Search Results - "Karen Maegley"

Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance by Brooun, Alexei, Gajiwala, Ketan S., Deng, Ya-Li, Liu, Wei, Bolaños, Ben, Bingham, Patrick, He, You-Ai, Diehl, Wade, Grable, Nicole, Kung, Pei-Pei, Sutton, Scott, Maegley, Karen A., Yu, Xiu, Stewart, Al E.

“…Polycomb repressive complex 2 (PRC2) mediates gene silencing through chromatin reorganization by methylation of histone H3 lysine 27 (H3K27). Overexpression of…”
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Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497) by Kung, Pei-Pei, Bingham, Patrick, Brooun, Alexei, Collins, Michael, Deng, Ya-Li, Dinh, Dac, Fan, Connie, Gajiwala, Ketan S, Grantner, Rita, Gukasyan, Hovhannes J, Hu, Wenyue, Huang, Buwen, Kania, Robert, Kephart, Susan E, Krivacic, Cody, Kumpf, Robert A, Khamphavong, Penney, Kraus, Manfred, Liu, Wei, Maegley, Karen A, Nguyen, Lisa, Ren, Shijian, Richter, Dan, Rollins, Robert A, Sach, Neal, Sharma, Shikhar, Sherrill, John, Spangler, Jillian, Stewart, Albert E, Sutton, Scott, Uryu, Sean, Verhelle, Dominique, Wang, Hui, Wang, Shuiwang, Wythes, Martin, Xin, Shuibo, Yamazaki, Shinji, Zhu, Huichun, Zhu, JinJiang, Zehnder, Luke, Edwards, Martin

“…A new series of lactam-derived EZH2 inhibitors was designed via ligand-based and physicochemical-property-based strategies to address metabolic stability and…”
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Discovery of a Novel and Selective Indoleamine 2,3-Dioxygenase (IDO-1) Inhibitor 3‑(5-Fluoro‑1H‑indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and Its Characterization as a Potential Clinical Candidate by Crosignani, Stefano, Bingham, Patrick, Bottemanne, Pauline, Cannelle, Hélène, Cauwenberghs, Sandra, Cordonnier, Marie, Dalvie, Deepak, Deroose, Frederik, Feng, Jun Li, Gomes, Bruno, Greasley, Samantha, Kaiser, Stephen E, Kraus, Manfred, Négrerie, Michel, Maegley, Karen, Miller, Nichol, Murray, Brion W, Schneider, Manfred, Soloweij, James, Stewart, Albert E, Tumang, Joseph, Torti, Vince R, Van Den Eynde, Benoit, Wythes, Martin

“…Tumors use tryptophan-catabolizing enzymes such as indoleamine 2,3-dioxygenase (IDO-1) to induce an immunosuppressive environment. IDO-1 is induced in response…”
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Conserved RNA-binding specificity of polycomb repressive complex 2 is achieved by dispersed amino acid patches in EZH2 by Long, Yicheng, Bolanos, Ben, Gong, Lihu, Liu, Wei, Goodrich, Karen J, Yang, Xin, Chen, Siming, Gooding, Anne R, Maegley, Karen A, Gajiwala, Ketan S, Brooun, Alexei, Cech, Thomas R, Liu, Xin

“…Polycomb repressive complex 2 (PRC2) is a key chromatin modifier responsible for methylation of lysine 27 in histone H3. PRC2 has been shown to interact with…”
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SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance by Jensen-Pergakes, Kristen, Tatlock, John, Maegley, Karen A, McAlpine, Indrawan J, McTigue, Michele, Xie, Tao, Dillon, Christopher P, Wang, Yuli, Yamazaki, Shinji, Spiegel, Noah, Shi, Manli, Nemeth, Amy, Miller, Natalie, Hendrickson, Eleanore, Lam, Hieu, Sherrill, John, Chung, Chi-Yeh, McMillan, Elizabeth A, Bryant, Shannon Karlicek, Palde, Prakash, Braganza, John, Brooun, Alexei, Deng, Ya-Li, Goshtasbi, Vesta, Kephart, Susan E, Kumpf, Robert A, Liu, Wei, Patman, Ryan L, Rui, Eugene, Scales, Stephanie, Tran-Dube, Michelle, Wang, Fen, Wythes, Martin, Paul, Thomas A

“…Protein arginine methyltransferase 5 (PRMT5) overexpression in hematologic and solid tumors methylates arginine residues on cellular proteins involved in…”
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Characterization of the Selective Indoleamine 2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy by Gomes, Bruno, Driessens, Gregory, Bartlett, Derek, Cai, Danying, Cauwenberghs, Sandra, Crosignani, Stefano, Dalvie, Deepak, Denies, Sofie, Dillon, Christopher P, Fantin, Valeria R, Guo, Jie, Letellier, Marie-Claire, Li, Wenlin, Maegley, Karen, Marillier, Reece, Miller, Nichol, Pirson, Romain, Rabolli, Virginie, Ray, Chad, Streiner, Nicole, Torti, Vince R, Tsaparikos, Konstantinos, Van den Eynde, Benoit J, Wythes, Martin, Yao, Li-Chin, Zheng, Xianxian, Tumang, Joseph, Kraus, Manfred

“…Tumors use indoleamine 2,3-dioxygenase-1 (IDO1) as a major mechanism to induce an immunosuppressive microenvironment. IDO1 expression is upregulated in many…”
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Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial by Thomas, Huw D, Calabrese, Christopher R, Batey, Michael A, Canan, Stacie, Hostomsky, Zdenek, Kyle, Suzanne, Maegley, Karen A, Newell, David R, Skalitzky, Donald, Wang, Lan-Zhen, Webber, Stephen E, Curtin, Nicola J

“…Poly(ADP-ribose) polymerase (PARP)-1 (EC 2.4.2.30) is a nuclear enzyme that promotes the base excision repair of DNA breaks. Inhibition of PARP-1 enhances the…”
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Structure of HIV-1 Reverse Transcriptase with the Inhibitor β-Thujaplicinol Bound at the RNase H Active Site by Himmel, Daniel M., Maegley, Karen A., Pauly, Tom A., Bauman, Joseph D., Das, Kalyan, Dharia, Chhaya, Clark, Arthur D., Ryan, Kevin, Hickey, Michael J., Love, Robert A., Hughes, Stephen H., Bergqvist, Simon, Arnold, Eddy

“…Novel inhibitors are needed to counteract the rapid emergence of drug-resistant HIV variants. HIV-1 reverse transcriptase (RT) has both DNA polymerase and…”
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SAH derived potent and selective EZH2 inhibitors by Kung, Pei-Pei, Huang, Buwen, Zehnder, Luke, Tatlock, John, Bingham, Patrick, Krivacic, Cody, Gajiwala, Ketan, Diehl, Wade, Yu, Xiu, Maegley, Karen A.

“…[Display omitted] A series of novel enhancer of zeste homolog 2 (EZH2) inhibitors was designed based on the chemical structure of the histone methyltransferase…”
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Characterization of Specific N -α-Acetyltransferase 50 (Naa50) Inhibitors Identified Using a DNA Encoded Library by Kung, Pei-Pei, Bingham, Patrick, Burke, Benjamin J., Chen, Qiuxia, Cheng, Xuemin, Deng, Ya-Li, Dou, Dengfeng, Feng, Junli, Gallego, Gary M., Gehring, Michael R., Grant, Stephan K., Greasley, Samantha, Harris, Anthony R., Maegley, Karen A., Meier, Jordan, Meng, Xiaoyun, Montano, Jose L., Morgan, Barry A., Naughton, Brigitte S., Palde, Prakash B., Paul, Thomas A., Richardson, Paul, Sakata, Sylvie, Shaginian, Alex, Sonnenburg, William K., Subramanyam, Chakrapani, Timofeevski, Sergei, Wan, Jinqiao, Yan, Wen, Stewart, Albert E.

“…Two novel compounds were identified as Naa50 binders/inhibitors using DNA-encoded technology screening. Biophysical and biochemical data as well as cocrystal…”
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Comparison of a High-Throughput Mass Spectrometry Method and Radioactive Filter Binding to Assay the Protein Methyltransferase PRMT5 by Maegley, Karen A, Krivacic, Cody, Bingham, Patrick, Liu, Wei, Brooun, Alexei

“…Conformational remodeling of chromatin in cells is known to alter gene expression. The histone code hypothesis postulates that multiple modifications present…”
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Ack1: activation and regulation by allostery by Gajiwala, Ketan S, Maegley, Karen, Ferre, RoseAnn, He, You-Ai, Yu, Xiu

“…The non-receptor tyrosine kinase Ack1 belongs to a unique multi-domain protein kinase family, Ack. Ack is the only family of SH3 domain containing kinases to…”
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Correction to Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)‑ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors by Kung, Pei-Pei, Rui, Eugene, Bergqvist, Simon, Bingham, Patrick, Braganza, John, Collins, Michael, Cui, Mei, Diehl, Wade, Dinh, Dac, Fan, Connie, Fantin, Valeria R, Gukasyan, Hovhannes J, Hu, Wenyue, Huang, Buwen, Kephart, Susan, Krivacic, Cody, Kumpf, Robert A, Li, Gary, Maegley, Karen A, McAlpine, Indrawan, Nguyen, Lisa, Ninkovic, Sacha, Ornelas, Martha, Ryskin, Michael, Scales, Stephanie, Sutton, Scott, Tatlock, John, Verhelle, Dominique, Wang, Fen, Wells, Peter, Wythes, Martin, Yamazaki, Shinji, Yip, Brian, Yu, Xiu, Zehnder, Luke, Zhang, Wei-Guo, Rollins, Robert A, Edwards, Martin

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Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)‑ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors by Kung, Pei-Pei, Rui, Eugene, Bergqvist, Simon, Bingham, Patrick, Braganza, John, Collins, Michael, Cui, Mei, Diehl, Wade, Dinh, Dac, Fan, Connie, Fantin, Valeria R, Gukasyan, Hovhannes J, Hu, Wenyue, Huang, Buwen, Kephart, Susan, Krivacic, Cody, Kumpf, Robert A, Li, Gary, Maegley, Karen A, McAlpine, Indrawan, Nguyen, Lisa, Ninkovic, Sacha, Ornelas, Martha, Ryskin, Michael, Scales, Stephanie, Sutton, Scott, Tatlock, John, Verhelle, Dominique, Wang, Fen, Wells, Peter, Wythes, Martin, Yamazaki, Shinji, Yip, Brian, Yu, Xiu, Zehnder, Luke, Zhang, Wei-Guo, Rollins, Robert A, Edwards, Martin

“…A new enhancer of zeste homolog 2 (EZH2) inhibitor series comprising a substituted phenyl ring joined to a dimethylpyridone moiety via an amide linkage has…”
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Resistance-Modifying Agents. 9. Synthesis and Biological Properties of Benzimidazole Inhibitors of the DNA Repair Enzyme Poly(ADP-ribose) Polymerase by White, Alex W, Almassy, Robert, Calvert, A. Hilary, Curtin, Nicola J, Griffin, Roger J, Hostomsky, Zdenek, Maegley, Karen, Newell, David R, Srinivasan, Sheila, Golding, Bernard T

“…The nuclear enzyme poly(ADP-ribose) polymerase (PARP) facilitates the repair of DNA strand breaks and is implicated in the resistance of cancer cells to…”
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Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone by KUNG, Pei-Pei, FUNK, Lee, RODGERS, Caroline, DAVIES, Jay F, BAYMAN, Eileen, SMEAL, Tod, MAEGLEY, Karen A, GEHRING, Michael R, MENG, Jerry, COLLINS, Michael, ZHONGXIANG ZHOU, Joe, JOHNSON, M. Catherine, EKKER, Anne, WANG, Jeff, MEHTA, Pramod, YIN, Min-Jean

“…Information from X-ray crystal structures were used to optimize the potency of a HTS hit in a Hsp90 competitive binding assay. A class of novel and potent…”
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Tricyclic Benzimidazoles as Potent Poly(ADP-ribose) Polymerase-1 Inhibitors by Skalitzky, Donald J, Marakovits, Joseph T, Maegley, Karen A, Ekker, Anne, Yu, Xiao-Hong, Hostomsky, Zdenek, Webber, Stephen E, Eastman, Brian W, Almassy, Robert, Li, Jianke, Curtin, Nicola J, Newell, David R, Calvert, A. Hilary, Griffin, Roger J, Golding, Bernard T

“…Novel tricyclic benzimidazole carboxamide poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors have been synthesized. Several compounds were found to be powerful…”
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The Crystal Structure of the RNA-Dependent RNA Polymerase from Human Rhinovirus: A Dual Function Target for Common Cold Antiviral Therapy by Love, Robert A, Maegley, Karen A, Yu, Xiu, Ferre, Rose Ann, Lingardo, Laura K, Diehl, Wade, Parge, Hans E, Dragovich, Peter S, Fuhrman, Shella A

“…Human rhinoviruses (HRV), the predominant members of the Picornaviridae family of positive-strand RNA viruses, are the major causative agents of the common…”
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Novel Tricyclic Poly(ADP-ribose) Polymerase-1 Inhibitors with Potent Anticancer Chemopotentiating Activity:  Design, Synthesis, and X-ray Cocrystal Structure by Canan Koch, Stacie S, Thoresen, Lars H, Tikhe, Jayashree G, Maegley, Karen A, Almassy, Robert J, Li, Jianke, Yu, Xiao-Hong, Zook, Scott E, Kumpf, Robert A, Zhang, Cathy, Boritzki, Theodore J, Mansour, Rena N, Zhang, Kanyin E, Ekker, Anne, Calabrese, Chris R, Curtin, Nicola J, Kyle, Suzanne, Thomas, Huw D, Wang, Lan-Zhen, Calvert, A. Hilary, Golding, Bernard T, Griffin, Roger J, Newell, David R, Webber, Stephen E, Hostomsky, Zdenek

“…A series of novel compounds have been designed that are potent inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1), and the activity and physical properties…”
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Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors by White, Alex W., Curtin, Nicola J., Eastman, Brian W., Golding, Bernard T., Hostomsky, Zdenek, Kyle, Suzanne, Li, Jianke, Maegley, Karen A., Skalitzky, Donald J., Webber, Stephen E., Yu, Xiao-Hong, Griffin, Roger J.

“…The synthesis and biological evaluation of a new series of amine-substituted 2-arylbenzimidazole-4-carboxamide inhibitors of the DNA-repair enzyme…”
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