未登录 Structure-Activity and Structure-Degradation Relationship Studies of 2-Amino-6-(benzimidazol-2-ylmethyl)-N9-heteroarylpurines as Potent and Selective CDK12/13 Inhibitors and Cyclin K Degraders Pandurangan, Thiyagamurthy; Zeleke, Solomon Tadesse; Iermolaieva, Anna; Ghosh, Pompom; Mosior, John; Sun, Luxin; Grassie, Dylan; Schmitz, Maximilian; Kalaga, Mahalakshmi Naidu; Albritton, William; Rodas, Manuel Manzanares; Chan, Sean Chin; Frydman, Sylvia; Sansil, Samer; Geyer, Matthias; Schoenbrunn, Ernst; Roush, William R.; Duckett, Derek R.; Monastyrskyi, Andrii 分享 收藏
Discovery of DFV890, a Potent Sulfonimidamide-Containing NLRP3 Inflammasome Inhibitor (vol 68, pg 5529, 2025) 发现DFV890,一种强效含磺酰胺亚胺基的NLRP3炎性小体抑制剂(第68卷,第5529页,2025年) Shen, Dong-Ming; Byth, Kate F.; Bertheloot, Damien; Braams, Simona; Bradley, Sarah; Dean, Dennis; Dekker, Carien; El-Kattan, Ayman F.; Franchi, Luigi; Glick, Gary D.; Ghosh, Shomir; Graves, Jonathan D.; Hinniger, Alexandra; Katz, Jason D.; Kitanovic, Ana; Lu, Xiaokang; Olhava, Edward J.; Opipari, Anthony W.; Sanchez, Brian; Seidel, H. Martin; Stunden, James; Stutz, Andrea; Telling, Alissa; Venkatraman, Shankar; Winkler, David G.; Roush, William R. 分享 收藏
Discovery and design of molecular glue enhancers of CDK12-DDB1 interactions for targeted degradation of cyclin K 用于靶向降解细胞周期蛋白K的CDK12-DDB1相互作用的分子胶增强剂的发现和设计 Ghosh, Pompom; Schmitz, Maximilian; Pandurangan, Thiyagamurthy; Zeleke, Solomon Tadesse; Chan, Sean Chin; Mosior, John; Sun, Luxin; Palve, Vinayak; Grassie, Dylan; Anand, Kanchan; Frydman, Sylvia; Roush, William R.; Schonbrunn, Ernst; Geyer, Matthias; Duckett, Derek; Monastyrskyi, Andrii 分享 收藏
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CK1δ and CK1ε Signaling Sustains Mitochondrial Metabolism and Cell Survival in Multiple Myeloma Burger, Karen L.; Fernandez, Mario R.; Meads, Mark B.; Sudalagunta, Praneeth; Oliveira, Paula S.; Canevarolo, Rafael Renatino; Alugubelli, Raghunandan Reddy; Tungsevik, Alexandre; De Avila, Gabe; Silva, Maria; Graeter, Allison I.; Dai, Hongyue A.; Vincelette, Nicole D.; Prabhu, Antony; Magaletti, Dario; Yang, Chunying; Li, Weimin; Kulkarni, Amit; Hampton, Oliver; Koomen, John M.; Roush, William R.; Monastyrskyi, Andrii; Berglund, Anders E.; Silva, Ariosto S.; Cleveland, John L.; Shain, Kenneth H. 分享 收藏
Structure-Based Development of Isoform-Selective Inhibitors of Casein Kinase 1ε vs Casein Kinase 1δ Choi, Jun Yong; Noguchi, Yoshihiko; Alburger, James M.; Bayle, Simon; Chung, Eugene; Grant, Wayne; Chaikuad, Apirat; Knapp, Stefan; Duckett, Derek R.; Roush, William R. 分享 收藏
Functional Roles of Acetylated Histone Marks at Mouse Meiotic Recombination Hot Spots Getun, Irina V.; Wu, Zhen; Fallahi, Mohammad; Ouizem, Souad; Liu, Qin; Li, Weimin; Costi, Roberta; Roush, William R.; Cleveland, John L.; Bois, Philippe R. J. 分享 收藏
Molecular Modeling of ABHD5 Structure and Ligand Recognition Shahoei, Rezvan; Pangeni, Susheel; Sanders, Matthew A.; Zhang, Huamei; Mladenovic-Lucas, Ljiljana; Roush, William R.; Halvorsen, Geoff; Kelly, Christopher V.; Granneman, James G.; Huang, Yu-ming M. 分享 收藏
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The Specific NLRP3 Antagonist IFM-514 Decreases Fibrosis and Inflammation in Experimental Murine Non-Alcoholic Steatohepatitis Torres, Sandra; Brol, Maximilian J.; Magdaleno, Fernando; Schierwagen, Robert; Uschner, Frank E.; Klein, Sabine; Ortiz, Cristina; Tyc, Olaf; Bachtler, Nadine; Stunden, James; Bertheloot, Damien; Kitanovic, Ana; Sanchez, Brian; Schrum, Jacob; Roush, William R.; Franchi, Luigi; Byth, Kate; Latz, Eicke; Trebicka, Jonel 分享 收藏
Host-Derived Matrix Metalloproteinase-13 Activity Promotes Multiple Myeloma-Induced Osteolysis and Reduces Overall Survival Lo, Chen Hao; Shay, Gemma; McGuire, Jeremy J.; Li, Tao; Shain, Kenneth H.; Choi, Jun Yong; Fuerst, Rita; Roush, William R.; Knapinska, Anna M.; Fields, Gregg B.; Lynch, Conor C. 分享 收藏
Druggable Hot Spots in the Schistosomiasis Cathepsin B1 Target Identified by Functional and Binding Mode Analysis of Potent Vinyl Sulfone Inhibitors Jilkova, Adela; Rubesova, Petra; Fanfrlik, Jindrich; Fajtova, Pavla; Rezacova, Pavlina; Brynda, Jiri; Lepsik, Martin; Mertlikova-Kaiserova, Helena; Emal, Cory D.; Renslo, Adam R.; Roush, William R.; Horn, Martin; Caffrey, Conor R.; Mares, Michael 分享 收藏
Targeting Casein Kinase 1 Delta Sensitizes Pancreatic and Bladder Cancer Cells to Gemcitabine Treatment by Upregulating Deoxycytidine Kinase Vena, Francesca; Bayle, Simon; Nieto, Ainhoa; Quereda, Victor; Aceti, Massimiliano; Frydman, Sylvia M.; Sansil, Samer S.; Grant, Wayne; Monastyrskyi, Andrii; McDonald, Patricia; Roush, William R.; Teng, Mingxiang; Duckett, Derek 分享 收藏
The dual PI3Kδ/CK1ε inhibitor umbralisib exhibits unique immunomodulatory effects on CLL T cells Maharaj, Kamira; Powers, John J.; Achille, Alex; Mediavilla-Varela, Melanie; Gamal, Wael; Burger, Karen L.; Fonseca, Renee; Jiang, Kun; Miskin, Hari P.; Maryanski, Dave; Monastyrskyi, Andrii; Duckett, Derek R.; Roush, William R.; Cleveland, John L.; Sahakian, Eva; Pinilla-Ibarz, Javier 分享 收藏
Restricting Glycolysis Preserves T Cell Effector Functions and Augments Checkpoint Therapy Renner, Kathrin; Bruss, Christina; Schnell, Annette; Koehl, Gudrun; Becker, Holger M.; Fante, Matthias; Menevse, Ayse-Nur; Kauer, Nathalie; Blazquez, Raquel; Hacker, Lisa; Decking, Sonja-Maria; Bohn, Toszka; Faerber, Stephanie; Evert, Katja; Aigle, Lisa; Amslinger, Sabine; Landa, Maria; Krijgsman, Oscar; Rozeman, Elisa A.; Brummer, Christina; Siska, Peter J.; Singer, Katrin; Pektor, Stefanie; Miederer, Matthias; Peter, Katrin; Gottfried, Eva; Herr, Wolfgang; Marchiq, Ibtisam; Pouyssegur, Jacques; Roush, William R.; Ong, SuFey; Warren, Sarah; Pukrop, Tobias; Beckhove, Philipp; Lang, Sven A.; Bopp, Tobias; Blank, Christian U.; Cleveland, John L.; Oefner, Peter J.; Dettmer, Katja; Selby, Mark; Kreutz, Marina 分享 收藏
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SR-4370, a potent and selective inhibitor of class I HDACs, suppresses AR signaling and in vivo prostate tumor growth Mahmud, Iqbal; Tian, Guimei; Wang, Jia; Stowe, Ryan; Huo, Zhiguang; Zhang, Yushan; Purayil, Hamsa Thayek; Helm, Eric; Drashansky, Theodore; Avram, Dorina; Daaka, Yehia; Roush, William R.; Liao, Daiqing 分享 收藏
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