scholarly journals 0009 Peroxisome proliferator-activated receptor (PPAR)-gamma ligand enhances the growth inhibitory activity of tamoxifen in MCF-7 cells

The Breast ◽  
2009 ◽  
Vol 18 ◽  
pp. S21
Author(s):  
H. Youn ◽  
B. Lee ◽  
M. Park ◽  
J. Yoon ◽  
S. Jung
Keyword(s):  
Inhibitory Activity ◽  
Ppar Gamma ◽  
Peroxisome Proliferator ◽  
Peroxisome Proliferator Activated Receptor ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Mcf 7

Obtusifoliol related steroids from Euphorbia sogdiana with cell growth inhibitory activity and apoptotic effects on breast cancer cells (MCF-7 and MDA-MB231)

Steroids ◽  
2016 ◽  
Vol 115 ◽  
pp. 90-97 ◽  
Author(s):  
Mahmoud Aghaei ◽  
Zeinab Yazdiniapour ◽  
Mustafa Ghanadian ◽  
Behzad Zolfaghari ◽  
Virginia Lanzotti ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Growth ◽  
Cancer Cells ◽  
Inhibitory Activity ◽  
Breast Cancer Cells ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Apoptotic Effects ◽  
Mcf 7

Cationic liposomes as efficient nanocarriers for the drug delivery of an anticancer cholesterol-based ruthenium complex

2015 ◽  
Vol 3 (15) ◽  
pp. 3011-3023 ◽  
Author(s):  
Giuseppe Vitiello ◽  
Alessandra Luchini ◽  
Gerardino D'Errico ◽  
Rita Santamaria ◽  
Antonella Capuozzo ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Cancer Cells ◽  
Inhibitory Activity ◽  
Ruthenium Complex ◽  
Human Cancer ◽  
High Growth ◽  
Human Cancer Cells ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Mcf 7

Cationic nanovectors loaded with Ru-based nucleolipids exert a high growth-inhibitory activity against human cancer cells (MCF-7 (A), WiDr (B), and HeLa (C)).

Troglitazone enhances tamoxifen-induced growth inhibitory activity of MCF-7 cells

2008 ◽  
Vol 377 (1) ◽  
pp. 242-247 ◽  
Author(s):  
Hong-Nu Yu ◽  
Eun-Mi Noh ◽  
Young-Rae Lee ◽  
Si-Gyun Roh ◽  
Eun-Kyung Song ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Mcf 7

New pyrimidines and triazolopyrimidines as antiproliferative and antioxidants with cyclooxygenase-1/2 inhibitory potential

2019 ◽  
Vol 11 (13) ◽  
pp. 1583-1603
Author(s):  
Ashraf M Omar ◽  
Heba A Abd El Razik ◽  
Aly A Hazzaa ◽  
Maryam AZ El-Attar ◽  
Maha A El Demellawy ◽  
...  
Keyword(s):  
Free Radicals ◽  
Inhibitory Activity ◽  
Docking Studies ◽  
Cyclooxygenase 1 ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Cox 2 ◽  
Inhibitory Potential ◽  
Cox 1 ◽  
Mcf 7

Aim: Cyclooxygenase-2 (COX-2) inhibition and scavenging-free radicals are important targets in cancer treatment. Materials & methods: Sulfanylpyrimidines and triazolopyrimidines were synthesized and evaluated as anticancer and antioxidant COX-1/2 inhibitors. Results: Compound 7 showed the same growth inhibitory activity as 5-fluorouracil against MCF-7. Compound 6f displayed broad-spectrum anticancer activity against the four tested cancer cell lines. Compounds 5b, 6a, 6c, 6d and 8 were found to be more active antioxidants than trolox. Compounds 6a, 6c, 6f and 8 revealed high COX-2 inhibitory activity and selectivity, which was confirmed by docking studies. Conclusion: Compound 6f could be considered as promising anticancer and antioxidant structural lead with COX-2 inhibition that deserve further derivatization and investigation.

A New Triterpenoid Alkaloid from Buxus sempervirens

2011 ◽  
Vol 66 (10) ◽  
pp. 1076-1078 ◽  
Author(s):  
Yu-Xin Yan ◽  
Yun Sun ◽  
Jian-Chao Chen ◽  
Jia Su ◽  
Yan Li ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Spectral Data ◽  
Human Cell ◽  
Spectral Methods ◽  
Inhibitory Activity ◽  
Human Cell Lines ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Buxus Sempervirens ◽  
Mcf 7

A new triterpenoid alkaloid, 16-deacetoxy-hyrcamine (1), together with six analogs, was isolated from the leaves and stems of Buxus sempervirens. Their structures were elucidated based on spectral methods and by comparison of the spectral data with those reported previously. All isolated compounds were evaluated for their growth inhibitory activity against human cell lines HL-60, SMMC-7721, A-549,MCF-7, and SW480. Compounds 1 - 4 and 6 showed modest cytotoxic activity against A-549, MCF-7, and SW480.

scholarly journals Modifications on the Tetrahydroquinoline Scaffold Targeting a Phenylalanine Cluster on GPER as Antiproliferative Compounds against Renal, Liver and Pancreatic Cancer Cells

2021 ◽  
Vol 14 (1) ◽  
pp. 49
Author(s):  
David Méndez-Luna ◽  
Loreley Araceli Morelos-Garnica ◽  
Juan Benjamín García-Vázquez ◽  
Martiniano Bello ◽  
Itzia Irene Padilla-Martínez ◽  
...  
Keyword(s):  
Binding Site ◽  
Cell Lines ◽  
Cancer Cell ◽  
Inhibitory Activity ◽  
In Silico ◽  
Cancer Cell Lines ◽  
Pancreatic Cancer Cells ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
New Compounds

The implementation of chemo- and bioinformatics tools is a crucial step in the design of structure-based drugs, enabling the identification of more specific and effective molecules against cancer without side effects. In this study, three new compounds were designed and synthesized with suitable absorption, distribution, metabolism, excretion and toxicity (ADME-tox) properties and high affinity for the G protein-coupled estrogen receptor (GPER) binding site by in silico methods, which correlated with the growth inhibitory activity tested in a cluster of cancer cell lines. Docking and molecular dynamics (MD) simulations accompanied by a molecular mechanics/generalized Born surface area (MMGBSA) approach yielded the binding modes and energetic features of the proposed compounds on GPER. These in silico studies showed that the compounds reached the GPER binding site, establishing interactions with a phenylalanine cluster (F206, F208 and F278) required for GPER molecular recognition of its agonist and antagonist ligands. Finally, a 3-(4,5-dimethylthiazol-2-yl)2,5-diphenyltetrazolium bromide (MTT) assay showed growth inhibitory activity of compounds 4, 5 and 7 in three different cancer cell lines—MIA Paca-2, RCC4-VA and Hep G2—at micromolar concentrations. These new molecules with specific chemical modifications of the GPER pharmacophore open up the possibility of generating new compounds capable of reaching the GPER binding site with potential growth inhibitory activities against nonconventional GPER cell models.

scholarly journals PPAR-gamma induced AKT3 expression increases levels of mitochondrial biogenesis driving prostate cancer

Oncogene ◽  
2021 ◽  
Vol 40 (13) ◽  
pp. 2355-2366
Author(s):  
Laura C. A. Galbraith ◽  
Ernest Mui ◽  
Colin Nixon ◽  
Ann Hedley ◽  
David Strachan ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Mitochondrial Biogenesis ◽  
Nuclear Export ◽  
Epithelial To Mesenchymal Transition ◽  
Ppar Gamma ◽  
Peroxisome Proliferator ◽  
Serine Threonine Kinase ◽  
Peroxisome Proliferator Activated Receptor ◽  
Mesenchymal Transition ◽  
And Function

AbstractPeroxisome Proliferator-Activated Receptor Gamma (PPARG) is one of the three members of the PPAR family of transcription factors. Besides its roles in adipocyte differentiation and lipid metabolism, we recently demonstrated an association between PPARG and metastasis in prostate cancer. In this study a functional effect of PPARG on AKT serine/threonine kinase 3 (AKT3), which ultimately results in a more aggressive disease phenotype was identified. AKT3 has previously been shown to regulate PPARG co-activator 1 alpha (PGC1α) localisation and function through its action on chromosome maintenance region 1 (CRM1). AKT3 promotes PGC1α localisation to the nucleus through its inhibitory effects on CRM1, a known nuclear export protein. Collectively our results demonstrate how PPARG over-expression drives an increase in AKT3 levels, which in turn has the downstream effect of increasing PGC1α localisation within the nucleus, driving mitochondrial biogenesis. Furthermore, this increase in mitochondrial mass provides higher energetic output in the form of elevated ATP levels which may fuel the progression of the tumour cell through epithelial to mesenchymal transition (EMT) and ultimately metastasis.

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