Search Results - "Bullock, Alex"

Targeted protein degradation: expanding the toolbox by Schapira, Matthieu, Calabrese, Matthew F., Bullock, Alex N., Crews, Craig M.

“…Proteolysis-targeting chimeras (PROTACs) and related molecules that induce targeted protein degradation by the ubiquitin–proteasome system represent a new…”
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Structural basis of Keap1 interactions with Nrf2 by Canning, Peter, Sorrell, Fiona J., Bullock, Alex N.

“…Keap1 is a highly redox-sensitive member of the BTB-Kelch family that assembles with the Cul3 protein to form a Cullin–RING E3 ligase complex for the…”
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Structural Basis of Intracellular TGF-β Signaling: Receptors and Smads by Chaikuad, Apirat, Bullock, Alex N

“…Stimulation of the transforming growth factor β (TGF-β) family receptors activates an intracellular phosphorylation-dependent signaling cascade that culminates…”
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Structural basis for the potent and selective binding of LDN-212854 to the BMP receptor kinase ALK2 by Williams, Eleanor, Bullock, Alex N.

“…Individuals with the rare developmental disorder fibrodysplasia ossificans progressiva (FOP) experience disabling heterotopic ossification caused by a gain of…”
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A new class of small molecule inhibitor of BMP signaling by Sanvitale, Caroline E, Kerr, Georgina, Chaikuad, Apirat, Ramel, Marie-Christine, Mohedas, Agustin H, Reichert, Sabine, Wang, You, Triffitt, James T, Cuny, Gregory D, Yu, Paul B, Hill, Caroline S, Bullock, Alex N

“…Growth factor signaling pathways are tightly regulated by phosphorylation and include many important kinase targets of interest for drug discovery. Small…”
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Ubiquitin ligases: guardians of mammalian development by Cruz Walma, David A., Chen, Zhuoyao, Bullock, Alex N., Yamada, Kenneth M.

“…Mammalian development demands precision. Millions of molecules must be properly located in temporal order, and their function regulated, to orchestrate…”
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Relationship between markers of malnutrition and clinical outcomes in older adults with cancer: systematic review, narrative synthesis and meta-analysis by Bullock, Alex F., Greenley, Sarah L., McKenzie, Gordon A. G., Paton, Lewis W., Johnson, Miriam J.

“…Malnutrition predicts poorer clinical outcomes for people with cancer. Older adults with cancer are a complex, growing population at high risk of weight-losing…”
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DFG‑1 Residue Controls Inhibitor Binding Mode and Affinity, Providing a Basis for Rational Design of Kinase Inhibitor Selectivity by Schröder, Martin, Bullock, Alex N, Fedorov, Oleg, Bracher, Franz, Chaikuad, Apirat, Knapp, Stefan

“…Selectivity remains a challenge for ATP-mimetic kinase inhibitors, an issue that may be overcome by targeting unique residues or binding pockets. However, to…”
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Structural Basis for Recruitment of DAPK1 to the KLHL20 E3 Ligase by Chen, Zhuoyao, Picaud, Sarah, Filippakopoulos, Panagis, D'Angiolella, Vincenzo, Bullock, Alex N.

“…BTB-Kelch proteins form the largest subfamily of Cullin-RING E3 ligases, yet their substrate complexes are mapped and structurally characterized only for KEAP1…”
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Recurrent activating ACVR1 mutations in diffuse intrinsic pontine glioma by Taylor, Kathryn R, Mackay, Alan, Truffaux, Nathalène, Butterfield, Yaron S, Morozova, Olena, Philippe, Cathy, Castel, David, Grasso, Catherine S, Vinci, Maria, Carvalho, Diana, Carcaboso, Angel M, de Torres, Carmen, Cruz, Ofelia, Mora, Jaume, Entz-Werle, Natacha, Ingram, Wendy J, Monje, Michelle, Hargrave, Darren, Bullock, Alex N, Puget, Stéphanie, Yip, Stephen, Jones, Chris, Grill, Jacques

“…Chris Jones, Jacques Grill and colleagues report the identification of recurrent activating mutations in ACVR1 in diffuse intrinsic pontine gliomas. Diffuse…”
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Structural and biochemical characterization establishes a detailed understanding of KEAP1-CUL3 complex assembly by Adamson, Roslin J., Payne, N Connor, Bartual, Sergio G., Mazitschek, Ralph, Bullock, Alex N.

“…KEAP1 promotes the ubiquitin-dependent degradation of NRF2 by assembling into a CUL3-dependent ubiquitin ligase complex. Oxidative and electrophilic stress…”
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ACVR1 Mutations in DIPG: Lessons Learned from FOP by TAYLOR, Kathryn R, VINCI, Maria, BULLOCK, Alex N, JONES, Chris

“…Whole-genome sequencing studies have recently identified a quarter of cases of the rare childhood brainstem tumor diffuse intrinsic pontine glioma to harbor…”
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Structural complexity in the KCTD family of Cullin3-dependent E3 ubiquitin ligases by Pinkas, Daniel M, Sanvitale, Caroline E, Bufton, Joshua C, Sorrell, Fiona J, Solcan, Nicolae, Chalk, Rod, Doutch, James, Bullock, Alex N

“…Members of the potassium channel tetramerization domain (KCTD) family are soluble non-channel proteins that commonly function as Cullin3 (Cul3)-dependent E3…”
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Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors by Zhang, Tinghu, Kwiatkowski, Nicholas, Olson, Calla M, Dixon-Clarke, Sarah E, Abraham, Brian J, Greifenberg, Ann K, Ficarro, Scott B, Elkins, Jonathan M, Liang, Yanke, Hannett, Nancy M, Manz, Theresa, Hao, Mingfeng, Bartkowiak, Bartlomiej, Greenleaf, Arno L, Marto, Jarrod A, Geyer, Matthias, Bullock, Alex N, Young, Richard A, Gray, Nathanael S

“…Editorial summary A small molecule inhibits CDK12 and CDK13 activity through covalent modification of Cys residues and reveals a role of the two kinases in…”
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Structure of the Bone Morphogenetic Protein Receptor ALK2 and Implications for Fibrodysplasia Ossificans Progressiva by Chaikuad, Apirat, Alfano, Ivan, Kerr, Georgina, Sanvitale, Caroline E., Boergermann, Jan H., Triffitt, James T., von Delft, Frank, Knapp, Stefan, Knaus, Petra, Bullock, Alex N.

“…Bone morphogenetic protein (BMP) receptor kinases are tightly regulated to control development and tissue homeostasis. Mutant receptor kinase domains escape…”
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Mutant ACVR1 Arrests Glial Cell Differentiation to Drive Tumorigenesis in Pediatric Gliomas by Fortin, Jerome, Tian, Ruxiao, Zarrabi, Ida, Hill, Graham, Williams, Eleanor, Sanchez-Duffhues, Gonzalo, Thorikay, Midory, Ramachandran, Parameswaran, Siddaway, Robert, Wong, Jong Fu, Wu, Annette, Apuzzo, Lorraine N., Haight, Jillian, You-Ten, Annick, Snow, Bryan E., Wakeham, Andrew, Goldhamer, David J., Schramek, Daniel, Bullock, Alex N., Dijke, Peter ten, Hawkins, Cynthia, Mak, Tak W.

“…Diffuse intrinsic pontine gliomas (DIPGs) are aggressive pediatric brain tumors for which there is currently no effective treatment. Some of these tumors…”
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Structural and biochemical characterization of the KLHL3-WNK kinase interaction important in blood pressure regulation by Schumacher, Frances-Rose, Sorrell, Fiona J, Alessi, Dario R, Bullock, Alex N, Kurz, Thimo

“…WNK1 [with no lysine (K)] and WNK4 regulate blood pressure by controlling the activity of ion co-transporters in the kidney. Groundbreaking work has revealed…”
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Structural Basis for Cul3 Protein Assembly with the BTB-Kelch Family of E3 Ubiquitin Ligases by Canning, Peter, Cooper, Christopher D.O., Krojer, Tobias, Murray, James W., Pike, Ashley C.W., Chaikuad, Apirat, Keates, Tracy, Thangaratnarajah, Chancievan, Hojzan, Viktorija, Marsden, Brian D., Gileadi, Opher, Knapp, Stefan, von Delft, Frank, Bullock, Alex N.

“…Cullin-RING ligases are multisubunit E3 ubiquitin ligases that recruit substrate-specific adaptors to catalyze protein ubiquitylation. Cul3-based Cullin-RING…”
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Structures of ABCB10, a human ATP-binding cassette transporter in apo- and nucleotide-bound states by Shintre, Chitra A., Pike, Ashley C. W., Li, Qiuhong, Kim, Jung-In, Barr, Alastair J., Goubin, Solenne, Shrestha, Leela, Yang, Jing, Berridge, Georgina, Ross, Jonathan, Stansfeld, Phillip J., Sansom, Mark S. P., Edwards, Aled M., Bountra, Chas, Marsden, Brian D., von Delft, Frank, Bullock, Alex N., Gileadi, Opher, Burgess-Brown, Nicola A., Carpenter, Elisabeth P.

“…ABCB10 is one of the three ATP-binding cassette (ABC) transporters found in the inner membrane of mitochondria. In mammals ABCB10 is essential for…”
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The DUF1669 domain of FAM83 family proteins anchor casein kinase 1 isoforms by Fulcher, Luke J, Bozatzi, Polyxeni, Tachie-Menson, Theresa, Wu, Kevin Z L, Cummins, Timothy D, Bufton, Joshua C, Pinkas, Daniel M, Dunbar, Karen, Shrestha, Sabin, Wood, Nicola T, Weidlich, Simone, Macartney, Thomas J, Varghese, Joby, Gourlay, Robert, Campbell, David G, Dingwell, Kevin S, Smith, James C, Bullock, Alex N, Sapkota, Gopal P

“…Members of the casein kinase 1 (CK1) family of serine-threonine protein kinases are implicated in the regulation of many cellular processes, including the cell…”
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