Search Results - "Dillman, Keith"

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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Mechanism for the allosteric regulation of phosphodiesterase 2A deduced from the X-ray structure of a near full-length construct by Pandit, Jayvardhan, Forman, Michael D, Fennell, Kimberly F, Dillman, Keith S, Menniti, Frank S

“…We report the X-ray crystal structure of a phosphodiesterase (PDE) that includes both catalytic and regulatory domains. PDE2A (215-900) crystallized as a dimer…”
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Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4 by Degorce, Sébastien L., Anjum, Rana, Dillman, Keith S., Drew, Lisa, Groombridge, Sam D., Halsall, Christopher T., Lenz, Eva M., Lindsay, Nicola A., Mayo, Michele F., Pink, Jennifer H., Robb, Graeme R., Scott, James S., Stokes, Stephen, Xue, Yafeng

“…[Display omitted] We have developed a series of orally efficacious IRAK4 inhibitors, based on a scaffold hopping strategy and using rational structure based…”
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Discovery of a Series of 5‑Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88L265P Mutant Diffuse Large B Cell Lymphoma by Degorce, Sébastien L, Anjum, Rana, Bloecher, Andrew, Carbajo, Rodrigo J, Dillman, Keith S, Drew, Lisa, Halsall, Christopher T, Lenz, Eva M, Lindsay, Nicola A, Mayo, Michele F, Pink, Jennifer H, Robb, Graeme R, Rosen, Alan, Scott, James S, Xue, Yafeng

“…In this article, we report the discovery of a series of 5-azaquinazolines as selective IRAK4 inhibitors. From modestly potent quinazoline 4, we introduced a…”
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Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88 L265P Mutant Diffuse Large B Cell Lymphoma by Degorce, Sébastien L, Anjum, Rana, Bloecher, Andrew, Carbajo, Rodrigo J, Dillman, Keith S, Drew, Lisa, Halsall, Christopher T, Lenz, Eva M, Lindsay, Nicola A, Mayo, Michele F, Pink, Jennifer H, Robb, Graeme R, Rosen, Alan, Scott, James S, Xue, Yafeng

“…In this article, we report the discovery of a series of 5-azaquinazolines as selective IRAK4 inhibitors. From modestly potent quinazoline , we introduced a…”
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Structure Guided Development of Novel Thymidine Mimetics Targeting Pseudomonas aeruginosa Thymidylate Kinase: From Hit to Lead Generation by Choi, Jun Yong, Plummer, Mark S, Starr, Jeremy, Desbonnet, Charlene R, Soutter, Holly, Chang, Jeanne, Miller, J. Richard, Dillman, Keith, Miller, Alita A, Roush, William R

“…Thymidylate kinase (TMK) is a potential chemotherapeutic target because it is directly involved in the synthesis of an essential component, thymidine…”
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Structural basis for the catalytic mechanism of human phosphodiesterase 9 by Liu, Shenping, Mansour, Mahmoud N, Dillman, Keith S, Perez, Jose R, Danley, Dennis E, Aeed, Paul A, Simons, Samuel P, LeMotte, Peter K, Menniti, Frank S

“…The phosphodiesterases (PDEs) are metal ion-dependent enzymes that regulate cellular signaling by metabolic inactivation of the ubiquitous second messengers…”
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Next-generation sequencing identifies a novel ELAVL1-TYK2 fusion gene in MOLM-16, an AML cell line highly sensitive to the PIM kinase inhibitor AZD1208 by Tron, Adriana E., Keeton, Erika K., Ye, Minwei, Casas-Selves, Matias, Chen, Huawei, Dillman, Keith S., Gale, Rosemary E., Stengel, Chloe, Zinda, Michael, Linch, David C., Lai, Zhongwu, Khwaja, Asim, Huszar, Dennis

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Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin‑1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B‑Cell Lymphoma by Scott, James S, Degorce, Sébastien L, Anjum, Rana, Culshaw, Janet, Davies, Robert D. M, Davies, Nichola L, Dillman, Keith S, Dowling, James E, Drew, Lisa, Ferguson, Andrew D, Groombridge, Sam D, Halsall, Christopher T, Hudson, Julian A, Lamont, Scott, Lindsay, Nicola A, Marden, Stacey K, Mayo, Michele F, Pease, J. Elizabeth, Perkins, David R, Pink, Jennifer H, Robb, Graeme R, Rosen, Alan, Shen, Minhui, McWhirter, Claire, Wu, Dedong

“…Herein we report the optimization of a series of pyrrolopyrimidine inhibitors of interleukin-1 receptor associated kinase 4 (IRAK4) using X-ray crystal…”
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Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88 L265P Diffuse Large B-Cell Lymphoma by Scott, James S, Degorce, Sébastien L, Anjum, Rana, Culshaw, Janet, Davies, Robert D M, Davies, Nichola L, Dillman, Keith S, Dowling, James E, Drew, Lisa, Ferguson, Andrew D, Groombridge, Sam D, Halsall, Christopher T, Hudson, Julian A, Lamont, Scott, Lindsay, Nicola A, Marden, Stacey K, Mayo, Michele F, Pease, J Elizabeth, Perkins, David R, Pink, Jennifer H, Robb, Graeme R, Rosen, Alan, Shen, Minhui, McWhirter, Claire, Wu, Dedong

“…Herein we report the optimization of a series of pyrrolopyrimidine inhibitors of interleukin-1 receptor associated kinase 4 (IRAK4) using X-ray crystal…”
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Towards the next generation of dual Bcl-2/Bcl-xL inhibitors by Varnes, Jeffrey G., Gero, Thomas, Huang, Shan, Diebold, R. Bruce, Ogoe, Claude, Grover, Paul T., Su, Mei, Mukherjee, Prasenjit, Saeh, Jamal Carlos, MacIntyre, Terry, Repik, Galina, Dillman, Keith, Byth, Kate, Russell, Daniel John, Ioannidis, Stephanos

“…Structural modifications of the left-hand side of compound 1 were identified which retained or improved potent binding to Bcl-2 and Bcl-xL in in vitro…”
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cAMP-Dependent Protein Kinase Mediates Activity-Regulated Synaptic Targeting of NMDA Receptors by Crump, F. Thomas, Dillman, Keith S, Craig, Ann Marie

“…Chronic activity blockade increases synaptic levels of NMDA receptor immunoreactivity in hippocampal neurons. We show here that blockade-induced synaptic NMDA…”
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Development of a Series of Pyrrolopyridone MAT2A Inhibitors by Atkinson, Stephen J., Bagal, Sharan K., Argyrou, Argyrides, Askin, Sean, Cheung, Tony, Chiarparin, Elisabetta, Coen, Muireann, Collie, Iain T., Dale, Ian L., De Fusco, Claudia, Dillman, Keith, Evans, Laura, Feron, Lyman J., Foster, Alison J., Grondine, Michael, Kantae, Vasudev, Lamont, Gillian M., Lamont, Scott, Lynch, James T., Nilsson Lill, Sten, Robb, Graeme R., Saeh, Jamal, Schimpl, Marianne, Scott, James S., Smith, James, Srinivasan, Bharath, Tentarelli, Sharon, Vazquez-Chantada, Mercedes, Wagner, David, Walsh, Jarrod J., Watson, David, Williamson, Beth

“…The optimization of an allosteric fragment, discovered by differential scanning fluorimetry, to an in vivo MAT2a tool inhibitor is discussed. The…”
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Application of Hyperpolarized 13C Magnetic Resonance Imaging to Detect Target Inhibition of NFkB Activation in Preclinical Patient-Derived Models of CNS Lymphoma by Geng, Huimin, Tiret, Brice, Gao, Hua-Xin, Kadoch, Cigall, Lu, Ming, Chen, Lingjing, Park, Ilwoo, Melkus, Gerd, Elkhaled, Adam, Kurhanewicz, John, Drew, Lisa, Degorce, Sebastien, Mayo, Michele, Dillman, Keith, Anjum, Rana, Bloecher, Andrew, Chaumeil, Myriam, Rubenstein, James

“…To gain insights into the tumor microenvironment in primary and secondary CNS lymphomas, we applied LC/MS and GC/MS for differential metabolomic profiling of…”
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Mechanism for the allosteric regulation of phosphodiesterase 2A deduced from the X-ray structure of a near full-length construct by Pandit, Jayvardhan, Forman, Michael D., Fennell, Kimberly F., Dillman, Keith S., Menniti, Frank S.

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EXTH-71. HYPERPOLARIZED [1-13C] PYRUVATE AS A BIOMARKER FOR TREATMENT MONITORING IN LYMPHOMA MURINE MODELS by Tiret, Brice, Autry, Adam, Park, Ilwoo, Lu, Ming, Anjum, Rana, Drew, Liza, Degorce, Sebastien, Mayo, Michele, Dillman, Keith, Rubenstein, James, Chaumeil, Myriam M

“…In primary central nervous system lymphoma (PCNSL), L265P mutation of the myeloid differentiation 88 (MYD88) protein is the most common, and induces a…”
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Targeting NF-KB Activation in Novel Intracranial Models of CNS Lymphoma by Geng, Huimin, Gao, Huaxin, Kadoch, Cigall, Lu, Ming, Chen, Lingjing, Anjum, Rana, Drew, Lisa, Degorce, Sebastien, Dillman, Keith, Mayo, Michele, Anderson, Shawn, Collins, Colin, Lowell, Clifford A., Rubenstein, James L.

“…Among the clinical subtypes of diffuse large B-cell lymphoma, central nervous system (CNS) lymphomas, both primary (PCNSL) and secondary (SCNSL), are generally…”
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Abstract 2063: A novel ELAVL1-TYK2 fusion protein drives STAT3/5 activation and PIM-1 expression, survival and growth in the MOLM-16 acute myeloid leukemia cell line by McEachern, Kristen, Keeton, Erika, Dillman, Keith, Ye, Minwei, Stengel, Chloe, Chen, Huawei, Wang, Suping, Grosskurth, Shaun, Gale, Rosemary E., Linch, David C., Khwaja, Asim, Lai, Zhongwu, Huszar, Dennis

“…Abstract Pim kinases are upregulated in leukemias and lymphomas and mediate cell growth and survival. Acute myeloid leukemia cell lines sensitive to the…”
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High-content screening for compounds that affect mtDNA-encoded protein levels in eukaryotic cells by Nadanaciva, Sashi, Dillman, Keith, Gebhard, David F, Shrikhande, Alka, Will, Yvonne

“…Compounds that interfere with the synthesis of either mitochondrial DNA or mtDNA-encoded proteins reduce the levels of 13 proteins essential for oxidative…”
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Towards the next generation of dual Bcl-2/Bcl-x sub(L) inhibitors by Varnes, Jeffrey G, Gero, Thomas, Huang, Shan, Diebold, RBruce, Ogoe, Claude, Grover, Paul T, Su, Mei, Mukherjee, Prasenjit, Saeh, Jamal Carlos, MacIntyre, Terry, Repik, Galina, Dillman, Keith, Byth, Kate, Russell, Daniel John, Ioannidis, Stephanos

“…Structural modifications of the left-hand side of compound 1 were identified which retained or improved potent binding to Bcl-2 and Bcl-x sub(L) in in vitro…”
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