Search Results - "Newitt, A"

Discovery of new acylaminopyridines as GSK-3 inhibitors by a structure guided in-depth exploration of chemical space around a pyrrolopyridinone core by Sivaprakasam, Prasanna, Han, Xiaojun, Civiello, Rita L, Jacutin-Porte, Swanee, Kish, Kevin, Pokross, Matt, Lewis, Hal A, Ahmed, Nazia, Szapiel, Nicolas, Newitt, John A, Baldwin, Eric T, Xiao, Hong, Krause, Carol M, Park, Hyunsoo, Nophsker, Michelle, Lippy, Jonathan S, Burton, Catherine R, Langley, David R, Macor, John E, Dubowchik, Gene M

“…Glycogen synthase kinase-3 (GSK-3) has been proposed to play a crucial role in the pathogenesis of many diseases including cancer, stroke, bipolar disorders,…”
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The structure of dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants by TOKARSKI, John S, NEWITT, John A, DIANLIN XIE, YAQUN ZHANG, KLEI, Herbert E, CHANG, Chieh Ying J, CHENG, Janet D, WITTEKIND, Michael, KIEFER, Susan E, KISH, Kevin, LEE, Francis Y. F, BORZILLERRI, Robert, LOMBARDO, Louis J

“…Chronic myeloid leukemia (CML) is caused by the constitutively activated tyrosine kinase breakpoint cluster (BCR)-ABL. Current frontline therapy for CML is…”
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The E. coli Signal Recognition Particle Is Required for the Insertion of a Subset of Inner Membrane Proteins by Ulbrandt, Nancy D, Newitt, John A, Bernstein, Harris D

“…E. coli homologs of the signal recognition particle (SRP) and its receptor are essential for viability, but their role in protein export is unclear. To…”
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Immune-modulating enzyme indoleamine 2,3-dioxygenase is effectively inhibited by targeting its apo-form by Nelp, Micah T., Kates, Patrick A., Hunt, John T., Newitt, John A., Balog, Aaron, Maley, Derrick, Zhu, Xiao, Abell, Lynn, Allentoff, Alban, Borzilleri, Robert, Lewis, Hal A., Lin, Zeyu, Seitz, Steven P., Yan, Chunhong, Groves, John T.

“…For cancer cells to survive and proliferate, they must escape normal immune destruction. One mechanism by which this is accomplished is through immune…”
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Discovery of the Selective CYP17A1 Lyase Inhibitor BMS-351 for the Treatment of Prostate Cancer by Huang, Audris, Jayaraman, Lata, Fura, Aberra, Vite, Gregory D, Trainor, George L, Gottardis, Marco M, Spires, Thomas E, Spires, Vanessa M, Rizzo, Cheryl A, Obermeier, Mary T, Elzinga, Paul A, Todderud, Gordon, Fan, Yi, Newitt, John A, Beyer, Sophie M, Zhu, Yongxin, Warrack, Bethanne M, Goodenough, Angela K, Tebben, Andrew J, Doweyko, Arthur M, Gold, David L, Balog, Aaron

“…Efforts to identify a potent, reversible, nonsteroidal CYP17A1 lyase inhibitor with good selectivity over CYP17A1 hydroxylase and CYPs 11B1 and 21A2 for the…”
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Bilateral angular carpal deformity in a dog with craniomandibular osteopathy by Pettitt, R, Fox, R, Comerford, E J, Newitt, A

“…A four-month-old West Highland White Terrier was presented to the Small Animal Teaching Hospital at the University of Liverpool with the complaint of a…”
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Inhibitors of human mitotic kinesin Eg5: Characterization of the 4-phenyl-tetrahydroisoquinoline lead series by Tarby, Christine M., Kaltenbach, Robert F., Huynh, Tram, Pudzianowski, Andrew, Shen, Henry, Ortega-Nanos, Marie, Sheriff, Steven, Newitt, John A., McDonnell, Patricia A., Burford, Neil, Fairchild, Craig R., Vaccaro, Wayne, Chen, Zhong, Borzilleri, Robert M., Naglich, Joseph, Lombardo, Louis J., Gottardis, Marco, Trainor, George L., Roussell, Deborah L.

“…In a high-throughput screening effort, a series of tetrahydroisoquinolines was identified as modest inhibitors of human Eg5. A medicinal chemistry optimization…”
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Native mass spectrometry and gas-phase fragmentation provide rapid and in-depth topological characterization of a PROTAC ternary complex by Song, Jong Hee, Wagner, Nicole D, Yan, Jing, Li, Jing, Huang, Richard Y-C, Balog, Aaron J, Newitt, John A, Chen, Guodong, Gross, Michael L

“…Proteolysis-targeting chimeras (PROTACs) represent a new direction in small-molecule therapeutics whereby a heterobifunctional linker to a protein of interest…”
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Improving the diffraction quality of heat‐shock protein 47 crystals by Kish, Kevin, Cobell, Stephen, Szapiel, Nicolas, Yan, Chunhong, Newitt, John A., Tredup, Jeffrey, Rodrigo, Iyoncy, Tomasco, Elizabeth, Gao, Mian, Marsilio, Frank, Haugner, John, Lipovšek, Dasa, Deng, Bi, Bousquet, Patrick, Zhang, Yihong, Schmidt, Holly, Sheriff, Steven

“…Heat‐shock protein 47 (HSP47) is a potential target for inhibitors that ameliorate fibrosis by reducing collagen assembly. In an effort to develop a…”
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Synthesis and biological evaluation of biaryl alkyl ethers as inhibitors of IDO1 by Markwalder, Jay A., Balog, Aaron J., Williams, David K., Nara, Susheel J., Reddy, Ratnakar, Roy, Saumya, Kanyaboina, Yadagiri, Li, Xin, Johnston, Kathy, Fan, Yi, Lewis, Hal, Marsilio, Frank, Yan, Chunhong, Critton, David, Newitt, John A., Traeger, Sarah C., Wu, Dauh-Rurng, Jure-Kunkel, Maria N., Jayaraman, Lata, Lin, Tai-An, Sinz, Michael W., Hunt, John T., Seitz, Steven P.

“…[Display omitted] Starting from the dialkylaniline indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor lead 3 (IDO1 HeLa IC50 = 7.0 nM), an iterative process of…”
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A Mutation in the Escherichia coli secY Gene That Produces Distinct Effects on Inner Membrane Protein Insertion and Protein Export by Newitt, John A., Bernstein, Harris D.

“…E. coli strains that contain thesecY40 mutation are cold-sensitive, but protein export defects have not been observed even at the nonpermissive temperature…”
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Crystal structures of apo and inhibitor-bound TGFβR2 kinase domain: insights into TGFβR isoform selectivity by Tebben, Andrew J., Ruzanov, Maxim, Gao, Mian, Xie, Dianlin, Kiefer, Susan E., Yan, Chunhong, Newitt, John A., Zhang, Liping, Kim, Kyoung, Lu, Hao, Kopcho, Lisa M., Sheriff, Steven

“…The cytokine TGF‐β modulates a number of cellular activities and plays a critical role in development, hemostasis and physiology, as well as in diseases…”
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Crystal structure of microtubule affinity-regulating kinase 4 catalytic domain in complex with a pyrazolopyrimidine inhibitor by Sack, John S., Gao, Mian, Kiefer, Susan E., Myers Jr, Joseph E., Newitt, John A., Wu, Sophie, Yan, Chunhong

“…Microtubule‐associated protein/microtubule affinity‐regulating kinase 4 (MARK4) is a serine/threonine kinase involved in the phosphorylation of MAP proteins…”
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Using yeast surface display to engineer a soluble and crystallizable construct of hematopoietic progenitor kinase 1 (HPK1) by Lau, Wai L., Pearce, Bradley, Malakian, Heather, Rodrigo, Iyoncy, Xie, Dianlin, Gao, Mian, Marsilio, Frank, Chang, Chiehying, Ruzanov, Max, Muckelbauer, Jodi K., Newitt, John A., Lipovšek, Daša, Sheriff, Steven

“…Hematopoietic progenitor kinase 1 (HPK1) is an intracellular kinase that plays an important role in modulating tumor immune response and thus is an attractive…”
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Discovery of Novel P1 Groups for Coagulation Factor VIIa Inhibition Using Fragment-Based Screening by Cheney, Daniel L, Bozarth, Jeffrey M, Metzler, William J, Morin, Paul E, Mueller, Luciano, Newitt, John A, Nirschl, Alexandra H, Rendina, Alan R, Tamura, James K, Wei, Anzhi, Wen, Xiao, Wurtz, Nicholas R, Seiffert, Dietmar A, Wexler, Ruth R, Priestley, E. Scott

“…A multidisciplinary, fragment-based screening approach involving protein ensemble docking and biochemical and NMR assays is described. This approach led to the…”
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Synthesis and SAR of pyrrolotriazine-4-one based Eg5 inhibitors by Kim, Kyoung Soon, Lu, Songfeng, Cornelius, Lyndon A., Lombardo, Louis J., Borzilleri, Robert M., Schroeder, Gretchen M., Sheng, Christopher, Rovnyak, George, Crews, Donald, Schmidt, Robert J., Williams, David K., Bhide, Rajeev S., Traeger, Sarah C., McDonnell, Patricia A., Mueller, Luciano, Sheriff, Steven, Newitt, John A., Pudzianowski, Andrew T., Yang, Zheng, Wild, Robert, Lee, Frances Y., Batorsky, Roberta, Ryder, James S., Ortega-Nanos, Marie, Shen, Henry, Gottardis, Marco, Roussell, Deborah L.

“…Synthesis and SAR of substituted pyrrolotriazine-4-one analogues as Eg5 inhibitors are described. Analogue 26 demonstrated in vivo efficacy in an iv P388…”
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Discovery of 4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a Clinical p38α MAP Kinase Inhibitor for the Treatment of Inflammatory Diseases by Liu, Chunjian, Lin, James, Wrobleski, Stephen T, Lin, Shuqun, Hynes, John, Wu, Hong, Dyckman, Alaric J, Li, Tianle, Wityak, John, Gillooly, Kathleen M, Pitt, Sidney, Shen, Ding Ren, Zhang, Rosemary F, McIntyre, Kim W, Salter-Cid, Luisa, Shuster, David J, Zhang, Hongjian, Marathe, Punit H, Doweyko, Arthur M, Sack, John S, Kiefer, Susan E, Kish, Kevin F, Newitt, John A, McKinnon, Murray, Dodd, John H, Barrish, Joel C, Schieven, Gary L, Leftheris, Katerina

“…The discovery and characterization of 7k (BMS-582949), a highly selective p38α MAP kinase inhibitor that is currently in phase II clinical trials for the…”
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Development and Fit-for-Purpose Validation of a Soluble Human Programmed Death-1 Protein Assay by Ni, Yan G., Yuan, Xiling, Newitt, John A., Peterson, Jon E., Gleason, Carol R., Haulenbeek, Jonathan, Santockyte, Rasa, Lafont, Virginie, Marsilio, Frank, Neely, Robert J., DeSilva, Binodh, Piccoli, Steven P.

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The structure of multiple polypeptide domains determines the signal recognition particle targeting requirement of Escherichia coli inner membrane proteins by Newitt, J A, Ulbrandt, N D, Bernstein, H D

“…The signal recognition particle (SRP) targeting pathway is required for the efficient insertion of many polytopic inner membrane proteins (IMPs) into the…”
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Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis by Nair, Satheesh, Kumar, Sreekantha Ratna, Paidi, Venkatram Reddy, Sistla, Ramesh, Kantheti, Durgarao, Polimera, Subba Rao, Thangavel, Soodamani, Mukherjee, Amrita Jha, Das, Mitalee, Bhide, Rajeev S, Pitts, William J, Murugesan, Natesan, Dudhgoankar, Shailesh, Nagar, Jignesh, Subramani, Siva, Mazumder, Debarati, Carman, Julie A, Holloway, Deborah A, Li, Xin, Fereshteh, Mark P, Ruepp, Stefan, Palanisamy, Kamalavenkatesh, Mariappan, T. Thanga, Maddi, Srinivas, Saxena, Ajay, Elzinga, Paul, Chimalakonda, Anjaneya, Ruan, Qian, Ghosh, Kaushik, Bose, Sucharita, Sack, John, Yan, Chunhong, Kiefer, Susan E, Xie, Dianlin, Newitt, John A, Saravanakumar, S. Pon, Rampulla, Richard A, Barrish, Joel C, Carter, Percy H, Hynes, John

“…IRAK4 is an attractive therapeutic target for the treatment of inflammatory conditions. Structure guided optimization of a nicotinamide series of inhibitors…”
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