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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
Autor:
Tonghui Ma, Yanling Niu, Chengyun Geng, Sheng Yang, Xiaoyan Zhang, Xiaohui He, Kan Liu, Xin Zhang
Publikováno v:
Cancer Research. 81:1199-1199
Introduction: Although the contribution of mosaicism to tumorigenesis emerges during embryonic development, it is a very rare phenomenon in tumor patients. Only a few mosaic RAS mutations have been identified, such as NRAS G12D, NRAS G12S, KRAS G12D.
Publikováno v:
Cancer Research. 81:1103-1103
Background: Since the discovery of the oncogenic mutation B-Raf proto-oncogene, serine threonine kinase (BRAF) V600E, dabrafenib and trametinib (DT) combination therapies have been shown to have great anti-tumor activities against V600E-mutated non-s
Publikováno v:
Cancer Research. 80:1453-1453
Ras proteins (HRAS, KRAS, and NRAS) are small GTPases that function as molecular switches by alternating between inactive GDP-bound and active GTP-bound states. Ras-GTP activates downstream pathways, including MAPK, by binding to Raf kinase and phosp
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
Autor:
Katherine Galvin, Shuntarou Tsuchiya, Jouhara Chouitar, Sei Yoshida, Tomoyasu Ishikawa, Jill Donelan, Elizabeth Carideo, Masanori Okaniwa, Takeo Arita, Akito Nakamura
Publikováno v:
Cancer Research. 73:7043-7055
The mitogen-activated protein kinase (MAPK) pathway is particularly important for the survival and proliferation of melanoma cells. Somatic mutations in BRAF and NRAS are frequently observed in melanoma. Recently, the BRAF inhibitors vemurafenib and
Abstract 1841: Integrative analysis of resistance to BRAF-targeted therapies in lung adenocarcinomas
Autor:
Pierre Saintingy, Solène Marteau, Anne Pradines, Karen Howarth, Emma Green, Aurélie Swalduz, Gilles Clapisson, Jean-Yves Blay, Etienne Brain, Etienne Giroux Leprieur, Frank de Kievit, C. Raynaud, Virginie Avrillon, Virginie Westeel, Isabelle Monnet, Xavier Quantin, Nathalie Hoog-Labouret, Julien Mazieres, Claire Tissot, Séverine Martinez, Radj Gervais, Clive Morris, Celine Mahier, Y. Loriot, Washington René Chumbi Flores, Sandra Ortiz-Cuaran, Séverine Neymarc, Nathalie Girerd-Chambaz, Maurice Pérol, Christelle Clément Duchene
Publikováno v:
Cancer Research. 78:1841-1841
Background: BRAF mutations occur in 2 to 3% of patients (pts) with non-small cell lung cancer (NSCLC). In these pts vemurafenib, a selective oral BRAF inhibitor is associated with a response rate (RR) of 42%, rising to 64% for combination treatment w
Autor:
Neal Rosen, Amy Allen, Christine A. Pratilas, David J. Pisapia, Barry S. Taylor, Jiawan Wang, Alice Can Ran Qin, Zhan Yao, Philip Jonsson
Publikováno v:
Molecular Cancer Therapeutics. 17:A129-A129
BRAF V600E drives tumors by hyperactivating ERK signaling, is activated in a RAS-independent manner, and signals as a monomer. Selective inhibitors of RAF potently inhibit BRAF V600E and downstream ERK signaling, and have been associated with impress
Autor:
Helen Mason, Simon Scrace, Richard Testar, Julie Rainard, Fatima Talab, Ryaka Poonawala, Philippa Smith, Harriet Brooke, Sarah Frith, Jonathan Ahmet, Jonathan Hall, David Sorrell, Jon Moore, Caroline Phillips, Dennis France, Matilda Bingham, Richard Armer
Publikováno v:
Cancer Research. 77:5160-5160
REDX05358 has been identified as a novel, highly selective and potent next generation pan RAF inhibitor with improved therapeutic potential and predicted safety profile. Aberrant signalling via the MAPK pathway is commonly seen in cancer. RAF inhibit
Autor:
Ahmed A. Samatar
Publikováno v:
Molecular Cancer Research. 12:IA06-IA06
The RAS /RAF /MEK / ERK signal transduction pathway is frequently activated in several human cancers, due to a gain of function mutations in KRAS, NRAS, or BRAF. Because of the high frequency of activating mutations, this pathway has become a focus f