Search Results - "Sklar, Larry"

Selective chemical inhibition of agr quorum sensing in Staphylococcus aureus promotes host defense with minimal impact on resistance by Sully, Erin K, Malachowa, Natalia, Elmore, Bradley O, Alexander, Susan M, Femling, Jon K, Gray, Brian M, DeLeo, Frank R, Otto, Michael, Cheung, Ambrose L, Edwards, Bruce S, Sklar, Larry A, Horswill, Alexander R, Hall, Pamela R, Gresham, Hattie D

“…Bacterial signaling systems are prime drug targets for combating the global health threat of antibiotic resistant bacterial infections including those caused…”
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Clioquinol: To harm or heal by Perez, Dominique R., Sklar, Larry A., Chigaev, Alexandre

“…Clioquinol, one of the first mass-produced drugs, was considered safe and efficacious for many years. It was used as an antifungal and an antiprotozoal drug…”
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Pharos: Collating protein information to shed light on the druggable genome by Nguyen, Dac-Trung, Mathias, Stephen, Bologa, Cristian, Brunak, Soren, Fernandez, Nicolas, Gaulton, Anna, Hersey, Anne, Holmes, Jayme, Jensen, Lars Juhl, Karlsson, Anneli, Liu, Guixia, Ma'ayan, Avi, Mandava, Geetha, Mani, Subramani, Mehta, Saurabh, Overington, John, Patel, Juhee, Rouillard, Andrew D, Schürer, Stephan, Sheils, Timothy, Simeonov, Anton, Sklar, Larry A, Southall, Noel, Ursu, Oleg, Vidovic, Dusica, Waller, Anna, Yang, Jeremy, Jadhav, Ajit, Oprea, Tudor I, Guha, Rajarshi

“…The 'druggable genome' encompasses several protein families, but only a subset of targets within them have attracted significant research attention and thus…”
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Estrogen signaling through the transmembrane G protein-coupled receptor GPR30 by Prossnitz, Eric R, Arterburn, Jeffrey B, Smith, Harriet O, Oprea, Tudor I, Sklar, Larry A, Hathaway, Helen J

“…Steroids play an important role in the regulation of normal physiology and the treatment of disease. Steroid receptors have classically been described as…”
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GPR30 Expression Is Required for the Mineralocorticoid Receptor–Independent Rapid Vascular Effects of Aldosterone by Gros, Robert, Ding, Qingming, Sklar, Larry A, Prossnitz, Eric E, Arterburn, Jeffrey B, Chorazyczewski, Jozef, Feldman, Ross D

“…It has been increasingly appreciated that steroids elicit acute vascular effects through rapid, so-called nongenomic signaling pathways. Though aldosterone,…”
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Unexplored therapeutic opportunities in the human genome by Oprea, Tudor I., Bologa, Cristian G., Brunak, Søren, Campbell, Allen, Gan, Gregory N., Gaulton, Anna, Gomez, Shawn M., Guha, Rajarshi, Hersey, Anne, Holmes, Jayme, Jadhav, Ajit, Jensen, Lars Juhl, Johnson, Gary L., Karlson, Anneli, Leach, Andrew R., Ma'ayan, Avi, Malovannaya, Anna, Mani, Subramani, Mathias, Stephen L., McManus, Michael T., Meehan, Terrence F., von Mering, Christian, Muthas, Daniel, Nguyen, Dac-Trung, Overington, John P., Papadatos, George, Qin, Jun, Reich, Christian, Roth, Bryan L., Schürer, Stephan C., Simeonov, Anton, Sklar, Larry A., Southall, Noel, Tomita, Susumu, Tudose, Ilinca, Ursu, Oleg, Vidović, Dušica, Waller, Anna, Westergaard, David, Yang, Jeremy J., Zahoránszky-Köhalmi, Gergely

“…In 2014, the Illuminating the Druggable Genome programme was launched to promote the exploration of currently understudied but potentially druggable proteins…”
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Best practices for managing and disseminating resources and outreach and evaluating the impact of the IDG Consortium by Vidović, Dušica, Waller, Anna, Holmes, Jayme, Sklar, Larry A., Schürer, Stephan C.

“…•The IDG consortium has generated numerous reagent and digital resources.•RDOC implemented infrastructure and processes for FAIR resource management.•IDG…”
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Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity by Dennis, Megan K., Field, Angela S., Burai, Ritwik, Ramesh, Chinnasamy, Petrie, Whitney K., Bologa, Cristian G., Oprea, Tudor I., Yamaguchi, Yuri, Hayashi, Shin-Ichi, Sklar, Larry A., Hathaway, Helen J., Arterburn, Jeffrey B., Prossnitz, Eric R.

“…► We identify a GPER antagonist G36 with increased selectivity against ERα/β. ► G36 exhibits reduced ER binding/activation compared to G15. ► G36 inhibits GPER…”
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Flow Cytometry: Impact on Early Drug Discovery by Edwards, Bruce S, Sklar, Larry A

“…Modern flow cytometers can make optical measurements of 10 or more parameters per cell at tens of thousands of cells per second and more than five orders of…”
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Drug repurposing for targeting cyclic nucleotide transporters in acute leukemias - A missed opportunity by Perez, Dominique R., Sklar, Larry A., Chigaev, Alexandre, Matlawska-Wasowska, Ksenia

“…While current treatment regimens for acute leukemia can dramatically improve patient survival, there remains room for improvement. Due to its roles in cell…”
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Transmembrane Intracellular Estrogen Receptor Mediates Rapid Cell Signaling by Revankar, Chetana M, Cimino, Daniel F, Sklar, Larry A, Arterburn, Jeffrey B, Prossnitz, Eric R

“…The steroid hormone estrogen regulates many functionally unrelated processes in numerous tissues. Although it is traditionally thought to control…”
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R-Ketorolac Targets Cdc42 and Rac1 and Alters Ovarian Cancer Cell Behaviors Critical for Invasion and Metastasis by Guo, Yuna, Kenney, S Ray, Muller, Carolyn Y, Adams, Sarah, Rutledge, Teresa, Romero, Elsa, Murray-Krezan, Cristina, Prekeris, Rytis, Sklar, Larry A, Hudson, Laurie G, Wandinger-Ness, Angela

“…Cdc42 (cell division control protein 42) and Rac1 (Ras-related C3 botulinum toxin substrate 1) are attractive therapeutic targets in ovarian cancer based on…”
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Distribution and characterization of estrogen receptor G protein-coupled receptor 30 in the rat central nervous system by Brailoiu, Eugen, Dun, Siok L, Brailoiu, G Cristina, Mizuo, Keisuke, Sklar, Larry A, Oprea, Tudor I, Prossnitz, Eric R, Dun, Nae J

“…The G protein-coupled receptor 30 (GPR 30) has been identified as the non-genomic estrogen receptor, and G-1, the specific ligand for GPR30. With the use of a…”
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GPR30: A G protein-coupled receptor for estrogen by Prossnitz, Eric R., Arterburn, Jeffrey B., Sklar, Larry A.

“…Estrogen is a critical steroid in human physiology exerting its effect both at the transcriptional level as well as at the level of rapid intracellular…”
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A Flow Cytometry-Based High-Throughput Technique for Screening Integrin-Inhibitory Drugs by Cao, Ziming, Garcia, Matthew J, Sklar, Larry A, Wandinger-Ness, Angela, Fan, Zhichao

“…This protocol aims to establish a method for identifying small molecular antagonists of β2 integrin activation, utilizing conformational-change-reporting…”
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Microbial efflux pump inhibition: tactics and strategies by Tegos, George P, Haynes, Mark, Strouse, J Jacob, Khan, Mohiuddin Md T, Bologa, Cristian G, Oprea, Tudor I, Sklar, Larry A

“…Traditional antimicrobials are increasingly suffering from the emergence of multidrug resistance among pathogenic microorganisms. To overcome these…”
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Novel Activities of Select NSAID R-Enantiomers against Rac1 and Cdc42 GTPases by Oprea, Tudor I, Sklar, Larry A, Agola, Jacob O, Guo, Yuna, Silberberg, Melina, Roxby, Joshua, Vestling, Anna, Romero, Elsa, Surviladze, Zurab, Murray-Krezan, Cristina, Waller, Anna, Ursu, Oleg, Hudson, Laurie G, Wandinger-Ness, Angela

“…Rho family GTPases (including Rac, Rho and Cdc42) collectively control cell proliferation, adhesion and migration and are of interest as functional therapeutic…”
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Characterization of a Cdc42 Protein Inhibitor and Its Use as a Molecular Probe by Hong, Lin, Kenney, S.Ray, Phillips, Genevieve K., Simpson, Denise, Schroeder, Chad E., Nöth, Julica, Romero, Elsa, Swanson, Scarlett, Waller, Anna, Strouse, J.Jacob, Carter, Mark, Chigaev, Alexandre, Ursu, Oleg, Oprea, Tudor, Hjelle, Brian, Golden, Jennifer E., Aubé, Jeffrey, Hudson, Laurie G., Buranda, Tione, Sklar, Larry A., Wandinger-Ness, Angela

“…Cdc42 plays important roles in cytoskeleton organization, cell cycle progression, signal transduction, and vesicle trafficking. Overactive Cdc42 has been…”
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In vivo effects of a GPR30 antagonist by Dennis, Megan K, Burai, Ritwik, Ramesh, Chinnasamy, Petrie, Whitney K, Alcon, Sara N, Nayak, Tapan K, Bologa, Cristian G, Leitao, Andrei, Brailoiu, Eugen, Deliu, Elena, Dun, Nae J, Sklar, Larry A, Hathaway, Helen J, Arterburn, Jeffrey B, Oprea, Tudor I, Prossnitz, Eric R

“…Estrogen is central to many physiological processes throughout the human body. We have previously shown that the G protein–coupled receptor GPR30 (also known…”
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Far away from the lamppost by Oprea, Tudor I, Jan, Lily, Johnson, Gary L, Roth, Bryan L, Ma'ayan, Avi, Schürer, Stephan, Shoichet, Brian K, Sklar, Larry A, McManus, Michael T

“…This Formal Comment responds to a recent Meta-Research Article by identifying initiatives that are already in place for funding risky exploratory research that…”
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