Search Results - "Bekes, Miklos"

Activity profiling and crystal structures of inhibitor-bound SARS-CoV-2 papain-like protease: A framework for anti-COVID-19 drug design by Rut, Wioletta, Lv, Zongyang, Zmudzinski, Mikolaj, Patchett, Stephanie, Nayak, Digant, Snipas, Scott J, El Oualid, Farid, Huang, Tony T, Bekes, Miklos, Drag, Marcin, Olsen, Shaun K

“…Viral papain-like cysteine protease (PLpro, NSP3) is essential for SARS-CoV-2 replication and represents a promising target for the development of antiviral…”
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The Auto-Generated Fragment of the Usp1 Deubiquitylase Is a Physiological Substrate of the N-End Rule Pathway by Piatkov, Konstantin I., Colnaghi, Luca, Békés, Miklos, Varshavsky, Alexander, Huang, Tony T.

“…Deamidation of N-terminal Gln by the Ntaq1 NtQ-amidase is a part of the Arg/N-end rule pathway, a ubiquitin-dependent proteolytic system. Here we identify…”
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Structure and Substrate Recognition of the Escherichia coli DNA Adenine Methyltransferase by Horton, John R., Liebert, Kirsten, Bekes, Miklos, Jeltsch, Albert, Cheng, Xiaodong

“…The structure of the Escherichia coli Dam DNA-(adenine-N6)-methyltransferase in complex with cognate DNA was determined at 1.89 Å resolution in the presence of…”
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Synthetic substrates for measuring activity of autophagy proteases-autophagins (Atg4): Autophagins (Atg4) by Shu, Chih-Wen, Drag, Marcin, Bekes, Miklos, Zhai, Dayong, Salvesen, Guy S., Reed, John C.

“…Atg4 cysteine proteases (autophagins) play crucial roles in autophagy by proteolytic activation of Atg8 paralogs for targeting to autophagic vesicles by lipid…”
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Positional-scanning fluorigenic substrate libraries reveal unexpected specificity determinants of DUBs (deubiquitinating enzymes) by Drag, Marcin, Mikolajczyk, Jowita, Bekes, Miklos, Reyes-Turcu, Francisca E, Ellman, Jonathan A, Wilkinson, Keith D, Salvesen, Guy S

“…DUBs (deubiquitinating enzymes) are a family of proteases responsible for the specific removal of ubiquitin attached to target proteins and thus control the…”
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A molecular sensor determines the ubiquitin substrate specificity of SARS-CoV-2 papain-like protease by Patchett, Stephanie, Lv, Zongyang, Rut, Wioletta, Békés, Miklos, Drag, Marcin, Olsen, Shaun K., Huang, Tony T.

“…The SARS-CoV-2 papain-like protease (PLpro) is a target for antiviral drug development. It is essential for processing viral polyproteins for replication and…”
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PROTAC targeted protein degraders: the past is prologue by Békés, Miklós, Langley, David R., Crews, Craig M.

“…Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to tackle disease-causing proteins that have historically been highly…”
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Engineered unnatural ubiquitin for optimal detection of deubiquitinating enzymes by Rut, Wioletta, Zmudzinski, Mikolaj, Snipas, Scott J, Bekes, Miklos, Huang, Tony T, Drag, Marcin

“…Deubiquitinating enzymes (DUBs) are responsible for removing ubiquitin (Ub) from its protein conjugates. DUBs have been implicated as attractive therapeutic…”
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Engineered unnatural ubiquitin for optimal detection of deubiquitinating enzymes† †Electronic supplementary information (ESI) available: DUBs substrate specificity, DUB labelling in cell lysates, pull-down experiment, structures of natural and unnatural amino acids and characterization of all compounds (PDF). See DOI: 10.1039/d0sc01347a by Rut, Wioletta, Zmudzinski, Mikolaj, Snipas, Scott J., Bekes, Miklos, Huang, Tony T., Drag, Marcin

“…Herein we present a workflow for design and synthesis of novel selective Ub-based tools for DUBs. Selectivity is achieved by incorporation of unnatural amino…”
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Recognition of Lys48-Linked Di-ubiquitin and Deubiquitinating Activities of the SARS Coronavirus Papain-like Protease by Békés, Miklós, van der Heden van Noort, Gerbrand J., Ekkebus, Reggy, Ovaa, Huib, Huang, Tony T., Lima, Christopher D.

“…Deubiquitinating enzymes (DUBs) recognize and cleave linkage-specific polyubiquitin (polyUb) chains, but mechanisms underlying specificity remain elusive in…”
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Deubiquitinases as a Signaling Target of Oxidative Stress by Cotto-Rios, Xiomaris M., Békés, Miklós, Chapman, Jessica, Ueberheide, Beatrix, Huang, Tony T.

“…Deubiquitinating enzymes (DUBs) constitute a large family of cysteine proteases that have a broad impact on numerous biological and pathological processes,…”
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Abstract PR09: KRAS-targeted PROTAC degraders are broadly efficacious against KRAS-dependent tumor models by Smith, Kathryn, Lopez-Arroyo, Andrea, Berk, Jason, Hegan, Peter, Nower, Peter, Tice, Samantha, Moutran, Aurelie, Pizzano, Jennifer, Dowtin, Amanda, Bookbinder, Mark, Bortolon, Elizabeth, Cadelina, Greg, Karim, Fazlul, Digianantonio, Katie, Bekes, Miklos, Medina, Jesus

“…Abstract KRAS is genomically altered in about one third of all human tumors. Due to its central role in oncogenesis, many attempts have been made in the last…”
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SENP8 limits aberrant neddylation of NEDD8 pathway components to promote cullin-RING ubiquitin ligase function by Coleman, Kate E, Békés, Miklós, Chapman, Jessica R, Crist, Sarah B, Jones, Mathew Jk, Ueberheide, Beatrix M, Huang, Tony T

“…NEDD8 is a ubiquitin-like modifier most well-studied for its role in activating the largest family of ubiquitin E3 ligases, the cullin-RING ligases (CRLs)…”
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Oral Estrogen Receptor PROTAC Vepdegestrant (ARV-471) Is Highly Efficacious as Monotherapy and in Combination with CDK4/6 or PI3K/mTOR Pathway Inhibitors in Preclinical ER+ Breast Cancer Models by Gough, Sheryl M, Flanagan, John J, Teh, Jessica, Andreoli, Monica, Rousseau, Emma, Pannone, Melissa, Bookbinder, Mark, Willard, Ryan, Davenport, Kim, Bortolon, Elizabeth, Cadelina, Gregory, Gordon, Debbie, Pizzano, Jennifer, Macaluso, Jennifer, Soto, Leofal, Corradi, John, Digianantonio, Katherine, Drulyte, Ieva, Morgan, Alicia, Quinn, Connor, Békés, Miklós, Ferraro, Caterina, Chen, Xin, Wang, Gan, Dong, Hanqing, Wang, Jing, Langley, David R, Houston, John, Gedrich, Richard, Taylor, Ian C

“…Estrogen receptor (ER) alpha signaling is a known driver of ER-positive (ER+)/human epidermal growth factor receptor 2 negative (HER2-) breast cancer…”
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Co-opting the E3 ligase KLHDC2 for targeted protein degradation by small molecules by Hickey, Christopher M., Digianantonio, Katherine M., Zimmermann, Kurt, Harbin, Alicia, Quinn, Connor, Patel, Avani, Gareiss, Peter, Chapman, Amanda, Tiberi, Bernadette, Dobrodziej, Jennifer, Corradi, John, Cacace, Angela M., Langley, David R., Békés, Miklós

“…Targeted protein degradation (TPD) by PROTAC (proteolysis-targeting chimera) and molecular glue small molecules is an emerging therapeutic strategy. To expand…”
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The Dynamics and Mechanism of SUMO Chain Deconjugation by SUMO-specific Proteases by Békés, Miklós, Prudden, John, Srikumar, Tharan, Raught, Brian, Boddy, Michael N., Salvesen, Guy S.

“…SUMOylation of proteins is a cyclic process that requires both conjugation and deconjugation of SUMO moieties. Besides modification by a single SUMO, SUMO…”
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Small ubiquitin-related modifier (SUMO)-specific proteases: profiling the specificities and activities of human SENPs by Mikolajczyk, Jowita, Drag, Marcin, Békés, Miklós, Cao, John T, Ronai, Ze'ev, Salvesen, Guy S

“…SENPs are proteases that participate in the regulation of SUMOylation by generating mature small ubiquitin-related modifiers (SUMO) for protein conjugation…”
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The COP9 signalosome inhibits Cullin-RING E3 ubiquitin ligases independently of its deneddylase activity by Suisse, Annabelle, Békés, Miklós, Huang, Tony T., Treisman, Jessica E.

“…The COP9 signalosome inhibits the activity of Cullin-RING E3 ubiquitin ligases by removing Nedd8 modifications from their Cullin subunits. Neddylation renders…”
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Protection from Isopeptidase-Mediated Deconjugation Regulates Paralog-Selective Sumoylation of RanGAP1 by Zhu, Shanshan, Goeres, Jacqueline, Sixt, Katherine M., Békés, Miklós, Zhang, Xiang-Dong, Salvesen, Guy S., Matunis, Michael J.

“…Vertebrates express three small ubiquitin-related modifiers (SUMO-1, SUMO-2, and SUMO-3) that are conjugated in part to unique subsets of proteins and,…”
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DUB-Resistant Ubiquitin to Survey Ubiquitination Switches in Mammalian Cells by Békés, Miklós, Okamoto, Keiji, Crist, Sarah B., Jones, Mathew J., Chapman, Jessica R., Brasher, Bradley B., Melandri, Francesco D., Ueberheide, Beatrix M., Lazzerini Denchi, Eros, Huang, Tony T.

“…The ubiquitin-modification status of proteins in cells is highly dynamic and maintained by specific ligation machineries (E3 ligases) that tag proteins with…”
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