Search Results - "Stauffer, Shaun R"

Structure-Based Optimization of ML300-Derived, Noncovalent Inhibitors Targeting the Severe Acute Respiratory Syndrome Coronavirus 3CL Protease (SARS-CoV‑2 3CLpro) by Han, Sang Hoon, Goins, Christopher M, Arya, Tarun, Shin, Woo-Jin, Maw, Joshua, Hooper, Alice, Sonawane, Dhiraj P, Porter, Matthew R, Bannister, Breyanne E, Crouch, Rachel D, Lindsey, A. Abigail, Lakatos, Gabriella, Martinez, Steven R, Alvarado, Joseph, Akers, Wendell S, Wang, Nancy S, Jung, Jae U, Macdonald, Jonathan D, Stauffer, Shaun R

“…Starting from the MLPCN probe compound ML300, a structure-based optimization campaign was initiated against the recent severe acute respiratory syndrome…”
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A TOX-ic axis of epigenetic stem cell maintenance and chemoresistance in colon cancer by Hubert, Christopher G, Stauffer, Shaun R, Lathia, Justin D

“…Cancer stem cells drive tumor growth and survival via self-renewal and therapeutic resistance, but the upstream mechanisms are not well defined. In this issue…”
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Discovery, Synthesis, And Structure-Based Optimization of a Series of N‑(tert-Butyl)-2‑(N‑arylamido)-2-(pyridin-3-yl) Acetamides (ML188) as Potent Noncovalent Small Molecule Inhibitors of the Severe Acute Respiratory Syndrome Coronavirus (SARS-CoV) 3CL Protease by Jacobs, Jon, Grum-Tokars, Valerie, Zhou, Ya, Turlington, Mark, Saldanha, S. Adrian, Chase, Peter, Eggler, Aimee, Dawson, Eric S, Baez-Santos, Yahira M, Tomar, Sakshi, Mielech, Anna M, Baker, Susan C, Lindsley, Craig W, Hodder, Peter, Mesecar, Andrew, Stauffer, Shaun R

“…A high-throughput screen of the NIH molecular libraries sample collection and subsequent optimization of a lead dipeptide-like series of severe acute…”
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Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity by Aho, Erin R., Wang, Jing, Gogliotti, Rocco D., Howard, Gregory C., Phan, Jason, Acharya, Pankaj, Macdonald, Jonathan D., Cheng, Ken, Lorey, Shelly L., Lu, Bin, Wenzel, Sabine, Foshage, Audra M., Alvarado, Joseph, Wang, Feng, Shaw, J. Grace, Zhao, Bin, Weissmiller, April M., Thomas, Lance R., Vakoc, Christopher R., Hall, Matthew D., Hiebert, Scott W., Liu, Qi, Stauffer, Shaun R., Fesik, Stephen W., Tansey, William P.

“…The chromatin-associated protein WDR5 is a promising target for pharmacological inhibition in cancer. Drug discovery efforts center on the blockade of the “WIN…”
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Chemical inhibition of fatty acid absorption and cellular uptake limits lipotoxic cell death by Ahowesso, Constance, Black, Paul N., Saini, Nipun, Montefusco, David, Chekal, Jessica, Malosh, Chrysa, Lindsley, Craig W., Stauffer, Shaun R., DiRusso, Concetta C.

“…[Display omitted] Chronic elevation of plasma free fatty acid (FFA) levels is commonly associated with obesity, type 2 diabetes, cardiovascular disease and…”
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Copper-Facilitated Suzuki Reactions: Application to 2-Heterocyclic Boronates by Deng, James Z, Paone, Daniel V, Ginnetti, Anthony T, Kurihara, Hideki, Dreher, Spencer D, Weissman, Steven A, Stauffer, Shaun R, Burgey, Christopher S

“…The palladium-catalyzed Suzuki−Miyaura reaction has been utilized as one of the most powerful methods for C−C bond formation. However, Suzuki reactions of…”
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A PAM of the α1A-Adrenergic receptor rescues biomarker, long-term potentiation, and cognitive deficits in Alzheimer’s disease mouse models without effects on blood pressure by Papay, Robert S., Stauffer, Shaun R., Perez, Dianne M.

“…α1-Adrenergic Receptors (ARs) regulate the sympathetic nervous system by the binding of norepinephrine (NE) and epinephrine (Epi) through different subtypes…”
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Characterization of a novel positive allosteric modulator of the α1A-Adrenergic receptor by Papay, Robert S., Macdonald, Jonathan D., Stauffer, Shaun R., Perez, Dianne M.

“…α1-Adrenergic Receptors (ARs) are G-protein Coupled Receptors (GPCRs) that regulate the sympathetic nervous system via the binding and activation of…”
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Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354 by Wen, Wandong, Young, Summer E., Duvernay, Matthew T., Schulte, Michael L., Nance, Kellie D., Melancon, Bruce J., Engers, Julie, Locuson, Charles W., Wood, Michael R., Daniels, J. Scott, Wu, Wenjun, Lindsley, Craig W., Hamm, Heidi E., Stauffer, Shaun R.

“…Herein we report the discovery and SAR of an indole-based protease activated receptor-4 (PAR-4) antagonist scaffold derived from a similarity search of the…”
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Fluorescence Resonance Energy Transfer (FRET) as a High-Throughput Assay for Coupling Reactions. Arylation of Amines as a Case Study by Stauffer, Shaun R, Hartwig, John F

“…A solution-phase assay based on fluorescence resonance energy transfer (FRET) was developed for high-throughput screening of palladium catalyzed aminations of…”
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High Turnover Number and Rapid, Room-Temperature Amination of Chloroarenes Using Saturated Carbene Ligands by Stauffer, Shaun R, Lee, Sunwoo, Stambuli, James P, Hauck, Sheila I, Hartwig, John F

“…A catalytic system for the mild amination of aryl chlorides is described. This system consists of a Pd(0) precursor and a dihydroimidazoline carbene ligand,…”
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361 WDR5 represents a therapeutically exploitable target for cancer stem cells in glioblastoma by Hubert, Christopher, Mitchell, Kelly, Sprowls, Samuel, Shakya, Sajina, Arora, Sonali, Silver, Daniel J., Goins, Christopher M., Wallace, Lisa, Roversi, Gustavo, Schafer, Rachel, Kay, Kristen, Miller, Tyler E., Lauko, Adam, Bassett, John, Kashyap, Anjali, Kass, J. D’Amato, Mulkearns-Hubert, Erin E., Johnson, Sadie, Alvarado, Joseph, Rich, Jeremy N., Paddison, Patrick J., Patel, Anoop P., Stauffer, Shaun R., Hubert, Christopher G., Lathia, Justin D.

“…OBJECTIVES/GOALS: Glioblastomas (GBMs) are heterogeneous, treatment-resistant tumors that are driven by populations of cancer stem cells (CSCs). In this study,…”
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Screening of Homogeneous Catalysts by Fluorescence Resonance Energy Transfer. Identification of Catalysts for Room-Temperature Heck Reactions by Stambuli, James P, Stauffer, Shaun R, Shaughnessy, Kevin H, Hartwig, John F

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Metabotropic glutamate receptor 5-positive allosteric modulators for the treatment of schizophrenia (2004-2012) by Lindsley, Craig W, Stauffer, Shaun R

“…The mGlu5, a class C G-protein-coupled receptor and member of the group I mGlu receptor family, has been demonstrated to play a role in a number of therapeutic…”
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ISGylation of the SARS-CoV-2 N protein by HERC5 impedes N oligomerization and thereby viral RNA synthesis by Zhu, Junji, Liu, GuanQun, Sayyad, Zuberwasim, Goins, Christopher M, Stauffer, Shaun R, Gack, Michaela U

“…Interferon (IFN)-stimulated gene 15 (ISG15), a ubiquitin-like protein, is covalently conjugated to host immune proteins such as MDA5 and IRF3 in a process…”
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CDK9 Inhibition by Dinaciclib Is a Therapeutic Vulnerability in Epithelioid Hemangioendothelioma by Pobbati, Ajaybabu V, Burtscher, Ashley, Rajaram Siva, Nandini, Hallett, Andrea, Romigh, Todd, Che, Kepeng, Zhao, Bin, Coker, Jesse A, Wang, Nancy, Stauffer, Shaun R, Rubin, Brian P

“…There are no effective treatment options for patients with aggressive epithelioid hemangioendothelioma (EHE) driven by the TAZ-CAMTA1 (TC) fusion gene. Here,…”
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Discovery of WD Repeat-Containing Protein 5 (WDR5)–MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design by Chacón Simon, Selena, Wang, Feng, Thomas, Lance R, Phan, Jason, Zhao, Bin, Olejniczak, Edward T, Macdonald, Jonathan D, Shaw, J. Grace, Schlund, Caden, Payne, William, Creighton, Joy, Stauffer, Shaun R, Waterson, Alex G, Tansey, William P, Fesik, Stephen W

“…The frequent deregulation of MYC and its elevated expression via multiple mechanisms drives cells to a tumorigenic state. Indeed, MYC is overexpressed in up to…”
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Palladium-Catalyzed Arylation of Ethyl Cyanoacetate. Fluorescence Resonance Energy Transfer as a Tool for Reaction Discovery by Stauffer, Shaun R, Beare, Neil A, Stambuli, James P, Hartwig, John F

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Progress toward Positive Allosteric Modulators of the Metabotropic Glutamate Receptor Subtype 5 (mGlu5) by Stauffer, Shaun R

“…This Review describes recent trends in the development of small molecule mGlu5 positive allosteric modulators (PAMs). A large body of pharmacological, genetic,…”
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Targeting zoonotic viruses: Structure-based inhibition of the 3C-like protease from bat coronavirus HKU4—The likely reservoir host to the human coronavirus that causes Middle East Respiratory Syndrome (MERS) by St. John, Sarah E., Tomar, Sakshi, Stauffer, Shaun R., Mesecar, Andrew D.

“…[Display omitted] The bat coronavirus HKU4 belongs to the same 2c lineage as that of the deadly Middle East Respiratory Syndrome coronavirus (MERS-CoV) and…”
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