Search Results - "Debreczeni, Judit É."

Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR) by Ward, Richard A, Anderton, Mark J, Ashton, Susan, Bethel, Paul A, Box, Matthew, Butterworth, Sam, Colclough, Nicola, Chorley, Christopher G, Chuaqui, Claudio, Cross, Darren A. E, Dakin, Les A, Debreczeni, Judit É, Eberlein, Cath, Finlay, M. Raymond V, Hill, George B, Grist, Matthew, Klinowska, Teresa C. M, Lane, Clare, Martin, Scott, Orme, Jonathon P, Smith, Peter, Wang, Fengjiang, Waring, Michael J

“…A novel series of small-molecule inhibitors has been developed to target the double mutant form of the epidermal growth factor receptor (EGFR) tyrosine kinase,…”
Get full text

Discovery and In Vivo Efficacy of AZ-PRMT5i-1, a Novel PRMT5 Inhibitor with High MTA Cooperativity by Smith, James M., Barlaam, Bernard, Beattie, David, Bradshaw, Lauren, Chan, Ho Man, Chiarparin, Elisabetta, Collingwood, Olga, Cooke, Sophie L., Cronin, Anna, Cumming, Iain, Dean, Emma, Debreczeni, Judit É., del Barco Barrantes, Iván, Diene, Coura, Gianni, Davide, Guerot, Carine, Guo, Xiaoxiao, Guven, Sinem, Hayhow, Thomas G., Hong, Ted, Kemmitt, Paul D., Lamont, Gillian M., Lamont, Scott, Lynch, James T., McWilliams, Lisa, Moore, Shaun, Raubo, Piotr, Robb, Graeme R., Robinson, James, Scott, James S., Srinivasan, Bharath, Steward, Oliver, Stubbs, Christopher J., Syson, Karl, Tan, Lixiang, Turner, Oliver, Underwood, Elizabeth, Urosevic, Jelena, Vazquez-Chantada, Mercedes, Whittaker, Amy L., Wilson, David M., Winter-Holt, Jon J.

“…PRMT5, a type 2 arginine methyltransferase, has a critical role in regulating cell growth and survival in cancer. With the aim of developing MTA-cooperative…”
Get full text

Ruthenium Half-Sandwich Complexes Bound to Protein Kinase Pim-1 by Debreczeni, Judit É., Bullock, Alex N., Atilla, G. Ekin, Williams, Douglas S., Bregman, Howard, Knapp, Stefan, Meggers, Eric

“…Keeping in shape with half a sandwich: The structure of a picomolar organoruthenium inhibitor bound to the ATP‐binding site of the protein kinase Pim‐1 (see…”
Get full text

Ligand complex structures in protein crystallography by Debreczeni, Judit É., Emsley, Paul

“…An introduction to the Proceedings of the 2016 CCP4 Study Weekend on protein‐ligand complex structures. An introduction to the Proceedings of the 2016 CCP4…”
Get full text

Structural Basis of Inhibitor Specificity of the Human Protooncogene Proviral Insertion Site in Moloney Murine Leukemia Virus (PIM-1) Kinase by Bullock, Alex N, Debreczeni, Judit É, Fedorov, Oleg Y, Nelson, Adam, Marsden, Brian D, Knapp, Stefan

“…The kinase PIM-1 plays a pivotal role in cytokine signaling and is implicated in the development of a number of tumors. The three-dimensional structure of…”
Get full text

Crystal Structures of the p21-Activated Kinases PAK4, PAK5, and PAK6 Reveal Catalytic Domain Plasticity of Active Group II PAKs by Eswaran, Jeyanthy, Lee, Wen Hwa, Debreczeni, Judit É., Filippakopoulos, Panagis, Turnbull, Andrew, Fedorov, Oleg, Deacon, Sean W., Peterson, Jeffrey R., Knapp, Stefan

“…p21-activated kinases have been classified into two groups based on their domain architecture. Group II PAKs (PAK4–6) regulate a wide variety of cellular…”
Get full text

Crystal structures and inhibitor identification for PTPN5, PTPRR and PTPN7: a family of human MAPK-specific protein tyrosine phosphatases by Eswaran, Jeyanthy, von Kries, Jens Peter, Marsden, Brian, Longman, Emma, Debreczeni, Judit E, Ugochukwu, Emilie, Turnbull, Andrew, Lee, Wen Hwa, Knapp, Stefan, Barr, Alastair J

“…Protein tyrosine phosphatases PTPN5, PTPRR and PTPN7 comprise a family of phosphatases that specifically inactivate MAPKs (mitogen-activated protein kinases)…”
Get full text

In-house measurement of the sulfur anomalous signal and its use for phasing by Debreczeni, Judit É., Bunkóczi, Gábor, Ma, Qingjun, Blaser, Heiko, Sheldrick, George M.

“…Five test structures (orthorhombic and trigonal trypsin, cubic and rhombohedral insulin and thaumatin) have been solved by the SAD (single‐wavelength anomalous…”
Get full text

Crystal structure of human protein tyrosine phosphatase 14 (PTPN14) at 1.65-Å resolution by Barr, Alastair J., Debreczeni, Judit É., Eswaran, Jeyanthy, Knapp, Stefan

Get full text

Cryo-EM structure determination of small therapeutic protein targets at 3 Å-resolution using a rigid imaging scaffold by Castells-Graells, Roger, Meador, Kyle, Arbing, Mark A, Sawaya, Michael R, Gee, Morgan, Cascio, Duilio, Gleave, Emma, Debreczeni, Judit É, Breed, Jason, Leopold, Karoline, Patel, Ankoor, Jahagirdar, Dushyant, Lyons, Bronwyn, Subramaniam, Sriram, Phillips, Chris, Yeates, Todd O

“…Cryoelectron microscopy (Cryo-EM) has enabled structural determination of proteins larger than about 50 kDa, including many intractable by any other method,…”
Get full text

Structure of Ecballium elaterium trypsin inhibitor II (EETI-II): a rigid molecular scaffold by Krätzner, Ralph, Debreczeni, Judit É., Pape, Thomas, Schneider, Thomas R., Wentzel, Alexander, Kolmar, Harald, Sheldrick, George M., Uson, Isabel

“…The Ecballium elaterium trypsin inhibitor II (EETI‐II) belongs to the family of squash inhibitors and is one of the strongest inhibitors known for trypsin. The…”
Get full text

The crystal structure of human receptor protein tyrosine phosphatase κ phosphatase domain 1 by Eswaran, Jeyanthy, Debreczeni, Judit É., Longman, Emma, Barr, Alastair J., Knapp, Stefan

“…The receptor‐type protein tyrosine phosphatases (RPTPs) are integral membrane proteins composed of extracellular adhesion molecule‐like domains, a single…”
Get full text

The structure of P-TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation by Baumli, Sonja, Lolli, Graziano, Lowe, Edward D, Troiani, Sonia, Rusconi, Luisa, Bullock, Alex N, Debreczeni, Judit É, Knapp, Stefan, Johnson, Louise N

“…The positive transcription elongation factor b (P‐TEFb) (CDK9/cyclin T (CycT)) promotes mRNA transcriptional elongation through phosphorylation of elongation…”
Get full text

Structure of viscotoxin A3: disulfide location from weak SAD data by Debreczeni, Judit É., Girmann, Beatrix, Zeeck, Axel, Krätzner, Ralph, Sheldrick, George M.

“…The crystal structure of viscotoxin A3 (VT A3) extracted from European mistletoe (Viscum album L.) has been solved using the anomalous diffraction of the…”
Get full text

Handling ligands with Coot by Debreczeni, Judit É., Emsley, Paul

“…Coot is a molecular‐graphics application primarily aimed to assist in model building and validation of biological macromolecules. Recently, tools have been…”
Get full text

Structure of the SOCS4-ElonginB/C Complex Reveals a Distinct SOCS Box Interface and the Molecular Basis for SOCS-Dependent EGFR Degradation by Bullock, Alex N., Rodriguez, Maria C., Debreczeni, Judit É., Songyang, Zhou, Knapp, Stefan

“…Tyrosine kinase signaling is tightly controlled by negative feedback inhibitors including suppressors of cytokine signaling (SOCS). SOCS assemble as SH2 domain…”
Get full text

Cryo-EM: The Resolution Revolution and Drug Discovery by de Oliveira, Taiana Maia, van Beek, Lotte, Shilliday, Fiona, Debreczeni, Judit É, Phillips, Chris

“…Single-particle cryogenic electron microscopy (cryo-EM) has been elevated to the mainstream of structural biology propelled by technological advancements in…”
Get more information

Crystal Structure of the SOCS2-Elongin C-Elongin B Complex Defines a Prototypical SOCS Box Ubiquitin Ligase by Bullock, Alex N., Debreczeni, Judit É., Edwards, Aled M., Sundström, Michael, Knapp, Stefan

“…Growth hormone (GH) signaling is tightly controlled by ubiquitination of GH receptors, phosphorylation levels, and accessibility of binding sites for…”
Get full text

Crystal structure of the PIM2 kinase in complex with an organoruthenium inhibitor by Bullock, Alex N, Russo, Santina, Amos, Ann, Pagano, Nicholas, Bregman, Howard, Debreczeni, Judit E, Lee, Wen Hwa, von Delft, Frank, Meggers, Eric, Knapp, Stefan

“…The serine/threonine kinase PIM2 is highly expressed in human leukemia and lymphomas and has been shown to positively regulate survival and proliferation of…”
Get full text

Structural Evidence for Non-canonical Binding of Ca2+ to a Canonical EF-hand of a Conventional Myosin by Debreczeni, Judit É., Farkas, László, Harmat, Veronika, Hetényi, Csaba, Hajdú, István, Závodszky, Péter, Kohama, Kazuhiro, Nyitray, László

“…We have previously identified a single inhibitory Ca2+-binding site in the first EF-hand of the essential light chain of Physarum conventional myosin (Farkas,…”
Get full text