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VPS34-IN1 induces apoptosis of ER  + breast cancer cells via activating PERK/ATF4/CHOP pathway
Biochem Pharmacol. 2023 Jun 6:115634. doi: 10.1016/j.bcp.2023.115634. Online ahead of print.ABSTRACTVPS34-IN1 is a specific selective inhibitor of Class III Phosphatidylinositol 3-kinase (PI3K) and has been shown to exhibit a significant antitumor effect in leukemia and liver cancer. In current study, we focused on the anticancer effect and potential mechanism of VPS34-IN1 in estrogen receptor positive (ER + ) breast cancer. Our results revealed that VPS34-IN1 inhibited the viability of ER + breast cancer cells in vitro and in vivo. Flow cytometry and western blot analyses showed that VPS34-IN1 treatment induced breast can...
Source: Biochemical Pharmacology - June 8, 2023 Category: Drugs & Pharmacology Authors: Qiuya Wu Duanfang Zhou Zhengze Shen Bo Chen Gang Wang Lihong Wu Limei Zhang Xiaoli Li Lie Yuan Yuanli Wu Na Qu Weiying Zhou Source Type: research

Acyl-CoA synthetase-4 mediates radioresistance of breast cancer cells by regulating FOXM1
Biochem Pharmacol. 2021 Aug 3:114718. doi: 10.1016/j.bcp.2021.114718. Online ahead of print.ABSTRACTThe development of radioresistance during radiotherapy is a major cause of tumor recurrence and metastasis. To provide new insights of the mechanisms underlying radioresistance, we established radioresistant cell lines derived from two different subtypes of breast cancer cells, HER2-positive SK-BR-3 and ER-positive MCF-7 breast cancer cells, by exposing cells to 48∼70 Gy of radiation delivered at 4-5 Gy twice weekly over 9∼10 months. The established radioresistant SK-BR-3 (SR) and MCF-7 (MR) cells were resistant not only...
Source: Biochemical Pharmacology - August 6, 2021 Category: Drugs & Pharmacology Authors: Yun-Suk Kwon Min-Gu Lee Junyoung Baek Nam-Yi Kim Hyunsoo Jang Soyoung Kim Source Type: research

Metformin-conjugated micellar system with intratumoral pH responsive de-shielding for co-delivery of doxorubicin and nucleic acid.
Abstract A novel PMet-P(cdmPEG2K) polymeric micellar carrier was developed for tumor-targeted co-delivery of DOX and nucleic acids (NA), based on polymetformin and a structure designed to lose the PEG shell in response to the acidic extracellular tumor environment. NA/DOX co-loaded micelleplexes exhibited enhanced inhibition of cell proliferation compared to DOX-loaded micelles, and displayed a higher level of cytotoxicity at an acidic pH (6.8) which mimicks the tumor microenvironment. The PMet-P(cdmPEG2K) micelles achieved significantly improved transfection with either a reporter plasmid or Cy3-siRNA, and enhanc...
Source: Biochemical Pharmacology - February 2, 2021 Category: Drugs & Pharmacology Authors: Liu Y, Sun J, Huang Y, Chen Y, Li J, Liang L, Xu J, Wan Z, Zhang B, Li Z, Li S Tags: Biochem Pharmacol Source Type: research

α-Linolenic acid inhibits the migration of human triple-negative breast cancer cells by attenuating twist1 expression and suppressing twist1-mediated epithelial-mesenchymal transition.
Abstract α-Linolenic acid (ALA), an essential fatty acid, has anticancer activity in breast cancer, but the mechanism of its effects in triple-negative breast cancer (TNBC) remains unclear. We investigated the effect of ALA on Twist1, which is required to initiate epithelial-mesenchymal transition (EMT) and promotes tumor metastasis, and Twist1-mediated migration in MDA-MB231, MDA-MB468 and Hs578T cells. Twist1 protein was constitutively expressed in these TNBC cells, particularly MDA-MB-231 cells. Treatment with 100 uM ALA and Twist1 siRNA markedly decreased the Twist1 protein level and cell migration. Moreover,...
Source: Biochemical Pharmacology - July 13, 2020 Category: Drugs & Pharmacology Authors: Wang SC, Sun HL, Hsu YH, Liu SH, Lii CK, Tsai CH, Liu KL, Huang CS, Li CC Tags: Biochem Pharmacol Source Type: research

Ribociclib mitigates cisplatin-associated kidney injury through retinoblastoma-1 dependent mechanisms.
Abstract Aberrant cell cycle activation is a hallmark of carcinogenesis. Recently three cell cycle targeting cyclin-dependent kinase 4/6 (CDK4/6) inhibitors have been approved for the treatment of metastatic breast cancer. CDK4/6 inhibitors suppress proliferation through inhibition of CDK4/6-dependent retinoblastoma-1 (Rb1) phosphorylation and inactivation, a key regulatory step in G1-to-S-phase transition. Interestingly, aberrant cell cycle activation is also linked with several non-oncological diseases including acute kidney injury (AKI). AKI is a common disorder caused by toxic, inflammatory, and ischemic damag...
Source: Biochemical Pharmacology - March 26, 2020 Category: Drugs & Pharmacology Authors: Young Kim J, Jayne LA, Bai Y, Feng MJHH, Clark MA, Chung S, W Christman J, Cianciolo RE, Singh Pabla N Tags: Biochem Pharmacol Source Type: research

Aryl hydrocarbon receptor (AHR) regulation of L-Type Amino Acid Transporter 1 (LAT-1) expression in MCF-7 and MDA-MB-231 breast cancer cells.
Abstract The aryl hydrocarbon receptor (AHR) is a ligand-activated transcription factor that is regulated by environmental toxicants that function as AHR agonists such as 2,3,7,8 tetrachlorodibenzo-p-dioxin (TCDD). L-Type Amino Acid Transporter 1 (LAT1) is a leucine transporter that is overexpressed in cancer. The regulation of LAT1 by AHR in MCF-7 and MDA-MB-231 breast cancer cells (BCCs) was investigated in this report. Ingenuity pathway analysis (IPA) revealed a significant association between TCDD-regulated genes (TRGs) and molecular transport. Overlapping the TCDD-RNA-Seq dataset obtained in this study with a...
Source: Biochemical Pharmacology - March 1, 2016 Category: Drugs & Pharmacology Authors: Tomblin JK, Arthur S, Primerano DA, Chaudhry AR, Fan J, Denvir J, Salisbury TB Tags: Biochem Pharmacol Source Type: research

Endogenous aryl hydrocarbon receptor promotes basal and inducible expression of tumor necrosis factor target genes in MCF-7 cancer cells.
The objective of this report was to identify AHR-dependent genes (ADGs) whose expression is regulated by AHR in the absence of toxicants. RNA-Seq analysis revealed that AHR regulated the expression of over 600 genes at an FDR<10% in MCF-7 breast cancer cells upon knockdown with short interfering RNA. Pathway analysis revealed that a significant number of ADGs were components of TCDD and tumor necrosis factor (TNF) pathways. We also demonstrated that siRNA knockdown of AHR modulated TNF induction of MNSOD and cytotoxicity in MCF-7 cells. Collectively, the major new findings of this report are: 1) endogenous AHR promotes ...
Source: Biochemical Pharmacology - June 24, 2014 Category: Drugs & Pharmacology Authors: Salisbury TB, Tomblin JK, Primerano DA, Boskovic G, Fan J, Mehmi I, Fletcher J, Santanam N, Hurn E, Morris GZ, Denvir J Tags: Biochem Pharmacol Source Type: research

A Tamoxifen Derivative, N,N-Diethyl-2-4-(phenylmethyl) phenoxy Ethanamine, Selectively Targets P-glycoprotein-Positive Multidrug Resistant Chinese Hamster Cells.
In this study we examined the effects of DPPE alone on the growth of drug sensitive and P-gp positive CHO cell line. Our results demonstrate DPPE is selectively toxic to P-gp positive cells and the sensitivity to DPPE alone correlated with the levels of P-gp expression. Moreover, in MDR cells, DPPE-induced apoptosis was significantly reduced with Bcl2 overexpression and in the presence of P-gp ATPase inhibitor, PSC833. Furthermore, knockdown of P-gp expression in MDR cells with P-gp-siRNA reversed DPPE sensitivity and increased their sensitivity to doxorubicin and taxol but not to cisplatin. The addition of DPPE to membran...
Source: Biochemical Pharmacology - May 9, 2014 Category: Drugs & Pharmacology Authors: Georges E, Lian J, Laberge R Tags: Biochem Pharmacol Source Type: research

p53 inactivation decreases dependence on estrogen/ERK signalling for proliferation but promotes EMT and susceptility to 3-bromopyruvate in ERα+ breast cancer MCF-7 cells.
Conclusions.- a) ERα(+) breast cancer cells dysfunctional for TP53 which proliferate irrespective of low estrogen and chemical MEK inhibition are likely to increase metabolic consumption becoming increasingly susceptible to 3-BrPA; b) targeting the pyruvate pathway may improve response to endocrine therapy in ERα(+) breast cancer with p53 dysfunction. PMID: 24486524 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - January 28, 2014 Category: Drugs & Pharmacology Authors: Rieber M, Strasberg-Rieber M Tags: Biochem Pharmacol Source Type: research

Identification of upregulated phosphoinositide 3-kinase γ as a target to suppress breast cancer cell migration and invasion.
Abstract Metastasis is the major cause of breast cancer mortality. We recently reported that aberrant G-protein coupled receptor (GPCR) signaling promotes breast cancer metastasis by enhancing cancer cell migration and invasion. Phosphatidylinositol 3-kinase γ (PI3Kγ) is specifically activated by GPCRs. The goal of the present study was to determine the role of PI3Kγ in breast cancer cell migration and invasion. Immunohistochemical staining showed that the expression of PI3Kγ protein was significantly increased in invasive human breast carcinoma when compared to adjacent benign breast tissue or ductal carcinom...
Source: Biochemical Pharmacology - May 15, 2013 Category: Drugs & Pharmacology Authors: Xie Y, Abel PW, Kirui JK, Deng C, Sharma P, Wolff DW, Toews ML, Tu Y Tags: Biochem Pharmacol Source Type: research

Saxifragifolin D induces the interplay between apoptosis and autophagy in breast cancer cells through ROS-dependent endoplasmic reticulum stress.
In conclusion, SD inhibits breast cancer cell growth and induces interplay between apoptosis and autophagy through ROS-mediated endoplasmic reticulum stress. It will provide molecular bases for developing SD into a drug candidate for the treatment of breast cancer. PMID: 23348250 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - January 21, 2013 Category: Drugs & Pharmacology Authors: Shi JM, Bai LL, Zhang DM, Yiu A, Yin ZQ, Han WL, Liu JS, Li Y, Fu DY, Ye WC Tags: Biochem Pharmacol Source Type: research