Results 201 to 210 of about 2,911,119 (244)

Abstract C65: TRK kinase domain mutations that induce resistance to a pan-TRK inhibitor

Molecular Cancer Therapeutics, 2015
Abstract Background: Gene fusions involving members of the NTRK family have been identified in several types of cancer. The use of TRK inhibitors in vitro and in vivo have demonstrated activity against a number of different NTRK fusions in different tumor types and most recently in a patient with an NTRK1 gene fusion (Doebele et al ...
Adriana Estrada-Bernal, Anh T. Le, Brian Tuch, Tatiana Kutateladze, Robert C. Doebele   +4 more
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Abstract 1798: Identification of pan-Trk inhibitors for the treatment of Trk-driven cancers

Cancer Research, 2012
Abstract The Trk family of genes, which includes trkA/NTRK1, trkB/NTRK2 and trkC/NTRK3, encode the tyrosine kinase receptors for the neurotrophin family of nerve growth factors. Deregulated kinase activity of trk family members is associated with human cancer.
Karyn S. Bouhana, Anna M. Gomez, Taylor J. Alford, Richard Woessner, Ira von Carlowitz, Patrice A. Lee, Steven D. Andrews, Shannon L. Winski   +7 more
openaire   +1 more source

Abstract 4179: Potent and selective TRK inhibitor CH7057288

Cancer Research, 2017
Abstract TRK receptor tyrosine kinases are expressed as fusion proteins encoded by various fusion genes across a wide variety of cancer types, including lung and colorectal cancer. These fusion proteins have potent oncogenic activity and are thought to be an attractive therapeutic target.
Hiroshi Tanaka, Hitoshi Sase, Toshiyuki Tsukaguchi, Hiromi Tanimura, Masami Hasegawa, Kiyoshi Hasegawa, Yoshiyuki Ono, Nobuhiro Oikawa, Hiroshi Sakamoto, Toshiyuki Mio   +9 more
openaire   +1 more source

Trk kinase inhibitors as new treatments for cancer and pain

Expert Opinion on Therapeutic Patents, 2009
Tropomyosin-related kinases (Trks) are a family of receptor tyrosine kinases activated by neurotrophins. Trks play important roles in pain sensation as well as tumour cell growth and survival signaling. Thus, inhibitors of Trk receptor kinases might provide targeted treatments for pain and cancer.This paper reviews those patent applications since 2002 ...
Tao, Wang, Dingwei, Yu, Michelle L, Lamb
openaire   +2 more sources

Identification of 4-Aminopyrazolylpyrimidines as Potent Inhibitors of Trk Kinases

Journal of Medicinal Chemistry, 2008
The design, synthesis and biological evaluation of a series of 4-aminopyrazolylpyrimidines as potent Trk kinase inhibitors is reported. High-throughput screening identified a promising hit in the 4-aminopyrazolylpyrimidine chemotype. Initial optimization of the series led to more potent Trk inhibitors. Further optimization using two strategies resulted
Tao, Wang, Michelle L, Lamb, David A, Scott, Haixia, Wang, Michael H, Block, Paul D, Lyne, John W, Lee, Audrey M, Davies, Hai-Jun, Zhang, Yanyi, Zhu, Fei, Gu, Yongxin, Han, Bin, Wang, Peter J, Mohr, Robert J, Kaus, John A, Josey, Ethan, Hoffmann, Ken, Thress, Terry, Macintyre, Haiyun, Wang, Charles A, Omer, Dingwei, Yu   +21 more
openaire   +2 more sources

Discovery of quinazoline derivatives CZw-124 as a pan-TRK inhibitor with potent anticancer effects in vitro and in vivo.

European journal of medicinal chemistry, 2022
Tianxiao Wu, Qiaohua Qin, Ruicheng Lv, Nian Liu, Wenbo Yin, Chenzhou Hao, Yin Sun, Chu Zhang, Yixiang Sun, Dongmei Zhao, M. Cheng   +10 more
semanticscholar   +1 more source

The Trk tyrosine kinase inhibitor K252a regulates growth of lung adenocarcinomas

Molecular and Cellular Biochemistry, 2006
The neurotrophin family of growth factors and their receptors support the survival of several neuronal and non-neuronal cell populations during embryonic development and adult life. Neurotrophins are also involved in malignant transformation. To seek the role of neurotrophin signaling in human lung cancer we studied the expression of neurotrophin ...
PEREZ PINERA P, HERNANDEZ T, GARCIA SUAREZ O, DE CARLOS F, GERMANA', Antonino, DEL VALLE M, ASTUDILLO A, VEGA JA   +7 more
openaire   +3 more sources

TAS-119, a novel selective Aurora A and TRK inhibitor, exhibits antitumor efficacy in preclinical models with deregulated activation of the Myc, β-Catenin, and TRK pathways

Investigational new drugs, 2021
A. Miura, H. Sootome, N. Fujita, Takamasa Suzuki, H. Fukushima, S. Mizuarai, N. Masuko, Kimihiro Ito, A. Hashimoto, Y. Uto, T. Sugimoto, H. Takahashi, M. Mitsuya, H. Hirai   +13 more
semanticscholar   +1 more source

pyrizolo[1,5-a]pyrimidine derivatives of the Second-generation TRK inhibitor: Design, synthesis and biological evaluation.

Bioorganic & Medicinal Chemistry Letters, 2022
Yiqing Fan, Yongjie Zhang, Yan Liu, Hongyu Jiang, Ying Zhou, Chunlei Tang, W. Fan   +6 more
semanticscholar   +1 more source

Discovery of novel indazole derivatives as second-generation TRK inhibitors

European Journal of Medicinal Chemistry
NTRK gene fusion leads to the activation of downstream signaling pathways, which is a oncogenic driver in various cancers. NTRK fusion-positive cancers can be treated with the first-generation TRK inhibitors, larotrectinib and entrectinib. Unfortunately, the patients eventually face the dilemma of no drugs available as the emergence of certain ...
Qiaohua Qin, Shuyu Lu, Zhiqiang Guo, Zhuo Li, Qinglin Fu, Xin Wang, Tianxiao Wu, Yixiang Sun, Nian Liu, Haoyu zhang, Dongmei Zhao, Maosheng Cheng   +11 more
openaire   +2 more sources