Results 31 to 40 of about 681,398 (156)

Retinoid X receptor activation is essential for docosahexaenoic acid protection of retina photoreceptors

Journal of Lipid Research, 2013
We have established that docosahexaenoic acid (DHA), the major polyunsaturated fatty acid in the retina, promotes survival of rat retina photoreceptors during early development in vitro and upon oxidative stress by activating the ERK/MAPK signaling ...
Olga L. German, Sandra Monaco, Daniela L. Agnolazza, Nora P. Rotstein, Luis E. Politi   +4 more
doaj   +1 more source

TRK xDFG Mutations Trigger a Sensitivity Switch from Type I to II Kinase Inhibitors

, 2021
On-target resistance to next-generation TRK inhibitors in TRK fusion-positive cancers is largely uncharacterized. In patients with these tumors, we found that TRK xDFG mutations confer resistance to type I next-generation TRK inhibitors designed to ...
Toska, Eneda, Scaltriti, Maurizio, Rix, Uwe, Jagadeeshan, Sankar, Schram, Alison M., Vasan, Neil, Baldino, Laura, Kulick, Amanda, Kannan, Srinivasaraghavan, Novoplansky, Ofra, Gorelick, Alexander N., Wu, Fan, Verma, Chandra S., Berger, Michael F., de Stanchina, Elisa, Drilon, Alexander, Hyman, David M., Kannan, Ram, Misale, Sandra, Shifman, Sophie, Arruabarrena-Aristorena, Amaia, Lee, Ji Eun, Kittane, Srushti, Bardelli, Alberto, Liao, Yi, Ventura, Andrea, Won, Helen H., Taylor, Barry S., Hechtman, Jaclyn F., Cocco, Emiliano, Mussolin, Benedetta, Elkabets, Moshe, Cai, Yanyan, Arena, Sabrina   +33 more
core   +1 more source

Discovery, Optimization, and Evaluation of Novel Pyridin-2(1H)‑one Analogues as Potent TRK Inhibitors for Cancer Treatment

Tropomyosin receptor kinase (TRK) fusion, an oncogenic form of kinase with pan-tumor occurrence, is a clinically validated important antitumor target. In this study, we screened our in-house kinase inhibitor library against TRK and identified a promising
Mingyue Zheng (180908), Chunpu Li (1601443), Zichao Xu (625519), Renjie Zhang (1476898), Yinchun Ji (1601434), Mengke You (17797836), Yanyan Shen (7302266), Hong Liu (50694), Danyi Wang (10776731), Jing Ai (271316), Xia Peng (1601440)   +10 more
core   +8 more sources

Discovery and preclinical characterization of novel small molecule TRK and ROS1 tyrosine kinase inhibitors for the treatment of cancer and inflammation.

PLoS ONE, 2013
Receptor tyrosine kinases (RTKs), in response to their growth factor ligands, phosphorylate and activate downstream signals important for physiological development and pathological transformation.
Ramesh Narayanan, Muralimohan Yepuru, Christopher C Coss, Zhongzhi Wu, Matthew N Bauler, Christina M Barrett, Michael L Mohler, Yun Wang, Juhyun Kim, Linda M Snyder, Yali He, Nelson Levy, Duane D Miller, James T Dalton   +13 more
doaj   +1 more source

Development and validation of an LC-MS/MS method for monitoring larotrectinib, a tropomyosin-related kinase inhibitor, in mouse and human plasma and application to pharmacokinetic studies

Journal of Analytical Science and Technology, 2020
Larotrectinib is an orally administered drug and the first and only selective pan-tropomyosin receptor kinase (TRK) inhibitor in clinical development to treat cancer patients harboring a neurotrophic receptor tyrosine kinase gene fusion.
Yoon-Jee Chae, Yoo-Kyung Song, Song-Hee Chae, Min Ju Kim, Jong Soon Kang, Jae-Young Lee, Tae-Sung Koo, Kyeong-Ryoon Lee   +7 more
doaj   +1 more source

Abstract 4179: Potent and selective TRK inhibitor CH7057288

, 2017
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.
Kiyoshi Hasegawa, Toshiyuki Tsukaguchi, Hiroshi Sakamoto, Hiroshi Tanaka, Yoshiyuki Ono, Hitoshi Sase, Nobuhiro Oikawa, Toshiyuki Mio, Hiromi Tanimura, Masami Hasegawa   +9 more
core   +1 more source

Dramatic Responses Seen with TRK Inhibitor

, 2017
Presenting data on 50 of 55 patients with advanced TRK fusion–positive tumors, researchers reported that 76% of patients responded to the selective pan-TRK inhibitor larotrectinib, and 12% of patients experienced complete responses; 93% of responders ...

core   +1 more source

Complete response to larotrectinib treatment in a patient with papillary thyroid cancer harboring an ETV6‐NTRK3 gene fusion

Clinical Case Reports, 2021
Larotrectinib, a highly selective TRK inhibitor, was administered to a patient with rapidly progressing radioactive iodine‐refractory papillary NTRK3 fusion‐positive thyroid cancer.
Fabián Pitoia
doaj   +1 more source

Brief Report: Potent clinical and radiological response to larotrectinib in TRK fusion-driven high-grade glioma [PDF]

, 2018
Genes encoding TRK are oncogenic drivers in multiple tumour types including infantile fibrosarcoma, papillary thyroid cancer and high-grade gliomas (HGG). TRK fusions have a critical role in tumourigenesis in 40% of infant HGG.
Cohn, RJ ; https://orcid.org/, Kumar, A, Lau, LMS, Mayoh, C ; https://orcid.org/, Mayoh, C, Haber, M, Gifford, A, Lau, LMS ; https://orcid.org/, Mould, E, Tsoli, M, Tsoli, M ; https://orcid.org/, Marshall, GM, Khuong-Quang, DA, Gayevskiy, V, Rodriguez, M, Cowley, MJ ; https://orcid.org/, Cohn, RJ, Gifford, A ; https://orcid.org/, Ekert, PG, Pinese, M ; https://orcid.org/, Reynolds, M, Cox, MC, Wong, M, Cowley, MJ, Wong-Erasmus, Marie ; https://orcid.org/, Tyrrell, V, Ekert, PG ; https://orcid.org/, Ziegler, DS ; https://orcid.org/, Haber, M ; https://orcid.org/, Ziegler, DS, Pinese, M   +30 more
core   +1 more source

Oncogenic TRK fusions are amenable to inhibition in hematologic malignancies [PDF]

, 2018
Rearrangements involving the neurotrophic receptor kinase genes ( NTRK1, NTRK2, and NTRK3 ; hereafter referred to as TRK) produce oncogenic fusions in a wide variety of cancers in adults and children.
Scaltriti, Maurizio, Lillian Bitner, Chung, Stephen S, Justin Taylor, Young Rock Chung, Yoshimi, Akihide, Roshal, Mikhail, Ali, Siraj, Inoue, Daichi, Arcila, Maria, Ryma Benayed, David M. Hyman, Abdel-Wahab, Omar, Ebata, Kevin, Pavlick, Dean, Omar Abdel-Wahab, Mullaney, Kerry, Watts, Justin M, Hyman, David M, Diamond, Eli L, Mughal, Tariq I, Kerry Mullaney, Emiliano Cocco, Akihide Yoshimi, Lee A. Albacker, Tariq I. Mughal, Siraj Ali, Jaclyn F. Hechtman, Tuch, Brian B, Bitner, Lillian, Christina Marcelus, Justin M. Watts, Eli L. Diamond, Kevin Ebata, Mikhail Roshal, Stephen S. Chung, Brian B. Tuch, Nora Ku, Chung, Young Rock, Daichi Inoue, Taylor, Justin, Durham, Benjamin H, Hechtman, Jaclyn F, Maria Arcila, Park, Jae H, Benjamin H. Durham, Dean Pavlick, Benayed, Ryma, Jae H. Park, Maurizio Scaltriti, Ku, Nora, Cocco, Emiliano, Marcelus, Christina, Albacker, Lee A   +53 more
core   +1 more source