Search Results - "Pilka, Ewa S."

Therapeutic Potential of Targeting Plasminogen Activator Inhibitor-1 in COVID-19 by Kellici, Tahsin F., Pilka, Ewa S., Bodkin, Michael J.

“…Latest research shows that SERPINE1 overexpression has an important role in Coronavirus 2019 (COVID-19)-associated coagulopathy leading to acute respiratory…”
Get full text

Structural definitions of Jumonji family demethylase selectivity by Pilka, Ewa S., James, Tim, Lisztwan, Joanna Hergovich

“…•Structural studies give insight into how demethylases selectively recognise targets.•Specific amino acids, methylation status and context are uniquely…”
Get full text

Structural Snapshots for the Conformation-dependent Catalysis by Human Medium-chain Acyl-coenzyme A Synthetase ACSM2A by Kochan, Grazyna, Pilka, Ewa S., von Delft, Frank, Oppermann, Udo, Yue, Wyatt W.

“…Acyl-CoA synthetases belong to the superfamily of adenylate-forming enzymes, and catalyze the two-step activation of fatty acids or carboxylate-containing…”
Get full text

Crystal structures of histone demethylase JMJD2A reveal basis for substrate specificity by NG, Stanley S, KAVANAGH, Kathryn L, ROSE, Nathan R, OFFER, John, SCHEINOST, Johanna C, BOROWSKI, Tomasz, SUNDSTROM, Michael, SCHOFIELD, Christopher J, OPPERMANN, Udo, MCDONOUGH, Michael A, BUTLER, Danica, PILKA, Ewa S, LIENARD, Benoit M. R, BRAY, James E, SAVITSKY, Pavel, GILEADI, Opher, VON DELFT, Frank

“…Post-translational histone modification has a fundamental role in chromatin biology and is proposed to constitute a 'histone code' in epigenetic regulation…”
Get full text

Insight into S-adenosylmethionine biosynthesis from the crystal structures of the human methionine adenosyltransferase catalytic and regulatory subunits by Shafqat, Naeem, Muniz, Joao R C, Pilka, Ewa S, Papagrigoriou, Evangelos, von Delft, Frank, Oppermann, Udo, Yue, Wyatt W

“…MAT (methionine adenosyltransferase) utilizes L-methionine and ATP to form SAM (S-adenosylmethionine), the principal methyl donor in biological methylation…”
Get more information

Structural basis for substrate specificity in human monomeric carbonyl reductases by Pilka, Ewa S, Niesen, Frank H, Lee, Wen Hwa, El-Hawari, Yasser, Dunford, James E, Kochan, Grazyna, Wsol, Vladimir, Martin, Hans-Joerg, Maser, Edmund, Oppermann, Udo

“…Carbonyl reduction constitutes a phase I reaction for many xenobiotics and is carried out in mammals mainly by members of two protein families, namely…”
Get full text

Small-molecule inhibition of METTL3 as a strategy against myeloid leukaemia by Yankova, Eliza, Blackaby, Wesley, Albertella, Mark, Rak, Justyna, De Braekeleer, Etienne, Tsagkogeorga, Georgia, Pilka, Ewa S., Aspris, Demetrios, Leggate, Dan, Hendrick, Alan G., Webster, Natalie A., Andrews, Byron, Fosbeary, Richard, Guest, Patrick, Irigoyen, Nerea, Eleftheriou, Maria, Gozdecka, Malgorzata, Dias, Joao M. L., Bannister, Andrew J., Vick, Binje, Jeremias, Irmela, Vassiliou, George S., Rausch, Oliver, Tzelepis, Konstantinos, Kouzarides, Tony

“…N 6 -methyladenosine (m 6 A) is an abundant internal RNA modification 1 , 2 that is catalysed predominantly by the METTL3–METTL14 methyltransferase complex 3 ,…”
Get full text

Structural and biochemical studies of a moderately thermophilic exonuclease I from Methylocaldum szegediense by Fei, Li, Tian, SiSi, Moysey, Ruth, Misca, Mihaela, Barker, John J, Smith, Myron A, McEwan, Paul A, Pilka, Ewa S, Crawley, Lauren, Evans, Tom, Sun, Dapeng

“…A novel exonuclease, designated as MszExo I, was cloned from Methylocaldum szegediense, a moderately thermophilic methanotroph. It specifically digests…”
Get full text

Crystal Structures of Malonyl-Coenzyme A Decarboxylase Provide Insights into Its Catalytic Mechanism and Disease-Causing Mutations by Froese, D. Sean, Forouhar, Farhad, Tran, Timothy H., Vollmar, Melanie, Kim, Yi Seul, Lew, Scott, Neely, Helen, Seetharaman, Jayaraman, Shen, Yang, Xiao, Rong, Acton, Thomas B., Everett, John K., Cannone, Giuseppe, Puranik, Sriharsha, Savitsky, Pavel, Krojer, Tobias, Pilka, Ewa S., Kiyani, Wasim, Lee, Wen Hwa, Marsden, Brian D., von Delft, Frank, Allerston, Charles K., Spagnolo, Laura, Gileadi, Opher, Montelione, Gaetano T., Oppermann, Udo, Yue, Wyatt W., Tong, Liang

“…Malonyl-coenzyme A decarboxylase (MCD) is found from bacteria to humans, has important roles in regulating fatty acid metabolism and food intake, and is an…”
Get full text

High-affinity inhibitors of human NAD-dependent 15-hydroxyprostaglandin dehydrogenase: mechanisms of inhibition and structure-activity relationships by Niesen, Frank H, Schultz, Lena, Jadhav, Ajit, Bhatia, Chitra, Guo, Kunde, Maloney, David J, Pilka, Ewa S, Wang, Minghua, Oppermann, Udo, Heightman, Tom D, Simeonov, Anton

“…15-Hydroxyprostaglandin dehydrogenase (15-PGDH, EC 1.1.1.141) is the key enzyme for the inactivation of prostaglandins, regulating processes such as…”
Get full text

Small-molecule modulators of serine protease inhibitor proteins (serpins) by Kellici, Tahsin F., Pilka, Ewa S., Bodkin, Michael J.

“…•Targeting serpins with drug-like molecules remains a challenge in drug discovery.•Compounds targeting HSP47, antitrypsin, antithrombin, PAI-1 and neuroserpin…”
Get full text

Analysis of the substrate-binding site of human carbonyl reductases CBR1 and CBR3 by site-directed mutagenesis by El-Hawari, Yasser, Favia, Angelo D., Pilka, Ewa S., Kisiela, Michael, Oppermann, Udo, Martin, Hans-Jörg, Maser, Edmund

“…Human carbonyl reductase is a member of the short-chain dehydrogenase/reductase (SDR) protein superfamily and is known to play an important role in the…”
Get full text

Discovery of a potent and selective inhibitor for human carbonyl reductase 1 from propionate scanning applied to the macrolide zearalenone by Zimmermann, Tobias J., Niesen, Frank H., Pilka, Ewa S., Knapp, Stefan, Oppermann, Udo, Maier, Martin E.

“…Zearalenone analogue 5 turned out to be an inhibitor of human carbonyl reductase 1 (CBR1). In order to extend the chemical diversity available for organic…”
Get full text

High Affinity Streptococcal Binding to Human Fibronectin Requires Specific Recognition of Sequential F1 Modules by Schwarz-Linek, Ulrich, Pilka, Ewa S., Pickford, Andrew R., Kim, Jung Hwa, Höök, Magnus, Campbell, Iain D., Potts, Jennifer R.

“…Fibronectin (Fn) binding by the Streptococcus pyogenes protein SfbI has been shown to trigger integrin-dependent internalization of this pathogen by human…”
Get full text

Crystal structure of the secretory isozyme of mammalian carbonic anhydrases CA VI: Implications for biological assembly and inhibitor development by Pilka, Ewa S., Kochan, Grazyna, Oppermann, Udo, Yue, Wyatt W.

“…► Structure of the only carbonic anhydrase secretory isoform CA VI is presented. ► CA VI forms a dimer both in crystal and in solution. ► Active site contains…”
Get full text

Ribosomal oxygenases are structurally conserved from prokaryotes to humans by Chowdhury, Rasheduzzaman, Sekirnik, Rok, Brissett, Nigel C., Krojer, Tobias, Ho, Chia-hua, Ng, Stanley S., Clifton, Ian J., Ge, Wei, Kershaw, Nadia J., Fox, Gavin C., Muniz, Joao R. C., Vollmar, Melanie, Phillips, Claire, Pilka, Ewa S., Kavanagh, Kathryn L., von Delft, Frank, Oppermann, Udo, McDonough, Michael A., Doherty, Aidan J., Schofield, Christopher J.

“…Crystal structures of human and prokaryotic ribosomal oxygenases reported here, with and without their ribosomal protein substrates, support their assignments…”
Get full text

The inhibition of human farnesyl pyrophosphate synthase by nitrogen-containing bisphosphonates. Elucidating the role of active site threonine 201 and tyrosine 204 residues using enzyme mutants by Tsoumpra, Maria K, Muniz, Joao R, Barnett, Bobby L, Kwaasi, Aaron A, Pilka, Ewa S, Kavanagh, Kathryn L, Evdokimov, Artem, Walter, Richard L, Von Delft, Frank, Ebetino, Frank H, Oppermann, Udo, Russell, R. Graham G, Dunford, James E

“…Abstract Farnesyl pyrophosphate synthase (FPPS) is the major molecular target of nitrogen-containing bisphosphonates (N-BPs), used clinically as bone…”
Get full text

Pathogenic bacteria attach to human fibronectin through a tandem β-zipper by Potts, Jennifer R, Schwarz-Linek, Ulrich, Werner, Jörn M, Pickford, Andrew R, Gurusiddappa, Sivashankarappa, Kim, Jung Hwa, Pilka, Ewa S, Briggs, John A. G, Gough, T. Sebastian, Höök, Magnus, Campbell, Iain D

“…Staphylococcus aureus and Streptococcus pyogenes, two important human pathogens, target host fibronectin (Fn) in their adhesion to and invasion of host cells…”
Get full text

Crystal structure of human carbonic anhydrase‐related protein VIII reveals the basis for catalytic silencing by Picaud, Sarah S., Muniz, João R. C., Kramm, Anneke, Pilka, Ewa S., Kochan, Grazyna, Oppermann, Udo, Yue, Wyatt W.

Get full text

Structure of human aspartyl aminopeptidase complexed with substrate analogue: insight into catalytic mechanism, substrate specificity and M18 peptidase family by Chaikuad, Apirat, Pilka, Ewa S, De Riso, Antonio, von Delft, Frank, Kavanagh, Kathryn L, Vénien-Bryan, Catherine, Oppermann, Udo, Yue, Wyatt W

“…Aspartyl aminopeptidase (DNPEP), with specificity towards an acidic amino acid at the N-terminus, is the only mammalian member among the poorly understood M18…”
Get full text