A comprehensive review of small molecules targeting PI3K pathway: Exploring the structural development for the treatment of breast cancer

Bioorganic Chemistry, Год журнала: 2023, Номер 143, С. 107077 - 107077

Опубликована: Дек. 30, 2023

Язык: Английский

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An Overview of Cancer in Djibouti: Current Status, Therapeutic Approaches, and Promising Endeavors in Local Essential Oil Treatment

Pharmaceuticals, Год журнала: 2023, Номер 16(11), С. 1617 - 1617

Опубликована: Ноя. 16, 2023

Djibouti, a developing economy, grapples with significant socioeconomic obstacles and the prevalence of infectious pathologies, including certain forms neoplasms. These challenges are exacerbated by limited access to affordable medical technologies for diagnosis, coupled lack preventive interventions, particularly in disadvantaged areas. The attention devoted local phytotherapeutic treatments underscores uniqueness Djibouti’s flora, resulting from its distinctive geographical position. International focus specifically centers on harnessing this potential as valuable resource, emphasizing phytoconstituents used counter notably carcinomas. This comprehensive overview covers broad spectrum, commencing an examination current state knowledge, namely in-depth investigation oncological risk factors. Essential elements control subsequently studied, highlighting fundamental prerequisites effective management. significance dietary habits cancer prevention support is explored depth, while traditional methods examined, cultural indigenous essential oil therapies encouraging further research based promising results.

Язык: Английский

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Down-regulation of ESRP2 inhibits breast cancer cell proliferation via inhibiting cyclinD1

Scientific Reports, Год журнала: 2024, Номер 14(1)

Опубликована: Ноя. 18, 2024

Epithelial splicing regulatory protein 2 (ESRP2),an important alternative of mRNA, is reported to have a dual role in tumors, which can promote or inhibit the occurrence and development tumors. However, function mechanism ESRP2 breast cancer (BC) remain unclear. The distribution expression correlation between overall survival rate were detected by Cancer Genome Atlas (TCGA) database. Gene Ontology(GO)analysis, containing biological process, cellular components, molecular function, was utilized evaluate potential cancer. cell lines real-time quantitative PCR analysis (RT-qPCR) western blotting. Cell clone performed examine proliferation knockdown MCF-7 cells. cycle measured flow cytometry assays. synergistic effect with chemotherapeutic agents also determined MTT assay. Bioinformatics demonstrated that gene elevated cells its overexpression strongly correlated shorter survival. GO revealed related proliferation. mRNA lines, compared normal human line MCF-10 A. Dwon-regulation inhibited promoted sensitivity chemotherapy drug, Cisplatin(DDP) Paclitaxel (TAXOL), cells.Additionally, obstructed at G1 phase caused decrease cyclinD1 expression. These findings reveal highly expressed poor prognosis patients. arresting promoting drugs (DDP TAXOL)in may be required for regulation progression, as well critical target clinical treatment

Язык: Английский

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Identification of potential therapeutic dual inhibitors of EGFR/HER2 in breast cancer

European Journal of Medicinal Chemistry Reports, Год журнала: 2024, Номер 11, С. 100143 - 100143

Опубликована: Март 3, 2024

Breast cancer (BC) is the leading cause of death among women worldwide. According to Cancer Research Foundation (BCRF), 25% all cases BC are positive for human epidermal growth factor receptor 2 (HER2), which most aggressive phenotype five subtypes. Previous studies have reported that (EGFR) also overexpressed in HER2-positive BC, elevates disease severity. Based on these findings, present study aimed identify dual inhibitors EGFR and HER2 by employing chemometric modelling techniques. A dataset chemical molecules with affinity both was prepared literature review. The split into training test sets based inhibitory concentration (IC50) HER2.The set used generate two pharmacophore models, one each (n = 30, R2 value 0.82 RMSD 1.4, Δ cost 151.84, configuration 20.3) 0.84 1.0, 68.47, 22.2). developed models were validated using 214 201, andR2pred 0.73 0.70, HER2, respectively), decoy (decoys 104, actives 18), an external 20). robustness Fischer's randomization method (at 95% confidence) applicability domain analysis. screen Asinex library 575,302) identifying consensus hits against targets. Molecules predicted IC50 < 20 nM subsequently screened, their toxicity profiles evaluated ProTox II. interactions, ligand efficiency, binding affinities selected compounds assessed from docking scores molecular mechanics generalized Born surface area solvation (MMGBSA) energy. Hit selection finally achieved dynamics simulations OPLS4 force field Desmond. identified hit can serve as a reference developing future.

Язык: Английский

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Design, synthesis, and biological evaluation of cathepsin B cleavage albumin-binding SN38 prodrug in breast cancer

Bioorganic Chemistry, Год журнала: 2024, Номер 147, С. 107370 - 107370

Опубликована: Апрель 14, 2024

Язык: Английский

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