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Regulation of breast cancer resistance protein and P ‐glycoprotein by ezrin, radixin and moesin in lung, intestinal and renal cancer cell lines
ConclusionsOur findings indicate that regulation of BCRP and P ‐gp functions by ERM proteins is organ‐specific. Thus, if the appropriate ERM protein(s) are functionally suppressed, accumulation of BCRP or P‐gp substrates in lung, intestine or kidney cancer tissue might be specifically increased.
Source: Journal of Pharmacy and Pharmacology - February 13, 2020 Category: Drugs & Pharmacology Authors: Kentaro Yano, Chiaki Okabe, Kenta Fujii, Yuko Kato, Takuo Ogihara Tags: Research Paper Source Type: research

Enabling Combinatorial siRNA Delivery against Apoptosis-Related Proteins with Linoleic Acid and α-Linoleic Acid Substituted Low Molecular Weight Polyethylenimines
ConclusionsThis study yielded effective siRNA carriers for combinational delivery of siRNAs. Careful choice of siRNA combinations will be critical since targeting individual genes might alter the expression of other critical mediators.
Source: Pharmaceutical Research - February 2, 2020 Category: Drugs & Pharmacology Source Type: research

Silencing of nucleostemin by siRNA induces apoptosis in MCF-7 and MDA-MB-468 cell lines
This study was designed to better elucidate the association between NS depletion status and apoptosis induction of both MCF-7 and MDA-MB-468 cell lines. We examined the effects of nucleostemin-targeting siRNA on the expression of NS in MCF-7 and MDA-MB-468 human breast cancer cell lines by the Real Time polymerase chain reaction method. In addition, we investigated the correlation between knockdown of NS and viability rates and apoptosis induction in MCF-7 and MDA-MB-468 cell lines using the MTT assay and flow-cytometry technique, respectively. The NS-targeting siRNA inhibited the viability of cells in a dose- and time-dep...
Source: Iranian Journal of Pharmaceutical Research - January 31, 2020 Category: Drugs & Pharmacology Source Type: research

Regulation of breast cancer resistance protein and P ‐glycoprotein by ezrin, radixin and moesin in lung, intestinal and renal cancer cell lines
ConclusionsOur findings indicate that regulation of BCRP and P ‐gp functions by ERM proteins is organ‐specific. Thus, if the appropriate ERM protein(s) are functionally suppressed, accumulation of BCRP or P‐gp substrates in lung, intestine or kidney cancer tissue might be specifically increased.
Source: Journal of Pharmacy and Pharmacology - January 23, 2020 Category: Drugs & Pharmacology Authors: Kentaro Yano, Chiaki Okabe, Kenta Fujii, Yuko Kato, Takuo Ogihara Tags: Research Paper Source Type: research

HMGB3 small interfere RNA suppresses mammosphere formation of MDA-MB-231 cells by down-regulating expression of HIF1 α.
CONCLUSIONS: HMGB3 small interfering RNA suppressed the formation of mammosphere in MDA-MB-231 cells by downregulating the expression of HIF1α. PMID: 31773719 [PubMed - in process]
Source: European Review for Medical and Pharmacological Sciences - November 28, 2019 Category: Drugs & Pharmacology Tags: Eur Rev Med Pharmacol Sci Source Type: research

RU486 Metabolite Inhibits CCN1/Cyr61 Secretion by MDA-MB-231-Endothelial Adhesion
Successful adhesion of circulating tumor cells (CTCs) to microvascular endothelium of distant metastatic tissue is the key starting step of metastatic cascade that could be effectively chemoprevented as we demonstrated previously. Here, we hypothesize that the hetero-adhesion may produce secretory biomarkers that may be important for both premetastatic diagnosis and chemoprevention. We show that co-incubation of triple-negative breast cancer (TNBC) cell line MDA-MB-231 with human pulmonary microvascular endothelial monolayers (HPMEC) secretes Cyr61 (CCN1), primarily from MDA-MB-231. However, addition of metapristone (RU486...
Source: Frontiers in Pharmacology - November 19, 2019 Category: Drugs & Pharmacology Source Type: research

Knockdown of PTEN decreases expression of estrogen receptor β and tamoxifen sensitivity of human breast cancer cells
In this study we examined whether expression of ER β in turn might be affected by tumor suppressor PTEN, analyzed the effect of this interaction on tamoxifen response and the co-expression of both genes in human breast cancer samples. After siRNA-mediated PTEN knockdown, Western blot analysis revealed a reduction of ER β protein expression by 67.2% in MCF-7 cells and by 73.6% in T-47D cells (both p<0.01), results which could be verified on the mRNA level. In cells with normal PTEN and ER β status, after 6 days of treatment with 1 µM 4-OH tamoxifen, E2-driven proliferation was decreased by 64.5% in MCF-7 and by 57.7...
Source: Steroids - October 9, 2019 Category: Drugs & Pharmacology Source Type: research

Ouabain impairs cancer metabolism and activates AMPK-Src signaling pathway in human cancer cell lines.
In this study we showed that treatment with ouabain (25 nM) caused simultaneous activation of AMPK and Src signaling pathways in human lung cancer A549 cells and human breast cancer MCF7 cells. Cotreatment with AMPK inhibitor compound C or siRNA greatly abrogates ouabain-induced Src activation, whereas cotreatment with Src inhibitor PP2 has little effect on ouabain-induced AMPK activity, suggesting that AMPK served as an upstream regulator of the Src signaling pathway. On the other hand, ouabain treatment greatly depletes ATP production in A549 and MCF7 cells, and supplement of ATP (100 μM) blocked ouabain-induced AMP...
Source: Acta Pharmacologica Sinica - September 11, 2019 Category: Drugs & Pharmacology Authors: Shen JJ, Zhan YC, Li HY, Wang Z Tags: Acta Pharmacol Sin Source Type: research

Flavopereirine induces cell cycle arrest and apoptosis via the AKT/p38 MAPK/ERK1/2 signaling pathway in human breast cancer cells.
Abstract Breast cancer, which is the most frequently diagnosed cancer, is quite heterogeneous. For breast cancer subtypes lacking targeted therapies, it is vitally essential to find novel agents that prevent chemoresistance and metastatic relapse. Flavopereirine is a β-carboline alkaloid that has antiplasmodial activity, and its antiproliferative effect in different cancers remains unclear. The effect of flavopereirine on cell cycle arrest and apoptosis signaling in breast cancer cells was analyzed by flow cytometry. An inhibitor and siRNA were used to confirm the related signaling pathways by Western blot analys...
Source: European Journal of Pharmacology - September 9, 2019 Category: Drugs & Pharmacology Authors: Yeh HT, Tsai YS, Chen MS, Li YZ, Lin WC, Lee YR, Tseng YS, Sheu SM Tags: Eur J Pharmacol Source Type: research

Long non-coding RNA (lncRNA) small nucleolar RNA host gene 7 (SNHG7) promotes breast cancer progression by sponging miRNA-381.
CONCLUSIONS: SNHG7 was significantly upregulated in breast cancer and acted as an oncogene to promote breast cancer cell proliferation and invasion by directly sponging miRNA-381. PMID: 31378900 [PubMed - in process]
Source: European Review for Medical and Pharmacological Sciences - August 6, 2019 Category: Drugs & Pharmacology Tags: Eur Rev Med Pharmacol Sci Source Type: research

Combination of photodynamic therapy and gene silencing achieved through the hierarchical self-assembly of porphyrin-siRNA complexes
Publication date: Available online 31 July 2019Source: International Journal of PharmaceuticsAuthor(s): Nabila Laroui, Maëva Coste, Laure Lichon, Yannick Bessin, Magali Gary-Bobo, Geneviève Pratviel, Colin Bonduelle, Nadir Bettache, Sébastien UlrichAbstractIn this work, we implemented a supramolecular approach in order to combine photodynamic therapy (PDT) with gene therapy. We made use of a simple cationic guanidylated porphyrin (H2‑PG) with the hypothesis that porphyrin aggregates should be capable of complexing siRNA through multivalent interactions and thus contribute to its intracellular delivery, while remaining...
Source: International Journal of Pharmaceutics - August 1, 2019 Category: Drugs & Pharmacology Source Type: research

Magnetic nanocarriers for the specific delivery of siRNA: contribution of breast cancer cells active targeting for down-regulation efficiency
In conclusion, TS-MSN are promising nanocarriers for the specific and efficient delivery of siRNA to HER2-overexpressing breast cancer cells.Graphical abstract
Source: International Journal of Pharmaceutics - July 26, 2019 Category: Drugs & Pharmacology Source Type: research

Carbonic Anhydrase 1-Mediated Calcification Is Associated With Atherosclerosis, and Methazolamide Alleviates Its Pathogenesis
Vascular calcification is an important pathogenic process in atherosclerosis (AS); however, its immediate cause is unknown. Our previous study demonstrated that carbonic anhydrase 1 (CA1) stimulates ossification and calcification in ankylosing spondylitis and breast cancer. The current study investigated whether CA1 plays an important role in AS calcification and whether the CA inhibitor methazolamide (MTZ) has a therapeutic effect on AS. We successfully established an AS model by administration of a high-fat diet to ApoE-/- mice. The treated animals had significantly increased serum levels of high-density lipoprotein chol...
Source: Frontiers in Pharmacology - July 9, 2019 Category: Drugs & Pharmacology Source Type: research

Let-7 miRNA and CDK4 siRNA co-encapsulated in Herceptin-conjugated liposome for breast cancer stem cells
In conclusion, an efficient liposomal delivery system for the combination of miRNA and siRNA to target the BCSCs was developed and could be used as an efficacious therapeutic modality for breast cancer.Graphical AbstractHerceptin-conjugated cationic liposome can enhance the cellular uptake of let-7 miRNA and CDK4 siRNA toward the HER-2 expressing breast cancer stem cells.
Source: Asian Journal of Pharmaceutical Sciences - May 8, 2019 Category: Drugs & Pharmacology Source Type: research

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