Search Results - "Wallweber, Heidi J.A."

The Identification of 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a Potent, Selective, Orally Bioavailable Inhibitor of Class I PI3 Kinase for the Treatment of Cancer by Folkes, Adrian J, Ahmadi, Khatereh, Alderton, Wendy K, Alix, Sonia, Baker, Stewart J, Box, Gary, Chuckowree, Irina S, Clarke, Paul A, Depledge, Paul, Eccles, Suzanne A, Friedman, Lori S, Hayes, Angela, Hancox, Timothy C, Kugendradas, Arumugam, Lensun, Letitia, Moore, Pauline, Olivero, Alan G, Pang, Jodie, Patel, Sonal, Pergl-Wilson, Giles H, Raynaud, Florence I, Robson, Anthony, Saghir, Nahid, Salphati, Laurent, Sohal, Sukhjit, Ultsch, Mark H, Valenti, Melanie, Wallweber, Heidi J.A, Wan, Nan Chi, Wiesmann, Christian, Workman, Paul, Zhyvoloup, Alexander, Zvelebil, Marketa J, Shuttleworth, Stephen J

“…Phosphatidylinositol-3-kinase (PI3K) is an important target in cancer due to the deregulation of the PI3K/Akt signaling pathway in a wide variety of tumors. A…”
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The Structural Basis for Class II Cytokine Receptor Recognition by JAK1 by Ferrao, Ryan, Wallweber, Heidi J.A., Ho, Hoangdung, Tam, Christine, Franke, Yvonne, Quinn, John, Lupardus, Patrick J.

“…JAK1 is a member of the Janus kinase (JAK) family of non-receptor tyrosine kinases that are activated in response to cytokines and interferons. Here, we…”
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Structural basis of recognition of interferon-α receptor by tyrosine kinase 2 by Wallweber, Heidi J A, Tam, Christine, Franke, Yvonne, Starovasnik, Melissa A, Lupardus, Patrick J

“…How the four JAK kinases discriminate between different cytokine receptors is not well understood. The first crystal structure of a JAK kinase (TYK2) bound to…”
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Positive Allosteric Modulators of GluN2A-Containing NMDARs with Distinct Modes of Action and Impacts on Circuit Function by Hackos, David H., Lupardus, Patrick J., Grand, Teddy, Chen, Yelin, Wang, Tzu-Ming, Reynen, Paul, Gustafson, Amy, Wallweber, Heidi J.A., Volgraf, Matthew, Sellers, Benjamin D., Schwarz, Jacob B., Paoletti, Pierre, Sheng, Morgan, Zhou, Qiang, Hanson, Jesse E.

“…To enhance physiological function of NMDA receptors (NMDARs), we identified positive allosteric modulators (PAMs) of NMDARs with selectivity for GluN2A…”
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Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design by Volgraf, Matthew, Sellers, Benjamin D, Jiang, Yu, Wu, Guosheng, Ly, Cuong Q, Villemure, Elisia, Pastor, Richard M, Yuen, Po-wai, Lu, Aijun, Luo, Xifeng, Liu, Mingcui, Zhang, Shun, Sun, Liang, Fu, Yuhong, Lupardus, Patrick J, Wallweber, Heidi J.A, Liederer, Bianca M, Deshmukh, Gauri, Plise, Emile, Tay, Suzanne, Reynen, Paul, Herrington, James, Gustafson, Amy, Liu, Yichin, Dirksen, Akim, Dietz, Matthias G. A, Liu, Yanzhou, Wang, Tzu-Ming, Hanson, Jesse E, Hackos, David, Scearce-Levie, Kimberly, Schwarz, Jacob B

“…The N-methyl-d-aspartate receptor (NMDAR) is a Na+ and Ca2+ permeable ionotropic glutamate receptor that is activated by the coagonists glycine and glutamate…”
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The Crystal Structure of the Catalytic Domain of the NF-κB Inducing Kinase Reveals a Narrow but Flexible Active Site by de Leon-Boenig, Gladys, Bowman, Krista K., Feng, Jianwen A., Crawford, Terry, Everett, Christine, Franke, Yvonne, Oh, Angela, Stanley, Mark, Staben, Steven T., Starovasnik, Melissa A., Wallweber, Heidi J.A., Wu, Jiansheng, Wu, Lawren C., Johnson, Adam R., Hymowitz, Sarah G.

“…The NF-κB inducing kinase (NIK) regulates the non-canonical NF-κB pathway downstream of important clinical targets including BAFF, RANKL, and LTβ. Despite…”
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The Crystal Structures of EDA-A1 and EDA-A2: Splice Variants with Distinct Receptor Specificity by Hymowitz, Sarah G, Compaan, Deanne M, Yan, Minhong, Wallweber, Heidi J.A, Dixit, Vishva M, Starovasnik, Melissa A, de Vos, Abraham M

“…EDA is a tumor necrosis factor family member involved in ectodermal development. Splice variants EDA-A1 and EDA-A2 differ only by the presence of Glu 308 and…”
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IAP Antagonists Induce Autoubiquitination of c-IAPs, NF-κB Activation, and TNFα-Dependent Apoptosis by Varfolomeev, Eugene, Blankenship, John W., Wayson, Sarah M., Fedorova, Anna V., Kayagaki, Nobuhiko, Garg, Parie, Zobel, Kerry, Dynek, Jasmin N., Elliott, Linda O., Wallweber, Heidi J.A., Flygare, John A., Fairbrother, Wayne J., Deshayes, Kurt, Dixit, Vishva M., Vucic, Domagoj

“…Inhibitor of apoptosis (IAP) proteins are antiapoptotic regulators that block cell death in response to diverse stimuli. They are expressed at elevated levels…”
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Antagonists Induce a Conformational Change in cIAP1 That Promotes Autoubiquitination by Dueber, Erin C., Schoeffler, Allyn J., Lingel, Andreas, Elliott, J. Michael, Fedorova, Anna V., Giannetti, Anthony M., Zobel, Kerry, Maurer, Brigitte, Varfolomeev, Eugene, Wu, Ping, Wallweber, Heidi J. A., Hymowitz, Sarah G., Deshayes, Kurt, Vucic, Domagoj, Fairbrother, Wayne J.

“…Inhibitor of apoptosis (IAP) proteins are negative regulators of cell death. IAP family members contain RING domains that impart E3 ubiquitin ligase activity…”
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Receptor-mediated dimerization of JAK2 FERM domains is required for JAK2 activation by Ferrao, Ryan D, Wallweber, Heidi Ja, Lupardus, Patrick J

“…Cytokines and interferons initiate intracellular signaling via receptor dimerization and activation of Janus kinases (JAKs). How JAKs structurally respond to…”
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A novel NMDA receptor positive allosteric modulator that acts via the transmembrane domain by Wang, Tzu-Ming, Brown, Brandon M., Deng, Lunbin, Sellers, Benjamin D., Lupardus, Patrick J., Wallweber, Heidi J.A., Gustafson, Amy, Wong, Evera, Volgraf, Matthew, Schwarz, Jacob B., Hackos, David H., Hanson, Jesse E.

“…Ionotropic glutamate receptors (iGluRs) mediate fast excitatory neurotransmission and are key nervous system drug targets. While diverse pharmacological tools…”
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Structural basis of IFNα receptor recognition by TYK2 by Wallweber, Heidi J.A., Tam, Christine, Franke, Yvonne, Starovasnik, Melissa A., Lupardus, Patrick J.

“…Tyrosine kinase 2 (TYK2) is a member of the Janus kinase (JAK) family of non-receptor tyrosine kinases, which are essential for proper signaling in immune…”
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Design, Synthesis, and Biological Activity of a Potent Smac Mimetic That Sensitizes Cancer Cells to Apoptosis by Antagonizing IAPs by Zobel, Kerry, Wang, Lan, Varfolomeev, Eugene, Franklin, Matthew C, Elliott, Linda O, Wallweber, Heidi J. A, Okawa, David C, Flygare, John A, Vucic, Domagoj, Fairbrother, Wayne J, Deshayes, Kurt

“…Designed second mitochondrial activator of caspases (Smac) mimetics based on an accessible [7,5]-bicyclic scaffold bind to and antagonize protein interactions…”
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GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved in Vivo Profile by Villemure, Elisia, Volgraf, Matthew, Jiang, Yu, Wu, Guosheng, Ly, Cuong Q, Yuen, Po-wai, Lu, Aijun, Luo, Xifeng, Liu, Mingcui, Zhang, Shun, Lupardus, Patrick J, Wallweber, Heidi J. A, Liederer, Bianca M, Deshmukh, Gauri, Plise, Emile, Tay, Suzanne, Wang, Tzu-Ming, Hanson, Jesse E, Hackos, David H, Scearce-Levie, Kimberly, Schwarz, Jacob B, Sellers, Benjamin D

“…The N-methyl-d-aspartate receptor (NMDAR) is an ionotropic glutamate receptor, gated by the endogenous coagonists glutamate and glycine, permeable to Ca2+ and…”
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Structures of APRIL-receptor complexes: like BCMA, TACI employs only a single cysteine-rich domain for high affinity ligand binding by Hymowitz, Sarah G, Patel, Darshana R, Wallweber, Heidi J A, Runyon, Steven, Yan, Minhong, Yin, Jianping, Shriver, Stephanie K, Gordon, Nathaniel C, Pan, Borlan, Skelton, Nicholas J, Kelley, Robert F, Starovasnik, Melissa A

“…TACI is a member of the tumor necrosis factor receptor superfamily and serves as a key regulator of B cell function. TACI binds two ligands, APRIL and BAFF,…”
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Engineering ML-IAP to produce an extraordinarily potent caspase 9 inhibitor: implications for Smac-dependent anti-apoptotic activity of ML-IAP by Vucic, Domagoj, Franklin, Matthew C, Wallweber, Heidi J A, Das, Kanad, Eckelman, Brendan P, Shin, Hwain, Elliott, Linda O, Kadkhodayan, Saloumeh, Deshayes, Kurt, Salvesen, Guy S, Fairbrother, Wayne J

“…ML-IAP (melanoma inhibitor of apoptosis) is a potent anti-apoptotic protein that is strongly up-regulated in melanoma and confers protection against a variety…”
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The Crystal Structure of A Proliferation-inducing Ligand, APRIL by Wallweber, Heidi J.A., Compaan, Deanne M., Starovasnik, Melissa A., Hymowitz, Sarah G.

“…A proliferation-inducing ligand (APRIL) is a TNF-like cytokine that stimulates tumor cell growth. Within the TNF ligand superfamily, APRIL is most similar to…”
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Multiple Novel Classes of APRIL-specific Receptor-blocking Peptides Isolated by Phage Display by Gordon, Nathaniel C., Lien, Samantha, Johnson, Jeremy, Wallweber, Heidi J.A., Tran, Thuy, Currell, Bridget, Mathieu, Mary, Quan, Clifford, Starovasnik, Melissa A., Hymowitz, Sarah G., Kelley, Robert F.

“…A proliferation-inducing ligand (APRIL) is a member of the tumor necrosis factor (TNF) ligand superfamily and has a proliferative effect on both normal and…”
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Engineering an APRIL-specific B Cell Maturation Antigen by Patel, Darshana R., Wallweber, Heidi J.A., Yin, JianPing, Shriver, Stephanie K., Marsters, Scot A., Gordon, Nathaniel C., Starovasnik, Melissa A., Kelley, Robert F.

“…B cell maturation antigen (BCMA) is a tumor necrosis factor receptor family member whose physiological role remains unclear. BCMA has been implicated as a…”
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The Crystal Structures of EDA-A1 and EDA-A2 by Hymowitz, Sarah G, Compaan, Deanne M, Yan, Minhong, Wallweber, Heidi J.A, Dixit, Vishva M, Starovasnik, Melissa A, de Vos, Abraham M

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