Search Results - "Harstad, Eric"

The Vedotin Antibody-Drug Conjugate Payload Drives Platform-Based Nonclinical Safety and Pharmacokinetic Profiles by Neff-LaFord, Haley D, Carratt, Sarah A, Carosino, Christopher, Everds, Nancy, Cardinal, Kristen A, Duniho, Steven, Schutten, Melissa M, Frantz, Christopher, Zuch de Zafra, Christina, Harstad, Eric B

“…Nonclinical safety and pharmacokinetic data for monomethyl auristatin E (MMAE) and 14 vedotin antibody-drug conjugates (ADC) were evaluated to determine…”
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Gut-Selective Design of Orally Administered Izencitinib (TD-1473) Limits Systemic Exposure and Effects of Janus Kinase Inhibition in Nonclinical Species by Hardwick, Rhiannon N, Brassil, Patrick, Badagnani, Ilaria, Perkins, Kimberly, Obedencio, Glenmar P, Kim, Andrea S, Conner, Michael W, Bourdet, David L, Harstad, Eric B

“…Abstract Izencitinib (TD-1473), an oral, gut-selective pan-Janus kinase (JAK) inhibitor under investigation for treatment of inflammatory bowel diseases, was…”
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Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma by Wang, Xiaojing, Blackaby, Wesley, Allen, Vivienne, Chan, Grace Ka Yan, Chang, Jae H, Chiang, Po-Chang, Diène, Coura, Drummond, Jason, Do, Steven, Fan, Eric, Harstad, Eric B, Hodges, Alastair, Hu, Huiyong, Jia, Wei, Kofie, William, Kolesnikov, Aleksandr, Lyssikatos, Joseph P, Ly, Justin, Matteucci, Mizio, Moffat, John G, Munugalavadla, Veerendra, Murray, Jeremy, Nash, David, Noland, Cameron L, Del Rosario, Geoff, Ross, Leanne, Rouse, Craig, Sharpe, Andrew, Slaga, Dionysos, Sun, Minghua, Tsui, Vickie, Wallweber, Heidi, Yu, Shang-Fan, Ebens, Allen J

“…Pim kinases have been targets of interest for a number of therapeutic areas. Evidence of durable single-agent efficacy in human clinical trials validated Pim…”
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DPP8 and DPP9 expression in cynomolgus monkey and Sprague Dawley rat tissues by Harstad, Eric. B., Rosenblum, Jonathan S., Gorrell, Mark D., Achanzar, William E., Minimo, Lauro, Wu, Jiangyue, Rosini-Marthaler, Laura, Gullo, Russell, Ordway, Nicole D., Kirby, Mark S., Chadwick, Kristina D., Cosma, Gregory N., Moyer, Carolyn F.

“…Dipeptidyl peptidases (DPPs) are proteolytic enzymes that regulate many physiological systems by degrading signaling peptides. DPP8 and DPP9 are distinct from…”
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Patent Ductus Venosus and Dioxin Resistance in Mice Harboring a Hypomorphic Arnt Allele by Walisser, Jacqueline A., Bunger, Maureen K., Glover, Edward, Harstad, Eric B., Bradfield, Christopher A.

“…The Ah receptor nuclear translocator (ARNT) is the dimeric partner of hypoxia-inducible factors and thus plays a pivotal role in cellular adaptation to low…”
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Pharmacokinetic drivers of toxicity for basic molecules: Strategy to lower pKa results in decreased tissue exposure and toxicity for a small molecule Met inhibitor by Diaz, Dolores, Ford, Kevin A., Hartley, Dylan P., Harstad, Eric B., Cain, Gary R., Achilles-Poon, Kirsten, Nguyen, Trung, Peng, Jing, Zheng, Zhong, Merchant, Mark, Sutherlin, Daniel P., Gaudino, John J., Kaus, Robert, Lewin-Koh, Sock C., Choo, Edna F., Liederer, Bianca M., Dambach, Donna M.

“…Several toxicities are clearly driven by free drug concentrations in plasma, such as toxicities related to on-target exaggerated pharmacology or off-target…”
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Liver deformation in Ahr-null mice: evidence for aberrant hepatic perfusion in early development by Harstad, Eric B, Guite, Christopher A, Thomae, Tami L, Bradfield, Christopher A

“…Mice harboring mutations in the Ahr locus display a patent ductus venosus and smaller livers throughout life. We tested the hypothesis that these hepatic…”
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Two stochastic mean-field polycrystal plasticity methods by Tonks, Michael R., Bingert, John F., Bronkhorst, Curt A., Harstad, Eric N., Tortorelli, Daniel A.

“…In this work, we develop two mean-field polycrystal plasticity models in which the crystal velocity gradients L c are approximated stochastically. Through…”
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Preclinical stereoselective disposition and toxicokinetics of two novel MET inhibitors by Liederer, Bianca M., Liu, Xingrong, Berezhkovskiy, Leonid M., Cain, Gary, Ding, Xiao, Gaudino, John, Kaus, Robert, Plise, Emile G., Sutherlin, Daniel P., Harstad, Eric B.

“…The R- and S-enantiomer of…”
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Tumor Necrosis Factor-α-Null Mice Are Not Resistant to Cadmium Chloride-Induced Hepatotoxicity by Harstad, Eric B., Klaassen, Curtis D.

“…Acute administration of cadmium results in hepatotoxicity. Recent reports indicate that Kupffer cells, the resident macrophages of the liver, participate in…”
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iNOS-null mice are not resistant to cadmium chloride-induced hepatotoxicity by Harstad, Eric B., Klaassen, Curtis D.

“…Acute administration of cadmium (Cd) to rats results in hepatotoxicity. Recent reports indicate that Kupffer cells, the resident macrophages of the liver,…”
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Analysis of Strain Difference in Sensitivity to Cadmium-Induced Hepatotoxicity in Fischer 344 and Sprague-Dawley Rats by Harstad, Eric B., Klaassen, Curtis D.

“…Acute administration of cadmium (Cd) in rats results in hepatotoxicity that appears to involve the activation of Kupffer cells and the subsequent production of…”
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Gadolinium Chloride Pretreatment Prevents Cadmium Chloride-Induced Liver Damage in Both Wild-Type and MT-Null Mice by Harstad, Eric B., Klaassen, Curtis D.

“…The heavy metal cadmium (Cd) causes hepatotoxicity upon acute administration. Kupffer cells, the resident macrophages of the liver, have been suggested to play…”
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Preclinical Development of an Anti-NaPi2b (SLC34A2) Antibody-Drug Conjugate as a Therapeutic for Non-Small Cell Lung and Ovarian Cancers by Lin, Kedan, Rubinfeld, Bonnee, Zhang, Crystal, Firestein, Ron, Harstad, Eric, Roth, Leslie, Tsai, Siao Ping, Schutten, Melissa, Xu, Keyang, Hristopoulos, Maria, Polakis, Paul

“…Antibody-drug conjugates (ADC) selectively deliver a cytotoxic drug to cells expressing an accessible antigenic target. Here, we have appended monomethyl…”
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Tankyrase Inhibition Causes Reversible Intestinal Toxicity in Mice with a Therapeutic Index < 1 by Zhong, Yu, Katavolos, Paula, Nguyen, Trung, Lau, Ted, Boggs, Jason, Sambrone, Amy, Kan, David, Merchant, Mark, Harstad, Eric, Diaz, Dolores, Costa, Mike, Schutten, Melissa

“…Activated Wnt/β-catenin signaling is frequently associated with colorectal cancer. Wnt inhibitors, including tankyrase inhibitors, are being explored as…”
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Lung-restricted ALK5 inhibition avoids systemic toxicities associated with TGFβ pathway inhibition by Maher, Jonathan M., Zhang, Rui, Palanisamy, Gopinath, Perkins, Kimberly, Liu, Lynda, Brassil, Patrick, McNamara, Alexander, Lo, Arthur, Hughes, Adam D., Kanodia, Jitendra, Kulyk, Svitlana, Nikula, Kristen J., Dengler, Hart S., Scandurra, Amy, Lua, Ingrid, Harstad, Eric

“…Systemic therapies targeting transforming growth factor beta (TGFβ) or TGFβR1 kinase (ALK5) have been plagued by toxicities including cardiac valvulopathy and…”
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Discovery of 5‑Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability by Wang, Xiaojing, Kolesnikov, Aleksandr, Tay, Suzanne, Chan, Grace, Chao, Qi, Do, Steven, Drummond, Jason, Ebens, Allen J, Liu, Ning, Ly, Justin, Harstad, Eric, Hu, Huiyong, Moffat, John, Munugalavadla, Veerendra, Murray, Jeremy, Slaga, Dionysos, Tsui, Vickie, Volgraf, Matthew, Wallweber, Heidi, Chang, Jae H

“…Pim kinases have been identified as promising therapeutic targets for hematologic–oncology indications, including multiple myeloma and certain leukemia. Here,…”
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Discovery of novel pyrazolo[1,5-a]pyrimidines as potent pan-Pim inhibitors by structure- and property-based drug design by Wang, Xiaojing, Magnuson, Steven, Pastor, Rich, Fan, Eric, Hu, Huiyong, Tsui, Vickie, Deng, Wei, Murray, Jeremy, Steffek, Micah, Wallweber, Heidi, Moffat, John, Drummond, Jason, Chan, Grace, Harstad, Eric, Ebens, Allen J.

“…Pim kinases are promising targets for the development of cancer therapeutics. Among the three Pim isoforms, Pim-2 is particularly important in multiple…”
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Identification of C‑2 Hydroxyethyl Imidazopyrrolopyridines as Potent JAK1 Inhibitors with Favorable Physicochemical Properties and High Selectivity over JAK2 by Zak, Mark, Hurley, Christopher A, Ward, Stuart I, Bergeron, Philippe, Barrett, Kathy, Balazs, Mercedesz, Blair, Wade S, Bull, Richard, Chakravarty, Paroma, Chang, Christine, Crackett, Peter, Deshmukh, Gauri, DeVoss, Jason, Dragovich, Peter S, Eigenbrot, Charles, Ellwood, Charles, Gaines, Simon, Ghilardi, Nico, Gibbons, Paul, Gradl, Stefan, Gribling, Peter, Hamman, Chris, Harstad, Eric, Hewitt, Peter, Johnson, Adam, Johnson, Tony, Kenny, Jane R, Koehler, Michael F. T, Bir Kohli, Pawan, Labadie, Sharada, Lee, Wyne P, Liao, Jiangpeng, Liimatta, Marya, Mendonca, Rohan, Narukulla, Raman, Pulk, Rebecca, Reeve, Austin, Savage, Scott, Shia, Steven, Steffek, Micah, Ubhayakar, Savita, van Abbema, Anne, Aliagas, Ignacio, Avitabile-Woo, Barbara, Xiao, Yisong, Yang, Jing, Kulagowski, Janusz J

“…Herein we report on the structure-based discovery of a C-2 hydroxyethyl moiety which provided consistently high levels of selectivity for JAK1 over JAK2 to the…”
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Balancing Blood Sample Volume with 3Rs: Implementation and Best Practices for Small Molecule Toxicokinetic Assessments in Rats by Harstad, Eric, Andaya, Roxanne, Couch, Jessica, Ding, Xiao, Liang, Xiaorong, Liederer, Bianca M, Messick, Kirsten, Nguyen, Trung, Schweiger, Michelle, Tarrant, Jacqueline, Zhong, Shelly, Dean, Brian

“…Improved small molecule bioanalytical sensitivity and concomitant decreased sample volume requirements provide an opportunity to reconsider how toxicokinetic…”
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