Search Results - "Palmer, Wylie"

The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies by Vangamudi, Bhavatarini, Paul, Thomas A, Shah, Parantu K, Kost-Alimova, Maria, Nottebaum, Lisa, Shi, Xi, Zhan, Yanai, Leo, Elisabetta, Mahadeshwar, Harshad S, Protopopov, Alexei, Futreal, Andrew, Tieu, Trang N, Peoples, Mike, Heffernan, Timothy P, Marszalek, Joseph R, Toniatti, Carlo, Petrocchi, Alessia, Verhelle, Dominique, Owen, Dafydd R, Draetta, Giulio, Jones, Philip, Palmer, Wylie S, Sharma, Shikhar, Andersen, Jannik N

“…The SWI/SNF multisubunit complex modulates chromatin structure through the activity of two mutually exclusive catalytic subunits, SMARCA2 and SMARCA4, which…”
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Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor by Palmer, Wylie S, Poncet-Montange, Guillaume, Liu, Gang, Petrocchi, Alessia, Reyna, Naphtali, Subramanian, Govindan, Theroff, Jay, Yau, Anne, Kost-Alimova, Maria, Bardenhagen, Jennifer P, Leo, Elisabetta, Shepard, Hannah E, Tieu, Trang N, Shi, Xi, Zhan, Yanai, Zhao, Shuping, Barton, Michelle C, Draetta, Giulio, Toniatti, Carlo, Jones, Philip, Geck Do, Mary, Andersen, Jannik N

“…The bromodomain containing proteins TRIM24 (tripartite motif containing protein 24) and BRPF1 (bromodomain and PHD finger containing protein 1) are involved in…”
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Discovery of IPN60090, a Clinical Stage Selective Glutaminase‑1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties by Soth, Michael J, Le, Kang, Di Francesco, Maria Emilia, Hamilton, Matthew M, Liu, Gang, Burke, Jason P, Carroll, Chris L, Kovacs, Jeffrey J, Bardenhagen, Jennifer P, Bristow, Christopher A, Cardozo, Mario, Czako, Barbara, de Stanchina, Elisa, Feng, Ningping, Garvey, Jill R, Gay, Jason P, Do, Mary K. Geck, Greer, Jennifer, Han, Michelle, Harris, Angela, Herrera, Zachary, Huang, Sha, Giuliani, Virginia, Jiang, Yongying, Johnson, Sarah B, Johnson, Troy A, Kang, Zhijun, Leonard, Paul G, Liu, Zhen, McAfoos, Timothy, Miller, Meredith, Morlacchi, Pietro, Mullinax, Robert A, Palmer, Wylie S, Pang, Jihai, Rogers, Norma, Rudin, Charles M, Shepard, Hannah E, Spencer, Nakia D, Theroff, Jay, Wu, Qi, Xu, Alan, Yau, Ju Anne, Draetta, Giulio, Toniatti, Carlo, Heffernan, Timothy P, Jones, Philip

“…Inhibition of glutaminase-1 (GLS-1) hampers the proliferation of tumor cells reliant on glutamine. Known glutaminase inhibitors have potential limitations, and…”
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Functional Genomics Reveals Synthetic Lethality between Phosphogluconate Dehydrogenase and Oxidative Phosphorylation by Sun, Yuting, Bandi, Madhavi, Lofton, Timothy, Smith, Melinda, Bristow, Christopher A., Carugo, Alessandro, Rogers, Norma, Leonard, Paul, Chang, Qing, Mullinax, Robert, Han, Jing, Shi, Xi, Seth, Sahil, Meyers, Brooke A., Miller, Meredith, Miao, Lili, Ma, Xiaoyan, Feng, Ningping, Giuliani, Virginia, Geck Do, Mary, Czako, Barbara, Palmer, Wylie S., Mseeh, Faika, Asara, John M., Jiang, Yongying, Morlacchi, Pietro, Zhao, Shuping, Peoples, Michael, Tieu, Trang N., Warmoes, Marc O., Lorenzi, Philip L., Muller, Florian L., DePinho, Ronald A., Draetta, Giulio F., Toniatti, Carlo, Jones, Philip, Heffernan, Timothy P., Marszalek, Joseph R.

“…The plasticity of a preexisting regulatory circuit compromises the effectiveness of targeted therapies, and leveraging genetic vulnerabilities in cancer cells…”
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Development of small molecule inhibitors of BRPF1 and TRIM24 bromodomains by Palmer, Wylie S.

“…The entry of small molecule inhibitors of the bromodomain and extra C-terminal domain (BET) family of bromodomains into the clinic has demonstrated the…”
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Observed bromodomain flexibility reveals histone peptide- and small molecule ligand-compatible forms of ATAD2 by Poncet-Montange, Guillaume, Zhan, Yanai, Bardenhagen, Jennifer P, Petrocchi, Alessia, Leo, Elisabetta, Shi, Xi, Lee, 4th, Gilbert R, Leonard, Paul G, Geck Do, Mary K, Cardozo, Mario G, Andersen, Jannik N, Palmer, Wylie S, Jones, Philip, Ladbury, John E

“…Preventing histone recognition by bromodomains emerges as an attractive therapeutic approach in cancer. Overexpression of ATAD2 (ATPase family AAA…”
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Discovery of Novel PI3-Kinase δ Specific Inhibitors for the Treatment of Rheumatoid Arthritis: Taming CYP3A4 Time-Dependent Inhibition by Safina, Brian S, Baker, Stewart, Baumgardner, Matt, Blaney, Paul M, Chan, Bryan K, Chen, Yung-Hsiang, Cartwright, Matthew W, Castanedo, Georgette, Chabot, Christine, Cheguillaume, Arnaud J, Goldsmith, Paul, Goldstein, David M, Goyal, Bindu, Hancox, Timothy, Handa, Raj K, Iyer, Pravin S, Kaur, Jasmit, Kondru, Rama, Kenny, Jane R, Krintel, Sussie L, Li, Jun, Lesnick, John, Lucas, Matthew C, Lewis, Cristina, Mukadam, Sophie, Murray, Jeremy, Nadin, Alan J, Nonomiya, Jim, Padilla, Fernando, Palmer, Wylie S, Pang, Jodie, Pegg, Neil, Price, Steve, Reif, Karin, Salphati, Laurent, Savy, Pascal A, Seward, Eileen M, Shuttleworth, Stephen, Sohal, Sukhjit, Sweeney, Zachary K, Tay, Suzanne, Tivitmahaisoon, Parcharee, Waszkowycz, Bohdan, Wei, Binqing, Yue, Qin, Zhang, Chenghong, Sutherlin, Daniel P

“…PI3Kδ is a lipid kinase and a member of a larger family of enzymes, PI3K class IA(α, β, δ) and IB (γ), which catalyze the phosphorylation of PIP2 to PIP3…”
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Development of novel cellular histone-binding and chromatin-displacement assays for bromodomain drug discovery by Zhan, Yanai, Kost-Alimova, Maria, Shi, Xi, Leo, Elisabetta, Bardenhagen, Jennifer P, Shepard, Hannah E, Appikonda, Srikanth, Vangamudi, Bhavatarini, Zhao, Shuping, Tieu, Trang N, Jiang, Shiming, Heffernan, Timothy P, Marszalek, Joseph R, Toniatti, Carlo, Draetta, Giulio, Tyler, Jessica, Barton, Michelle, Jones, Philip, Palmer, Wylie S, Geck Do, Mary K, Andersen, Jannik N

“…Proteins that 'read' the histone code are central elements in epigenetic control and bromodomains, which bind acetyl-lysine motifs, are increasingly recognized…”
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Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): Kinase profiling guided optimization of a 1,2,3-benzotriazole lead by Palmer, Wylie S., Alam, Muzaffar, Arzeno, Humberto B., Chang, Kung-Ching, Dunn, James P., Goldstein, David M., Gong, Leyi, Goyal, Bindu, Hermann, Johannes C., Hogg, J. Heather, Hsieh, Gary, Jahangir, Alam, Janson, Cheryl, Jin, Sue, Ursula Kammlott, R., Kuglstatter, Andreas, Lukacs, Christine, Michoud, Christophe, Niu, Linghao, Reuter, Deborah C., Shao, Ada, Silva, Tania, Trejo-Martin, Teresa A., Stein, Karin, Tan, Yun-Chou, Tivitmahaisoon, Parcharee, Tran, Patricia, Wagner, Paul, Weller, Paul, Wu, Shao-Yong

“…Structure and kinase profiling guided the optimization of a CDK2 1,2,3-benzotriazole hit to give a series of indoles that are selective and potent dual JNK1…”
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Palladium-Catalyzed Reactions of Di-tert-butylsiliranes with Electron-Deficient Alkynes and Investigations of the Catalytic Cycle by Palmer, Wylie S, Woerpel, K. A

“…Siliranes undergo palladium-catalyzed reactions with alkynes to give a variety of silacycles depending upon the alkyne. When terminal and electron-poor alkynes…”
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Synthesis of Silirenes by Palladium-Catalyzed Transfer of Silylene from Siliranes to Alkynes by Palmer, Wylie S, Woerpel, K. A

“…Palladium-catalyzed reactions of cis-1,1-di-tert-butyl-2,3-dimethylsilirane with disubstituted alkynes produced thermally stable silirenes in high yields…”
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Stereospecific Palladium-Catalyzed Reactions of Siliranes with Alkynes by Palmer, Wylie S, Woerpel, K. A

“…Palladium-catalyzed insertion of alkynes into siliranes and silylene extrusion reactions proceed with stereospecific retention of configuration at the carbon…”
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Stereospecific and Regioselective Isocyanide Insertions into Siliranes and Reactions of the Resulting Iminosilacyclobutanes by Nguyen, Phuc T, Palmer, Wylie S, Woerpel, K. A

“…The insertions of p-tolyl and tert-butyl isocyanide into siliranes yielded iminosilacyclobutanes with stereospecific retention of configuration…”
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N-Arylpiperazinyl-N‘-propylamino Derivatives of Heteroaryl Amides as Functional Uroselective α1-Adrenoceptor Antagonists by Elworthy, Todd R, Ford, Anthony P. D. W, Bantle, Gary W, Morgans, David J, Ozer, Rachel S, Palmer, Wylie S, Repke, David B, Romero, Magarita, Sandoval, Leticia, Sjogren, Eric B, Talamás, Francisco X, Vazquez, Alfredo, Wu, Helen, Arredondo, Nicolas F, Blue, David R, DeSousa, Andrea, Gross, Lisa M, Kava, M. Shannon, Lesnick, John D, Vimont, Rachel L, Williams, Timothy J, Zhu, Quan-Ming, Pfister, Jürg R, Clarke, David E

“…Novel arylpiperazines were identified as α1-adrenoceptor (AR) subtype-selective antagonists by functional in vitro screening. 3-[4-(ortho-Substituted…”
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Stereo- and Regiochemistry of Aldehyde Insertions into the C-Si Bonds of Siliranes by Bodnar, Paul M, Palmer, Wylie S, Shaw, Jared T, Smitrovich, Jacqueline H, Sonnenberg, Jennifer D, Presley, Alice L, Woerpel, K. A

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Stereo- and Regioselectivity of Reactions of Siliranes with Aldehydes and Related Substrates by Bodnar, Paul M, Palmer, Wylie S, Ridgway, Brian H, Shaw, Jared T, Smitrovich, Jacqueline H, Woerpel, K. A

“…Siliranes undergo stereoselective and regioselective insertions of benzaldehyde to provide oxasilacyclopentane products. The thermal reaction (>100 °C) leads…”
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Abstract 1023: Functional genomics reveals dependency on 6-phosphogluconate dehydrogenase in OXPHOS-deficient tumors by Sun, Yuting, Bandi, Madhavi, Lofton, Timothy, Smith, Melinda, Bristow, Christopher, Rogers, Norma, Edward, Chang, Geck Do, Mary, Jiang, Yongying, Morlacchi, Pietro, Muller, Florian, Mseeh, Faika, Czako, Barbara, Palmer, Wylie, Toniatti, Carlo, Jones, Philip, Draetta, Giulio, Heffernan, Timothy, Marszalek, Joseph

“…Abstract Cancer cells display metabolic properties distinct from normal cells and are therefore believed to be dependent on key metabolic enzymes. The…”
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Abstract 3528: The SMARCA2/4 catalytic activity, but not the bromodomain, is a drug target in SWI/SNF mutant cancers by Vangamudi, Bhavatarini, Paul, Thomas, Shah, Parantu K., Alimova, Maria K., Nottebaum, Lisa, Shi, Xi, Zhan, Yanai, Leo, Elisabetta, Mahadeshwar, Harshad S., Protopopov, Alexei, Futreal, Andrew, Tieu, Trang N., Peoples, Mike, Petrocchi, Alessia, Marszalek, Joseph R., Toniatti, Carlo, Heffernan, Timothy P., Verhelle, Dominique, Draetta, Giulio, Owen, Dafydd, Jones, Philip, Palmer, Wylie, Sharma, Shikhar, Andersen, Jannik N.

“…Abstract The SWI/SNF multi-subunit complex modulates chromatin structure through the activity of two mutually exclusive catalytic subunits, SMARCA2 and…”
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Development of indole/indazole-aminopyrimidines as inhibitors of c-Jun N-terminal kinase (JNK): Optimization for JNK potency and physicochemical properties by Gong, Leyi, Han, Xiaochun, Silva, Tania, Tan, Yun-Chou, Goyal, Bindu, Tivitmahaisoon, Parch, Trejo, Alejandra, Palmer, Wylie, Hogg, Heather, Jahagir, Alam, Alam, Muzaffar, Wagner, Paul, Stein, Karin, Filonova, Lubov, Loe, Brad, Makra, Ferenc, Rotstein, David, Rapatova, Lubica, Dunn, James, Zuo, Fengrong, Porto, Joseph Dal, Wong, Brian, Jin, Sue, Chang, Alice, Tran, Patricia, Hsieh, Gary, Niu, Linghao, Shao, Ada, Reuter, Deborah, Hermann, Johaness, Kuglstatter, Andreas, Goldstein, David

“…Structure guided optimization led to a potent series of JNK inhibitors with good physicochemical properties and desirable kinase selectivity as exemplified by…”
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Joint Meeting on Medicinal Chemistry in Vienna by Martin, Rainer E., Mohr, Peter, Palmer, Wylie, Stalder, Henri

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