Search Results - "Belyanskaya, Svetlana"

Discovering Drugs with DNA‐Encoded Library Technology: From Concept to Clinic with an Inhibitor of Soluble Epoxide Hydrolase by Belyanskaya, Svetlana L., Ding, Yun, Callahan, James F., Lazaar, Aili L., Israel, David I.

“…DNA‐encoded chemical library technology was developed with the vision of its becoming a transformational platform for drug discovery. The hope was that a new…”
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Discovery of Thieno[3,2‑d]pyrimidine-6-carboxamides as Potent Inhibitors of SIRT1, SIRT2, and SIRT3 by Disch, Jeremy S, Evindar, Ghotas, Chiu, Cynthia H, Blum, Charles A, Dai, Han, Jin, Lei, Schuman, Eli, Lind, Kenneth E, Belyanskaya, Svetlana L, Deng, Jianghe, Coppo, Frank, Aquilani, Leah, Graybill, Todd L, Cuozzo, John W, Lavu, Siva, Mao, Cheney, Vlasuk, George P, Perni, Robert B

“…The sirtuins SIRT1, SIRT2, and SIRT3 are NAD+ dependent deacetylases that are considered potential targets for metabolic, inflammatory, oncologic, and…”
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Design, synthesis and selection of DNA-encoded small-molecule libraries by Morgan, Barry A, Clark, Matthew A, Acharya, Raksha A, Arico-Muendel, Christopher C, Belyanskaya, Svetlana L, Benjamin, Dennis R, Carlson, Neil R, Centrella, Paolo A, Chiu, Cynthia H, Creaser, Steffen P, Cuozzo, John W, Davie, Christopher P, Ding, Yun, Franklin, G Joseph, Franzen, Kurt D, Gefter, Malcolm L, Hale, Steven P, Hansen, Nils J V, Israel, David I, Jiang, Jinwei, Kavarana, Malcolm J, Kelley, Michael S, Kollmann, Christopher S, Li, Fan, Lind, Kenneth, Mataruse, Sibongile, Medeiros, Patricia F, Messer, Jeffrey A, Myers, Paul, O'Keefe, Heather, Oliff, Matthew C, Rise, Cecil E, Satz, Alexander L, Skinner, Steven R, Svendsen, Jennifer L, Tang, Lujia, van Vloten, Kurt, Wagner, Richard W, Yao, Gang, Zhao, Baoguang

“…Biochemical combinatorial techniques such as phage display, RNA display and oligonucleotide aptamers have proven to be reliable methods for generation of…”
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Discovery of Highly Potent and Selective Small Molecule ADAMTS‑5 Inhibitors That Inhibit Human Cartilage Degradation via Encoded Library Technology (ELT) by Deng, Hongfeng, O’Keefe, Heather, Davie, Christopher P, Lind, Kenneth E, Acharya, Raksha A, Franklin, G. Joseph, Larkin, Jonathan, Matico, Rosalie, Neeb, Michael, Thompson, Monique M, Lohr, Thomas, Gross, Jeffrey W, Centrella, Paolo A, O’Donovan, Gary K, Bedard, Katie L. (Sargent), van Vloten, Kurt, Mataruse, Sibongile, Skinner, Steven R, Belyanskaya, Svetlana L, Carpenter, Tiffany Y, Shearer, Todd W, Clark, Matthew A, Cuozzo, John W, Arico-Muendel, Christopher C, Morgan, Barry A

“…The metalloprotease ADAMTS-5 is considered a potential target for the treatment of osteoarthritis. To identify selective inhibitors of ADAMTS-5, we employed…”
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Predicting Electrophoretic Mobility of Protein–Ligand Complexes for Ligands from DNA-Encoded Libraries of Small Molecules by Bao, Jiayin, Krylova, Svetlana M, Cherney, Leonid T, Hale, Robert L, Belyanskaya, Svetlana L, Chiu, Cynthia H, Shaginian, Alex, Arico-Muendel, Christopher C, Krylov, Sergey N

“…Selection of target-binding ligands from DNA-encoded libraries of small molecules (DELSMs) is a rapidly developing approach in drug-lead discovery. Methods of…”
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Development of a small molecule that corrects misfolding and increases secretion of Z α1‐antitrypsin by Lomas, David A, Irving, James A, Arico‐Muendel, Christopher, Belyanskaya, Svetlana, Brewster, Andrew, Brown, Murray, Chung, Chun‐wa, Dave, Hitesh, Denis, Alexis, Dodic, Nerina, Dossang, Anthony, Eddershaw, Peter, Klimaszewska, Diana, Haq, Imran, Holmes, Duncan S, Hutchinson, Jonathan P, Jagger, Alistair M, Jakhria, Toral, Jigorel, Emilie, Liddle, John, Lind, Ken, Marciniak, Stefan J, Messer, Jeff, Neu, Margaret, Olszewski, Allison, Ordonez, Adriana, Ronzoni, Riccardo, Rowedder, James, Rüdiger, Martin, Skinner, Steve, Smith, Kathrine J, Terry, Rebecca, Trottet, Lionel, Uings, Iain, Wilson, Steve, Zhu, Zhengrong, Pearce, Andrew C

“…Severe α 1 ‐antitrypsin deficiency results from the Z allele (Glu342Lys) that causes the accumulation of homopolymers of mutant α 1 ‐antitrypsin within the…”
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In vitro and in vivo characterization of a novel soluble epoxide hydrolase inhibitor by Podolin, Patricia L., Bolognese, Brian J., Foley, Joseph F., Long, Edward, Peck, Brian, Umbrecht, Sandra, Zhang, Xiaojun, Zhu, Penny, Schwartz, Benjamin, Xie, Wensheng, Quinn, Chad, Qi, Hongwei, Sweitzer, Sharon, Chen, Stephanie, Galop, Marc, Ding, Yun, Belyanskaya, Svetlana L., Israel, David I., Morgan, Barry A., Behm, David J., Marino, Joseph P., Kurali, Edit, Barnette, Mary S., Mayer, Ruth J., Booth-Genthe, Catherine L., Callahan, James F.

“…► A novel, potent, selective inhibitor of human, rat and mouse sEH, GSK2256294A, is described. ► In vitro, GSK2256294A exhibits concentration-dependent…”
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Discovery, SAR, and X‑ray Binding Mode Study of BCATm Inhibitors from a Novel DNA-Encoded Library by Deng, Hongfeng, Zhou, Jingye, Sundersingh, Flora S, Summerfield, Jennifer, Somers, Don, Messer, Jeffrey A, Satz, Alexander L, Ancellin, Nicolas, Arico-Muendel, Christopher C, (Sargent) Bedard, Katie L, Beljean, Arthur, Belyanskaya, Svetlana L, Bingham, Ryan, Smith, Sarah E, Boursier, Eric, Carter, Paul, Centrella, Paolo A, Clark, Matthew A, Chung, Chun-wa, Davie, Christopher P, Delorey, Jennifer L, Ding, Yun, Franklin, G. Joseph, Grady, LaShadric C, Herry, Kenny, Hobbs, Clare, Kollmann, Christopher S, Morgan, Barry A, (Pothier) Kaushansky, Laura J, Zhou, Quan

“…As a potential target for obesity, human BCATm was screened against more than 14 billion DNA encoded compounds of distinct scaffolds followed by off-DNA…”
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Prediction of Protein–DNA Complex Mobility in Gel-Free Capillary Electrophoresis by Bao, Jiayin, Krylova, Svetlana M, Cherney, Leonid T, Hale, Robert L, Belyanskaya, Svetlana L, Chiu, Cynthia H, Arico-Muendel, Christopher C, Krylov, Sergey N

“…Selection of protein binders from highly diverse combinatorial libraries of DNA-encoded small molecules is a highly promising approach for discovery of…”
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Profiling cells with DELs: Small molecule fingerprinting of cell surfaces by Deng, Jason, Belyanskaya, Svetlana, Prabhu, Ninad, Arico-Muendel, Christopher, Deng, Hongfeng, Phelps, Christopher B., Israel, David I., Yang, Hongfang, Boyer, Joseph, Franklin, G. Joseph, Yap, Jeremy L., Lind, Kenneth E., Tsai, Ching-Hsuan, Donahue, Christine, Summerfield, Jennifer D.

“…•We demonstrate distinct binding profiles for small molecule ligands from DNA encoded libraries (DELs) affinity selected to various mouse and human cell…”
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Discovery of 1-(1,3,5-triazin-2-yl)piperidine-4-carboxamides as inhibitors of soluble epoxide hydrolase by Thalji, Reema K., McAtee, Jeff J., Belyanskaya, Svetlana, Brandt, Martin, Brown, Gregory D., Costell, Melissa H., Ding, Yun, Dodson, Jason W., Eisennagel, Steve H., Fries, Rusty E., Gross, Jeffrey W., Harpel, Mark R., Holt, Dennis A., Israel, David I., Jolivette, Larry J., Krosky, Daniel, Li, Hu, Lu, Quinn, Mandichak, Tracy, Roethke, Theresa, Schnackenberg, Christine G., Schwartz, Benjamin, Shewchuk, Lisa M., Xie, Wensheng, Behm, David J., Douglas, Stephen A., Shaw, Ami L., Marino, Joseph P.

“…1-(1,3,5-Triazin-yl)piperidine-4-carboxamide inhibitors of soluble epoxide hydrolase were identified from high through-put screening using encoded library…”
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Discovery and Optimization of Potent, Selective, and in Vivo Efficacious 2‑Aryl Benzimidazole BCATm Inhibitors by Deng, Hongfeng, Zhou, Jingye, Sundersingh, Flora, Messer, Jeffrey A, Somers, Donald O, Ajakane, Myriam, Arico-Muendel, Christopher C, Beljean, Arthur, Belyanskaya, Svetlana L, Bingham, Ryan, Blazensky, Emily, Boullay, Anne-Benedicte, Boursier, Eric, Chai, Jing, Carter, Paul, Chung, Chun-Wa, Daugan, Alain, Ding, Yun, Herry, Kenny, Hobbs, Clare, Humphries, Eric, Kollmann, Christopher, Nguyen, Van Loc, Nicodeme, Edwige, Smith, Sarah E, Dodic, Nerina, Ancellin, Nicolas

“…To identify BCATm inhibitors suitable for in vivo study, Encoded Library Technology (ELT) was used to affinity screen a 117 million member benzimidazole based…”
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Granulocyte-Macrophage Colony-Stimulating Factor Induces an Expression Program in Neonatal Microglia That Primes Them for Antigen Presentation by Re, Fabio, Belyanskaya, Svetlana L, Riese, Richiard J, Cipriani, Barbara, Fischer, Falko R, Granucci, Francesca, Ricciardi-Castagnoli, Paola, Brosnan, Celia, Stern, Lawrence J, Strominger, Jack L, Santambrogio, Laura

“…Neonatal microglial cells respond to GM-CSF and M-CSF by acquiring different morphologies and phenotypes. To investigate the extent and consequences of this…”
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Extracellular Antigen Processing and Presentation by Immature Dendritic Cells by Santambrogio, Laura, Sato, Aaron K., Carven, Gregory J., Belyanskaya, Svetlana L., Strominger, Jack L., Stern, Lawrence J.

“…In antigen presentation to CD4+T cells, proteins are degraded to peptide fragments and loaded onto class II MHC molecules in a process involving the peptide…”
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Building Block-Based Binding Predictions for DNA-Encoded Libraries by Zhang, Chris, Pitman, Mary, Dixit, Anjali, Leelananda, Sumudu, Palacci, Henri, Lawler, Meghan, Belyanskaya, Svetlana, Grady, LaShadric, Franklin, Joe, Tilmans, Nicolas, Mobley, David L.

“…DNA-encoded libraries (DELs) provide the means to make and screen millions of diverse compounds against a target of interest in a single experiment. However,…”
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Design and Synthesis of Biaryl DNA-Encoded Libraries by Ding, Yun, Franklin, G. Joseph, DeLorey, Jennifer L, Centrella, Paolo A, Mataruse, Sibongile, Clark, Matthew A, Skinner, Steven R, Belyanskaya, Svetlana

“…DNA-encoded library technology (ELT) is a powerful tool for the discovery of new small-molecule ligands to various protein targets. Here we report the design…”
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How to Develop and Prove High-Efficiency Selection of Ligands from Oligonucleotide Libraries: A Universal Framework for Aptamers and DNA-Encoded Small-Molecule Ligands by Le, An T. H, Krylova, Svetlana M, Beloborodov, Stanislav S, Wang, Tong Y, Hili, Ryan, Johnson, Philip E, Li, Feng, Veedu, Rakesh N, Belyanskaya, Svetlana, Krylov, Sergey N

“…Screening molecular libraries for ligands capable of binding proteins is widely used for hit identification in the early drug discovery process…”
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Discovery of soluble epoxide hydrolase inhibitors through DNA-encoded library technology (ELT) by Ding, Yun, Belyanskaya, Svetlana, DeLorey, Jennifer L., Messer, Jeffrey A., Joseph Franklin, G., Centrella, Paolo A., Morgan, Barry A., Clark, Matthew A., Skinner, Steven R., Dodson, Jason W., Li, Peng, Marino, Joseph P., Israel, David I.

“…[Display omitted] Inhibition of soluble epoxide hydrolase (sEH) has recently emerged as a new approach to treat cardiovascular disease and respiratory disease…”
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The development of highly potent and selective small molecule correctors of Z α1-antitrypsin misfolding by Liddle, John, Pearce, Andrew C., Arico-Muendel, Christopher, Belyanskaya, Svetlana, Brewster, Andrew, Brown, Murray, Chung, Chun-wa, Denis, Alexis, Dodic, Nerina, Dossang, Anthony, Eddershaw, Peter, Klimaszewska, Diana, Haq, Imran, Holmes, Duncan S., Jagger, Alistair, Jakhria, Toral, Jigorel, Emilie, Lind, Ken, Messer, Jeff, Neu, Margaret, Olszewski, Allison, Ronzoni, Riccardo, Rowedder, James, Rüdiger, Martin, Skinner, Steve, Smith, Kathrine J., Trottet, Lionel, Uings, Iain, Zhu, Zhengrong, Irving, James A., Lomas, David A.

“…[Display omitted] α1-antitrypsin deficiency is characterised by the misfolding and intracellular polymerisation of mutant α1-antitrypsin protein within the…”
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The development of highly potent and selective small molecule correctors of Z α 1 -antitrypsin misfolding by Liddle, John, Pearce, Andrew C, Arico-Muendel, Christopher, Belyanskaya, Svetlana, Brewster, Andrew, Brown, Murray, Chung, Chun-Wa, Denis, Alexis, Dodic, Nerina, Dossang, Anthony, Eddershaw, Peter, Klimaszewska, Diana, Haq, Imran, Holmes, Duncan S, Jagger, Alistair, Jakhria, Toral, Jigorel, Emilie, Lind, Ken, Messer, Jeff, Neu, Margaret, Olszewski, Allison, Ronzoni, Riccardo, Rowedder, James, Rüdiger, Martin, Skinner, Steve, Smith, Kathrine J, Trottet, Lionel, Uings, Iain, Zhu, Zhengrong, Irving, James A, Lomas, David A

“…α1-antitrypsin deficiency is characterised by the misfolding and intracellular polymerisation of mutant α1-antitrypsin protein within the endoplasmic reticulum…”
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