Search Results - "Vinković, Mladen"

Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein–Protein Interaction by Chessari, Gianni, Hardcastle, Ian R, Ahn, Jong Sook, Anil, Burcu, Anscombe, Elizabeth, Bawn, Ruth H, Bevan, Luke D, Blackburn, Timothy J, Buck, Ildiko, Cano, Celine, Carbain, Benoit, Castro, Juan, Cons, Ben, Cully, Sarah J, Endicott, Jane A, Fazal, Lynsey, Golding, Bernard T, Griffin, Roger J, Haggerty, Karen, Harnor, Suzannah J, Hearn, Keisha, Hobson, Stephen, Holvey, Rhian S, Howard, Steven, Jennings, Claire E, Johnson, Christopher N, Lunec, John, Miller, Duncan C, Newell, David R, Noble, Martin E. M, Reeks, Judith, Revill, Charlotte H, Riedinger, Christiane, St. Denis, Jeffrey D, Tamanini, Emiliano, Thomas, Huw, Thompson, Neil T, Vinković, Mladen, Wedge, Stephen R, Williams, Pamela A, Wilsher, Nicola E, Zhang, Bian, Zhao, Yan

“…Inhibition of murine double minute 2 (MDM2)-p53 protein–protein interaction with small molecules has been shown to reactivate p53 and inhibit tumor growth…”
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A Diverse Array of Large Capsules Transform in Response to Stimuli by Wu, Kai, Ronson, Tanya K., Goh, Leonard, Xue, Weichao, Heard, Andrew W., Su, Pingru, Li, Xiaopeng, Vinković, Mladen, Nitschke, Jonathan R.

“…The allosteric regulation of biomolecules, such as enzymes, enables them to adapt and alter their conformation to fit specific substrates, expressing different…”
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Fragment-Based Discovery of the Pyrazol-4-yl Urea (AT9283), a Multitargeted Kinase Inhibitor with Potent Aurora Kinase Activity by Howard, Steven, Berdini, Valerio, Boulstridge, John A, Carr, Maria G, Cross, David M, Curry, Jayne, Devine, Lindsay A, Early, Theresa R, Fazal, Lynsey, Gill, Adrian L, Heathcote, Michelle, Maman, Sarita, Matthews, Julia E, McMenamin, Rachel L, Navarro, Eva F, O’Brien, Michael A, O’Reilly, Marc, Rees, David C, Reule, Matthias, Tisi, Dominic, Williams, Glyn, Vinković, Mladen, Wyatt, Paul G

“…Here, we describe the identification of a clinical candidate via structure-based optimization of a ligand efficient pyrazole-benzimidazole fragment. Aurora…”
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Systematic construction of progressively larger capsules from a fivefold linking pyrrole-based subcomponent by Wu, Kai, Ronson, Tanya K., Su, Pingru, Chen, Zhi, Goh, Leonard, Heard, Andrew W., Li, Xiaopeng, Klautzsch, Fabian, Schalley, Christoph A., Vinković, Mladen, Nitschke, Jonathan R.

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Discovery of (2,4-Dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a Novel Inhibitor of the Molecular Chaperone Hsp90 by Fragment Based Drug Design by Woodhead, Andrew J, Angove, Hayley, Carr, Maria G, Chessari, Gianni, Congreve, Miles, Coyle, Joseph E, Cosme, Jose, Graham, Brent, Day, Philip J, Downham, Robert, Fazal, Lynsey, Feltell, Ruth, Figueroa, Eva, Frederickson, Martyn, Lewis, Jonathan, McMenamin, Rachel, Murray, Christopher W, O’Brien, M. Alistair, Parra, Lina, Patel, Sahil, Phillips, Theresa, Rees, David C, Rich, Sharna, Smith, Donna-Michelle, Trewartha, Gary, Vinkovic, Mladen, Williams, Brian, Woolford, Alison J.-A

“…Inhibitors of the molecular chaperone heat shock protein 90 (Hsp90) are currently generating significant interest in clinical development as potential…”
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Fragment-Based Discovery of Mexiletine Derivatives as Orally Bioavailable Inhibitors of Urokinase-Type Plasminogen Activator by Frederickson, Martyn, Callaghan, Owen, Chessari, Gianni, Congreve, Miles, Cowan, Suzanna R, Matthews, Julia E, McMenamin, Rachel, Smith, Donna-Michelle, Vinković, Mladen, Wallis, Nicola G

“…Fragment-based lead discovery has been applied to urokinase-type plasminogen activator (uPA). The (R)-enantiomer of the orally active drug mexiletine 5 (a…”
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High-throughput protein crystallography and drug discovery by Tickle, Ian, Sharff, Andrew, Vinkovic, Mladen, Yon, Jeff, Jhoti, Harren

“…Single crystal X-ray diffraction is the technique of choice for studying the interactions of small organic molecules with proteins by determining their…”
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High throughput protein crystallography: Developments in crystallisation, data collection and data processing by O’Reilly, Marc, Vinković, Mladen, Sharff, Andrew, Jhoti, Harren

“…Until recently, individual protein structure determination using protein X-ray crystallography was often a protracted and resource intensive process, sometimes…”
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Abstract 7073: Integrating fragment-based crystallographic screening with dTAG-PROTAC degradation and genetic rescue to explore the function of eIF4E by Clarke, Paul A., Sharp, Swee Y., Martella, Marianna, Milton, Christopher I., East, Charlotte, Vinkovic, Mladen, Wallis, Nicola, Ward, George, Richardson, Caroline, Woodhead, Andrew

“…Abstract The translation initiation factor eIF4E is a rate-limiting factor for protein synthesis that binds the mRNA m7G-cap to initiate the recruitment and…”
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Crystal Structure of Escherichia coli Ketopantoate Reductase at 1.7 Å Resolution and Insight into the Enzyme Mechanism by Matak-Vinković, Dijana, Vinković, Mladen, Saldanha, S. Adrian, Ashurst, Jennifer L, von Delft, Frank, Inoue, Tsuyoshi, Miguel, Ricardo Nunez, Smith, Alison G, Blundell, Tom L, Abell, Chris

“…Ketopantoate reductase (KPR, EC 1.1.1.169) catalyzes the NADPH-dependent reduction of ketopantoate to pantoate on the pantothenate (vitamin B5) biosynthetic…”
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Abstract 6588: Discovery of ASTX295, a potent, next-generation small molecule antagonist of MDM2 with differentiated pharmacokinetic profile by Ahn, Maria, Bevan, Luke, Buck, Ildiko, Cano, Celine, Castro, Juan, Cons, Ben, Endicott, Jane, Fazal, Lynsey, Ferrari, Nicola, Hardcastle, Ian, Hearn, Keisha, Holvey, Rhian, Howard, Steven, Johnson, Chris, Jennings, Claire, Kucia-Tran, Justyna, Kyle, Suzanne, Lunec, John, Lyons, John, Miller, Duncan, Rees, David, Noble, Martin, Newell, David R., Reeks, Judith, Saini, Harpreet, St. Denis, Jeffrey, Tamanini, Emiliano, Thomas, Huw, Thompson, Neil, Vinkovic, Mladen, Ward, George, Wallis, Nicola, Walton, Hugh, Wedge, Stephen, Williams, Pamela, Willmore, Elaine, Wilshire, Nicola, Zhao, Yan, Chessari, Gianni

“…Abstract In response to cellular stress, the tumor suppressor p53 is activated to modulate cell cycle progression, DNA repair, and apoptosis. Inhibition of the…”
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Crystal Structure of Human Soluble Adenylate Cyclase Reveals a Distinct, Highly Flexible Allosteric Bicarbonate Binding Pocket by Saalau-Bethell, Susanne M., Berdini, Valerio, Cleasby, Anne, Congreve, Miles, Coyle, Joseph E., Lock, Victoria, Murray, Christopher W., O'Brien, M. Alistair, Rich, Sharna J., Sambrook, Tracey, Vinkovic, Mladen, Yon, Jeff R., Jhoti, Harren

“…Soluble adenylate cyclases catalyse the synthesis of the second messenger cAMP through the cyclisation of ATP and are the only known enzymes to be directly…”
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Identification of novel allosteric inhibitors through fragment-based drug discovery and X-ray crystallography by Pathuri, Puja, Saalau-Bethell, Susanne M., Woodhead, Andrew J., Berdini, Valerio, Carr, Maria G., Chessari, Gianni, Cleasby, Anne, Congreve, Miles, Coyle, Joseph E., Graham, Brent, Hiscock, Steven D., Lock, Victoria, Murray, Christopher W., O'Brien, M. Alistair, Rich, Sharna J., Richardson, Caroline J., Sambrook, Tracey, Vinkovic, Mladen, Williams, Pamela A., Yon, Jeff R., Jhoti, Harren

“…Abstract only…”
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4-Acetamido-N-(λ-triphenyl-phospho-ranyl-idene)benzene-sulfonamide by Prugovečki, Biserka, Marinković, Marina, Vinković, Mladen, Dumić, Miljenko

“…There are two independent mol-ecules per asymmetric unit of the title compound, C(26)H(23)N(2)O(3)PS. Their superposition shows that they differ in the…”
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Functional derivatives of 4-oxoazetidine-2-sulfinic acids in asymmetric synthesis of 2-azacepham sulfoxides and their transformation by Herak, Jure J., Vinković, Mladen, Lukić, Irena

“…The enantiomerically pure 2-azacepham sulfoxide 2a was synthesized by stereocontrolled intramolecular cyclization of sulfinates 3 or sulfinamides 8 in the…”
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Nitro derivatives of glutethimide by Danilovski, A., Vinkovic, M., Filic, D.

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Antihyperglycemic N-sulfonyl-1a,2,6,6a-tetrahydro-1H,4H- [1,3]dioxepino[5,6-b]azirines: synthesis, X-ray structure analysis, conformational behavior, quantitative structure-property relationships, and quantitative structure-activity relationships by Dumić, M, Vinković, M, Filić, D, Jamnicky, B, Eskinja, M, Kamenar, B

“…A series of 1-sulfonyl-1a,2,6,6a-tetrahydro-1H,4H- [1,3]dioxepino[5,6-b]azirines, 4, has been synthesized and evaluated for its effects on blood…”
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Abstract A1: The physiological form of MetAP2 can be inhibited through binding to either of the two active-site metals by Wallis, Nicola G., Berdini, Valerio, Besong, Gilbert, Chessari, Gianni, Coyle, Joe, Graham, Brent, Madin, Andrew, O'Brien, Alistair, Richardson, Caroline J., Smith, Kirsten, Thompson, Neil T., Vinkovic, Mladen, Williams, Pamela A.

“…Abstract Methionine aminopeptidases (MetAP) are metalloenzymes that remove the N-terminal initiator methionine from newly synthesized polypeptides allowing…”
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Structural constraints on protein self-processing in L-aspartate-α-decarboxylase by Schmitzberger, Florian, Kilkenny, Mairi L., Lobley, Carina M. C., Webb, Michael E., Vinkovic, Mladen, Matak-Vinkovic, Dijana, Witty, Michael, Chirgadze, Dimitri Y., Smith, Alison G., Abell, Chris, Blundell, Tom L.

“…Aspartate decarboxylase, which is translated as a pro‐protein, undergoes intramolecular self‐cleavage at Gly24–Ser25. We have determined the crystal structures…”
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4-Acetamido- N -(λ 5 -triphenylphosphoranylidene)benzenesulfonamide by Prugovečki, Biserka, Marinković, Marina, Vinković, Mladen, Dumić, Miljenko

“…There are two independent molecules per asymmetric unit of the title compound, C26H23N2O3PS. Their superposition shows that they differ in the conformation of…”
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