Search Results - "CHOO, Edna"

Venetoclax combines synergistically with FLT3 inhibition to effectively target leukemic cells in FLT3-ITD+ acute myeloid leukemia models by Singh Mali, Raghuveer, Zhang, Qi, DeFilippis, Rosa Anna, Cavazos, Antonio, Kuruvilla, Vinitha Mary, Raman, Jayant, Mody, Vidhi, Choo, Edna F, Dail, Monique, Shah, Neil P, Konopleva, Marina, Sampath, Deepak, Lasater, Elisabeth A

“…FLT3 internal tandem duplication (FLT3-ITD) mutations account for ~25% of adult acute myeloid leukemia cases and are associated with poor prognosis…”
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Leveraging Humanized Animal Models to Understand Human Drug Disposition: Opportunities, Challenges, and Future Directions by Choo, Edna F., Salphati, Laurent

“…The utility of animal models in understanding drug disposition and extrapolating to human in a direct manner is limited, confounded by differences in enzyme…”
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Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer by Jin, Lingyan, Garcia, Jesse, Chan, Emily, de la Cruz, Cecile, Segal, Ehud, Merchant, Mark, Kharbanda, Samir, Raisner, Ryan, Haverty, Peter M, Modrusan, Zora, Ly, Justin, Choo, Edna, Kaufman, Susan, Beresini, Maureen H, Romero, F Anthony, Magnuson, Steven, Gascoigne, Karen E

“…Resistance invariably develops to antiandrogen therapies used to treat newly diagnosed prostate cancers, but effective treatments for castration-resistant…”
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A Novel Tankyrase Small-Molecule Inhibitor Suppresses APC Mutation―Driven Colorectal Tumor Growth by LAU, Ted, CHAN, Emily, MACHON, Ondrej, KORINEK, Vladimir, CHOO, Edna, DIAZ, Dolores, MERCHANT, Mark, POLAKIS, Paul, HOLSWORTH, Daniel D, KRAUSS, Stefan, COSTA, Mike, CALLOW, Marinella, WAALER, Jo, BOGGS, Jason, BLAKE, Robert A, MAGNUSON, Steven, SAMBRONE, Amy, SCHUTTEN, Melissa, FIRESTEIN, Ron

“…Most colorectal cancers (CRC) are initiated by mutations of APC, leading to increased β-catenin-mediated signaling. However, continued requirement of…”
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Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300 by Crawford, Terry D, Romero, F. Anthony, Lai, Kwong Wah, Tsui, Vickie, Taylor, Alexander M, de Leon Boenig, Gladys, Noland, Cameron L, Murray, Jeremy, Ly, Justin, Choo, Edna F, Hunsaker, Thomas L, Chan, Emily W, Merchant, Mark, Kharbanda, Samir, Gascoigne, Karen E, Kaufman, Susan, Beresini, Maureen H, Liao, Jiangpeng, Liu, Wenfeng, Chen, Kevin X, Chen, Zhongguo, Conery, Andrew R, Côté, Alexandre, Jayaram, Hariharan, Jiang, Ying, Kiefer, James R, Kleinheinz, Tracy, Li, Yingjie, Maher, Jonathan, Pardo, Eneida, Poy, Florence, Spillane, Kerry L, Wang, Fei, Wang, Jian, Wei, Xiaocang, Xu, Zhaowu, Xu, Zhongya, Yen, Ivana, Zawadzke, Laura, Zhu, Xiaoyu, Bellon, Steven, Cummings, Richard, Cochran, Andrea G, Albrecht, Brian K, Magnuson, Steven

“…The single bromodomain of the closely related transcriptional regulators CBP/EP300 is a target of much recent interest in cancer and immune system regulation…”
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Identification of a Discrete Diglucuronide of GDC-0810 in Human Plasma after Oral Administration by Zhang, Chenghong, Su, Dian, Choo, Edna F, Liu, Lichuan, Bobba, Sudheer, Jorski, Jamie, Ho, Quynh, Wang, Jing, Kenny, Jane, Khojasteh, S Cyrus, Zhang, Donglu

“…is a small molecule therapeutic agent having potential to treat breast cancer. In plasma of the first-in-human study, metabolite accounting for 20.7% of total…”
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GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) by Romero, F. Anthony, Murray, Jeremy, Lai, Kwong Wah, Tsui, Vickie, Albrecht, Brian K, An, Le, Beresini, Maureen H, de Leon Boenig, Gladys, Bronner, Sarah M, Chan, Emily W, Chen, Kevin X, Chen, Zhongguo, Choo, Edna F, Clagg, Kyle, Clark, Kevin, Crawford, Terry D, Cyr, Patrick, de Almeida Nagata, Denise, Gascoigne, Karen E, Grogan, Jane L, Hatzivassiliou, Georgia, Huang, Wei, Hunsaker, Thomas L, Kaufman, Susan, Koenig, Stefan G, Li, Ruina, Li, Yingjie, Liang, Xiaorong, Liao, Jiangpeng, Liu, Wenfeng, Ly, Justin, Maher, Jonathan, Masui, Colin, Merchant, Mark, Ran, Yingqing, Taylor, Alexander M, Wai, John, Wang, Fei, Wei, Xiaocang, Yu, Dong, Zhu, Bing-Yan, Zhu, Xiaoyu, Magnuson, Steven

“…Inhibition of the bromodomain of the transcriptional regulator CBP/P300 is an especially interesting new therapeutic approach in oncology. We recently…”
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Bioactivation of α , β -Unsaturated Carboxylic Acids Through Acyl Glucuronidation by Mulder, Teresa, Bobba, Sudheer, Johnson, Kevin, Grandner, Jessica M., Wang, Wei, Zhang, Chenghong, Cai, Jingwei, Choo, Edna F., Khojasteh, S. Cyrus, Zhang, Donglu

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Antitumor Activity of Targeted and Cytotoxic Agents in Murine Subcutaneous Tumor Models Correlates with Clinical Response by WONG, Harvey, CHOO, Edna F, GOULD, Stephen E, ALICKE, Bruno, XIAO DING, LA, Hank, MCNAMARA, Erin, THEIL, Frank-Peter, TIBBITTS, Jay, FRIEDMAN, Lori S, HOP, Cornelis E. C. A

“…Immunodeficient mice transplanted with subcutaneous tumors (xenograft or allograft) are widely used as a model of preclinical activity for the discovery and…”
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Development of Potent and Selective Pyrazolopyrimidine IRAK4 Inhibitors by Bryan, Marian C, Drobnick, Joy, Gobbi, Alberto, Kolesnikov, Aleksandr, Chen, Yongsheng, Rajapaksa, Naomi, Ndubaku, Chudi, Feng, Jianwen, Chang, Willy, Francis, Ross, Yu, Christine, Choo, Edna F, DeMent, Kevin, Ran, Yingqing, An, Le, Emson, Claire, Huang, Zhiyu, Sujatha-Bhaskar, Swathi, Brightbill, Hans, DiPasquale, Antonio, Maher, Jonathan, Wai, John, McKenzie, Brent S, Lupardus, Patrick J, Zarrin, Ali A, Kiefer, James R

“…A series of pyrazolopyrimidine inhibitors of IRAK4 were developed from a high-throughput screen (HTS). Modification of an HTS hit led to a series of bicyclic…”
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Utility of CYP3A4 and PXR-CAR-CYP3A4/3A7 Transgenic Mouse Models To Assess the Magnitude of CYP3A4 Mediated Drug–Drug Interactions by Ly, Justin Q, Messick, Kirsten, Qin, Ann, Takahashi, Ryan H, Choo, Edna F

“…Species differences in the expression, activity, regulation, and substrate specificity of metabolizing enzymes preclude the use of animal models to predict…”
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Role of P‑Glycoprotein on the Brain Penetration and Brain Pharmacodynamic Activity of the MEK Inhibitor Cobimetinib by Choo, Edna F, Ly, Justin, Chan, Jocelyn, Shahidi-Latham, Sheerin K, Messick, Kirsten, Plise, Emile, Quiason, Cristine M, Yang, Lulu

“…Cobimetinib is a MEK inhibitor currently in clinical trials as an anticancer agent. The objectives of this study were to determine in vitro and in vivo if…”
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Use of transgenic mouse models to understand the oral disposition and drug-drug interaction potential of cobimetinib, a MEK inhibitor by Choo, Edna F, Woolsey, Sarah, DeMent, Kevin, Ly, Justin, Messick, Kirsten, Qin, Ann, Takahashi, Ryan

“…Data from the clinical absolute bioavailability (F) study with cobimetinib suggested that F was lower than predicted based on its low hepatic extraction and…”
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Effect of OATP1B1/1B3 Inhibitor GDC‐0810 on the Pharmacokinetics of Pravastatin and Coproporphyrin I/III in Healthy Female Subjects by Liu, Lichuan, Cheeti, Sravanthi, Yoshida, Kenta, Choo, Edna, Chen, Eugene, Chen, Buyun, Gates, Mary, Singel, Stina, Morley, Roland, Ware, Joseph, Sahasranaman, Srikumar

“…Developed as an oral anticancer drug to treat estrogen receptor–positive breast cancer, GDC‐0810 was shown to be a potent inhibitor of organic…”
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Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs by Katavolos, Paula, Cain, Gary, Farman, Cindy, Romero, F. Anthony, Magnuson, Steven, Ly, Justin Q., Choo, Edna F., Katakam, Anand Kumar, Andaya, Roxanne, Maher, Jonathan

“…Cyclic adenosine monophosphate-response element (CREB)-binding protein (CBP) and EP300E1A-binding protein (p300) are members of the bromodomain and…”
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Bridging the Gap between Preclinical and Clinical Studies Using Pharmacokinetic-Pharmacodynamic Modeling: An Analysis of GDC-0973, a MEK Inhibitor by WONG, Harvey, VERNILLET, Laurent, HOEFLICH, Klaus P, YONGCHANG SHI, AFTAB, Blake T, AOYAMA, Ron, TAN LAM, Sanh, BELVIN, Marcia, PRESCOTT, John, PETERSON, Amy, WARE, Joseph A, LEE, Lillian, MARTINI, Jean-Francois, PEIWEN YU, CONGFEN LI, DEL ROSARIO, Geoffrey, CHOO, Edna F

“…GDC-0973 is a potent and selective mitogen-activated protein (MAP)/extracellular signal-regulated kinase (ERK) kinase (MEK) inhibitor…”
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The role of lymphatic transport on the systemic bioavailability of the Bcl-2 protein family inhibitors navitoclax (ABT-263) and ABT-199 by Choo, Edna F, Boggs, Jason, Zhu, Chunqiang, Lubach, Joseph W, Catron, Nathaniel D, Jenkins, Gary, Souers, Andrew J, Voorman, Richard

“…Navitoclax (ABT-263), a Bcl-2 family inhibitor and ABT-199, a Bcl-2 selective inhibitor, are high molecular weight, high logP molecules that show low…”
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A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors by Bronner, Sarah M, Murray, Jeremy, Romero, F. Anthony, Lai, Kwong Wah, Tsui, Vickie, Cyr, Patrick, Beresini, Maureen H, de leon Boenig, Gladys, Chen, Zhongguo, Choo, Edna F, Clark, Kevin R, Crawford, Terry D, Jayaram, Hariharan, Kaufman, Susan, Li, Ruina, Li, Yingjie, Liao, Jiangpeng, Liang, Xiaorong, Liu, Wenfeng, Ly, Justin, Maher, Jonathan, Wai, John, Wang, Fei, Zheng, Aijun, Zhu, Xiaoyu, Magnuson, Steven

“…The epigenetic regulator CBP/P300 presents a novel therapeutic target for oncology. Previously, we disclosed the development of potent and selective CBP…”
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Overview of SLC22A and SLCO families of drug uptake transporters in the context of cancer treatments by Cutler, Murray J, Choo, Edna F

“…The effectiveness of many anticancer agents is dependent on their disposition to the intracellular space of cancerous tissue. Accumulation of anticancer drugs…”
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Discovery of GNE-6893, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of HPK1 by Tellis, John C, Wei, BinQing, Siu, Michael, An, Le, Chan, Grace Kayan, Chen, Yong, Du, Xiangnan, Gazzard, Lewis, Hu, Baihua, Kiefer, James, Kakiuchi-Kiyota, Satoko, Lainchbury, Michael, Linehan, Jonathan L, Luo, Xifeng, Malhotra, Sushant, Mendonca, Rohan, Pang, Jodie, Ran, Yinqing, Sethuraman, Vijay, Seward, Eileen, Sneeringer, Chris, Su, Dian, Wang, Weiru, Wu, Ping, Moffat, John G, Heffron, Timothy P, Choo, Edna F, Chan, Bryan K

“…Hematopoietic progenitor kinase 1 (HPK1) serves a key immunosuppressive role as a negative regulator of T-cell receptor (TCR) signaling. HPK1 loss-of-function…”
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