IOA-244 is a Non-ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance.
Cancer Research Communications
Johnson, Zoë Z; Tarantelli, Chiara C; Civanelli, Elisa E; Cascione, Luciano L; Spriano, Filippo F; Fraser, Amy A; Shah, Pritom P; Nomanbhoy, Tyzoon T; Napoli, Sara S; Rinaldi, Andrea A; Niewola-Staszkowska, Karolina K; Lahn, Michael M; Perrin, Dominique D; Wenes, Mathias M; Migliorini, Denis D; Bertoni, Francesco F; van der Veen, Lars L; Di Conza, Giusy G
Mapping the landscape of genetic dependencies in chordoma.
Nature Communications
Sharifnia, Tanaz T; Wawer, Mathias J MJ; Goodale, Amy A; Lee, Yenarae Y; Kazachkova, Mariya M; Dempster, Joshua M JM; Muller, Sandrine S; Levy, Joan J; Freed, Daniel M DM; Sommer, Josh J; Kalfon, Jérémie J; Vazquez, Francisca F; Hahn, William C WC; Root, David E DE; Clemons, Paul A PA; Schreiber, Stuart L SL
Combined inhibition of EZH2 and ATM is synthetic lethal in BRCA1-deficient breast cancer.
Breast Cancer Research : Bcr
Ratz, Leonie L; Brambillasca, Chiara C; Bartke, Leandra L; Huetzen, Maxim A MA; Goergens, Jonas J; Leidecker, Orsolya O; Jachimowicz, Ron D RD; van de Ven, Marieke M; Proost, Natalie N; Siteur, Bjørn B; de Korte-Grimmerink, Renske R; Bouwman, Peter P; Pulver, Emilia M EM; de Bruijn, Roebi R; Isensee, Jörg J; Hucho, Tim T; Pandey, Gaurav G; van Lohuizen, Maarten M; Mallmann, Peter P; Reinhardt, Hans Christian HC; Jonkers, Jos J; Puppe, Julian J
Phenotypic Screening for Small Molecules that Protect β-Cells from Glucolipotoxicity.
Acs Chemical Biology
Small, Jonnell C JC; Joblin-Mills, Aidan A; Carbone, Kaycee K; Kost-Alimova, Maria M; Ayukawa, Kumiko K; Khodier, Carol C; Dancik, Vlado V; Clemons, Paul A PA; Munkacsi, Andrew B AB; Wagner, Bridget K BK
CHK1 protects oncogenic KRAS-expressing cells from DNA damage and is a target for pancreatic cancer treatment.
Cell Reports
Klomp, Jennifer E JE; Lee, Ye S YS; Goodwin, Craig M CM; Papke, Björn B; Klomp, Jeff A JA; Waters, Andrew M AM; Stalnecker, Clint A CA; DeLiberty, Jonathan M JM; Drizyte-Miller, Kristina K; Yang, Runying R; Diehl, J Nathaniel JN; Yin, Hongwei H HH; Pierobon, Mariaelena M; Baldelli, Elisa E; Ryan, Meagan B MB; Li, Siqi S; Peterson, Jackson J; Smith, Amber R AR; Neal, James T JT; McCormick, Aaron K AK; Kuo, Calvin J CJ; Counter, Christopher M CM; Petricoin, Emanuel F EF; Cox, Adrienne D AD; Bryant, Kirsten L KL; Der, Channing J CJ
MAPK-pathway inhibition mediates inflammatory reprogramming and sensitizes tumors to targeted activation of innate immunity sensor RIG-I.
Nature Communications
Brägelmann, Johannes J; Lorenz, Carina C; Borchmann, Sven S; Nishii, Kazuya K; Wegner, Julia J; Meder, Lydia L; Ostendorp, Jenny J; Ast, David F DF; Heimsoeth, Alena A; Nakasuka, Takamasa T; Hirabae, Atsuko A; Okawa, Sachi S; Dammert, Marcel A MA; Plenker, Dennis D; Klein, Sebastian S; Lohneis, Philipp P; Gu, Jianing J; Godfrey, Laura K LK; Forster, Jan J; Trajkovic-Arsic, Marija M; Zillinger, Thomas T; Haarmann, Mareike M; Quaas, Alexander A; Lennartz, Stefanie S; Schmiel, Marcel M; D'Rozario, Joshua J; Thomas, Emily S ES; Li, Henry H; Schmitt, Clemens A CA; George, Julie J; Thomas, Roman K RK; von Karstedt, Silvia S; Hartmann, Gunther G; Büttner, Reinhard R; Ullrich, Roland T RT; Siveke, Jens T JT; Ohashi, Kadoaki K; Schlee, Martin M; Sos, Martin L ML
Mutant p53-reactivating compound APR-246 synergizes with asparaginase in inducing growth suppression in acute lymphoblastic leukemia cells.
Cell Death & Disease
Ceder, Sophia S; Eriksson, Sofi E SE; Liang, Ying Yu YY; Cheteh, Emarndeena H EH; Zhang, Si Min SM; Fujihara, Kenji M KM; Bianchi, Julie J; Bykov, Vladimir J N VJN; Abrahmsen, Lars L; Clemons, Nicholas J NJ; Nordlund, Pär P; Rudd, Sean G SG; Wiman, Klas G KG
In Vitro Systematic Drug Testing Reveals Carboplatin, Paclitaxel, and Alpelisib as a Potential Novel Combination Treatment for Adult Granulosa Cell Tumors.
Cancers
Roze, Joline J; Sendino Garví, Elena E; Stelloo, Ellen E; Stangl, Christina C; Sereno, Ferdinando F; Duran, Karen K; Groeneweg, Jolijn J; Paijens, Sterre S; Nijman, Hans H; van Meurs, Hannah H; van Lonkhuijzen, Luc L; Piek, Jurgen J; Lok, Christianne C; Jonges, Geertruida G; Witteveen, Petronella P; Verheijen, René R; van Haaften, Gijs G; Zweemer, Ronald R; Monroe, Glen G
SHP2 Inhibition Influences Therapeutic Response to Tepotinib in Tumors with MET Alterations.
Iscience
Pudelko, Linda L; Jaehrling, Frank F; Reusch, Christof C; Vitri, Sanziago S; Stroh, Christopher C; Linde, Nina N; Sanderson, Michael P MP; Musch, Doreen D; Lebrun, Catherine Jorand CJ; Keil, Marina M; Esdar, Christina C; Blaukat, Andree A; Rosell, Rafael R; Schumacher, Karl Maria KM; Karachaliou, Niki N
Perturbation biology links temporal protein changes to drug responses in a melanoma cell line.
Plos Computational Biology
Nyman, Elin E; Stein, Richard R RR; Jing, Xiaohong X; Wang, Weiqing W; Marks, Benjamin B; Zervantonakis, Ioannis K IK; Korkut, Anil A; Gauthier, Nicholas P NP; Sander, Chris C
Multiple low dose therapy as an effective strategy to treat EGFR inhibitor-resistant NSCLC tumours.
Nature Communications
Fernandes Neto, João M JM; Nadal, Ernest E; Bosdriesz, Evert E; Ooft, Salo N SN; Farre, Lourdes L; McLean, Chelsea C; Klarenbeek, Sjoerd S; Jurgens, Anouk A; Hagen, Hannes H; Wang, Liqin L; Felip, Enriqueta E; Martinez-Marti, Alex A; Vidal, August A; Voest, Emile E; Wessels, Lodewyk F A LFA; van Tellingen, Olaf O; Villanueva, Alberto A; Bernards, René R
High-throughput dynamic BH3 profiling may quickly and accurately predict effective therapies in solid tumors.
Science Signaling
Bhola, Patrick D PD; Ahmed, Eman E; Guerriero, Jennifer L JL; Sicinska, Ewa E; Su, Emily E; Lavrova, Elizaveta E; Ni, Jing J; Chipashvili, Otari O; Hagan, Timothy T; Pioso, Marissa S MS; McQueeney, Kelley K; Ng, Kimmie K; Aguirre, Andrew J AJ; Cleary, James M JM; Cocozziello, David D; Sotayo, Alaba A; Ryan, Jeremy J; Zhao, Jean J JJ; Letai, Anthony A
Ricker, Cora A CA; Crawford, Kenneth K; Matlock, Kevin K; Lathara, Melvin M; Seguin, Bernard B; Rudzinski, Erin R ER; Berlow, Noah E NE; Keller, Charles C
Atypical KRASG12R Mutant Is Impaired in PI3K Signaling and Macropinocytosis in Pancreatic Cancer.
Cancer Discovery
Hobbs, G Aaron GA; Baker, Nicole M NM; Miermont, Anne M AM; Thurman, Ryan D RD; Pierobon, Mariaelena M; Tran, Timothy H TH; Anderson, Andrew O AO; Waters, Andrew M AM; Diehl, J Nathaniel JN; Papke, Bjoern B; Hodge, Richard G RG; Klomp, Jennifer E JE; Goodwin, Craig M CM; DeLiberty, Jonathan M JM; Wang, Junning J; Ng, Raymond W S RWS; Gautam, Prson P; Bryant, Kirsten L KL; Esposito, Dominic D; Campbell, Sharon L SL; Petricoin, Emanuel F EF; Simanshu, Dhirendra K DK; Aguirre, Andrew J AJ; Wolpin, Brian M BM; Wennerberg, Krister K; Rudloff, Udo U; Cox, Adrienne D AD; Der, Channing J CJ
Isoform-Specific Destabilization of the Active Site Reveals a Molecular Mechanism of Intrinsic Activation of KRas G13D.
Cell Reports
Johnson, Christian W CW; Lin, Yi-Jang YJ; Reid, Derion D; Parker, Jillian J; Pavlopoulos, Spiro S; Dischinger, Patrick P; Graveel, Carrie C; Aguirre, Andrew J AJ; Steensma, Matthew M; Haigis, Kevin M KM; Mattos, Carla C
Application of a MYC degradation screen identifies sensitivity to CDK9 inhibitors in KRAS-mutant pancreatic cancer.
Science Signaling
Blake, Devon R DR; Vaseva, Angelina V AV; Hodge, Richard G RG; Kline, McKenzie P MP; Gilbert, Thomas S K TSK; Tyagi, Vikas V; Huang, Daowei D; Whiten, Gabrielle C GC; Larson, Jacob E JE; Wang, Xiaodong X; Pearce, Kenneth H KH; Herring, Laura E LE; Graves, Lee M LM; Frye, Stephen V SV; Emanuele, Michael J MJ; Cox, Adrienne D AD; Der, Channing J CJ
A Multi-center Study on the Reproducibility of Drug-Response Assays in Mammalian Cell Lines.
Cell Systems
Niepel, Mario M; Hafner, Marc M; Mills, Caitlin E CE; Subramanian, Kartik K; Williams, Elizabeth H EH; Chung, Mirra M; Gaudio, Benjamin B; Barrette, Anne Marie AM; Stern, Alan D AD; Hu, Bin B; Korkola, James E JE; , ; Gray, Joe W JW; Birtwistle, Marc R MR; Heiser, Laura M LM; Sorger, Peter K PK
TAS-120 Overcomes Resistance to ATP-Competitive FGFR Inhibitors in Patients with FGFR2 Fusion-Positive Intrahepatic Cholangiocarcinoma.
Cancer Discovery
Goyal, Lipika L; Shi, Lei L; Liu, Leah Y LY; Fece de la Cruz, Ferran F; Lennerz, Jochen K JK; Raghavan, Srivatsan S; Leschiner, Ignaty I; Elagina, Liudmila L; Siravegna, Giulia G; Ng, Raymond W S RWS; Vu, Phuong P; Patra, Krushna C KC; Saha, Supriya K SK; Uppot, Raul N RN; Arellano, Ron R; Reyes, Stephanie S; Sagara, Takeshi T; Otsuki, Sachie S; Nadres, Brandon B; Shahzade, Heather A HA; Dey-Guha, Ipsita I; Fetter, Isobel J IJ; Baiev, Islam I; Van Seventer, Emily E EE; Murphy, Janet E JE; Ferrone, Cristina R CR; Tanabe, Kenneth K KK; Deshpande, Vikram V; Harding, James J JJ; Yaeger, Rona R; Kelley, Robin K RK; Bardelli, Alberto A; Iafrate, A John AJ; Hahn, William C WC; Benes, Cyril H CH; Ting, David T DT; Hirai, Hiroshi H; Getz, Gad G; Juric, Dejan D; Zhu, Andrew X AX; Corcoran, Ryan B RB; Bardeesy, Nabeel N
Genomic and Functional Fidelity of Small Cell Lung Cancer Patient-Derived Xenografts.
Cancer Discovery
Drapkin, Benjamin J BJ; George, Julie J; Christensen, Camilla L CL; Mino-Kenudson, Mari M; Dries, Ruben R; Sundaresan, Tilak T; Phat, Sarah S; Myers, David T DT; Zhong, Jun J; Igo, Peter P; Hazar-Rethinam, Mehlika H MH; Licausi, Joseph A JA; Gomez-Caraballo, Maria M; Kem, Marina M; Jani, Kandarp N KN; Azimi, Roxana R; Abedpour, Nima N; Menon, Roopika R; Lakis, Sotirios S; Heist, Rebecca S RS; Büttner, Reinhard R; Haas, Stefan S; Sequist, Lecia V LV; Shaw, Alice T AT; Wong, Kwok-Kin KK; Hata, Aaron N AN; Toner, Mehmet M; Maheswaran, Shyamala S; Haber, Daniel A DA; Peifer, Martin M; Dyson, Nicholas N; Thomas, Roman K RK; Farago, Anna F AF
Targeting mutant RAS in patient-derived colorectal cancer organoids by combinatorial drug screening.
Elife
Verissimo, Carla S CS; Overmeer, René M RM; Ponsioen, Bas B; Drost, Jarno J; Mertens, Sander S; Verlaan-Klink, Ingrid I; Gerwen, Bastiaan van BV; van der Ven, Marieke M; Wetering, Marc van de MV; Egan, David A DA; Bernards, René R; Clevers, Hans H; Bos, Johannes L JL; Snippert, Hugo J HJ