Search Results - "BONIN, PAUL D."

Efficacy and Pharmacology of the NLRP3 Inflammasome Inhibitor CP-456,773 (CRID3) in Murine Models of Dermal and Pulmonary Inflammation by Primiano, Michael J, Lefker, Bruce A, Bowman, Michael R, Bree, Andrea G, Hubeau, Cedric, Bonin, Paul D, Mangan, Matthew, Dower, Ken, Monks, Brian G, Cushing, Leah, Wang, Stephen, Guzova, Julia, Jiao, Aiping, Lin, Lih-Ling, Latz, Eicke, Hepworth, David, Hall, J Perry

“…A critical component of innate immune response to infection and tissue damage is the NACHT, LRR, and PYD domains-containing protein 3 (NLRP3) inflammasome, and…”
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Evaluating the Role of Multidrug Resistance Protein 3 (MDR3) Inhibition in Predicting Drug-Induced Liver Injury Using 125 Pharmaceuticals by Aleo, Michael D, Shah, Falgun, He, Kan, Bonin, Paul D, Rodrigues, A. David

“…The role of bile salt export protein (BSEP) inhibition in drug-induced liver injury (DILI) has been investigated widely, while inhibition of the canalicular…”
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PF-1355, a mechanism-based myeloperoxidase inhibitor, prevents immune complex vasculitis and anti-glomerular basement membrane glomerulonephritis by Zheng, Wei, Warner, Roscoe, Ruggeri, Roger, Su, Chunyan, Cortes, Christian, Skoura, Athanasia, Ward, Jessica, Ahn, Kay, Kalgutkar, Amit, Sun, Dexue, Maurer, Tristan S, Bonin, Paul D, Okerberg, Carlin, Bobrowski, Walter, Kawabe, Thomas, Zhang, Yanwei, Coskran, Timothy, Bell, Sammy, Kapoor, Bhupesh, Johnson, Kent, Buckbinder, Leonard

“…Small vessel vasculitis is a life-threatening condition and patients typically present with renal and pulmonary injury. Disease pathogenesis is associated with…”
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Cryo-EM structures of the human glutamine transporter SLC1A5 (ASCT2) in the outward-facing conformation by Yu, Xiaodi, Plotnikova, Olga, Bonin, Paul D, Subashi, Timothy A, McLellan, Thomas J, Dumlao, Darren, Che, Ye, Dong, Yin Yao, Carpenter, Elisabeth P, West, Graham M, Qiu, Xiayang, Culp, Jeffrey S, Han, Seungil

“…Alanine-serine-cysteine transporter 2 (ASCT2, SLC1A5) is the primary transporter of glutamine in cancer cells and regulates the mTORC1 signaling pathway. The…”
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Activation of the G-Protein-Coupled Receptor 119: A Conformation-Based Hypothesis for Understanding Agonist Response by McClure, Kim F, Darout, Etzer, Guimarães, Cristiano R. W, DeNinno, Michael P, Mascitti, Vincent, Munchhof, Michael J, Robinson, Ralph P, Kohrt, Jeffrey, Harris, Anthony R, Moore, Dianna E, Li, Bryan, Samp, Lacey, Lefker, Bruce A, Futatsugi, Kentaro, Kung, Daniel, Bonin, Paul D, Cornelius, Peter, Wang, Ruduan, Salter, Eben, Hornby, Sam, Kalgutkar, Amit S, Chen, Yue

“…The synthesis and properties of the bridged piperidine (oxaazabicyclo) compounds 8, 9, and 11 are described. A conformational analysis of these structures is…”
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Oxidative Metabolism of a Quinoxaline Derivative by Xanthine Oxidase in Rodent Plasma by Sharma, Raman, Eng, Heather, Walker, Gregory S, Barreiro, Gabriela, Stepan, Antonia F, McClure, Kim F, Wolford, Angela, Bonin, Paul D, Cornelius, Peter, Kalgutkar, Amit S

“…As part of efforts directed at the G protein-coupled receptor 119 agonist program for type 2 diabetes, a series of cyanopyridine derivatives exemplified by…”
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Human drug‐induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump by Aleo, Michael D., Luo, Yi, Swiss, Rachel, Bonin, Paul D., Potter, David M., Will, Yvonne

“…Drug‐induced liver injury (DILI) accounts for 20‐40% of all instances of clinical hepatic failure and is a common reason for withdrawal of an approved drug or…”
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Phase I study of PF‐04895162, a Kv7 channel opener, reveals unexpected hepatotoxicity in healthy subjects, but not rats or monkeys: clinical evidence of disrupted bile acid homeostasis by Aleo, Michael D., Aubrecht, Jiri, D. Bonin, Paul, Burt, Deborah A., Colangelo, Jennifer, Luo, Lina, Schomaker, Shelli, Swiss, Rachel, Kirby, Simon, C. Rigdon, Greg, Dua, Pinky

“…During a randomized Phase 1 clinical trial the drug candidate, PF‐04895162 (ICA‐105665), caused transaminase elevations (≥grade 1) in six of eight healthy…”
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Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists by Humphries, Paul S., Benbow, John W., Bonin, Paul D., Boyer, David, Doran, Shawn D., Frisbie, Richard K., Piotrowski, David W., Balan, Gayatri, Bechle, Bruce M., Conn, Edward L., Dirico, Kenneth J., Oliver, Robert M., Soeller, Walter C., Southers, James A., Yang, Xiaojing

“…The development of a series of novel 1,2,3,4-tetrahydroisoquinolin-1-ones as antagonists of G protein-coupled receptor 40 (GPR40) is described. The synthesis,…”
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Design and evaluation of a 2-(2,3,6-trifluorophenyl)acetamide derivative as an agonist of the GPR119 receptor by Mascitti, Vincent, Stevens, Benjamin D., Choi, Chulho, McClure, Kim F., Guimarães, Cristiano R.W., Farley, Kathleen A., Munchhof, Michael J., Robinson, Ralph P., Futatsugi, Kentaro, Lavergne, Sophie Y., Lefker, Bruce A., Cornelius, Peter, Bonin, Paul D., Kalgutkar, Amit S., Sharma, Raman, Chen, Yue

“…The design and synthesis of a GPR119 agonist bearing a 2-(2,3,6-trifluorophenyl)acetamide group is described. The design capitalized on the conformational…”
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Discovery of 2‑(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)‑yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases by Ruggeri, Roger B, Buckbinder, Leonard, Bagley, Scott W, Carpino, Philip A, Conn, Edward L, Dowling, Matthew S, Fernando, Dilinie P, Jiao, Wenhua, Kung, Daniel W, Orr, Suvi T. M, Qi, Yingmei, Rocke, Benjamin N, Smith, Aaron, Warmus, Joseph S, Zhang, Yan, Bowles, Daniel, Widlicka, Daniel W, Eng, Heather, Ryder, Tim, Sharma, Raman, Wolford, Angela, Okerberg, Carlin, Walters, Karen, Maurer, Tristan S, Zhang, Yanwei, Bonin, Paul D, Spath, Samantha N, Xing, Gang, Hepworth, David, Ahn, Kay, Kalgutkar, Amit S

“…Myeloperoxidase (MPO) is a heme peroxidase that catalyzes the production of hypochlorous acid. Clinical evidence suggests a causal role for MPO in various…”
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Correction to Evaluating the Role of Multidrug Resistance Protein 3 (MDR3) Inhibition in Predicting Drug-Induced Liver Injury Using 125 Pharmaceuticals by Aleo, Michael D, Shah, Falgun, He, Kan, Bonin, Paul D, Rodrigues, A. David

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Transcriptional Profiling of a Selective CREB Binding Protein Bromodomain Inhibitor Highlights Therapeutic Opportunities by Chekler, Eugene L. Piatnitski, Pellegrino, Jessica A., Lanz, Thomas A., Denny, R. Aldrin, Flick, Andrew C., Coe, Jotham, Langille, Jonathan, Basak, Arindrajit, Liu, Shenping, Stock, Ingrid A., Sahasrabudhe, Parag, Bonin, Paul D., Lee, Kevin, Pletcher, Mathew T., Jones, Lyn H.

“…Bromodomains are involved in transcriptional regulation through the recognition of acetyl lysine modifications on diverse proteins. Selective pharmacological…”
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Design and Synthesis of Diazatricyclodecane Agonists of the G‑Protein-Coupled Receptor 119 by Darout, Etzer, Robinson, Ralph P, McClure, Kim F, Corbett, Matthew, Li, Bryan, Shavnya, Andrei, Andrews, Melissa P, Jones, Christopher S, Li, Qifang, Minich, Martha L, Mascitti, Vincent, Guimarães, Cristiano R. W, Munchhof, Michael J, Bahnck, Kevin B, Cai, Cuiman, Price, David A, Liras, Spiros, Bonin, Paul D, Cornelius, Peter, Wang, Ruduan, Bagdasarian, Victoria, Sobota, Colleen P, Hornby, Sam, Masterson, Victoria M, Joseph, Reena M, Kalgutkar, Amit S, Chen, Yue

“…A series of GPR119 agonists based on a 2,6-diazatricyclo[3.3.1.1∼3,7∼]decane ring system is described. Also provided is a detailed account of the development…”
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From partial to full agonism: Identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor by Futatsugi, Kentaro, Mascitti, Vincent, Guimarães, Cristiano R.W., Morishita, Nao, Cai, Cuiman, DeNinno, Michael P., Gao, Hua, Hamilton, Michael D., Hank, Richard, Harris, Anthony R., Kung, Daniel W., Lavergne, Sophie Y., Lefker, Bruce A., Lopaze, Michael G., McClure, Kim F., Munchhof, Michael J., Preville, Cathy, Robinson, Ralph P., Wright, Stephen W., Bonin, Paul D., Cornelius, Peter, Chen, Yue, Kalgutkar, Amit S.

“…A novel GPR119 agonist based on the 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole scaffold was designed through lead optimization starting from pyrazole-based…”
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Resistance mapping and mode of action of a novel class of antibacterial anthranilic acids: evidence for disruption of cell wall biosynthesis by Mott, John E., Shaw, Bailin A., Smith, James F., Bonin, Paul D., Romero, Donna L., Marotti, Keith R., Miller, Alita A.

“…Objectives The aim of this study was to characterize the mechanism of action of a novel class of bacterial protein synthesis inhibitors identified in a…”
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Development of a Fluorescence Polarization Assay for Peptidyl–tRNA Hydrolase by Bonin, Paul D., Erickson, Laurence A.

“…Peptidyl–tRNA hydrolase (Pth) activity ensures the rapid recycling of peptidyl–tRNAs that result from premature termination of translation. Historically, the…”
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Adding Precise Nanoliter Volume Capabilities to Liquid-Handling Automation for Compound Screening Experimentation by Murthy, Tal V., Kroncke, Doug, Bonin, Paul D.

“…Miniaturizing experimental sample volumes to the nanoliter volume range is one of the most economical ways to perform mid- and high-throughput compound…”
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Expression, Purification, and Characterization of Peptidyl-tRNA Hydrolase from Staphylococcus aureus by Bonin, Paul D., Choi, Gil H., Trepod, Catherine M., Mott, John E., Lyle, Stephen B., Cialdella, Joyce I., Sarver, Ronald W., Marshall, Vincent P., Erickson, Laurence A.

“…Bacterial peptidyl-tRNA hydrolase (Pth) activity ensures the rapid recycling of peptidyl-tRNAs that result from premature termination of translation. Pth has…”
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Synthesis of 2,6-disubstituted-7,8-dihydro-6H-pyrano[2,3-6]pyrazines by Li, Jian-Cheng, Munchhof, Michael, Warmus, Joseph S., Bonin, Paul D., McClure, Kim F.

“…A straightforward synthesis of a 2,6-disubstituted-7,8-dihydro-6H-pyrano[2,3-6]pyrazine is described. The synthesis relies on a versatile…”
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