VEGFR

Preclinical Characterization of XL092, a Novel Receptor Tyrosine Kinase Inhibitor of MET, VEGFR2, AXL, and MER

42 views | Jan 15 2024

XL092, a multi-receptor tyrosine kinase inhibitor, exhibits potent antitumor effects and immunomodulatory properties in preclinical models, supporting its potential for clinical evaluation, particularly in combination with immune checkpoint inhibitors. [Read the Full Post]

PP121, a dual inhibitor of tyrosine and phosphoinositide kinases, relieves airway hyperresponsiveness, mucus hypersecretion and inflammation in a murine asthma model

35 views | Jan 14 2024

PP121, a dual tyrosine and phosphoinositide kinase inhibitor, demonstrates promising anti-contractile and anti-inflammatory effects in asthma treatment, suggesting its potential as a novel therapeutic compound for managing the condition. [Read the Full Post]

Polypharmacologic Reprogramming of Tumor-Associated Macrophages toward an Inflammatory Phenotype

50 views | Jan 11 2024

This study's establishment of a physiologically relevant in vitro system for TAM polarization unveils BMS-794833 as a potent inhibitor, independent of primary targets but reliant on multiple signaling pathways, offering a promising strategy to reprogram TAMs and suppress cancer growth. [Read the Full Post]

Sulfatinib, a novel multi-targeted tyrosine kinase inhibitor of FGFR1, CSF1R, and VEGFR1-3, suppresses osteosarcoma proliferation and invasion via dual role in tumor cells and tumor microenvironment

46 views | Jan 05 2024

Sulfatinib demonstrates promise in inhibiting osteosarcoma growth while altering the tumor microenvironment towards an immune-activated state, offering potential for clinical translation. [Read the Full Post]

E7050 Suppresses the Growth of Multidrug-Resistant Human Uterine Sarcoma by Inhibiting Angiogenesis via Targeting of VEGFR2-Mediated Signaling Pathways

38 views | Dec 24 2023

E7050 demonstrates potent anti-tumor and anti-angiogenic effects by inhibiting VEGFR2 phosphorylation and downstream signaling pathways in endothelial cells, reducing neovessel formation in vitro and in vivo, and attenuating tumor growth and angiogenesis in a xenograft model, suggesting its promising potential as a therapeutic agent for cancer and angiogenesis-related disorders. [Read the Full Post]

Single-cell RNA sequencing identifies an Il1rn+/Trem1+ macrophage subpopulation as a cellular target for mitigating the progression of thoracic aortic aneurysm and dissection

39 views | Dec 08 2023

The study on thoracic aortic aneurysm and dissection (TAAD) utilizing single-cell RNA sequencing in a mouse model identified the Il1rn+/Trem1+ pro-inflammatory macrophage subpopulation as the predominant source of detrimental molecules, highlighting the potential of targeted therapy, specifically via Trem1 blockade, as a promising medical treatment for TAAD. [Read the Full Post]

Identification of potential RapJ hits as sporulation pathway inducer candidates in Bacillus coagulans via structure-based virtual screening and molecular dynamics simulation studies

55 views | Dec 01 2023

Computational analyses identified acarbose as a potential inhibitor of the RapJ enzyme, crucial for inducing the sporulation pathway in Bacillus coagulans, but experimental validation is necessary to confirm its effectiveness. [Read the Full Post]

NR4A1 as a potential therapeutic target in colon adenocarcinoma: a computational analysis of immune infiltration and drug response

18 views | Dec 01 2023

Targeting NR4A1 with OSI-930 may offer a promising therapeutic strategy for colon adenocarcinoma patients with high immune infiltration, pending rigorous clinical validation. [Read the Full Post]

Safety and tolerability of oral vorolanib for neovascular (wet) age-related macular degeneration: a phase I, open-label study

27 views | Oct 01 2023

The study demonstrated that oral vorolanib improved visual outcomes in participants with neovascular age-related macular degeneration (nAMD) while maintaining a manageable safety profile. [Read the Full Post]

Diazoxide improves muscle function in association with improved dyslipidemia and decreased muscle oxidative stress in streptozotocin-induced diabetic rats

27 views | Sep 27 2023

Diazoxide administration in diabetic rats improves muscle strength development, reduces fatigue, lowers cholesterol and triglyceride levels, and improves oxidative stress parameters, suggesting its potential as a therapeutic intervention for diabetes-related complications. [Read the Full Post]