Search Results - "FAN, Peter W"

Characterization of Differential Tissue Abundance of Major Non-CYP Enzymes in Human by Basit, Abdul, Neradugomma, Naveen K, Wolford, Christopher, Fan, Peter W, Murray, Bernard, Takahashi, Ryan H, Khojasteh, S. Cyrus, Smith, Bill J, Heyward, Scott, Totah, Rheem A, Kelly, Edward J, Prasad, Bhagwat

“…The availability of assays that predict the contribution of cytochrome P450 (CYP) metabolism allows for the design of new chemical entities (NCEs) with minimal…”
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Regional proteomic quantification of clinically relevant non-cytochrome P450 enzymes along the human small intestine by Zhang, Haeyoung, Wolford, Chris, Basit, Abdul, Li, Albert P, Fan, Peter W, Takahashi, Ryan H, Khojasteh, S Cyrus, Smith, Bill J, Murray, Bernard P, Thummel, Kenneth, Prasad, Bhagwat

“…Current challenges in accurately predicting intestinal metabolism arise from the complex nature of the intestine, leading to limited applicability of available…”
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Carboxylesterase catalyzed 18O-labeling of carboxylic acid and its potential application in LC-MS/MS based quantification of drug metabolites by Yu, Zaikuan J., Roesner, Joseph M., Lutz, Ryan, Liang, Yuexia, Baker, James, Smith, Dustin M., Fan, Peter W.

“…LC-MS quantification of drug metabolites is sometimes impeded by the availability of internal standards that often requires customized synthesis and/or…”
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Characterization of Raloxifene Glucuronidation in Vitro: Contribution of Intestinal Metabolism to Presystemic Clearance by KEMP, Daniel C, FAN, Peter W, STEVENS, Jeffrey C

“…Raloxifene, a selective estrogen receptor modulator used for the treatment of osteoporosis, undergoes extensive conjugation to the 6-β- and…”
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Investigation of Drug Delivery in Rats via Subcutaneous Injection: Case Study of Pharmacokinetic Modeling of Suspension Formulations by Chiang, Po-Chang, Nagapudi, Karthik, Fan, Peter W, Liu, Jia

“…With the rising cost of drug research, "do more with less" has become a new emphasis in the pharmaceutical industry. Consequently, the early analysis of…”
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Comparison of Tissue Abundance of Non-Cytochrome P450 Drug-Metabolizing Enzymes by Quantitative Proteomics between Humans and Laboratory Animal Species by Basit, Abdul, Fan, Peter W, Khojasteh, S Cyrus, Murray, Bernard P, Smith, Bill J, Heyward, Scott, Prasad, Bhagwat

“…The use of animal pharmacokinetic models as surrogates for humans relies on the assumption that the drug disposition mechanisms are similar between preclinical…”
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Rate-Determining and Rate-Limiting Steps in the Clearance and Excretion of a Potent and Selective p21-Activated Kinase Inhibitor: A Case Study of Rapid Hepatic Uptake and Slow Elimination in Rat by Fan, Peter W, Chen, Jacob Z, Allan Jaochico, M, La, Hank, Liu, Ning, Mulder, Teresa, Cass, Robert T, Durk, Matthew, Messick, Kirsten, Valle, Nicole, Liu, Shannon, Lee, Wendy, Crawford, James J, Rudolf, Joachim, Murray, Lesley J, Cyrus Khojasteh, S, Wright, Matthew

“…Significant under-prediction of in vivo clearance in rat was observed for a potent p21-activated kinase (PAK1) inhibitor, GNE1. Rate-determining (rapid uptake)…”
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NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus by Brightbill, Hans D., Suto, Eric, Blaquiere, Nicole, Ramamoorthi, Nandhini, Sujatha-Bhaskar, Swathi, Gogol, Emily B., Castanedo, Georgette M., Jackson, Benjamin T., Kwon, Youngsu C., Haller, Susan, Lesch, Justin, Bents, Karin, Everett, Christine, Kohli, Pawan Bir, Linge, Sandra, Christian, Laura, Barrett, Kathy, Jaochico, Allan, Berezhkovskiy, Leonid M., Fan, Peter W., Modrusan, Zora, Veliz, Kelli, Townsend, Michael J., DeVoss, Jason, Johnson, Adam R., Godemann, Robert, Lee, Wyne P., Austin, Cary D., McKenzie, Brent S., Hackney, Jason A., Crawford, James J., Staben, Steven T., Alaoui Ismaili, Moulay H., Wu, Lawren C., Ghilardi, Nico

“…NF-κB-inducing kinase (NIK) mediates non-canonical NF-κB signaling downstream of multiple TNF family members, including BAFF, TWEAK, CD40, and OX40, which are…”
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Going Beyond Common Drug Metabolizing Enzymes: Case Studies of Biotransformation Involving Aldehyde Oxidase, γ-Glutamyl Transpeptidase, Cathepsin B, Flavin-Containing Monooxygenase, and ADP-Ribosyltransferase by Fan, Peter W, Zhang, Donglu, Halladay, Jason S, Driscoll, James P, Khojasteh, S Cyrus

“…The significant roles that cytochrome P450 (P450) and UDP-glucuronosyl transferase (UGT) enzymes play in drug discovery cannot be ignored, and these enzyme…”
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Bioactivation of Tamoxifen to Metabolite E Quinone Methide: Reaction with Glutathione and DNA by FAN, Peter W, BOLTON, Judy L

“…Despite the beneficial effects of tamoxifen in the treatment and prevention of breast cancer, long-term usage of this popular antiestrogen has been linked to…”
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Filling a nick in NIK: Extending the half-life of a NIK inhibitor through structure-based drug design by Crawford, James J., Feng, Jianwen, Brightbill, Hans D., Johnson, Adam R., Wright, Matthew, Kolesnikov, Aleksandr, Lee, Wendy, Castanedo, Georgette M., Do, Steven, Blaquiere, Nicole, Staben, Steven T., Chiang, Po-Chang, Fan, Peter W., Baumgardner, Matt, Wong, Susan, Godemann, Robert, Grabbe, Alice, Wiegel, Catharina, Sujatha-Bhaskar, Swathi, Hymowitz, Sarah G., Liau, Nicholas, Hsu, Peter L., McEwan, Paul A., Ismaili, Moulay Hicham Alaoui, Landry, Matthew L.

“…[Display omitted] Inhibition of NF-κB inducing kinase (NIK) has been pursued as a promising therapeutic target for autoimmune disorders due to its highly…”
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Structure-Guided Design of Group I Selective p21-Activated Kinase Inhibitors by Crawford, James J, Lee, Wendy, Aliagas, Ignacio, Mathieu, Simon, Hoeflich, Klaus P, Zhou, Wei, Wang, Weiru, Rouge, Lionel, Murray, Lesley, La, Hank, Liu, Ning, Fan, Peter W, Cheong, Jonathan, Heise, Christopher E, Ramaswamy, Sreemathy, Mintzer, Robert, Liu, Yanzhou, Chao, Qi, Rudolph, Joachim

“…The p21-activated kinases (PAKs) play important roles in cytoskeletal organization, cellular morphogenesis, and survival and have generated significant…”
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Structure-Based Discovery of Proline-Derived Arginase Inhibitors with Improved Oral Bioavailability for Immuno-Oncology by Lu, Min, Zhang, Hongjun, Li, Derun, Childers, Matthew, Pu, Qinglin, Palte, Rachel L, Gathiaka, Symon, Lyons, Thomas W, Palani, Anandan, Fan, Peter W, Spacciapoli, Peter, Miller, J. Richard, Cho, Hyelim, Cheng, Mangeng, Chakravarthy, Kalyan, O’Neil, Jennifer, Eangoor, Padmanabhan, Beard, Adam, Kim, Hai-Young, Saurí, Josep, Gunaydin, Hakan, Sloman, David L, Siliphaivanh, Phieng, Cumming, Jared, Fischer, Christian

“…Recent data suggest that the inhibition of arginase (ARG) has therapeutic potential for the treatment of a number of indications ranging from pulmonary and…”
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Synthesis and Reactivity of a Potential Carcinogenic Metabolite of Tamoxifen:  3,4-Dihydroxytamoxifen-o-quinone by Zhang, Fagen, Fan, Peter W, Liu, Xuemei, Shen, Lixin, van Breemen, Richard B, Bolton, Judy L

“…Although tamoxifen is approved for the treatment of hormone-dependent breast cancer as well as for the prevention of breast cancer in high-risk women, several…”
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Mechanism-Based Inactivation of Cytochrome P450 2B6 by a Novel Terminal Acetylene Inhibitor by FAN, Peter W, CHUNGANG GU, MARSH, Sandra A, STEVENS, Jeffrey C

“…N -(3,5-Dichloro-4-pyridyl)-3-(cyclopentyloxy)-4-methoxybenzamide (DCMB) is a known marker substrate for cytochrome P450 2B6. Based on the chemical template of…”
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Solving time-dependent CYP3A4 inhibition for a series of indole-phenylacetic acid dual antagonists of the PGD(2) receptors CRTH2 and DP by Johnson, Michael G, Liu, Jim Jiwen, Li, An-Rong, van Lengerich, Bettina, Wang, Sophie, Medina, Julio C, Collins, Tassie L, Danao, Jay, Seitz, Lisa, Willee, Angela, D'Souza, Warren, Budelsky, Alison L, Fan, Peter W, Wong, Simon G W

“…Based on their structural similarity to previously described compound AMG 009, indole-phenyl acetic acids were proposed to be potent dual inhibitors of…”
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Probing Mechanisms of CYP3A Time-Dependent Inhibition Using a Truncated Model System by Wang, Xiaojing, Sun, Minghua, New, Connie, Nam, Spencer, Blackaby, Wesley P, Hodges, Alastair J, Nash, David, Matteucci, Mizio, Lyssikatos, Joseph P, Fan, Peter W, Tay, Suzanne, Chang, Jae H

“…Time-dependent inhibition (TDI) of cytochrome P450 (CYP) enzymes may incur serious undesirable drug–drug interactions and in rare cases drug-induced…”
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Practical permeability-based hepatic clearance classification system (HepCCS) in drug discovery by Fan, Peter W, Song, Yang, Berezhkovskiy, Leonid M, Cheong, Jonathan, Plise, Emile G, Khojasteh, S Cyrus

“…The use of liver microsomes and hepatocytes to predict total in vivo clearance is standard practice in the pharmaceutical industry; however, metabolic…”
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Elucidation of the mechanism of ribose conjugation in a pyrazole-containing compound in rodent liver by Le, Hoa, Ford, Kevin A., Khojasteh, S. Cyrus, Fan, Peter W.

“…1. Here we report on the mechanism of ribose conjugation, through NADH as a cofactor, of a pyrazole-containing compound (PT). Incubation of PT in rat liver…”
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Novel Mechanism for Dehalogenation and Glutathione Conjugation of Dihalogenated Anilines in Human Liver Microsomes: Evidence for ipso Glutathione Addition by Zhang, Chenghong, Kenny, Jane R, Le, Hoa, Deese, Alan, Ford, Kevin A, Lightning, Luke K, Fan, Peter W, Driscoll, James P, Halladay, Jason S, Hop, Cornelis E. C. A, Khojasteh, S. Cyrus

“…The objective of the present study was to investigate the influence of halogen position on the formation of reactive metabolites from dihalogenated anilines…”
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