Search Results - "Kawatkar, Aarti"

Discovery of Clinical Candidate AZD0095, a Selective Inhibitor of Monocarboxylate Transporter 4 (MCT4) for Oncology by Goldberg, Frederick W., Kettle, Jason G., Lamont, Gillian M., Buttar, David, Ting, Attilla K. T., McGuire, Thomas M., Cook, Calum R., Beattie, David, Morentin Gutierrez, Pablo, Kavanagh, Stefan L., Komen, Jasper C., Kawatkar, Aarti, Clark, Roger, Hopcroft, Lorna, Hughes, Gareth, Critchlow, Susan E.

“…Due to increased reliance on glycolysis, which produces lactate, monocarboxylate transporters (MCTs) are often upregulated in cancer. MCT4 is associated with…”
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Integrated Proteomics Characterization of NLRP3 Inflammasome Inhibitor MCC950 in Monocytic Cell Line Confirms Direct MCC950 Engagement with Endogenous NLRP3 by Zhao, Heng, Kumar, Praveen, Sobreira, Tiago Jose Paschoal, Smith, Mackenzie, Novick, Steven, Johansson, Anders, Luchniak, Anna, Zhang, Andrew, Woollard, Kevin J, Larsson, Niklas, Kawatkar, Aarti

“…Inhibition of the NLRP3 inflammasome is a promising strategy for the development of new treatments for inflammatory diseases. MCC950 is a potent and selective…”
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Development of a Novel B‑Cell Lymphoma 6 (BCL6) PROTAC To Provide Insight into Small Molecule Targeting of BCL6 by McCoull, William, Cheung, Tony, Anderson, Erica, Barton, Peter, Burgess, Jonathan, Byth, Kate, Cao, Qing, Castaldi, M. Paola, Chen, Huawei, Chiarparin, Elisabetta, Carbajo, Rodrigo J, Code, Erin, Cowan, Suzanna, Davey, Paul R, Ferguson, Andrew D, Fillery, Shaun, Fuller, Nathan O, Gao, Ning, Hargreaves, David, Howard, Martin R, Hu, Jun, Kawatkar, Aarti, Kemmitt, Paul D, Leo, Elisabetta, Molina, Daniel M, O’Connell, Nichole, Petteruti, Philip, Rasmusson, Timothy, Raubo, Piotr, Rawlins, Philip B, Ricchiuto, Piero, Robb, Graeme R, Schenone, Monica, Waring, Michael J, Zinda, Michael, Fawell, Stephen, Wilson, David M

“…B-cell lymphoma 6 (BCL6) inhibition is a promising mechanism for treating hematological cancers but high quality chemical probes are necessary to evaluate its…”
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CETSA beyond Soluble Targets: a Broad Application to Multipass Transmembrane Proteins by Kawatkar, Aarti, Schefter, Michelle, Hermansson, Nils-Olov, Snijder, Arjan, Dekker, Niek, Brown, Dean G, Lundbäck, Thomas, Zhang, Andrew X, Castaldi, M. Paola

“…Demonstration of target binding is a key requirement for understanding the mode of action of new therapeutics. The cellular thermal shift assay (CETSA) has…”
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Chemical Biology Approaches Confirm MCT4 as the Therapeutic Target of a Cellular Optimized Hit by Kawatkar, Aarti, Clark, Roger A., Hopcroft, Lorna, Roaquin, Debora Ann, Tomlinson, Ronald, Zuhl, Andrea M., Lamont, Gillian M., Kettle, Jason G., Critchlow, Susan E., Castaldi, M. Paola, Goldberg, Frederick W., Zhang, Andrew X.

“…Lactic acid transport is a key process maintaining glycolytic flux in tumors. Inhibition of this process will result in glycolytic shutdown, impacting on cell…”
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Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors by Grimster, Neil P, Anderson, Erica, Alimzhanov, Marat, Bebernitz, Geraldine, Bell, Kirsten, Chuaqui, Claudio, Deegan, Tracy, Ferguson, Andrew D, Gero, Thomas, Harsch, Andreas, Huszar, Dennis, Kawatkar, Aarti, Kettle, Jason G, Lyne, Paul, Read, Jon A, Rivard Costa, Caroline, Ruston, Linette, Schroeder, Patricia, Shi, Jie, Su, Qibin, Throner, Scott, Toader, Dorin, Vasbinder, Melissa, Woessner, Richard, Wang, Haixia, Wu, Allan, Ye, Minwei, Zheng, Weijia, Zinda, Michael

“…Janus kinases (JAKs) have been demonstrated to be critical in cytokine signaling and have thus been implicated in both cancer and inflammatory diseases. The…”
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Direct activation of KCC2 arrests benzodiazepine refractory status epilepticus and limits the subsequent neuronal injury in mice by Jarvis, Rebecca, Josephine Ng, Shu Fun, Nathanson, Anna J., Cardarelli, Ross A., Abiraman, Krithika, Wade, Fergus, Evans-Strong, Aidan, Fernandez-Campa, Marina P., Deeb, Tarek Z., Smalley, Joshua L., Jamier, Tanguy, Gurrell, Ian K., McWilliams, Lisa, Kawatkar, Aarti, Conway, Leslie C., Wang, Qi, Burli, Roland W., Brandon, Nicholas J., Chessell, Iain P., Goldman, Aaron J., Maguire, Jamie L., Moss, Stephen J.

“…Hyperpolarizing GABAAR currents, the unitary events that underlie synaptic inhibition, are dependent upon efficient Cl− extrusion, a process that is…”
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Identification of azabenzimidazoles as potent JAK1 selective inhibitors by Vasbinder, Melissa M., Alimzhanov, Marat, Augustin, Martin, Bebernitz, Geraldine, Bell, Kirsten, Chuaqui, Claudio, Deegan, Tracy, Ferguson, Andrew D., Goodwin, Kelly, Huszar, Dennis, Kawatkar, Aarti, Kawatkar, Sameer, Read, Jon, Shi, Jie, Steinbacher, Stefan, Steuber, Holger, Su, Qibin, Toader, Dorin, Wang, Haixia, Woessner, Richard, Wu, Allan, Ye, Minwei, Zinda, Michael

“…[Display omitted] We have identified a class of azabenzimidazoles as potent and selective JAK1 inhibitors. Investigations into the SAR are presented along with…”
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Target Deconvolution Efforts on Wnt Pathway Screen Reveal Dual Modulation of Oxidative Phosphorylation and SERCA2 by Casás‐Selves, Matias, Zhang, Andrew X., Dowling, James E., Hallén, Stefan, Kawatkar, Aarti, Pace, Nicholas J., Denz, Christopher R., Pontz, Timothy, Garahdaghi, Farzin, Cao, Qing, Sabirsh, Alan, Thakur, Kumar, O'Connell, Nichole, Hu, Jun, Cornella‐Taracido, Iván, Weerapana, Eranthie, Zinda, Michael, Goodnow, Robert A., Castaldi, M. Paola

“…Wnt signaling is critical for development, cell proliferation and differentiation, and mutations in this pathway resulting in constitutive signaling have been…”
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Cover Picture: Target Deconvolution Efforts on Wnt Pathway Screen Reveal Dual Modulation of Oxidative Phosphorylation and SERCA2 (ChemMedChem 12/2017) by Casás‐Selves, Matias, Zhang, Andrew X., Dowling, James E., Hallén, Stefan, Kawatkar, Aarti, Pace, Nicholas J., Denz, Christopher R., Pontz, Timothy, Garahdaghi, Farzin, Cao, Qing, Sabirsh, Alan, Thakur, Kumar, O'Connell, Nichole, Hu, Jun, Cornella‐Taracido, Iván, Weerapana, Eranthie, Zinda, Michael, Goodnow, Robert A., Castaldi, M. Paola

“…The front cover picture shows the process of photocrosslinking a small molecule functionalized with a diaziridino group to its putative target upon UV…”
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