Double PIK3CA mutations in cis increase oncogenicity and sensitivity to PI3Kα inhibitors
Vasan, Neil, Razavi, Pedram, Johnson, Jared L, Shao, Hong, Shah, Hardik, Antoine, Alesia, Ladewig, Erik, Gorelick, Alexander, Lin, Ting-Yu, Toska, Eneda, Xu, Guotai, Kazmi, Abiha, Chang, Matthew T, Taylor, Barry S, Dickler, Maura N, Jhaveri, Komal, Chandarlapaty, Sarat, Rabadan, Raul, Reznik, Ed, Smith, Melissa L, Sebra, Robert, Schimmoller, Frauke, Wilson, Timothy R, Friedman, Lori S, Cantley, Lewis C, Scaltriti, Maurizio, Baselga, José
Published in Science (American Association for the Advancement of Science) (08.11.2019)
Published in Science (American Association for the Advancement of Science) (08.11.2019)
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RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth
Hatzivassiliou, Georgia, Song, Kyung, Yen, Ivana, Brandhuber, Barbara J., Anderson, Daniel J., Alvarado, Ryan, Ludlam, Mary J. C., Stokoe, David, Gloor, Susan L., Vigers, Guy, Morales, Tony, Aliagas, Ignacio, Liu, Bonnie, Sideris, Steve, Hoeflich, Klaus P., Jaiswal, Bijay S., Seshagiri, Somasekar, Koeppen, Hartmut, Belvin, Marcia, Friedman, Lori S., Malek, Shiva
Published in Nature (London) (18.03.2010)
Published in Nature (London) (18.03.2010)
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Therapeutic Ligands Antagonize Estrogen Receptor Function by Impairing Its Mobility
Guan, Jane, Zhou, Wei, Hafner, Marc, Blake, Robert A., Chalouni, Cecile, Chen, Irene P., De Bruyn, Tom, Giltnane, Jennifer M., Hartman, Steven J., Heidersbach, Amy, Houtman, Rene, Ingalla, Ellen, Kategaya, Lorn, Kleinheinz, Tracy, Li, Jun, Martin, Scott E., Modrusan, Zora, Nannini, Michelle, Oeh, Jason, Ubhayakar, Savita, Wang, Xiaojing, Wertz, Ingrid E., Young, Amy, Yu, Mamie, Sampath, Deepak, Hager, Jeffrey H., Friedman, Lori S., Daemen, Anneleen, Metcalfe, Ciara
Published in Cell (08.08.2019)
Published in Cell (08.08.2019)
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First-in-human phase I study of pictilisib (GDC-0941), a potent pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor, in patients with advanced solid tumors
Sarker, Debashis, Ang, Joo Ern, Baird, Richard, Kristeleit, Rebecca, Shah, Krunal, Moreno, Victor, Clarke, Paul A, Raynaud, Florence I, Levy, Gallia, Ware, Joseph A, Mazina, Kathryn, Lin, Ray, Wu, Jenny, Fredrickson, Jill, Spoerke, Jill M, Lackner, Mark R, Yan, Yibing, Friedman, Lori S, Kaye, Stan B, Derynck, Mika K, Workman, Paul, de Bono, Johann S
Published in Clinical cancer research (01.01.2015)
Published in Clinical cancer research (01.01.2015)
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Ligand-Independent HER2/HER3/PI3K Complex Is Disrupted by Trastuzumab and Is Effectively Inhibited by the PI3K Inhibitor GDC-0941
Junttila, Teemu T., Akita, Robert W., Parsons, Kathryn, Fields, Carter, Lewis Phillips, Gail D., Friedman, Lori S., Sampath, Deepak, Sliwkowski, Mark X.
Published in Cancer cell (05.05.2009)
Published in Cancer cell (05.05.2009)
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Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers
Hatzivassiliou, Georgia, Haling, Jacob R., Chen, Huifen, Song, Kyung, Price, Steve, Heald, Robert, Hewitt, Joanne F. M., Zak, Mark, Peck, Ariana, Orr, Christine, Merchant, Mark, Hoeflich, Klaus P., Chan, Jocelyn, Luoh, Shiuh-Ming, Anderson, Daniel J., Ludlam, Mary J. C., Wiesmann, Christian, Ultsch, Mark, Friedman, Lori S., Malek, Shiva, Belvin, Marcia
Published in Nature (London) (12.09.2013)
Published in Nature (London) (12.09.2013)
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In vivo Antitumor Activity of MEK and Phosphatidylinositol 3-Kinase Inhibitors in Basal-Like Breast Cancer Models
HOEFLICH, Klaus P, O'BRIEN, Carol, WEI ZHOU, BERRY, Leanne, MURRAY, Lesley, AMLER, Lukas, BELVIN, Marcia, FRIEDMAN, Lori S, LACKNER, Mark R, BOYD, Zachary, CAVET, Guy, GUERRERO, Steve, JUNG, Kenneth, JANUARIO, Tom, SAVAGE, Heidi, PUNNOOSE, Elizabeth, TRUONG, Tom
Published in Clinical cancer research (15.07.2009)
Published in Clinical cancer research (15.07.2009)
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Intermittent Administration of MEK Inhibitor GDC-0973 plus PI3K Inhibitor GDC-0941 Triggers Robust Apoptosis and Tumor Growth Inhibition
HOEFLICH, Klaus P, MERCHANT, Mark, ENGST, Stefan, JOHNSTON, Stuart, FRIEDMAN, Lori S, BELVIN, Marcia, ORR, Christine, CHAN, Jocelyn, DOUG DEN OTTER, BERRY, Leanne, KASMAN, Ian, KOEPPEN, Hartmut, RICE, Ken, YANG, Nai-Ying
Published in Cancer research (Chicago, Ill.) (2012)
Published in Cancer research (Chicago, Ill.) (2012)
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GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer
Liang, Jun, Zbieg, Jason R., Blake, Robert A., Chang, Jae H., Daly, Stephen, DiPasquale, Antonio G., Friedman, Lori S., Gelzleichter, Thomas, Gill, Matthew, Giltnane, Jennifer M., Goodacre, Simon, Guan, Jane, Hartman, Steven J., Ingalla, Ellen Rei, Kategaya, Lorn, Kiefer, James R., Kleinheinz, Tracy, Labadie, Sharada S., Lai, Tommy, Li, Jun, Liao, Jiangpeng, Liu, Zhiguo, Mody, Vidhi, McLean, Neville, Metcalfe, Ciara, Nannini, Michelle A., Oeh, Jason, O’Rourke, Martin G., Ortwine, Daniel F., Ran, Yingqing, Ray, Nicholas C., Roussel, Fabien, Sambrone, Amy, Sampath, Deepak, Schutt, Leah K., Vinogradova, Maia, Wai, John, Wang, Tao, Wertz, Ingrid E., White, Jonathan R., Yeap, Siew Kuen, Young, Amy, Zhang, Birong, Zheng, Xiaoping, Zhou, Wei, Zhong, Yu, Wang, Xiaojing
Published in Journal of medicinal chemistry (26.08.2021)
Published in Journal of medicinal chemistry (26.08.2021)
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Predictive Biomarkers of Sensitivity to the Phosphatidylinositol 3' Kinase Inhibitor GDC-0941 in Breast Cancer Preclinical Models
O'BRIEN, Carol, WALLIN, Jeffrey J, BEIVIN, Marcia, FRIEDMAN, Lori S, LACKNER, Mark R, SAMPATH, Deepak, GUHATHAKURTA, Debraj, SAVAGE, Heidi, PUNNOOSE, Elizabeth A, GUAN, Jane, BERRY, Leanne, PRIOR, Wei Wei, AMLER, Lukas C
Published in Clinical cancer research (15.07.2010)
Published in Clinical cancer research (15.07.2010)
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The Identification of 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a Potent, Selective, Orally Bioavailable Inhibitor of Class I PI3 Kinase for the Treatment of Cancer
Folkes, Adrian J, Ahmadi, Khatereh, Alderton, Wendy K, Alix, Sonia, Baker, Stewart J, Box, Gary, Chuckowree, Irina S, Clarke, Paul A, Depledge, Paul, Eccles, Suzanne A, Friedman, Lori S, Hayes, Angela, Hancox, Timothy C, Kugendradas, Arumugam, Lensun, Letitia, Moore, Pauline, Olivero, Alan G, Pang, Jodie, Patel, Sonal, Pergl-Wilson, Giles H, Raynaud, Florence I, Robson, Anthony, Saghir, Nahid, Salphati, Laurent, Sohal, Sukhjit, Ultsch, Mark H, Valenti, Melanie, Wallweber, Heidi J.A, Wan, Nan Chi, Wiesmann, Christian, Workman, Paul, Zhyvoloup, Alexander, Zvelebil, Marketa J, Shuttleworth, Stephen J
Published in Journal of medicinal chemistry (25.09.2008)
Published in Journal of medicinal chemistry (25.09.2008)
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Targeting Activated Akt with GDC-0068, a Novel Selective Akt Inhibitor That Is Efficacious in Multiple Tumor Models
JIE LIN, SAMPATH, Deepak, LEE, Leslie B, RISOM, Tyler, GROSS, Stefan, LIEDERER, Bianca M, KOEPPEN, Hartmut, SKELTON, Nicholas J, WALLIN, Jeffrey J, BELVIN, Marcia, PUNNOOSE, Elizabeth, FRIEDMAN, Lori S, NANNINI, Michelle A, KUI LIN, LEE, Brian B, DEGTYAREV, Michael, OEH, Jason, SAVAGE, Heidi, ZHENGYU GUAN, HONG, Rebecca, KASSEES, Robert
Published in Clinical cancer research (01.04.2013)
Published in Clinical cancer research (01.04.2013)
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Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα
Hanan, Emily J., Braun, Marie-Gabrielle, Heald, Robert A., MacLeod, Calum, Chan, Connie, Clausen, Saundra, Edgar, Kyle A., Eigenbrot, Charles, Elliott, Richard, Endres, Nicholas, Friedman, Lori S., Gogol, Emily, Gu, Xiao-Hui, Thibodeau, Rebecca Hong, Jackson, Philip S., Kiefer, James R., Knight, Jamie D., Nannini, Michelle, Narukulla, Raman, Pace, Amanda, Pang, Jodie, Purkey, Hans E., Salphati, Laurent, Sampath, Deepak, Schmidt, Stephen, Sideris, Steve, Song, Kyung, Sujatha-Bhaskar, Swathi, Ultsch, Mark, Wallweber, Heidi, Xin, Jianfeng, Yeap, SiewKuen, Young, Amy, Zhong, Yu, Staben, Steven T.
Published in Journal of medicinal chemistry (22.12.2022)
Published in Journal of medicinal chemistry (22.12.2022)
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Targeting p21-activated kinase 1 (PAK1) to induce apoptosis of tumor cells
Ong, Christy C, Jubb, Adrian M, Haverty, Peter M, Zhou, Wei, Tran, Victoria, Truong, Tom, Turley, Helen, O'Brien, Tom, Vucic, Domagoj, Harris, Adrian L, Belvin, Marcia, Friedman, Lori S, Blackwood, Elizabeth M, Koeppen, Hartmut, Hoeflich, Klaus P
Published in Proceedings of the National Academy of Sciences - PNAS (26.04.2011)
Published in Proceedings of the National Academy of Sciences - PNAS (26.04.2011)
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Doubling Down on the PI3K-AKT-mTOR Pathway Enhances the Antitumor Efficacy of PARP Inhibitor in Triple Negative Breast Cancer Model beyond BRCA-ness
De, Pradip, Sun, Yuling, Carlson, Jennifer H, Friedman, Lori S, Leyland-Jones, Brian R, Dey, Nandini
Published in Neoplasia (New York, N.Y.) (2014)
Published in Neoplasia (New York, N.Y.) (2014)
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ERK inhibition overcomes acquired resistance to MEK inhibitors
Hatzivassiliou, Georgia, Liu, Bonnie, O'Brien, Carol, Spoerke, Jill M, Hoeflich, Klaus P, Haverty, Peter M, Soriano, Robert, Forrest, William F, Heldens, Sherry, Chen, Huifen, Toy, Karen, Ha, Connie, Zhou, Wei, Song, Kyung, Friedman, Lori S, Amler, Lukas C, Hampton, Garret M, Moffat, John, Belvin, Marcia, Lackner, Mark R
Published in Molecular cancer therapeutics (01.05.2012)
Published in Molecular cancer therapeutics (01.05.2012)
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Phosphoinositide 3-Kinase (PI3K) Pathway Alterations Are Associated with Histologic Subtypes and Are Predictive of Sensitivity to PI3K Inhibitors in Lung Cancer Preclinical Models
SPOERKE, Jill M, O'BRIEN, Carol, FRIEDMAN, Lori S, ROSS, Leanne, HAMPTON, Garret M, AMLER, Lukas C, SHAMES, David S, LACKNER, Mark R, HUW, Ling, KOEPPEN, Hartmut, FRIDLYAND, Jane, BRACHMANN, Rainer K, HAVERTY, Peter M, PANDITA, Ajay, MOHAN, Sankar, SAMPATH, Deepak
Published in Clinical cancer research (15.12.2012)
Published in Clinical cancer research (15.12.2012)
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Orally Bioavailable Small-Molecule CD73 Inhibitor (OP-5244) Reverses Immunosuppression through Blockade of Adenosine Production
Du, Xiaohui, Moore, Jared, Blank, Brian R, Eksterowicz, John, Sutimantanapi, Dena, Yuen, Natalie, Metzger, Todd, Chan, Brenda, Huang, Tom, Chen, Xi, Chen, Yuping, Duong, Frank, Kong, Wayne, Chang, Jae H, Sun, Jessica, Zavorotinskaya, Tatiana, Ye, Qiuping, Junttila, Melissa R, Ndubaku, Chudi, Friedman, Lori S, Fantin, Valeria R, Sun, Daqing
Published in Journal of medicinal chemistry (24.09.2020)
Published in Journal of medicinal chemistry (24.09.2020)
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Akt inhibition promotes autophagy and sensitizes PTEN-null tumors to lysosomotropic agents
Degtyarev, Michael, De Mazière, Ann, Orr, Christine, Lin, Jie, Lee, Brian B, Tien, Janet Y, Prior, Wei W, van Dijk, Suzanne, Wu, Hong, Gray, Daniel C, Davis, David P, Stern, Howard M, Murray, Lesley J, Hoeflich, Klaus P, Klumperman, Judith, Friedman, Lori S, Lin, Kui
Published in The Journal of cell biology (06.10.2008)
Published in The Journal of cell biology (06.10.2008)
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RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy
Song, Kyung W, Edgar, Kyle A, Hanan, Emily J, Hafner, Marc, Oeh, Jason, Merchant, Mark, Sampath, Deepak, Nannini, Michelle A, Hong, Rebecca, Phu, Lilian, Forrest, William F, Stawiski, Eric, Schmidt, Stephen, Endres, Nicholas, Guan, Jane, Wallin, Jeffrey J, Cheong, Jonathan, Plise, Emile G, Lewis Phillips, Gail D, Salphati, Laurent, Heffron, Timothy P, Olivero, Alan G, Malek, Shiva, Staben, Steven T, Kirkpatrick, Donald S, Dey, Anwesha, Friedman, Lori S
Published in Cancer discovery (01.01.2022)
Published in Cancer discovery (01.01.2022)
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