Search Results - "Glickman, J."

Development of human cGAS-specific small-molecule inhibitors for repression of dsDNA-triggered interferon expression by Lama, Lodoe, Adura, Carolina, Xie, Wei, Tomita, Daisuke, Kamei, Taku, Kuryavyi, Vitaly, Gogakos, Tasos, Steinberg, Joshua I., Miller, Michael, Ramos-Espiritu, Lavoisier, Asano, Yasutomi, Hashizume, Shogo, Aida, Jumpei, Imaeda, Toshihiro, Okamoto, Rei, Jennings, Andy J., Michino, Mayako, Kuroita, Takanobu, Stamford, Andrew, Gao, Pu, Meinke, Peter, Glickman, J. Fraser, Patel, Dinshaw J., Tuschl, Thomas

“…Cyclic GMP-AMP synthase (cGAS) is the primary sensor for aberrant intracellular dsDNA producing the cyclic dinucleotide cGAMP, a second messenger initiating…”
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Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice by Vincent, Jessica, Adura, Carolina, Gao, Pu, Luz, Antonio, Lama, Lodoe, Asano, Yasutomi, Okamoto, Rei, Imaeda, Toshihiro, Aida, Jumpei, Rothamel, Katherine, Gogakos, Tasos, Steinberg, Joshua, Reasoner, Seth, Aso, Kazuyoshi, Tuschl, Thomas, Patel, Dinshaw J., Glickman, J. Fraser, Ascano, Manuel

“…Cyclic GMP-AMP synthase is essential for innate immunity against infection and cellular damage, serving as a sensor of DNA from pathogens or mislocalized…”
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Human cGAS catalytic domain has an additional DNA-binding interface that enhances enzymatic activity and liquid-phase condensation by Xie, Wei, Lama, Lodoe, Adura, Carolina, Tomita, Daisuke, Glickman, J. Fraser, Tuschl, Thomas, Patel, Dinshaw J.

“…The cyclic GMP-AMP synthase (cGAS)–cGAMP–STING pathway plays a key role in innate immunity, with cGAS sensing both pathogenic and mislocalized DNA in the…”
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Small-Molecule Agonists of Ae. aegypti Neuropeptide Y Receptor Block Mosquito Biting by Duvall, Laura B., Ramos-Espiritu, Lavoisier, Barsoum, Kyrollos E., Glickman, J. Fraser, Vosshall, Leslie B.

“…Female Aedes aegypti mosquitoes bite humans to obtain blood to develop their eggs. Remarkably, their strong attraction to humans is suppressed for days after…”
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Small-molecule targeting of MUSASHI RNA-binding activity in acute myeloid leukemia by Minuesa, Gerard, Albanese, Steven K., Xie, Wei, Kazansky, Yaniv, Worroll, Daniel, Chow, Arthur, Schurer, Alexandra, Park, Sun-Mi, Rotsides, Christina Z., Taggart, James, Rizzi, Andrea, Naden, Levi N., Chou, Timothy, Gourkanti, Saroj, Cappel, Daniel, Passarelli, Maria C., Fairchild, Lauren, Adura, Carolina, Glickman, J. Fraser, Schulman, Jessica, Famulare, Christopher, Patel, Minal, Eibl, Joseph K., Ross, Gregory M., Bhattacharya, Shibani, Tan, Derek S., Leslie, Christina S., Beuming, Thijs, Patel, Dinshaw J., Goldgur, Yehuda, Chodera, John D., Kharas, Michael G.

“…The MUSASHI (MSI) family of RNA binding proteins (MSI1 and MSI2) contribute to a wide spectrum of cancers including acute myeloid leukemia. We find that the…”
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Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling by Petrova, Elissaveta, Rios-Esteves, Jessica, Ouerfelli, Ouathek, Glickman, J Fraser, Resh, Marilyn D

“…Hedgehog acyltransferase (Hhat) attaches a palmitate to Sonic hedgehog, but the importance of this enzyme has been difficult to discern. RU-SKI 43 is a potent…”
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MALT1 Small Molecule Inhibitors Specifically Suppress ABC-DLBCL In Vitro and In Vivo by Fontan, Lorena, Yang, Chenghua, Kabaleeswaran, Venkataraman, Volpon, Laurent, Osborne, Michael J., Beltran, Elena, Garcia, Monica, Cerchietti, Leandro, Shaknovich, Rita, Yang, Shao Ning, Fang, Fang, Gascoyne, Randy D., Martinez-Climent, Jose Angel, Glickman, J. Fraser, Borden, Katherine, Wu, Hao, Melnick, Ari

“…MALT1 cleavage activity is linked to the pathogenesis of activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL), a chemoresistant form of DLBCL. We…”
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A novel Aβ-fibrinogen interaction inhibitor rescues altered thrombosis and cognitive decline in Alzheimer's disease mice by Ahn, Hyung Jin, Glickman, J Fraser, Poon, Ka Lai, Zamolodchikov, Daria, Jno-Charles, Odella C, Norris, Erin H, Strickland, Sidney

“…Many Alzheimer's disease (AD) patients suffer from cerebrovascular abnormalities such as altered cerebral blood flow and cerebral microinfarcts. Recently,…”
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Alzheimer's disease peptide β-amyloid interacts with fibrinogen and induces its oligomerization by Ahn, Hyung Jin, Zamolodchikov, Daria, Cortes-Canteli, Marta, Norris, Erin H., Glickman, J. Fraser, Strickland, Sidney, Cerami, Anthony

“…Increasing evidence supports a vascular contribution to Alzheimer's disease (AD), but a direct connection between AD and the circulatory system has not been…”
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An allosteric inhibitor of bacterial Hsp70 chaperone potentiates antibiotics and mitigates resistance by Hosfelt, Jordan, Richards, Aweon, Zheng, Meng, Adura, Carolina, Nelson, Brock, Yang, Amy, Fay, Allison, Resager, William, Ueberheide, Beatrix, Glickman, J Fraser, Lupoli, Tania J

“…DnaK is the bacterial homolog of Hsp70, an ATP-dependent chaperone that helps cofactor proteins to catalyze nascent protein folding and salvage misfolded…”
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Nonsteroidal anti-inflammatory drug sensitizes Mycobacterium tuberculosis to endogenous and exogenous antimicrobials by Gold, Ben, Pingle, Maneesh, Brickner, Steven J, Shah, Nilesh, Roberts, Julia, Rundell, Mark, Bracken, W. Clay, Warrier, Thulasi, Somersan, Selin, Venugopal, Aditya, Darby, Crystal, Jiang, Xiuju, Warren, J. David, Fernandez, Joseph, Ouerfelli, Ouathek, Nuermberger, Eric L, Cunningham-Bussel, Amy, Rath, Poonam, Chidawanyika, Tamutenda, Deng, Haiteng, Realubit, Ronald, Glickman, J. Fraser, Nathan, Carl F

“…Existing drugs are slow to eradicate Mycobacterium tuberculosis (Mtb) in patients and have failed to control tuberculosis globally. One reason may be that host…”
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Targeting Mycobacterium tuberculosis response to environmental cues for the development of effective antitubercular drugs by Lavin, Richard C, Johnson, Calvin, Ahn, Yong-Mo, Kremiller, Kyle M, Sherwood, Matthew, Patel, Jimmy S, Pan, Yan, Russo, Riccardo, MacGilvary, Nathan J, Giacalone, David, Kevorkian, Yuzo L, Zimmerman, Matthew D, Glickman, J. Fraser, Freundlich, Joel S, Tan, Shumin

“…Sensing and response to environmental cues, such as pH and chloride (Cl − ), is critical in enabling Mycobacterium tuberculosis (Mtb) colonization of its host…”
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Discovery of LRE1 as a specific and allosteric inhibitor of soluble adenylyl cyclase by Ramos-Espiritu, Lavoisier, Kleinboelting, Silke, Navarrete, Felipe A, Alvau, Antonio, Visconti, Pablo E, Valsecchi, Federica, Starkov, Anatoly, Manfredi, Giovanni, Buck, Hannes, Adura, Carolina, Zippin, Jonathan H, van den Heuvel, Joop, Glickman, J Fraser, Steegborn, Clemens, Levin, Lonny R, Buck, Jochen

“…Editorial summary A high-throughput screen using a mass-spectrometry-based assay results in the identification of LRE1 as an inhibitor of HCO 3 − /Ca 2+…”
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Arabinose- and xylose-modified analogs of 2',3'-cGAMP act as STING agonists by Xie, Wei, Lama, Lodoe, Yang, Xuejing, Kuryavyi, Vitaly, Bhattacharya, Shibani, Nudelman, Ilona, Yang, Guangli, Ouerfelli, Ouathek, Glickman, J Fraser, Jones, Roger A, Tuschl, Thomas, Patel, Dinshaw J

“…Stimulator of interferon genes (STING) agonists are promising candidates for vaccine adjuvants and antitumor immune stimulants. The most potent natural agonist…”
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Discovery of a Small Molecule Promoting Mouse and Human Osteoblast Differentiation via Activation of p38 MAPK-β by Cook, Brandoch, Rafiq, Ruhina, Lee, Heejin, Banks, Kelly M, El-Debs, Mohammed, Chiaravalli, Jeanne, Glickman, J Fraser, Das, Bhaskar C, Chen, Shuibing, Evans, Todd

“…Disorders of bone healing and remodeling are indications with an unmet need for effective pharmacological modulators. We used a high-throughput screen to…”
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A genome-wide arrayed CRISPR screen identifies PLSCR1 as an intrinsic barrier to SARS-CoV-2 entry that recent virus variants have evolved to resist by Le Pen, Jérémie, Paniccia, Gabrielle, Kinast, Volker, Moncada-Velez, Marcela, Ashbrook, Alison W, Bauer, Michael, Hoffmann, H-Heinrich, Pinharanda, Ana, Ricardo-Lax, Inna, Stenzel, Ansgar F, Rosado-Olivieri, Edwin A, Dinnon, 3rd, Kenneth H, Doyle, William C, Freije, Catherine A, Hong, Seon-Hui, Lee, Danyel, Lewy, Tyler, Luna, Joseph M, Peace, Avery, Schmidt, Carltin, Schneider, William M, Winkler, Roni, Yip, Elaine Z, Larson, Chloe, McGinn, Timothy, Menezes, Miriam-Rose, Ramos-Espiritu, Lavoisier, Banerjee, Priyam, Poirier, John T, Sànchez-Rivera, Francisco J, Cobat, Aurélie, Zhang, Qian, Casanova, Jean-Laurent, Carroll, Thomas S, Glickman, J Fraser, Michailidis, Eleftherios, Razooky, Brandon, MacDonald, Margaret R, Rice, Charles M

“…Interferons (IFNs) play a crucial role in the regulation and evolution of host-virus interactions. Here, we conducted a genome-wide arrayed CRISPR knockout…”
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Identification of Novel Therapeutic Targets for Fibrolamellar Carcinoma Using Patient-Derived Xenografts and Direct-from-Patient Screening by Lalazar, Gadi, Requena, David, Ramos-Espiritu, Lavoisier, Ng, Denise, Bhola, Patrick D, de Jong, Ype P, Wang, Ruisi, Narayan, Nicole J C, Shebl, Bassem, Levin, Solomon, Michailidis, Eleftherios, Kabbani, Mohammad, Vercauteren, Koen O A, Hurley, Arlene M, Farber, Benjamin A, Hammond, William J, Saltsman, 3rd, James A, Weinberg, Ethan M, Glickman, J Fraser, Lyons, Barbara A, Ellison, Jessica, Schadde, Erik, Hertl, Martin, Leiting, Jennifer L, Truty, Mark J, Smoot, Rory L, Tierney, Faith, Kato, Tomoaki, Wendel, Hans-Guido, LaQuaglia, Michael P, Rice, Charles M, Letai, Anthony, Coffino, Philip, Torbenson, Michael S, Ortiz, Michael V, Simon, Sanford M

“…To repurpose therapeutics for fibrolamellar carcinoma (FLC), we developed and validated patient-derived xenografts (PDX) from surgical resections. Most agents…”
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Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery by Jahnke, Wolfgang, Rondeau, Jean-Michel, Cotesta, Simona, Marzinzik, Andreas, Pellé, Xavier, Geiser, Martin, Strauss, André, Götte, Marjo, Bitsch, Francis, Hemmig, René, Henry, Chrystèle, Lehmann, Sylvie, Glickman, J Fraser, Roddy, Thomas P, Stout, Steven J, Green, Jonathan R

“…Although FPPS is a potential anti-cancer target, the high bone affinity of nitrogen-containing bisphosphonates, FPPS inhibitors used clinically to treat bone…”
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Bithionol Potently Inhibits Human Soluble Adenylyl Cyclase through Binding to the Allosteric Activator Site by Kleinboelting, Silke, Ramos-Espiritu, Lavoisier, Buck, Hannes, Colis, Laureen, van den Heuvel, Joop, Glickman, J. Fraser, Levin, Lonny R., Buck, Jochen, Steegborn, Clemens

“…The signaling molecule cAMP regulates functions ranging from bacterial transcription to mammalian memory. In mammals, cAMP is synthesized by nine transmembrane…”
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Scintillation proximity assays in high-throughput screening by Glickman, J Fraser, Schmid, Andres, Ferrand, Sandrine

“…Scintillation proximity assays (SPAs) have become a powerful tool for high-throughput screening (HTS) because they can measure the activity and binding of very…”
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