Phase II study investigating the efficacy and safety of glesatinib (MGCD265) in patients with advanced NSCLC containing MET activating alterations

Authors: Hong, David S., Cappuzzo, Federico, Chul Cho, Byoung, Dowlati, Afshin, Hussein, Maen, Kim, Dong-Wan, Percent, Ivor, Christensen, James G., Morin, Josée, Potvin, Diane, Faltaos, Demiana, Tassell, Vanessa, Der-Torossian, Hirak, Chao, Richard

Source: In Lung Cancer April 2024 190

Adeno-to-squamous transition drives resistance to KRAS inhibition in LKB1 mutant lung cancer

Authors: Tong, Xinyuan, Patel, Ayushi S., Kim, Eejung, Li, Hongjun, Chen, Yueqing, Li, Shuai, Liu, Shengwu, Dilly, Julien, Kapner, Kevin S., Zhang, Ningxia, Xue, Yun, Hover, Laura, Mukhopadhyay, Suman, Sherman, Fiona, Myndzar, Khrystyna, Sahu, Priyanka, Gao, Yijun, Li, Fei, Li, Fuming, Fang, Zhaoyuan, Jin, Yujuan, Gao, Juntao, Shi, Minglei, Sinha, Satrajit, Chen, Luonan, Chen, Yang, Kheoh, Thian, Yang, Wenjing, Yanai, Itai, Moreira, Andre L., Velcheti, Vamsidhar, Neel, Benjamin G., Hu, Liang, Christensen, James G., Olson, Peter, Gao, Dong, Zhang, Michael Q., Aguirre, Andrew J., Wong, Kwok-Kin, Ji, Hongbin

Source: In Cancer Cell 11 March 2024 42(3):413-428

Design and evaluation of achiral, non-atropisomeric 4-(aminomethyl)phthalazin-1(2H)-one derivatives as novel PRMT5/MTA inhibitors

Authors: Smith, Christopher R., Aranda, Ruth, Christensen, James G., Engstrom, Lars D., Gunn, Robin J., Ivetac, Anthony, Ketcham, John M., Kuehler, Jon, David Lawson, J., Marx, Matthew A., Olson, Peter, Thomas, Nicole C., Wang, Xiaolun, Waters, Laura M., Kulyk, Svitlana

Source: In Bioorganic & Medicinal Chemistry 1 October 2022 71

First-in-Human Phase I/IB Dose-Finding Study of Adagrasib (MRTX849) in Patients With Advanced KRASG12C Solid Tumors (KRYSTAL-1)

Authors: Ou, Sai-Hong Ignatius, Jänne, Pasi A., Leal, Ticiana A., Rybkin, Igor I., Sabari, Joshua K., Barve, Minal A., Bazhenova, Lyudmila, Johnson, Melissa L., Velastegui, Karen L., Cilliers, Cornelius, Christensen, James G., Yan, Xiaohong, Chao, Richard C., Papadopoulos, Kyriakos P.

Source: Journal of clinical oncology. 40(23):2530-2538

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100168784072.0x000001&indx=1&recIds=ETOCvdc_100168784072.0x000001

Fragment optimization and elaboration strategies – the discovery of two lead series of PRMT5/MTA inhibitors from five fragment hitsElectronic supplementary information (ESI) available. See DOI: https://doi.org/10.1039/d2md00163b

Authors: Smith, Christopher R., Kulyk, Svitlana, Ahmad, Misbha Ud Din, Arkhipova, Valentina, Christensen, James G., Gunn, Robin J., Ivetac, Anthony, Ketcham, John M., Kuehler, Jon, Lawson, J. David, Thomas, Nicole C., Wang, Xiaolun, Marx, Matthew A.

Source: RSC medicinal chemistry. 13(12):1549-1564

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100168310453.0x000001&indx=1&recIds=ETOCvdc_100168310453.0x000001

Absorption, single-dose and steady-state metabolism, excretion, and pharmacokinetics of adagrasib, a KRAS^G12C inhibitor.

Authors: Rahbaek, Lisa, Cilliers, Cornelius, Wegerski, Christopher J., Nguyen, Natalie, Otten, Jennifer, Hargis, Lauren, Marx, Matthew A., Christensen, James G., Tran, Jonathan Q.

Source: Cancer Chemotherapy & Pharmacology; 2025, Vol. 95 Issue 1, p1-17, 17p

Sitravatinib in patients with solid tumors selected by molecular alterations: results from a Phase Ib study.

Authors: Bazhenova, Lyudmila, Kim, Dong-Wan, Cho, Byoung Chul, Goel, Sanjay, Heist, Rebecca, Werner, Theresa L, Eaton, Keith D, Wang, Judy S, Pant, Shubham, Adkins, Douglas R, Blakely, Collin M, Yan, Xiaohong, Neuteboom, Saskia, Christensen, James G, Chao, Richard, Bauer, Todd

Source: Future Oncology; 2024, Vol. 20 Issue 39, p3213-3227, 15p

Dose-escalation trial of the ALK, MET & ROS1 inhibitor, crizotinib, in patients with advanced cancer

Authors: Clark, Jeffrey W, Camidge, D Ross, Kwak, Eunice L, Maki, Robert G, Shapiro, Geoffrey I, Chen, Isan, Tan, Weiwei, Randolph, Sophia, Christensen, James G, Ozeck, Mark, Tang, Yiyun, Wilner, Keith D, Salgia, Ravi

Source: Future oncology. 16(1):4289-4301

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100186821270.0x000001&indx=1&recIds=ETOCvdc_100186821270.0x000001

A Transient Pseudosenescent Secretome Promotes Tumor Growth after Antiangiogenic Therapy Withdrawal

Authors: Mastri, Michalis, Tracz, Amanda, Lee, Christina R., Dolan, Melissa, Attwood, Kristopher, Christensen, James G., Liu, Song, Ebos, John M.L.

Source: In Cell Reports 26 December 2018 25(13):3706-3720

Mocetinostat for patients with previously treated, locally advanced/metastatic urothelial carcinoma and inactivating alterations of acetyltransferase genes

Authors: Grivas, Petros, Mortazavi, Amir, Picus, Joel, Hahn, Noah M., Milowsky, Matthew I., Hart, Lowell L., Alva, Ajjai, Bellmunt, Joaquim, Pal, Sumanta K., Bambury, Richard M., O'Donnell, Peter H., Gupta, Sumati, Guancial, Elizabeth A., Sonpavde, Guru P., Faltaos, Demiana, Potvin, Diane, Christensen, James G., Chao, Richard C., Rosenberg, Jonathan E.

Source: Cancer. 125(4):533-540

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100082854454.0x000001&indx=1&recIds=ETOCvdc_100082854454.0x000001

Discovery of Five SOS2 Fragment Hits with Binding Modes Determined by SOS2 X‑Ray Cocrystallography.

Authors: Smith, Christopher R., Chen, Dan, Christensen, James G., Coulombe, René, Féthière, James, Gunn, Robin J., Hollander, Johan, Jones, Benjamin, Ketcham, John M., Khare, Shilpi, Kuehler, Jon, Lawson, J. David, Marx, Matthew A., Olson, Peter, Pearson, Kelly E., Ren, Cynthia, Tsagris, Denise, Ulaganathan, Thirumalaiselvi, Van't Veer, Inge, Wang, Xiaolun

Source: Journal of Medicinal Chemistry; 1/11/2024, Vol. 67 Issue 1, p774-781, 8p

The class I/IV HDAC inhibitor mocetinostat increases tumor antigen presentation, decreases immune suppressive cell types and augments checkpoint inhibitor therapy

Authors: Briere, David, Sudhakar, Niranjan, Woods, David M., Hallin, Jill, Engstrom, Lars D., Aranda, Ruth, Chiang, Harrah, Sodré, Andressa L., Olson, Peter, Weber, Jeffrey S., Christensen, James G.

Source: Cancer immunology, immunotherapy. 67(3):381-392

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Intracranial Efficacy of Adagrasib in Patients From the KRYSTAL-1 Trial With KRAS G12C -Mutated Non–Small-Cell Lung Cancer Who Have Untreated CNS Metastases.

Authors: Negrao, Marcelo V., Spira, Alexander I., Heist, Rebecca S., Jänne, Pasi A., Pacheco, Jose M., Weiss, Jared, Gadgeel, Shirish M., Velastegui, Karen, Yang, Wenjing, Der-Torossian, Hirak, Christensen, James G., Sabari, Joshua K.

Source: Journal of Clinical Oncology; 10/1/2023, Vol. 41 Issue 28, p4472-4477, 8p

Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein

Authors: Ketcham, John M., Harwood, Stephen J., Aranda, Ruth, Aloiau, Athenea N., Bobek, Briana M., Briere, David M., Burns, Aaron C., Caddell Haatveit, Kersti, Calinisan, Andrew, Clarine, Jeffery, Elliott, Adam, Engstrom, Lars D., Gunn, Robin J., Ivetac, Anthony, Jones, Benjamin, Kuehler, Jon, Lawson, J. David, Nguyen, Natalie, Parker, Cody, Pearson, Kelly E., Rahbaek, Lisa, Saechao, Barbara, Wang, Xiaolun, Waters, Anna, Waters, Laura, Watkins, Ashlee H., Olson, Peter, Smith, Christopher R., Christensen, James G., Marx, Matthew A.

Source: Journal of Medicinal Chemistry; March 2024, Vol. 67 Issue: 6 p4936-4949, 14p

Synergistic inhibition of ovarian cancer cell growth by combining selective PI3K/mTOR and RAS/ERK pathway inhibitors

Authors: Sheppard, Karen E., Cullinane, Carleen, Hannan, Katherine M., Wall, Meaghan, Chan, Joanna, Barber, Frances, Foo, Jung, Cameron, Donald, Neilsen, Amelia, Ng, Pui, Ellul, Jason, Kleinschmidt, Margarete, Kinross, Kathryn M., Bowtell, David D., Christensen, James G., Hicks, Rodney J., Johnstone, Ricky W., McArthur, Grant A., Hannan, Ross D., Phillips, Wayne A., Pearson, Richard B.

Source: In European Journal of Cancer December 2013 49(18):3936-3944

Multiplexed deep sequencing analysis of ALK kinase domain identifies resistance mutations in relapsed patients following crizotinib treatment

Authors: Huang, Donghui, Kim, Dong-Wan, Kotsakis, Athanasios, Deng, Shibing, Lira, Paul, Ho, Steffan N., Lee, Nathan V., Vizcarra, Pamela, Cao, Joan Q., Christensen, James G., Kim, Tae Min, Sun, Jong-mu, Ahn, Jin Seok, Ahn, Myung-Ju, Park, Keunchil, Mao, Mao

Source: In Genomics September 2013 102(3):157-162

Metabolism, excretion and pharmacokinetics of [14C]crizotinib following oral administration to healthy subjects

Authors: Johnson, Theodore R., Tan, Weiwei, Goulet, Lance, Smith, Evan B., Yamazaki, Shinji, Walker, Gregory S., O'Gorman, Melissa T., Bedarida, Gabriella, Zou, Helen Y., Christensen, James G., Nguyen, Leslie N., Shen, Zhongzhou, Dalvie, Deepak, Bello, Akintunde, Smith, Bill J.

Source: Xenobiotica. 45(1):45-59

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100103788273.0x000001&indx=1&recIds=ETOCvdc_100103788273.0x000001

HGF/c-Met pathway is one of the mediators of sunitinib-induced tumor cell type-dependent metastasis

Authors: Shojaei, Farbod, Simmons, Brett H., Lee, Joseph H., Lappin, Patrick B., Christensen, James G.

Source: In Cancer Letters 1 July 2012 320(1):48-55

Pharmacokinetic/Pharmacodynamic Modeling of Crizotinib for Anaplastic Lymphoma Kinase Inhibition and Antitumor Efficacy in Human Tumor Xenograft Mouse Models

Authors: Yamazaki, Shinji ^*, Vicini, Paolo, Shen, Zhongzhou, Zou, Helen Y., Lee, Joseph, Li, Qiuhua, Christensen, James G., Smith, Bill J., Shetty, Bhasker

Source: In The Journal of Pharmacology and Experimental Therapeutics March 2012 340(3):549-557

Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth

Authors: Murray, Brion W., Guo, Chuangxing, Piraino, Joseph, Westwick, John K., Zhang, Cathy, Lamerdin, Jane, Dagostino, Eleanor, Knighton, Daniel, Loi, Cho-Ming, Zager, Michael, Kraynov, Eugenia, Popoff, Ian, Christensen, James G., Martinez, Ricardo, Kephart, Susan E., Marakovits, Joseph, Karlicek, Shannon, Bergqvist, Simon, Smeal, Tod, Caskey, C. Thomas

Source: Proceedings of the National Academy of Sciences of the United States of America, 2010 May . 107(20), 9446-9451.

Access URL: https://www.jstor.org/stable/25681612