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Drug design tools--in silico, in vitro and in vivo ADME/PK prediction and interpretation: is PK in monkey an essential part of a good human PK prediction? by Hosea, Natilie A

“…Quantitative human pharmacokinetic (PK) predictions play a critical role in assessing the quality of potential drug candidates and in selecting a human…”
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Discovery of Aryloxy Tetramethylcyclobutanes as Novel Androgen Receptor Antagonists by Guo, Chuangxing, Linton, Angelica, Kephart, Susan, Ornelas, Martha, Pairish, Mason, Gonzalez, Javier, Greasley, Samantha, Nagata, Asako, Burke, Benjamin J, Edwards, Martin, Hosea, Natilie, Kang, Ping, Hu, Wenyue, Engebretsen, Jon, Briere, David, Shi, Manli, Gukasyan, Hovik, Richardson, Paul, Dack, Kevin, Underwood, Toby, Johnson, Patrick, Morell, Andrew, Felstead, Robert, Kuruma, Hidetoshi, Matsimoto, Hiroaki, Zoubeidi, Amina, Gleave, Martin, Los, Gerrit, Fanjul, Andrea N

“…An aryloxy tetramethylcyclobutane was identified as a novel template for androgen receptor (AR) antagonists via cell-based high-throughput screening. Follow-up…”
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Evaluation of Cerebrospinal Fluid Concentration and Plasma Free Concentration As a Surrogate Measurement for Brain Free Concentration by XINGRONG LIU, SMITH, Bill J, HOSEA, Natilie, JIANHUA LIU, NELSON, Frederick R, SZEWC, Mark A, VAN DEUSEN, Jeffrey, CUIPING CHEN, CALLEGARI, Ernesto, BECKER, Stacey L, XI CHEN, CIANFROGNA, Julie, DORAN, Angela C, DORAN, Shawn D, GIBBS, John P

“…This study was designed to evaluate the use of cerebrospinal fluid (CSF) drug concentration and plasma unbound concentration ( C u,plasma ) to predict brain…”
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Elucidation of Distinct Ligand Binding Sites for Cytochrome P450 3A4 by Hosea, Natilie A, Miller, Grover P, Guengerich, F. Peter

“…Cytochrome P450 (P450) 3A4 is the most abundant human P450 enzyme and has broad selectivity for substrates. The enzyme can show marked catalytic…”
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Use of a physiologically based pharmacokinetic model to study the time to reach brain equilibrium: an experimental analysis of the role of blood-brain barrier permeability, plasma protein binding, and brain tissue binding by Liu, Xingrong, Smith, Bill J, Chen, Cuiping, Callegari, Ernesto, Becker, Stacey L, Chen, Xi, Cianfrogna, Julie, Doran, Angela C, Doran, Shawn D, Gibbs, John P, Hosea, Natilie, Liu, Jianhua, Nelson, Frederick R, Szewc, Mark A, Van Deusen, Jeffery

“…This study was designed 1) to examine the effects of blood-brain barrier (BBB) permeability [quantified as permeability-surface area product (PS)], unbound…”
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Intermittent Oral Coadministration of a Gamma Secretase Inhibitor with Dexamethasone Mitigates Intestinal Goblet Cell Hyperplasia in Rats by Aguirre, Shirley A., Liu, Ling, Hosea, Natilie A., Scott, Wesley, May, Jeffrey R., Burns-Naas, Leigh Ann, Randolph, Sophia, Denlinger, Robert H., Han, Bora

“…Dexamethasone was given in 2 oral dosing regimens with repeat dose oral administration of the gamma secretase inhibitor (GSI), PF-03084014, in Sprague-Dawley…”
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N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275 by Siu, Michael, Johnson, Theodore O., Wang, Yong, Nair, Sajiv K., Taylor, Wendy D., Cripps, Stephan J., Matthews, Jean J., Edwards, Martin P., Pauly, Thomas A., Ermolieff, Jacques, Castro, Arturo, Hosea, Natilie A., LaPaglia, Amy, Fanjul, Andrea N., Vogel, Jennifer E.

“…N-(Pyridin-2-yl) arylsulfonamides are identified as inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1), an enzyme that catalyzes the reduction of…”
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Discovery of 3-aryloxy-lactam analogs as potent androgen receptor full antagonists for treating castration resistant prostate cancer by Guo, Chuangxing, Kephart, Susan, Ornelas, Martha, Gonzalez, Javier, Linton, Angelica, Pairish, Mason, Nagata, Asako, Greasley, Samantha, Elleraas, Jeff, Hosea, Natilie, Engebretsen, Jon, Fanjul, Andrea N.

“…A series of novel, non-steroidal AR antagonists were discovered through HTS. ADME profile was also improved by designing more ligand-efficient molecules. High…”
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Dose-dependent effects of small-molecule antagonists on the genomic landscape of androgen receptor binding by Zhu, Zhou, Shi, Manli, Hu, Wenyue, Estrella, Heather, Engebretsen, Jon, Nichols, Tim, Briere, David, Hosea, Natilie, Los, Gerrit, Rejto, Paul A, Fanjul, Andrea

“…The androgen receptor plays a critical role throughout the progression of prostate cancer and is an important drug target for this disease. While chromatin…”
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N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: Strategies to eliminate reactive metabolites by Nair, Sajiv K., Matthews, Jean J., Cripps, Stephan J., Cheng, Hengmiao, Hoffman, Jacqui E., Smith, Christopher, Kupchinsky, Stanley, Siu, Michael, Taylor, Wendy D., Wang, Yong, Johnson, Theodore O., Dress, Klaus R., Edwards, Martin P., Zhou, Sue, Hosea, Natilie A., LaPaglia, Amy, Kang, Ping, Castro, Arturo, Ermolieff, Jacques, Fanjul, Andrea, Vogel, Jennifer E., Rejto, Paul, Dalvie, Deepak

“…N-(Pyridin-2-yl) arylsulfonamides 1 and 2 (PF-915275) were identified as potent inhibitors of 11β-hydroxysteroid dehydrogenase type 1. A screen for…”
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Factors affecting the clinical development of cytochrome P450 3A substrates by GIBBS, Megan A, HOSEA, Natilie A

“…The objective of this review is to evaluate the risks associated with the discovery and development of cytochrome p450 (CYP) 3A substrates. CYP3A is the most…”
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Specificity and Orientation of Trigonal Carboxyl Esters and Tetrahedral Alkylphosphonyl Esters in Cholinesterases by Hosea, Natilie A, Berman, Harvey A, Taylor, Palmer

“…We have examined the specificity of planar carboxyl and tetrahedral phosphonyl esters for mouse cholinesterases and have delineated the orientation of these…”
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Abstract 3220: Application of GastroPlus™ modeling and simulation for predicting mouse and human pharmacokinetic profiles in oncology research and development by Hosea, Natilie

“…Abstract Pharmacokinetic modeling plays an integral role in the drug discovery and development process. In particular, modeling and simulation has broad…”
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Aspartate 74 as a Primary Determinant in Acetylcholinesterase Governing Specificity to Cationic Organophosphonates by Hosea, Natilie A, Radić, Zoran, Tsigelny, Igor, Berman, Harvey Alan, Quinn, Daniel M, Taylor, Palmer

“…Through site-specific mutagenesis, we examined the determinants on acetylcholinesterase which govern the specificity and reactivity of three classes of…”
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Structural bases for the specificity of cholinesterase catalysis and inhibition by Taylor, Palmer, Radic, Zoran, Hosea, Natilie A., Camp, Shelley, Marchot, Pascale, Berman, Harvey A.

“…The availability of a crystal structure and comparative sequences of the cholinesterases has provided templates suitable for analyzing the molecular bases of…”
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Evaluation of selective gamma-secretase inhibitor PF-03084014 for its antitumor efficacy and gastrointestinal safety to guide optimal clinical trial design by Wei, Ping, Walls, Marlena, Qiu, Ming, Ding, Richard, Denlinger, Robert H, Wong, Anthony, Tsaparikos, Kosta, Jani, Jitesh P, Hosea, Natilie, Sands, Michelle, Randolph, Sophia, Smeal, Tod

“…Aberrant regulation of Notch signaling has been implicated in tumorigenesis. Proteolytic release of the Notch intracellular domain (NICD) by gamma-secretase…”
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Inactivation studies of acetylcholinesterase with phenylmethylsulfonyl fluoride by Kraut, D, Goff, H, Pai, R K, Hosea, N A, Silman, I, Sussman, J L, Taylor, P, Voet, J G

“…Acetylcholinesterase (AChE), a serine hydrolase, is potentially susceptible to inactivation by phenylmethylsulfonyl fluoride (PMSF) and benzenesulfonyl…”
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