Search Results - "Tatlock, John"

SETD7 Controls Intestinal Regeneration and Tumorigenesis by Regulating Wnt/β-Catenin and Hippo/YAP Signaling by Oudhoff, Menno J., Braam, Mitchell J.S., Freeman, Spencer A., Wong, Denise, Rattray, David G., Wang, Jia, Antignano, Frann, Snyder, Kimberly, Refaeli, Ido, Hughes, Michael R., McNagny, Kelly M., Gold, Michael R., Arrowsmith, Cheryl H., Sato, Toshiro, Rossi, Fabio M.V., Tatlock, John H., Owen, Dafydd R., Brown, Peter J., Zaph, Colby

“…Intestinal tumorigenesis is a result of mutations in signaling pathways that control cellular proliferation, differentiation, and survival. Mutations in the…”
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Symmetric Arginine Dimethylation Is Selectively Required for mRNA Splicing and the Initiation of Type I and Type III Interferon Signaling by Metz, Patrick J., Ching, Keith A., Xie, Tao, Delgado Cuenca, Paulina, Niessen, Sherry, Tatlock, John H., Jensen-Pergakes, Kristen, Murray, Brion W.

“…Alternative splicing is well understood to enhance proteome diversity as cells respond to stimuli. However, mechanistic understanding for how the spliceosome…”
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(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells by Barsyte-Lovejoy, Dalia, Li, Fengling, Oudhoff, Menno J., Tatlock, John H., Dong, Aiping, Zeng, Hong, Wu, Hong, Freeman, Spencer A., Schapira, Matthieu, Senisterra, Guillermo A., Kuznetsova, Ekaterina, Marcellus, Richard, Allali-Hassani, Abdellah, Kennedy, Steven, Lambert, Jean-Philippe, Couzens, Amber L., Aman, Ahmed, Gingras, Anne-Claude, Al-Awar, Rima, Fish, Paul V., Gerstenberger, Brian S., Roberts, Lee, Benn, Caroline L., Grimley, Rachel L., Braam, Mitchell J. S., Rossi, Fabio M. V., Sudol, Marius, Brown, Peter J., Bunnage, Mark E., Owen, Dafydd R., Zaph, Colby, Vedadi, Masoud, Arrowsmith, Cheryl H.

“…SET domain containing (lysine methyltransferase) 7 (SETD7) is implicated in multiple signaling and disease related pathways with a broad diversity of reported…”
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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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Small molecule inhibitors reveal PTK6 kinase is not an oncogenic driver in breast cancers by Qiu, Luping, Levine, Kymberly, Gajiwala, Ketan S, Cronin, Ciarán N, Nagata, Asako, Johnson, Eric, Kraus, Michelle, Tatlock, John, Kania, Robert, Foley, Timothy, Sun, Shaoxian

“…Protein tyrosine kinase 6 (PTK6, or BRK) is aberrantly expressed in breast cancers, and emerging as an oncogene that promotes tumor cell proliferation,…”
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Preclinical Characterization of PF-00868554, a Potent Nonnucleoside Inhibitor of the Hepatitis C Virus RNA-Dependent RNA Polymerase by SHI, Stephanie T, HERLIHY, Koleen J, GONZALEZ, Javier, LINTON, Angelica, PATICK, Amy K, LEWIS, Cristina, GRAHAM, Joanne P, NONOMIYA, Jim, RAHAVENDRAN, Sadayappan V, SKOR, Heather, IRVINE, Rebecca, BINFORD, Susan, TATLOCK, John, HUI LI

“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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Viracept (Nelfinavir Mesylate, AG1343):  A Potent, Orally Bioavailable Inhibitor of HIV-1 Protease by Kaldor, Stephen W, Kalish, Vincent J, Davies, Jay F, Shetty, Bhasker V, Fritz, James E, Appelt, Krzysztof, Burgess, Jeffrey A, Campanale, Kristina M, Chirgadze, Nickolay Y, Clawson, David K, Dressman, Bruce A, Hatch, Steven D, Khalil, Deborah A, Kosa, Maha B, Lubbehusen, Penny P, Muesing, Mark A, Patick, Amy K, Reich, Siegfried H, Su, Kenneth S, Tatlock, John H

“…Using a combination of iterative structure-based design and an analysis of oral pharmacokinetics and antiviral activity, AG1343 (Viracept, nelfinavir…”
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Oxidation of Alkynyl Ethers with Potassium Permanganate. A New Acyl Anion Equivalent for the Preparation of .alpha.-Keto Esters by Tatlock, John H

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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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Structure-Based Design of Novel, Urea-Containing FKBP12 Inhibitors by Dragovich, Peter S, Barker, John E, French, Judy, Imbacuan, Michael, Kalish, Vincent J, Kissinger, Charles R, Knighton, Daniel R, Lewis, Cristina T, Moomaw, Ellen W, Parge, Hans E, Pelletier, Laura A. K, Prins, Thomas J, Showalter, Richard E, Tatlock, John H, Tucker, Kathleen D, Villafranca, J. Ernest

“…The structure-based design and subsequent chemical synthesis of novel, urea-containing FKBP12 inhibitors are described. These compounds are shown to disrupt…”
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Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3–9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase by Taylor, Alexandria P, Swewczyk, Magdalena, Kennedy, Steven, Trush, Viacheslav V, Wu, Hong, Zeng, Hong, Dong, Aiping, Ferreira de Freitas, Renato, Tatlock, John, Kumpf, Robert A, Wythes, Martin, Casimiro-Garcia, Agustin, Denny, Rajiah Aldrin, Parikh, Mihir D, Li, Fengling, Barsyte-Lovejoy, Dalia, Schapira, Matthieu, Vedadi, Masoud, Brown, Peter J, Arrowsmith, Cheryl H, Owen, Dafydd R

“…The first chemical probe to primarily occupy the co-factor binding site of a Su­(var)­3−9, enhancer of a zeste, trithorax (SET) domain containing protein…”
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Abstract 1160: SAM competitive PRMT5 inhibitor PF06939999 demonstrates antitumor activity in splicing dysregulated NSCLC with decreased liability of drug resistance by Jensen-Pergakes, Kristen, Tatlock, John, Maegley, Karen, McAlpine, Indrawan, McTigue, Michele, Xie, Tao, Dillon, Christopher, Wang, Yuli, Yamazaki, Shinji, Spiegel, Noah, Shi, Manli, Nemeth, Amy, Miller, Natalie, Hendrickson, Eleanore, Lam, Hieu, Sherrill, John, Liu, Wei, Deng, Ya-Li, Chung, Chi-Yeh, McMillan, Elizabeth A., Palde, Prakash, Brooun, Alexei, Braganza, John, Kephart, Susan E., Kumpf, Robert, Patman, Ryan, Rui, Eugene, Scales, Stephanie, Tran-Dube, Michelle, Wang, Fen, Wythes, Martin, Paul, Thomas

“…Abstract Protein arginine methyltransferase 5 (PRMT5) overexpression in hematological and solid tumors promotes symmetrical di-methyl arginine (SDMA) on…”
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Discovery of (R)-6-Cyclopentyl-6-(2-(2,6-diethylpyridin-4-yl)ethyl)-3-((5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methyl)-4-hydroxy-5,6-dihydropyran-2-one (PF-00868554) as a Potent and Orally Available Hepatitis C Virus Polymerase Inhibitor by Li, Hui, Tatlock, John, Linton, Angelica, Gonzalez, Javier, Jewell, Tanya, Patel, Leena, Ludlum, Sarah, Drowns, Matthew, Rahavendran, Sadayappan V, Skor, Heather, Hunter, Robert, Shi, Stephanie T, Herlihy, Koleen J, Parge, Hans, Hickey, Michael, Yu, Xiu, Chau, Fannie, Nonomiya, Jim, Lewis, Cristina

“…The HCV RNA-dependent RNA polymerase has emerged as one of the key targets for novel anti-HCV therapy development. Herein, we report the optimization of the…”
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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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Abstract 4857: Discovery of PF-06855800, a SAM competitive PRMT5 inhibitor with potent antitumor activity by Mcalpine, Indrawan J., Tatlock, John, Billitti, Joseph, Braganza, John, Brooun, Alexei, Ya-Li, Deng, Hirakawa, Brad, Jensen-Pergakes, Kristen, Kumpf, Robert, Liu, Wei, Maegley, Karen, McTigue, Michele, Patman, Ryan, Rui, Eugene, Scales, Stephanie, Spiegel, Noah, Tran-Dubé, Michelle, Wang, Fen, Wang, Zhenxiong, Yamazaki, Shinji, Zhang, Tao, Wythes, Martin

“…Abstract Protein arginine methyltransferase 5 (PRMT5) is the primary type II arginine methyltransferase responsible for symmetric dimethylation of protein…”
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Crystal-Structure-Based Design and Synthesis of Novel C-Terminal Inhibitors of HIV Protease by Varney, Michael D, Appelt, Krzysztof, Kalish, Vince, Reddy, M. Rami, Tatlock, John, Palmer, Cindy L, Romines, William H, Wu, Bor-Wen, Musick, Linda

“…The X-ray crystal-structure-based design, synthesis, computational evaluation, and activity of a novel class of HIV protease inhibitors are described. The…”
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Optimization of Potent, Selective, and Orally Bioavailable Pyrrolodinopyrimidine-Containing Inhibitors of Heat Shock Protein 90. Identification of Development Candidate 2-Amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide by Zehnder, Luke, Bennett, Michael, Meng, Jerry, Huang, Buwen, Ninkovic, Sacha, Wang, Fen, Braganza, John, Tatlock, John, Jewell, Tanya, Zhou, Joe Zhongxiang, Burke, Ben, Wang, Jeff, Maegley, Karen, Mehta, Pramod P, Yin, Min-Jean, Gajiwala, Ketan S, Hickey, Michael J, Yamazaki, Shinji, Smith, Evan, Kang, Ping, Sistla, Anand, Dovalsantos, Elena, Gehring, Michael R, Kania, Robert, Wythes, Martin, Kung, Pei-Pei

“…A novel class of heat shock protein 90 (Hsp90) inhibitors was discovered by high-throughput screening and was subsequently optimized using a combination of…”
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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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Structure-based design of novel calcineurin (PP2B) inhibitors by Tatlock, John H., Angelica Linton, M., Hou, Xinjun J., Kissinger, Charles R., Pelletier, Laura A., Showalter, Richard E., Tempczyk, Anna, Ernest Villafranca, J.

“…The design, synthesis, and evaluation of small molecule, in vitro, inhibitors of human calcineurin is described. These ligands were derived from the known…”
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Identification and structure-based optimization of novel dihydropyrones as potent HCV RNA polymerase inhibitors by Li, Hui, Tatlock, John, Linton, Angelica, Gonzalez, Javier, Borchardt, Allen, Dragovich, Peter, Jewell, Tanya, Prins, Tom, Zhou, Ru, Blazel, Julie, Parge, Hans, Love, Robert, Hickey, Michael, Doan, Chau, Shi, Stephanie, Duggal, Rohit, Lewis, Cristina, Fuhrman, Shella

“…The discovery and SAR of a novel series of HCV polymerase inhibitors are described. A novel class of non-nucleoside HCV NS5B polymerase inhibitors has been…”
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