Results 211 to 220 of about 107,195 (244)

The efficacy of larotrectinib (LOXO-101), a selective tropomyosin receptor kinase (TRK) inhibitor, in adult and pediatric TRK fusion cancers.

, 2017
LBA2501Background: Larotrectinib is the first selective small-molecule pan-TRK inhibitor. TRK fusions appear oncogenic independent of tumor lineage, are widely distributed across cancers, and affect all ages.
D. Hyman, T. Laetsch, S. Kummar, S. DuBois, A. Farago, A. Pappo, G. Demetri, W. El-Deiry, U. Lassen, A. Dowlati, M. Brose, V. Boni, B. Turpin, R. Nagasubramanian, S. Cruickshank, M. Cox, N. Ku, D. Hawkins, D. Hong, A. Drilon   +19 more
semanticscholar   +1 more source

Abstract PR07: A pediatric phase 1 study of larotrectinib, a highly selective inhibitor of the tropomyosin receptor kinase (TRK) family: An updated analysis

Oral Presentations - Proffered Abstracts, 2018
Background: NTRK gene fusions occur in a broad range of pediatric and adult malignancies at low frequencies, but are present in the vast majority of infantile fibrosarcomas.
B. Turpin, C. Albert, L. Mascarenhas, N. Federman, R. Nagasubramanian, M. Reynolds, Steven G. Smith, S. Cruickshank, M. Cox, A. Pappo, D. Hawkins, S. DuBois, T. Laetsch   +12 more
semanticscholar   +1 more source

Luteolin stimulates the NGF-induced neurite outgrowth in cultured PC12 cells through binding with NGF and potentiating its receptor signaling.

Food & Function, 2021
Luteolin, a flavonoid in fruits and vegetables, has neurotrophic functions without a well-characterized mechanism. Here, we hypothesize a direct interaction of luteolin with nerve growth factor (NGF); as such, the functionality of the NGF could be ...
Alex Xiong Gao, Tracy Chen-Xi Xia, Marvin Shing-Hung Mak, Kenneth Kin-Leung Kwan, Brody Zhong-Yu Zheng, Jian Xiao, T. Dong, K. Tsim   +7 more
semanticscholar   +1 more source

A pediatric phase I study of larotrectinib, a highly selective inhibitor of the tropomyosin receptor kinase (TRK) family.

, 2017
10510Background: Larotrectinib is the first selective small-molecule inhibitor of TRKA, B, and C in clinical development. Data from the adult phase I trial demonstrate prolonged responses in patients (pts) with TRK fusions and a favorable tolerability ...
T. Laetsch, S. DuBois, R. Nagasubramanian, B. Turpin, L. Mascarenhas, N. Federman, M. Reynolds, Steven G. Smith, S. Cruickshank, M. Cox, A. Pappo, D. Hawkins   +11 more
semanticscholar   +1 more source

First-in-Human Brain Imaging of [18F]TRACK, a PET tracer for Tropomyosin Receptor Kinases.

ACS Chemical Neuroscience, 2019
The tropomyosin receptor kinase TrkA/B/C family is responsible for human neuronal growth, survival, and differentiation from early nervous system development stages onward.
Justin J Bailey, L. Kaiser, S. Lindner, M. Wüst, A. Thiel, J. Soucy, P. Rosa-Neto, P. Scott, M. Unterrainer, D. Kaplan, C. Wängler, B. Wängler, P. Bartenstein, V. Bernard-Gauthier, R. Schirrmacher   +14 more
semanticscholar   +1 more source

A first-in-human study of LOXO-101, a highly selective inhibitor of the tropomyosin receptor kinase (TRK) family.

, 2015
TPS2624 Background: TheTRK family of neurotrophin receptors, TRKA, TRKB, and TRKC (encoded by NTRK1, NTRK2, and NTRK3 genes, respectively) and their neurotrophin ligands regulate growth, differentiation and survival of neurons.
H. Burris, M. Brose, A. Shaw, T. Bauer, A. Farago, R. Doebele, Steven M. L. Smith, Michèle Fernandes, S. Cruickshank, J. Low   +9 more
semanticscholar   +1 more source

Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain.

Journal of Medicinal Chemistry, 2018
Hormones of the neurotrophin family, nerve growth factor (NGF), brain derived neurotrophic factor (BDNF), neurotrophin 3 (NT3), and neurotrophin 4 (NT4), are known to activate the family of Tropomyosin receptor kinases (TrkA, TrkB, and TrkC).
S. Bagal, M. Andrews, B. Bechle, J. Bian, J. Bilsland, D. Blakemore, J. Braganza, P. Bungay, M. Corbett, C. Cronin, J. Cui, R. Dias, Neil J Flanagan, S. Greasley, R. Grimley, K. James, Eric Johnson, Linda Kitching, M. Kraus, Indrawan J. McAlpine, Asako Nagata, S. Ninkovic, Kiyoyuki Omoto, S. Scales, S. Skerratt, Jianmin Sun, M. Tran-Dube, Gareth J Waldron, Fen Wang, J. Warmus   +29 more
semanticscholar   +1 more source

Towards tropomyosin-related kinase B (TrkB) receptor ligands for brain imaging with PET: radiosynthesis and evaluation of 2-(4-[(18)F]fluorophenyl)-7,8-dihydroxy-4H-chromen-4-one and 2-(4-([N-methyl-(11)C]-dimethylamino)phenyl)-7,8-dihydroxy-4H-chromen-4-one.

Bioorganic & medicinal chemistry, 2014
The interaction of tropomyosin-related kinase B (TrkB) with the cognate ligand brain-derived neurotrophic factor (BDNF) mediates fundamental pathways in the development of the nervous system. TrkB signaling alterations are linked to numerous neurodegenerative diseases and conditions.
Vadim, Bernard-Gauthier, Mehdi, Boudjemeline, Pedro, Rosa-Neto, Alexander, Thiel, Ralf, Schirrmacher   +4 more
openaire   +1 more source

Toward Imaging Tropomyosin Receptor Kinase (Trk) with Positron Emission Tomography

PET and SPECT of Neurobiological Systems, 2020
R. Schirrmacher, V. Bernard-Gauthier, Carolin Jaworski, C. Wängler, B. Wängler, Justin J Bailey   +5 more
semanticscholar   +1 more source

Synthesis and Characterization of Sulfonamide-Imidazole Hybrids with In Vitro Antiproliferative Activity Against Anthracycline-Sensitive and Resistant H69 SCLC Cells.

ChemMedChem
A series of novel sulfonamide-imidazole hybrid derivatives was synthesized, and their antiproliferative properties were evaluated. The global challenge of cancer, highlighted by rising morbidity and mortality rates, is further intensified by the ...
Valdas Vainauskas, P. Kavaliauskas, Birutė Grybaitė, V. Petraitis, R. Petraitienė, R. Grigalevičiūtė, R. Prakapaitė, Waldo Acevedo, V. Mickevičius   +8 more
semanticscholar   +1 more source