[HTML][HTML] Recent progress on vascular endothelial growth factor receptor inhibitors with dual targeting capabilities for tumor therapy

Y Liu, Y Li, Y Wang, C Lin, D Zhang, J Chen… - Journal of Hematology & …, 2022 - Springer
Vascular endothelial growth factor receptors (VEGFRs) are a family of receptor protein
tyrosine kinases that play an important role in the regulation of tumor-induced angiogenesis …

New treatment strategies for advanced-stage gastrointestinal stromal tumours

LR Klug, HM Khosroyani, JD Kent… - Nature reviews Clinical …, 2022 - nature.com
When gastrointestinal stromal tumour (GIST), the most common form of sarcoma, was first
recognized as a distinct pathological entity in the 1990s, patients with advanced-stage …

[HTML][HTML] NTRK fusion in non-small cell lung cancer: diagnosis, therapy, and TRK inhibitor resistance

F Liu, Y Wei, H Zhang, J Jiang, P Zhang… - Frontiers in oncology, 2022 - frontiersin.org
Neurotrophic tropomyosin receptor kinase (NTRK) gene fusion has been identified as an
oncogenic driver of various solid tumors, and it is rare in non-smalll cell lung cancer …

Targeting gatekeeper mutations for kinase drug discovery

Y Zhou, S Xiang, F Yang, X Lu - Journal of medicinal chemistry, 2022 - ACS Publications
Clinically acquired resistance is a major challenge in cancer therapies with small-molecule
kinase inhibitors (SMKIs). Gatekeeper mutations in the ATP-binding pocket of kinases are …

Recent advances in the discovery of tropomyosin receptor kinases TRKs inhibitors: a mini review

HB El-Nassan, MA Al-Qadhi - European journal of medicinal chemistry, 2023 - Elsevier
The tropomyosin receptor tyrosine kinases (TRKs) control the cell proliferation mainly in the
nervous system and are encoded by NTRK genes. Fusion and mutation of NTRK genes …

[HTML][HTML] Clinical relevance of targeted therapy and immune-checkpoint inhibition in lung cancer

GM Leone, S Candido, A Lavoro, S Vivarelli, G Gattuso… - Pharmaceutics, 2023 - mdpi.com
Lung cancer (LC) represents the second most diagnosed tumor and the malignancy with the
highest mortality rate. In recent years, tremendous progress has been made in the treatment …

Discovery of the first highly selective and broadly effective macrocycle-based type II TRK inhibitors that overcome clinically acquired resistance

Z Wang, J Wang, Y Wang, S Xiang… - Journal of Medicinal …, 2022 - ACS Publications
Tropomyosin receptor kinase (TRK) secondary mutations mediating acquired resistance,
especially at the solvent-front (SF) and the DFG motif, represent an unmet clinical need …

[HTML][HTML] Generating in vitro models of NTRK-fusion mesenchymal neoplasia as tools for investigating kinase oncogenic activation and response to targeted therapy

F Vanoli, L Herviou, Y Tsuda, P Sung, Z Xie… - Oncogenesis, 2023 - nature.com
The discovery of neurotrophic tyrosine receptor kinase (NTRK) gene fusions as pan-tumor
oncogenic drivers has led to new personalized therapies in oncology. Recent studies …

[HTML][HTML] CRTC3, a sensor and key regulator for melanogenesis, as a tunable therapeutic target for pigmentary disorders

H Yoo, HR Lee, KH Kim, MA Kim, S Bang, YH Kang… - Theranostics, 2021 - ncbi.nlm.nih.gov
Background: Although CREB phosphorylation is known to be essential in UVB/cAMP-
stimulated melanogenesis, CREB null mice did not show identifiable pigmentation …

Switch type I to type II TRK inhibitors for combating clinical resistance induced by xDFG mutation for cancer therapy

S Xiang, J Wang, H Huang, Z Wang, X Song… - European Journal of …, 2023 - Elsevier
TRK xDFG mutation-induced acquired resistance of 1 st generation inhibitors larotrectinib
and entrectinib remains an unmet clinical need. Here we report a series of 6-(pyrrolidin-1-yl) …