Search Results - "Foley, Timothy L."

Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase by Butler, Christopher R., Beck, Elizabeth M., Harris, Anthony, Huang, Zhen, McAllister, Laura A., am Ende, Christopher W., Fennell, Kimberly, Foley, Timothy L., Fonseca, Kari, Hawrylik, Steven J., Johnson, Douglas S., Knafels, John D., Mente, Scot, Noell, G. Stephen, Pandit, Jayvardhan, Phillips, Tracy B., Piro, Justin R., Rogers, Bruce N., Samad, Tarek A., Wang, Jane, Wan, Shuangyi, Brodney, Michael A.

“…Monoacylglycerol lipase (MAGL) is the main enzyme responsible for degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG) in the CNS. MAGL catalyzes…”
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Toward the assembly and characterization of an encoded library hit confirmation platform: Bead-Assisted Ligand Isolation Mass Spectrometry (BALI-MS) by Ratnayake, Anokha S., Flanagan, Mark E., Foley, Timothy L., Hultgren, Scott L., Bellenger, Justin, Montgomery, Justin I., Lall, Manjinder S., Liu, Bo, Ryder, Tim, Kölmel, Dominik K., Shavnya, Andre, Feng, Xidong, Lefker, Bruce, Byrnes, Laura J., Sahasrabudhe, Parag V., Farley, Kathleen A., Chen, Shi, Wan, Jinqiao

“…[Display omitted] The ability to predict chemical structure from DNA sequence has to date been a necessary cornerstone of DNA-encoded library technology…”
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Selecting Approaches for Hit Identification and Increasing Options by Building the Efficient Discovery of Actionable Chemical Matter from DNA-Encoded Libraries by Foley, Timothy L, Burchett, Woodrow, Chen, Qiuxia, Flanagan, Mark E, Kapinos, Brendon, Li, Xianyang, Montgomery, Justin I, Ratnayake, Anokha S, Zhu, Hongyao, Peakman, Marie-Claire

“…Over the past 20 years, the toolbox for discovering small-molecule therapeutic starting points has expanded considerably. Pharmaceutical researchers can now…”
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Fluorescent techniques for discovery and characterization of phosphopantetheinyl transferase inhibitors by Kosa, Nicolas M, Foley, Timothy L, Burkart, Michael D

“…Phosphopantetheinyl transferase (PPTase; E.C. 2.7.8.-) activates biosynthetic pathways that synthesize both primary and secondary metabolites in bacteria…”
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Phosphopantetheinyl transferase inhibition and secondary metabolism by Foley, Timothy L, Young, Brian S, Burkart, Michael D

“…Efforts to isolate carrier protein-mediated synthases from natural product-producing organisms using reporter-linked post-translational modification have been…”
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An Orthogonal Active Site Identification System (OASIS) for Proteomic Profiling of Natural Product Biosynthesis by Meier, Jordan L, Niessen, Sherry, Hoover, Heather S, Foley, Timothy L, Cravatt, Benjamin F, Burkart, Michael D

“…A significant gap exists between genetics-based investigations of polyketide synthase (PKS) and nonribosomal peptide synthetase (NRPS) biosynthetic pathways…”
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An Optimized Immunoaffinity Fluorescent Method for Natural Product Target Elucidation by Yu, Wei-luen, Guizzunti, Gianni, Foley, Timothy L, Burkart, Michael D, La Clair, James J

“…Understanding the mode of action of small molecules is an integral facet of drug discovery. We report an optimized immunoaffinity fluorescent method that…”
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Preparation of FRET reporters to support chemical probe development by Foley, Timothy L, Yasgar, Adam, Garcia, Christopher J, Jadhav, Ajit, Simeonov, Anton, Burkart, Michael D

“…In high throughput screening (HTS) campaigns, the quality and cost of commercial reagents suitable for pilot studies often create obstacles upon scale-up to a…”
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A strategy to discover inhibitors of Bacillus subtilis surfactin-type phosphopantetheinyl transferase by Yasgar, Adam, Foley, Timothy L, Jadhav, Ajit, Inglese, James, Burkart, Michael D, Simeonov, Anton

“…Surfactin-type phosphopantetheinyl transferases (Sfp-PPTases) are responsible for modifying type I polyketide and non-ribosomal peptide synthases of…”
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Understanding Data Noise and Uncertainty through Analysis of Replicate Samples in DNA-Encoded Library Selection by Zhu, Hongyao, Foley, Timothy L, Montgomery, Justin I, Stanton, Robert V

“…By analyzing data sets of replicate DNA-Encoded Library (DEL) selections, an approach for estimating the noise level of the experiment has been developed…”
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A method for estimating binding affinity from primary DEL selection data by Chen, Qiuxia, Hall, Justin, Foley, Timothy L., Wan, Jinqiao, Li, You, Israel, David I.

“…DEL selections are binding assays conducted with mixtures of chemically diverse DNA-tagged ligands and a screening target. DEL selections use DNA sequence…”
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Targeting iron assimilation to develop new antibacterials by Foley, Timothy L, Simeonov, Anton

“…Since the first application of antibiotics to treat bacterial infections, the development and spread of resistance has been a persistent threat. An ever…”
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A simple method for determining compound affinity and chemical yield from DNA-encoded library selections by Hall, Justin, Foley, Timothy L., Chen, Qiuxia, Israel, David I., Xu, Yanshan, Ford, Kristin K., Xie, Ping, Fan, Jing, Wan, Jinqiao

“…DNA-encoded libraries (DELs) can contain billions of unique chemical species; selecting against such large inputs, it is typical to find more candidate binders…”
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A Solution Phase Platform to Characterize Chemical Reaction Compatibility with DNA-Encoded Chemical Library Synthesis by Ratnayake, Anokha S, Flanagan, Mark E, Foley, Timothy L, Smith, Justin D, Johnson, Jillian G, Bellenger, Justin, Montgomery, Justin I, Paegel, Brian M

“…DNA-encoded chemical library (DECL) synthesis must occur in aqueous media under conditions that preserve the integrity of the DNA encoding tag. While the…”
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Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation by McAllister, Laura A, Butler, Christopher R, Mente, Scot, O’Neil, Steven V, Fonseca, Kari R, Piro, Justin R, Cianfrogna, Julie A, Foley, Timothy L, Gilbert, Adam M, Harris, Anthony R, Helal, Christopher J, Johnson, Douglas S, Montgomery, Justin I, Nason, Deane M, Noell, Stephen, Pandit, Jayvardhan, Rogers, Bruce N, Samad, Tarek A, Shaffer, Christopher L, da Silva, Rafael G, Uccello, Daniel P, Webb, Damien, Brodney, Michael A

“…Monoacylglycerol lipase (MAGL) inhibition provides a potential treatment approach to neuroinflammation through modulation of both the endocannabinoid pathway…”
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Fluorophosphonates on‐Demand: A General and Simplified Approach toward Fluorophosphonate Synthesis by Dutra, Jason K., Foley, Timothy L., Huang, Zhen, Fisher, Ethan L., Lachapelle, Erik A., Mahapatra, Subham, Ogilvie, Kevin, Butler, Todd W., Bellenger, Justin, Devraj Majmudar, Jaimeen, am Ende, Christopher W.

“…Herein, we report a general and simplified synthesis of fluorophosphonates directly from p‐nitrophenylphosphonates. This FP on‐demand reaction is mediated by a…”
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Structural basis of the acyl-transfer mechanism of human GPAT1 by Johnson, Zachary Lee, Ammirati, Mark, Wasilko, David Jonathan, Chang, Jeanne S., Noell, Stephen, Foley, Timothy L., Yoon, Hyejin, Smith, Kathleen, Asano, Shoh, Hales, Katherine, Wan, Min, Yang, Qingyi, Piotrowski, Mary A., Farley, Kathleen A., Gilbert, Tamara, Aschenbrenner, Lisa M., Fennell, Kimberly F., Dutra, Jason K., Xu, Mary, Guo, Chunyang, Varghese, Alison E., Bellenger, Justin, Quinn, Alandra, am Ende, Christopher W., West, Graham M., Griffor, Matthew C., Bennett, Donald, Calabrese, Matthew, Steppan, Claire M., Han, Seungil, Wu, Huixian

“…Glycerol-3-phosphate acyltransferase (GPAT)1 is a mitochondrial outer membrane protein that catalyzes the first step of de novo glycerolipid biosynthesis…”
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Site-specific protein modification: advances and applications by Foley, Timothy L, Burkart, Michael D

“…Although chemical methods to modify proteins in a sequence-specific manner have yet to be developed, site-specific post-translational modification of proteins…”
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Covalent Small Molecule Inhibitors of Ca2+-Bound S100B by Cavalier, Michael C, Pierce, Adam D, Wilder, Paul T, Alasady, Milad J, Hartman, Kira G, Neau, David B, Foley, Timothy L, Jadhav, Ajit, Maloney, David J, Simeonov, Anton, Toth, Eric A, Weber, David J

“…Elevated levels of the tumor marker S100B are observed in malignant melanoma, and this EF-hand-containing protein was shown to directly bind wild-type (wt) p53…”
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4‑(3-Chloro-5-(trifluoromethyl)pyridin-2-yl)‑N‑(4-methoxypyridin-2-yl)piperazine-1-carbothioamide (ML267), a Potent Inhibitor of Bacterial Phosphopantetheinyl Transferase That Attenuates Secondary Metabolism and Thwarts Bacterial Growth by Foley, Timothy L, Rai, Ganesha, Yasgar, Adam, Daniel, Thomas, Baker, Heather L, Attene-Ramos, Matias, Kosa, Nicolas M, Leister, William, Burkart, Michael D, Jadhav, Ajit, Simeonov, Anton, Maloney, David J

“…4′-Phosphopantetheinyl transferases (PPTases) catalyze a post-translational modification essential to bacterial cell viability and virulence. We present the…”
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