Imidazopyridine-based kinase inhibitors as potential anticancer agents: A review

F Peytam, Z Emamgholipour, A Mousavi, M Moradi… - Bioorganic …, 2023 - Elsevier
Considering the fundamental role of protein kinases in the mechanism of protein
phosphorylation in critical cellular processes, their dysregulation, especially in cancers, has …

Small Molecule c-KIT Inhibitors for the Treatment of Gastrointestinal Stromal Tumors: A Review on Synthesis, Design Strategies, and Structure–Activity Relationship …

S Godesi, J Lee, H Nada, G Quan… - International journal of …, 2023 - mdpi.com
The proto-oncogenic protein, c-KIT, plays a crucial role in regulating cellular transformation
and differentiation processes, such as proliferation, survival, adhesion, and chemotaxis. The …

Overall survival of patients with KIT-mutant metastatic GIST in the era of multiple kinase inhibitor availability

V Haller, C Reiff, R Hamacher, K Kostbade… - Journal of cancer …, 2024 - Springer
Purpose The prognosis of patients with metastatic GIST and imatinib-sensitive primary
mutations has significantly improved. However, limited data are available to inform patients …

KIT/PDGFRA inhibitors for the treatment of gastrointestinal stromal tumors: getting to the gist of the problem

CM Cicala, I Olivares-Rivas… - Expert Opinion on …, 2024 - Taylor & Francis
Introduction Approximately 90% of gastrointestinal stromal tumors (GISTs) are driven by
activating mutations in receptor tyrosine-kinases KIT or PDGFRA. Despite the outstanding …

[PDF][PDF] anti-tumor effects of the novel KIT mutant inhibitor M4205 in patient-derived gastrointestinal stromal tumor (GIST) xenograft models

L De Sutter, A Wozniak, J Verreet, U Vanleeuw… - Cancer …, 2022 - lirias.kuleuven.be
Background: The majority of GIST are driven by constitutively activated KIT/PDGFRA kinases
and are susceptible to treatment with tyrosine kinase inhibitors. During treatment, most of …

Advances in Small-Molecule C-KIT/PDGFRα Inhibitors for the Treatment of Gastrointestinal Stromal Tumors

X Zheng, H Liang, Y Zhou, X Lu - Pharmaceutical Fronts, 2024 - thieme-connect.com
Stem cell factor receptor (C-KIT) or platelet-derived growth factor receptor α (PDGFRα) gene
mutations have been identified as oncogenic drivers for most gastrointestinal stromal tumors …

Antitumor Efficacy of the Novel KIT Inhibitor IDRX-42 (Formerly M4205) in Patient-and Cell Line–Derived Xenograft Models of Gastrointestinal Stromal Tumor (GIST)

L De Sutter, A Wozniak, J Verreet, U Vanleeuw… - Clinical Cancer …, 2023 - AACR
Purpose: The majority of gastrointestinal stromal tumors (GIST) are driven by constitutively
activated KIT/PDGFRA kinases and are susceptible to treatment with tyrosine kinase …

Research progress on drug treatment and drug resistance mechanism of gastrointestinal stromal tumors

Q ZHAO, M YANG, Y HU, Y SU… - Chinese Journal of …, 2024 - manu41.magtech.com.cn
Gastrointestinal stromal tumors (GIST) are the most common mesenchymal-derived tumors
of the gastrointestinal tract. Tyrosine kinase inhibitors (TKIs) are the cornerstone of GIST …

[PDF][PDF] Phase 1 Study of IDRX-42 in Patients With Advanced Gastrointestinal Stromal Tumors Resistant to Prior Systemic Therapy: Early Results

P Schöffski, M Heinrich, J Trent, C Serrano, S Bauer… - idrx.com
BACKGROUND RESULTS Patrick Schöffski1, Michael Heinrich2, Jonathan Trent3, César
Serrano4, Sebastian Bauer5, Margaret von Mehren6, George Demetri7, Nick Lydon7, Jaap …