Mast cell activation induced by tamoxifen citrate via MRGPRX2 plays a potential adverse role in breast cancer treatment.

Breast cancer is the most common malignant tumor endangering women's life and health. Tamoxifen citrate (TAM) is the first-line drug of adjuvant endocrine therapy for estrogen receptor-positive (ER) breast cancer patients. Some sporadic cases have described rare adverse reactions of TAM with potentially life-threatening dermatological manifestations, which were associated with skin allergy.

Proguanil inhibits proliferation and migration in glioblastoma development through targeting CSF1R receptor.

Glioblastoma (GBM) is the most common and aggressive malignant tumor of the central nervous system, characterized by high morbidity and invasive potential, necessitating urgent development of novel therapeutic strategies. Studies have shown that colony stimulating factor-1 receptor (CSF1R) is abnormally expressed in a variety of solid tumors, which is closely related to the development of tumor cells. In this study, the CSF1R/cell membrane Chromatographic model was successfully constructed, and was used to screen active compounds targeting CSF1R from more than 60 compounds.

Cell membrane chromatography relative competitive method for the accurate determination of relative K values of drug-receptor interactions.

The specific binding of a drug to the receptor is a prerequisite for its action. The equilibrium dissociation constant (K) is an important parameter for measuring the strength of drug-receptor interactions. Cell membrane chromatography (CMC) is a powerful way to determine the K value; however, the common disadvantage is that the attenuation of biological activity with the analysis process leads to corresponding errors in comparing K values of a series of drugs.

Harringtonine metabolites: 5'-de-O-methylharringtonine and cephalotaxine, targeting spike protein and TMPRSS2 to double block membrane fusion of SARS-CoV-2 and its variants.

Membrane fusion is the main pathway for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) to invade host cells. Harringtonine (HT), derived from cephalotaxus fortunei Hook. f.

Pseudolaric Acid B Inhibits FLT4-induced Proliferation and Migration in Non-small Cell Lung Cancer.

Objectives: Non-Small Cell Lung Cancer (NSCLC) has attracted much attention on account of the high incidence and mortality of cancers. Vascular Endothelial Growth Factor Receptor 3 (VEGFR3/FLT4), which is a highly expressed receptor in NSCLC, greatly regulates cancer proliferation and migration. Pseudolaric Acid B (PAB) is a diterpenoid acid with antitumor activity isolated from This study aimed to explore the inhibitory effect of PAB targeting FLT4 in NSCLC.

In vitro pharmacokinetic behavior in lung of harringtonine, an antagonist of SARS-CoV-2 associated proteins: New insights of inhalation therapy for COVID-19.

Background: Recent studies have shown that harringtonine (HT) could specifically bind with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) spike (S) protein and host cell transmembrane serine protease 2 (TMPRSS2) to block membrane fusion, which is an effective antagonist for SARS-CoV-2.

Purpose: Our study focused on in-depth exploration of in vitro pharmacokinetic characteristics of HT in lung.

Methods: HPLC-fluorescence detection method was used to detect changes of HT content.

Dauricine Inhibits Non-small Cell Lung Cancer Development by Regulating PTEN/AKT/mTOR and Ras/MEK1/2/ERK1/2 Pathways in a FLT4-dependent Manner.

Objective: Non-small cell lung cancer (NSCLC) is still a solid tumor with high malignancy and poor prognosis. Vascular endothelial growth factor receptor 3 (FLT4, VEGFR3) is overexpressed in NSCLC cells, making it a potential target for NSCLC treatment. In this study, we aimed to explore the anti-cancer effects of dauricine on NSCLC cells and its mechanism targeting FLT4.

HPLC-fluorescence detection for stability of harringtonine, and identification of degradation products by UPLC-Q-TOF-MS.

Harringtonine (HT) is an anticancer alkaloid early extracted and isolated from cephalotaxus fortunei Hook. f., also has various pharmacological activities such as antiviral, antibacterial, antimalarial, anti-inflammatory, antioxidant, herbicidal and insecticidal.