Search Results - "Duke, Gerald J."

Structural basis for CARM1 inhibition by indole and pyrazole inhibitors by Sack, John S, Thieffine, Sandrine, Bandiera, Tiziano, Fasolini, Marina, Duke, Gerald J, Jayaraman, Lata, Kish, Kevin F, Klei, Herbert E, Purandare, Ashok V, Rosettani, Pamela, Troiani, Sonia, Xie, Dianlin, Bertrand, Jay A

“…CARM1 (co-activator-associated arginine methyltransferase 1) is a PRMT (protein arginine N-methyltransferase) family member that catalyses the transfer of…”
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Small molecule and macrocyclic pyrazole derived inhibitors of myeloperoxidase (MPO) by Hu, Carol H., Neissel Valente, Meriah W., Halpern, O. Scott, Jusuf, Sutjano, Khan, Javed A., Locke, Gregory A., Duke, Gerald J., Liu, Xiaoqin, Duclos, Franck J., Wexler, Ruth R., Kick, Ellen K., Smallheer, Joanne M.

“…[Display omitted] Myeloperoxidase (MPO), a critical enzyme in antimicrobial host-defense, has been implicated in chronic inflammatory diseases such as coronary…”
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Triazolopyrimidines identified as reversible myeloperoxidase inhibitors by Duclos, Franck, Abell, Lynn M, Harden, David G, Pike, Kristen, Nowak, Kimberly, Locke, Gregory A, Duke, Gerald J, Liu, Xiaoqin, Fernando, Gayani, Shaw, Scott A, Vokits, Benjamin P, Wurtz, Nicholas R, Viet, Andrew, Valente, Meriah N, Stachura, Sylwia, Sleph, Paul, Khan, Javed A, Gao, Ji, Dongre, Ashok R, Zhao, Lei, Wexler, Ruth R, Gordon, David A, Kick, Ellen K

“…Myeloperoxidase, a mammalian peroxidase involved in the immune system as an anti-microbial first responder, can produce hypochlorous acid in response to…”
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Design, synthesis, functional and structural characterization of an inhibitor of N-acetylneuraminate-9-phosphate phosphatase: Observation of extensive dynamics in an enzyme/inhibitor complex by Kim, Soong-Hoon, Constantine, Keith L., Duke, Gerald J., Goldfarb, Valentina, Hunt, John T., Johnson, Stephen, Kish, Kevin, Klei, Herbert E., McDonnell, Patricia A., Metzler, William J., Mueller, Luciano, Poss, Michael A., Fairchild, Craig R., Bhide, Rajeev S.

“…The design, synthesis and characterization of a phosphonate inhibitor of N-acetylneuraminate-9-phosphate phosphatase (HDHD4) is described. Compound 3, where…”
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Assessing compound binding to the Eg5 motor domain using a thermal shift assay by McDonnell, Patricia A., Yanchunas, Joseph, Newitt, John A., Tao, Li, Kiefer, Susan E., Ortega, Marie, Kut, Stephanie, Burford, Neil, Goldfarb, Valentina, Duke, Gerald J., Shen, Henry, Metzler, William, Doyle, Michael, Chen, Zhong, Tarby, Christine, Borzilleri, Robert, Vaccaro, Wayne, Gottardis, Marco, Lu, Songfeng, Crews, Donald, Kim, Kyoung, Lombardo, Louis, Roussell, Deborah L.

“…Eg5 is a kinesin whose inhibition leads to cycle arrest during mitosis, making it a potential therapeutic target in cancers. Circular dichroism and isothermal…”
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Synthesis and SAR of new pyrrolo[2,1- f][1,2,4]triazines as potent p38α MAP kinase inhibitors by Wrobleski, Stephen T., Lin, Shuqun, Hynes, John, Wu, Hong, Pitt, Sidney, Shen, Ding Ren, Zhang, Rosemary, Gillooly, Kathleen M., Shuster, David J., McIntyre, Kim W., Doweyko, Arthur M., Kish, Kevin F., Tredup, Jeffrey A., Duke, Gerald J., Sack, John S., McKinnon, Murray, Dodd, John, Barrish, Joel C., Schieven, Gary L., Leftheris, Katerina

“…Synthesis of a novel series of substituted pyrrolo[2,1- f][1,2,4]triazines have resulted in the identification of subnanomolar inhibitors of the p38α MAP…”
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Structural basis for the high-affinity binding of pyrrolotriazine inhibitors of p38 MAP kinase by Sack, John S., Kish, Kevin F., Pokross, Matthew, Xie, Dianlin, Duke, Gerald J., Tredup, Jeffrey A., Kiefer, Susan E., Newitt, John A.

“…The crystal structure of unphosphorylated p38α MAP kinase complexed with a representative pyrrolotriazine‐based inhibitor led to the elucidation of the…”
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Fast quantitation of recombinant plasminogen activator inhibitor type 1 in bacterial lysates by micropellicular reversed-phase liquid chromatography by O’Keefe, Donald O, Duke, Gerald J

“…A rapid reversed-phase HPLC assay is described for quantitating recombinant plasminogen activator inhibitor type 1 (PAI-1) in cultures of Escherichia coli. The…”
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Abstract 1140: A novel MTA non-competitive PRMT5 inhibitor by Malik, Rohit, Park, Peter K., Barbieri, Christopher M., Blat, Yuval, Sheriff, Steven, Weigelt, Carolyn A., Kopcho, Lisa M., Celiktas, Muge, Ruzanov, Max, Naglich, Joseph G., Price, Jennifer L., Harner, Mary, Omalley, Kevin M., Deng, JIngjing, Schmitz, William, Li, Guo, Ruan, Zheming, Qin, Lan-ying, Duke, Gerald J., Rodrigo, Iyoncy, Witmer, Mark R., Harden, David G., Demes, Shilpa, Arey, Brian J., Soars, Matt, Fink, Brian E., Gavai, Ashvinikumar V., Vite, Gregory D., Voliva, Charles F.

“…Abstract The chromosome 9p21 (chr9p21) locus is deleted in almost 10% of all cancer types. This locus includes the CDKN2A gene that encodes the critical tumor…”
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Triazolopyrimidines identified as reversible myeloperoxidase inhibitorsElectronic supplementary information (ESI) available: General synthetic methods, key compound characterization, assay methods, and crystallographic information are available in the ESI. See DOI: 10.1039/c7md00268h by Duclos, Franck, Abell, Lynn M, Harden, David G, Pike, Kristen, Nowak, Kimberly, Locke, Gregory A, Duke, Gerald J, Liu, Xiaoqin, Fernando, Gayani, Shaw, Scott A, Vokits, Benjamin P, Wurtz, Nicholas R, Viet, Andrew, Valente, Meriah N, Stachura, Sylwia, Sleph, Paul, Khan, Javed A, Gao, Ji, Dongre, Ashok R, Zhao, Lei, Wexler, Ruth R, Gordon, David A, Kick, Ellen K

“…Myeloperoxidase, a mammalian peroxidase involved in the immune system as an anti-microbial first responder, can produce hypochlorous acid in response to…”
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Triazolopyrimidines identified as reversible myeloperoxidase inhibitors† †Electronic supplementary information (ESI) available: General synthetic methods, key compound characterization, assay methods, and crystallographic information are available in the ESI. See DOI: 10.1039/c7md00268h by Duclos, Franck, Abell, Lynn M., Harden, David G., Pike, Kristen, Nowak, Kimberly, Locke, Gregory A., Duke, Gerald J., Liu, Xiaoqin, Fernando, Gayani, Shaw, Scott A., Vokits, Benjamin P., Wurtz, Nicholas R., Viet, Andrew, Valente, Meriah N., Stachura, Sylwia, Sleph, Paul, Khan, Javed A., Gao, Ji, Dongre, Ashok R., Zhao, Lei, Wexler, Ruth R., Gordon, David A., Kick, Ellen K.

“…A novel myeloperoxidase inhibitor, 7-benzylether triazolopyrimidine was discovered which reversibly inhibits enzyme activity and shows pharmacodynamic effects…”
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Mechanistic investigations on hypusine formation by Duke, Gerald J

“…Hypusine formation uniquely occurs on the eukaryotic translation initiation factor-5A (eIF5A) and progresses by way of two enzymes, deoxyhypusine synthase (DS)…”
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