Search Results - "Statsyuk, Alexander V."

Development of Activity-Based Probes for Ubiquitin and Ubiquitin-like Protein Signaling Pathways by An, Heeseon, Statsyuk, Alexander V

“…Ubiquitin and ubiquitin-like (UBL) proteins regulate a vast variety of cellular functions. Some UBL proteins are present in all cell types, while others are…”
Get full text

An inhibitor of ubiquitin conjugation and aggresome formation by An, Heeseon, Statsyuk, Alexander V

“…Proteasome inhibitors have revolutionized the treatment of multiple myeloma, and validated the therapeutic potential of the ubiquitin proteasome system (UPS)…”
Get full text

Dissecting the Specificity of Adenosyl Sulfamate Inhibitors Targeting the Ubiquitin-Activating Enzyme by Misra, Mohit, Kuhn, Maximilian, Löbel, Mark, An, Heeseon, Statsyuk, Alexander V., Sotriffer, Christoph, Schindelin, Hermann

“…Targeting the activating enzymes (E1) of ubiquitin (Ub) and ubiquitin-like modifiers (Ubls) has emerged as a promising anti-cancer strategy, possibly…”
Get full text

Catalytically Important Residues of E6AP Ubiquitin Ligase Identified Using Acid-Cleavable Photo-Cross-Linkers by Krist, David T, Statsyuk, Alexander V

“…Inactivation of the E6AP E3 ubiquitin ligase (UBE3A gene) causes Angelman syndrome, while aberrant degradation of p53 by E6AP is implicated in cervical…”
Get full text

Inhibiting protein synthesis to treat malaria by Statsyuk, Alexander V

“…Covalent prodrugs inhibit protein synthesis targets killing parasites but not human cells…”
Get full text

A Fragment-Based Method to Discover Irreversible Covalent Inhibitors of Cysteine Proteases by Kathman, Stefan G, Xu, Ziyang, Statsyuk, Alexander V

“…A novel fragment-based drug discovery approach is reported which irreversibly tethers drug-like fragments to catalytic cysteines. We attached an electrophile…”
Get full text

Let K-Ras activate its own inhibitor by Statsyuk, Alexander V.

“…Traditional approaches to covalent drug design postulate that noncovalent binding affinity ( K i ) should be in the nanomolar range for the lead compound to be…”
Get full text

Facile synthesis of covalent probes to capture enzymatic intermediates during E1 enzyme catalysis by An, Heeseon, Statsyuk, Alexander V

“…We report a facile synthetic strategy to prepare UBL-AMP electrophilic probes that form a covalent bond with the catalytic cysteine of cognate E1s, mimicking…”
Get more information

A Small Molecule That Switches a Ubiquitin Ligase From a Processive to a Distributive Enzymatic Mechanism by Kathman, Stefan G, Span, Ingrid, Smith, Aaron T, Xu, Ziyang, Zhan, Jennifer, Rosenzweig, Amy C, Statsyuk, Alexander V

“…E3 ligases are genetically implicated in many human diseases, yet E3 enzyme mechanisms are not fully understood, and there is a strong need for pharmacological…”
Get full text

UbMES and UbFluor: Novel probes for ring-between-ring (RBR) E3 ubiquitin ligase PARKIN by Park, Sungjin, Foote, Peter K., Krist, David T., Rice, Sarah E., Statsyuk, Alexander V.

“…Ring-between-ring (RBR) E3 ligases have been implicated in autoimmune disorders and neurodegenerative diseases. The functions of many RBR E3s are poorly…”
Get full text

Mapping low-affinity/high-specificity peptide–protein interactions using ligand-footprinting mass spectrometry by Parker, Benjamin W., Goncz, Edward J., Krist, David T., Statsyuk, Alexander V., Nesvizhskii, Alexey I., Weiss, Eric L.

“…Short linear peptide motifs that are intracellular ligands of folded proteins are a modular, incompletely understood molecular interaction language in…”
Get full text

Covalent-Fragment Screening of BRD4 Identifies a Ligandable Site Orthogonal to the Acetyl-Lysine Binding Sites by Olp, Michael D, Sprague, Daniel J, Goetz, Christopher J, Kathman, Stefan G, Wynia-Smith, Sarah L, Shishodia, Shifali, Summers, Steven B, Xu, Ziyang, Statsyuk, Alexander V, Smith, Brian C

“…BRD4, a member of the bromodomain and extraterminal domain (BET) family, has emerged as a promising epigenetic target in cancer and inflammatory disorders. All…”
Get full text

Protein ubiquitination and formation of polyubiquitin chains without ATP, E1 and E2 enzymes by Park, Sungjin, Krist, David T, Statsyuk, Alexander V

“…Studying protein ubiquitination is difficult due to the complexity of the E1-E2-E3 ubiquitination cascade. Here we report the discovery that C-terminal…”
Get full text

Discovery of covalent enzyme inhibitors using virtual docking of covalent fragments by Chowdhury, Sandipan Roy, Kennedy, Steven, Zhu, Kai, Mishra, Rama, Chuong, Patrick, Nguyen, Alyssa-uyen, Kathman, Stefan G., Statsyuk, Alexander V.

“…[Display omitted] •Virtual docking of 1648 covalent fragments is performed.•Covalent inhibitor of Cathepsin L is identified.•Cathepsin L inhibitor did not…”
Get full text

Structural Basis of Substrate Recognition and Covalent Inhibition of Cdu1 from Chlamydia trachomatis by Ramirez, Yesid A., Adler, Thomas B., Altmann, Eva, Klemm, Theresa, Tiesmeyer, Christian, Sauer, Florian, Kathman, Stefan G., Statsyuk, Alexander V., Sotriffer, Christoph, Kisker, Caroline

“…Based on the similarity between the active sites of the deubiquitylating and deneddylating enzyme ChlaDub1 (Cdu1) and the evolutionarily related protease…”
Get full text

UbFluor: A Mechanism-Based Probe for HECT E3 Ligases by Krist, David T, Park, Sungjin, Boneh, Galyah H, Rice, Sarah E, Statsyuk, Alexander V

“…Homologous to E6AP Carboxyl Terminus E3 ubiquitin ligases (HECT, ~28 known) are genetically implicated in cancer, neurological, hypertensive, and autoimmune…”
Get full text

The development of a one pot, regiocontrolled, three-component reaction for the synthesis of thieno[2,3-c]pyrroles by Hong, Cynthia M, Statsyuk, Alexander V

“…A three-component reaction has been developed that allows the regioselective synthesis of thieno[2,3-c]pyrroles. The reaction is based on the ability of…”
Get more information

Crosstalk between kinases and Nedd4 family ubiquitin ligases by An, Heeseon, Krist, David T, Statsyuk, Alexander V

“…A dazzling array of human biological processes achieves coordination and balance through the posttranslational modification of protein residues with phosphate…”
Get more information

High-Throughput Screening of HECT E3 Ubiquitin Ligases Using UbFluor by Foote, Peter K, Krist, David T, Statsyuk, Alexander V

“…HECT E3 ubiquitin ligases are responsible for many human disease phenotypes and are promising drug targets; however, screening assays for HECT E3 inhibitors…”
Get more information

An inhibitor of ubiquitin conjugation and aggresome formationElectronic supplementary information (ESI) available. See DOI: 10.1039/c5sc01351h by An, Heeseon, Statsyuk, Alexander V

“…Proteasome inhibitors have revolutionized the treatment of multiple myeloma, and validated the therapeutic potential of the ubiquitin proteasome system (UPS)…”
Get full text