Search Results - "Lyne, Paul"

BRD4 amplification facilitates an oncogenic gene expression program in high-grade serous ovarian cancer and confers sensitivity to BET inhibitors by Rhyasen, Garrett W, Yao, Yi, Zhang, Jingwen, Dulak, Austin, Castriotta, Lillian, Jacques, Kelly, Zhao, Wei, Gharahdaghi, Farzin, Hattersley, Maureen M, Lyne, Paul D, Clark, Edwin, Zinda, Michael, Fawell, Stephen E, Mills, Gordon B, Chen, Huawei

“…BRD4 is a transcriptional co-activator functioning to recruit regulatory complexes to acetylated chromatin. A subset of High-grade Serous Ovarian Cancer…”
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Accurate Prediction of the Relative Potencies of Members of a Series of Kinase Inhibitors Using Molecular Docking and MM-GBSA Scoring by Lyne, Paul D, Lamb, Michelle L, Saeh, Jamal C

“…The ability of molecular docking, using the program Glide and an MM-GBSA postdocking scoring protocol, to correctly rank a number of congeneric kinase…”
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AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia by Keeton, Erika K., McEachern, Kristen, Dillman, Keith S., Palakurthi, Sangeetha, Cao, Yichen, Grondine, Michael R., Kaur, Surinder, Wang, Suping, Chen, Yuching, Wu, Allan, Shen, Minhui, Gibbons, Francis D., Lamb, Michelle L., Zheng, Xiaolan, Stone, Richard M., DeAngelo, Daniel J., Platanias, Leonidas C., Dakin, Les A., Chen, Huawei, Lyne, Paul D., Huszar, Dennis

“…Upregulation of Pim kinases is observed in several types of leukemias and lymphomas. Pim-1, -2, and -3 promote cell proliferation and survival downstream of…”
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Structure-based virtual screening: an overview by Lyne, Paul D

“…Enormous advances in genomics have resulted in a large increase in the number of potential therapeutic targets that are available for investigation. This…”
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AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies by Rhyasen, Garrett W, Hattersley, Maureen M, Yao, Yi, Dulak, Austin, Wang, Wenxian, Petteruti, Philip, Dale, Ian L, Boiko, Scott, Cheung, Tony, Zhang, Jingwen, Wen, Shenghua, Castriotta, Lillian, Lawson, Deborah, Collins, Michael, Bao, Larry, Ahdesmaki, Miika J, Walker, Graeme, O'Connor, Greg, Yeh, Tammie C, Rabow, Alfred A, Dry, Jonathan R, Reimer, Corinne, Lyne, Paul, Mills, Gordon B, Fawell, Stephen E, Waring, Michael J, Zinda, Michael, Clark, Edwin, Chen, Huawei

“…The bromodomain and extraterminal (BET) protein BRD4 regulates gene expression via recruitment of transcriptional regulatory complexes to acetylated chromatin…”
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Discovery of (2R)‑N‑[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]‑1H‑indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor by Su, Qibin, Banks, Erica, Bebernitz, Geraldine, Bell, Kirsten, Borenstein, Cassandra F, Chen, Huawei, Chuaqui, Claudio E, Deng, Nanhua, Ferguson, Andrew D, Kawatkar, Sameer, Grimster, Neil P, Ruston, Linette, Lyne, Paul D, Read, Jon A, Peng, Xianyou, Pei, Xiaohui, Fawell, Stephen, Tang, Zhanlei, Throner, Scott, Vasbinder, Melissa M, Wang, Haoyu, Winter-Holt, Jon, Woessner, Richard, Wu, Allan, Yang, Wenzhan, Zinda, Michael, Kettle, Jason G

“…JAK1, JAK2, JAK3, and TYK2 belong to the JAK (Janus kinase) family. They play critical roles in cytokine signaling. Constitutive activation of JAK/STAT…”
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STAT3 antisense oligonucleotide AZD9150 in a subset of patients with heavily pretreated lymphoma: results of a phase 1b trial by Reilley, Matthew J, McCoon, Patricia, Cook, Carl, Lyne, Paul, Kurzrock, Razelle, Kim, Youngsoo, Woessner, Richard, Younes, Anas, Nemunaitis, John, Fowler, Nathan, Curran, Michael, Liu, Qinying, Zhou, Tianyuan, Schmidt, Joanna, Jo, Minji, Lee, Samantha J, Yamashita, Mason, Hughes, Steven G, Fayad, Luis, Piha-Paul, Sarina, Nadella, Murali V P, Xiao, Xiaokun, Hsu, Jeff, Revenko, Alexey, Monia, Brett P, MacLeod, A Robert, Hong, David S

“…The Janus kinase (JAK) and signal transduction and activation of transcription (STAT) signaling pathway is an attractive target in multiple cancers. Activation…”
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On Evaluating Molecular-Docking Methods for Pose Prediction and Enrichment Factors by Chen, Hongming, Lyne, Paul D, Giordanetto, Fabrizio, Lovell, Timothy, Li, Jin

“…Four of the most well-known, commercially available docking programs, FlexX, GOLD, GLIDE, and ICM, have been examined for their ligand-docking and…”
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Pharmacological Inhibition of PARP6 Triggers Multipolar Spindle Formation and Elicits Therapeutic Effects in Breast Cancer by Wang, Zebin, Grosskurth, Shaun E, Cheung, Tony, Petteruti, Philip, Zhang, Jingwen, Wang, Xin, Wang, Wenxian, Gharahdaghi, Farzin, Wu, Jiaquan, Su, Nancy, Howard, Ryan T, Mayo, Michele, Widzowski, Dan, Scott, David A, Johannes, Jeffrey W, Lamb, Michelle L, Lawson, Deborah, Dry, Jonathan R, Lyne, Paul D, Tate, Edward W, Zinda, Michael, Mikule, Keith, Fawell, Stephen E, Reimer, Corinne, Chen, Huawei

“…: PARP proteins represent a class of post-translational modification enzymes with diverse cellular functions. Targeting PARPs has proven to be efficacious…”
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Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases by Dakin, Les A., Block, Michael H., Chen, Huawei, Code, Erin, Dowling, James E., Feng, Xiaomei, Ferguson, Andrew D., Green, Isabelle, Hird, Alexander W., Howard, Tina, Keeton, Erika K., Lamb, Michelle L., Lyne, Paul D., Pollard, Hannah, Read, Jon, Wu, Allan J., Zhang, Tao, Zheng, Xiaolan

“…Novel substituted benzylidene-1,3-thiazolidine-2,4-diones (TZDs) have been identified as potent and highly selective inhibitors of the PIM kinases. The…”
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Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors by Yang, Bin, Vasbinder, Melissa M, Hird, Alexander W, Su, Qibin, Wang, Haixia, Yu, Yan, Toader, Dorin, Lyne, Paul D, Read, Jon A, Breed, Jason, Ioannidis, Stephanos, Deng, Chun, Grondine, Michael, DeGrace, Nancy, Whitston, David, Brassil, Patrick, Janetka, James W

“…Checkpoint kinase 1 (CHK1) inhibitors are potential cancer therapeutics that can be utilized for enhancing the efficacy of DNA damaging agents. Multiple small…”
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Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering by Johannes, Jeffrey W., Almeida, Lynsie, Daly, Kevin, Ferguson, Andrew D., Grosskurth, Shaun E., Guan, Huiping, Howard, Tina, Ioannidis, Stephanos, Kazmirski, Steven, Lamb, Michelle L., Larsen, Nicholas A., Lyne, Paul D., Mikule, Keith, Ogoe, Claude, Peng, Bo, Petteruti, Philip, Read, Jon A., Su, Nancy, Sylvester, Mark, Throner, Scott, Wang, Wenxian, Wang, Xin, Wu, Jiaquan, Ye, Qing, Yu, Yan, Zheng, Xiaolan, Scott, David A.

“…[Display omitted] The propensity for cancer cells to accumulate additional centrosomes relative to normal cells could be exploited for therapeutic benefit in…”
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Direct targeting of FOXP3 in Tregs with AZD8701, a novel antisense oligonucleotide to relieve immunosuppression in cancer by Revenko, Alexey, Carnevalli, Larissa S, Sinclair, Charles, Johnson, Ben, Peter, Alison, Taylor, Molly, Hettrick, Lisa, Chapman, Melissa, Klein, Stephanie, Solanki, Anisha, Gattis, Danielle, Watt, Andrew, Hughes, Adina M, Magiera, Lukasz, Kar, Gozde, Ireland, Lucy, Mele, Deanna A, Sah, Vasu, Singh, Maneesh, Walton, Josephine, Mairesse, Maelle, King, Matthew, Edbrooke, Mark, Lyne, Paul, Barry, Simon T, Fawell, Stephen, Goldberg, Frederick W, MacLeod, A Robert

“…BackgroundThe Regulatory T cell (Treg) lineage is defined by the transcription factor FOXP3, which controls immune-suppressive gene expression profiles. Tregs…”
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Discovery of (2 R )- N -[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1 H -indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor by Su, Qibin, Banks, Erica, Bebernitz, Geraldine, Bell, Kirsten, Borenstein, Cassandra F, Chen, Huawei, Chuaqui, Claudio E, Deng, Nanhua, Ferguson, Andrew D, Kawatkar, Sameer, Grimster, Neil P, Ruston, Linette, Lyne, Paul D, Read, Jon A, Peng, Xianyou, Pei, Xiaohui, Fawell, Stephen, Tang, Zhanlei, Throner, Scott, Vasbinder, Melissa M, Wang, Haoyu, Winter-Holt, Jon, Woessner, Richard, Wu, Allan, Yang, Wenzhan, Zinda, Michael, Kettle, Jason G

“…JAK1, JAK2, JAK3, and TYK2 belong to the JAK (Janus kinase) family. They play critical roles in cytokine signaling. Constitutive activation of JAK/STAT…”
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Discovery of Checkpoint Kinase Inhibitor (S)-5-(3-Fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by Structure-Based Design and Optimization of Thiophenecarboxamide Ureas by Oza, Vibha, Ashwell, Susan, Almeida, Lynsie, Brassil, Patrick, Breed, Jason, Deng, Chun, Gero, Thomas, Grondine, Michael, Horn, Candice, Ioannidis, Stephanos, Liu, Dongfang, Lyne, Paul, Newcombe, Nicholas, Pass, Martin, Read, Jon, Ready, Shannon, Rowsell, Siân, Su, Mei, Toader, Dorin, Vasbinder, Melissa, Yu, Dingwei, Yu, Yan, Xue, Yafeng, Zabludoff, Sonya, Janetka, James

“…Checkpoint kinases CHK1 and CHK2 are activated in response to DNA damage that results in cell cycle arrest, allowing sufficient time for DNA repair. Agents…”
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Discovery of 2,6-disubstituted pyrazine derivatives as inhibitors of CK2 and PIM kinases by Gingipalli, Lakshmaiah, Block, Michael H., Bao, Larry, Cooke, Emma, Dakin, Les A., Denz, Christopher R., Ferguson, Andrew D., Johannes, Jeffrey W., Larsen, Nicholas A., Lyne, Paul D., Pontz, Timothy W., Wang, Tao, Wu, Xiaoyun, Wu, Allan, Zhang, Hai-Jun, Zheng, Xiaolan, Dowling, James E., Lamb, Michelle L.

“…[Display omitted] The design and synthesis of a novel series of 2,6-disubstituted pyrazine derivatives as CK2 kinase inhibitors is described. Structure-guided…”
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Potent and Selective CK2 Kinase Inhibitors with Effects on Wnt Pathway Signaling in Vivo by Dowling, James E, Alimzhanov, Marat, Bao, Larry, Chuaqui, Claudio, Denz, Christopher R, Jenkins, Emma, Larsen, Nicholas A, Lyne, Paul D, Pontz, Timothy, Ye, Qing, Holdgate, Geoff A, Snow, Lindsay, O’Connell, Nichole, Ferguson, Andrew D

“…The Wnt pathway is an evolutionarily conserved and tightly regulated signaling network with important roles in embryonic development and adult tissue…”
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Modulating the strength of hydrogen bond acceptors to achieve low Caco2 efflux for oral bioavailability of PARP inhibitors blocking centrosome clustering by Gu, Chungang, Lamb, Michelle L., Johannes, Jeffrey W., Sylvester, Mark A., Eisman, Mark S., Harrison, Rane A., Hu, Haiqing, Kazmirski, Steven, Mikule, Keith, Peng, Bo, Su, Nancy, Wang, Wenxian, Ye, Qing, Zheng, Xiaolan, Lyne, Paul D., Scott, David A.

“…[Display omitted] During the lead generation and optimization of PARP inhibitors blocking centrosome clustering, it was discovered that increasing hydrogen…”
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Abstract 979: Discovery of the JAK1 selective kinase inhibitor AZD4205 by Kettle, Jason G., Su, Qibin, Grimster, Neil, Kawatkar, Sameer, Throner, Scott, Woessner, Richard, Chen, Huawei, Bebernitz, Geraldine, Bell, Kristen, Anderson, Erica, Ruston, Linette, Winter-Holt, Jon, Lyne, Paul, Vasbinder, Melissa, Chuaqui, Claudio

“…Abstract Janus kinases are a family of four enzymes; JAK1, JAK2, JAK3 and tyrosine kinase 2 (TYK2) that are critical in cytokine signalling, with constitutive…”
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Identification of 4-Aminopyrazolylpyrimidines as Potent Inhibitors of Trk Kinases by Wang, Tao, Lamb, Michelle L, Scott, David A, Wang, Haixia, Block, Michael H, Lyne, Paul D, Lee, John W, Davies, Audrey M, Zhang, Hai-Jun, Zhu, Yanyi, Gu, Fei, Han, Yongxin, Wang, Bin, Mohr, Peter J, Kaus, Robert J, Josey, John A, Hoffmann, Ethan, Thress, Ken, MacIntyre, Terry, Wang, Haiyun, Omer, Charles A, Yu, Dingwei

“…The design, synthesis and biological evaluation of a series of 4-aminopyrazolylpyrimidines as potent Trk kinase inhibitors is reported. High-throughput…”
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