Zobrazeno 1 - 10
of 22
pro vyhledávání: ''
Autor:
Peter S. Hammerman, Jing Yuan, Lesley A. Mathews Griner, Peter Aspesi, Daniel J. McKay, Gwynn Pardee, Hui Qin Wang, Kelli-Ann Monaco, Ribo Guo, Kenneth Crawford, Stephania Widger, Darrin Stuart, Vesselina G. Cooke, Karen Bui, Felipa A. Mapa, Yuji Mishina, Mariela Jaskelioff, Jeffrey A. Engelman, Paul Fordjour, Emma Labrot, Giordano Caponigro, Stacy Higgins, Jessi Ambrose, John Fuller, Jinsheng Liang, John Green, Scott Delach
Publikováno v:
Clinical Cancer Research. 27:2061-2073
Purpose: Targeting RAF for antitumor therapy in RAS-mutant tumors holds promise. Herein, we describe in detail novel properties of the type II RAF inhibitor, LXH254. Experimental Design: LXH254 was profiled in biochemical, in vitro, and in vivo assay
Publikováno v:
Molecular Cancer Research. 18:835-846
Through the use of an unbiased, genome-scale CRISPR modifier screen, we identified NF1 suppression as a mechanism of resistance to EGFR inhibition in NRAS/KRAS/BRAFV600-wild-type colorectal cancer cells. Reduced NF1 expression permitted sustained sig
Autor:
Amit Aggarwal, Gregory P. Donoho, Gregory D. Plowman, Ramon V. Tiu, Robert D. Van Horn, Sheng Bin Peng, Youyan Zhang, Jason C. Ting, Ruslan D. Novosiadly, Yue Webster, Yung Mae M. Yao, Amelie Forest, Philip W. Iversen, Henry James Robert, Philip J. Ebert, Steven M. Bray
Publikováno v:
Clinical Cancer Research. 23:5547-5560
Purpose: To evaluate the antitumor efficacy of cetuximab in combination with LSN3074753, an analog of LY3009120 and pan-RAF inhibitor in 79 colorectal cancer patient-derived xenograft (PDX) models. Experimental Design: Seventy-nine well-characterized
Autor:
Ilaria Conti, Sheng-Bin Peng, James J. Starling, Igor Mochalkin, Henry James Robert, Sean Buchanan, Robert D. Van Horn, Lysiane Huber, Gregory D. Plowman, Swee Seong Wong, Youyan Zhang, Vipin Yadav, Yong Gang Yue, Shih-Hsun Chen, Tinggui Yin
Publikováno v:
Cancer Discovery. 6:300-315
We have identified previously undiscovered BRAF in-frame deletions near the αC-helix region of the kinase domain in pancreatic, lung, ovarian, and thyroid cancers. These deletions are mutually exclusive with KRAS mutations and occur in 4.21% of KRAS
Autor:
Lars D. Engstrom, Peter Olson, James G. Christensen, Lauren Hargis, Andrew Calinisan, David Briere, Matthew A. Marx, Ruth Aranda, Jill Hallin
Publikováno v:
Cancer Research. 80:LB-098
The ability to develop effective therapies for KRAS mutant cancers has remained elusive despite decades of research. MRTX849 was identified as a potent, selective, and covalent KRASG12C inhibitor presently under evaluation in clinical trials. MRTX849
Autor:
Daniel Gerlach, Thomas Gerstberger, Dirk Kessler, Tobias Wunberg, Jessica Teh, Francesca Trapani, Marco H. Hofmann, Christopher P. Vellano, Szu-Chin Fu, Mark Pearson, Joseph R. Marszalek, Heribert Arnhof, Timothy P. Heffernan, Norbert Kraut, Peter Ettmayer, Michael Gmachl, Christiane Kofink, Klaus Rumpel, Dana-Adriana Botesteanu, Darryl B. McConnell, Juergen Ramharter
Publikováno v:
Cancer Research. 80:1091-1091
KRAS is the most frequently mutated oncogene with high prevalence of alterations in pancreatic, colorectal, and non-small cell lung tumors. The alleviation of negative feedback control of KRAS activity upon downstream inhibition has limited the clini
Autor:
Andrew J. Dropsey, Jason Manro, Sheng-Bin Peng, Melinda D. Willard, Weihua Shen, Sajan Joseph, Eunice Yuen, Shripad V. Bhagwat, Baohui Zhao, Denis J. McCann, Shufen Cai, William T. McMillen, Lisa Kindler
Publikováno v:
Cancer Research. 80:5225-5225
The combination of BRAF and MEK inhibitors have been clinically studied, and three different combinations (dabrafenib plus trametinib, vemurafenib plus cobimetinib and encorafenib plus binimetinib) are approved by the FDA for treatment of melanoma pa
Publikováno v:
Molecular Cancer Research. 13:659-669
KRAS mutations are frequently detected in human colorectal cancer and contribute to de novo apoptosis resistance and ultimately therapeutic failure. To overcome KRAS-mediated apoptosis resistance, the irreversible proteasome inhibitor, carfilzomib, w
Autor:
Richard A. Scolyer, Adnan Nagrial, Georgina V. Long, Hamideh Shahheydari, Carina Fung, Suzanah C. Boyd, Jason R. Todd, Mal Irvine, Helen Rizos, Richard F. Kefford, Matteo S. Carlino
Publikováno v:
Clinical Cancer Research. 21:98-105
Background: MEK1 mutations in melanoma can confer resistance to BRAF inhibitors, although preexisting MEK1P124 mutations do not preclude clinical responses. We sought to determine whether recurrent, preexisting MEK1P124 mutations affected clinical ou
Autor:
Dong-Jun Bae, Joo-Yun Byun, Sang-Yeob Kim, Young-Gil Ahn, Kwee Hyun Suh, InHwan Bae, Young Hoon Kim
Publikováno v:
Cancer Research. 79:1305-1305
The mitogen-activated protein kinase (MAPK) pathway plays an important role for the survival and proliferation of tumor cells. For example, the activation of the MAPK pathway due to mutations in BRAF, NRAS and KRAS kinases is known to be the causes o