scholarly journals Chimeric molecules facilitate the degradation of androgen receptors and repress the growth of LNCaP cells

2008 ◽  
Vol 11 (1) ◽  
pp. 119-126 ◽  
Author(s):  
Yue-Qing Tang ◽  
Bang-Min Han ◽  
Xin-Quan Yao ◽  
Yan Hong ◽  
Yan Wang ◽  
...  
Keyword(s):  
Androgen Receptors ◽  
Lncap Cells ◽  
Chimeric Molecules

Anti‐androgenic effect of astaxanthin in LNCaP cells is mediated through the aryl hydrocarbon‐androgen receptors cross talk

2021 ◽  
Vol 45 (4) ◽  
Author(s):  
Nima Montazeri‐Najafabady ◽  
Nazanin Chatrabnous ◽  
Mohammad‐Reza Arabnezhad ◽  
Negar Azarpira
Keyword(s):  
Cross Talk ◽  
Androgen Receptors ◽  
Lncap Cells ◽  
Aryl Hydrocarbon ◽  
Androgenic Effect

Dehydroepiandrosterone Activates Mutant Androgen Receptors Expressed in the Androgen-Dependent Human Prostate Cancer Xenograft CWR22 and LNCaP Cells

1997 ◽  
Vol 11 (4) ◽  
pp. 450-459 ◽  
Author(s):  
Jiann-an Tan ◽  
Yousuf Sharief ◽  
Katherine G. Hamil ◽  
Christopher W. Gregory ◽  
De-Ying Zang ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptors ◽  
Human Prostate ◽  
Human Prostate Cancer ◽  
Lncap Cells

scholarly journals Kaempferol Promotes Apoptosis While Inhibiting Cell Proliferation via Androgen-Dependent Pathway and Suppressing Vasculogenic Mimicry and Invasion in Prostate Cancer

2019 ◽  
Vol 2019 ◽  
pp. 1-10 ◽  
Author(s):  
Jun Da ◽  
Mingxi Xu ◽  
Yiwei Wang ◽  
Wenfeng Li ◽  
Mujun Lu ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Androgen Receptors ◽  
Vasculogenic Mimicry ◽  
In Vitro Study ◽  
Luciferase Assay ◽  
Nuclear Accumulation ◽  
Dependent Manner ◽  
Lncap Cells ◽  
Dose Dependent

Kaempferol is a well-known natural flavonol reported to be a potential treatment for multiple cancers. In this study, we demonstrated that cell growth of androgen-sensitive LNCaP cells could be inhibited 33% by 5 μM kaempferol, around 60% by 10 μM kaempferol, and almost 100% by 15 μM kaempferol. Also, kaempferol showed relatively limited effect on PC-3 cells and nonmalignant RWPE-1 cells. In the presence of DHT, the IC50 for kaempferol was 28.8±1.5 μM in LNCaP cells, 58.3±3.5 μM in PC-3 cells, and 69.1±1.2 μM in RWPE-1 cells, respectively. Kaempferol promotes apoptosis of LNCaP cells in a dose-dependent manner in the presence of dihydrotestosterone (DHT). Then, luciferase assay data showed that kaempferol could inhibit the activation of androgen receptors induced by DHT significantly. The downstream targets of androgen receptors, such as PSA, TMPRSS2, and TMEPA1, were found decreased in the presence of kaempferol in qPCR data. It was then confirmed that the protein level of PSA was decreased. Kaempferol inhibits AR protein expression and nuclear accumulation. Kaempferol suppressed vasculogenic mimicry of PC-3 cells in an in vitro study. In conclusion, kaempferol is a promising therapeutic candidate for treatment of prostate cancer, where the androgen signaling pathway as well as vasculogenic mimicry are involved.

Anti-androgenic effect of 6-formylindolo[3,2-b]carbazole (FICZ) in LNCaP cells is mediated by the aryl hydrocarbon-androgen receptors cross-talk

Steroids ◽  
2020 ◽  
Vol 153 ◽  
pp. 108508 ◽  
Author(s):  
Mohammad-Reza Arabnezhad ◽  
Nima Montazeri-Najafabady ◽  
Nazanin Chatrabnous ◽  
Ali Ghafarian Bahreman ◽  
Afshin Mohammadi-Bardbori
Keyword(s):  
Cross Talk ◽  
Androgen Receptors ◽  
Lncap Cells ◽  
Aryl Hydrocarbon ◽  
Androgenic Effect

Design and synthesis of peptide-based chimeric molecules to induce degradation of the estrogen and androgen receptors

2020 ◽  
Vol 28 (15) ◽  
pp. 115595
Author(s):  
Hidetomo Yokoo ◽  
Nobumichi Ohoka ◽  
Mikihiko Naito ◽  
Yosuke Demizu
Keyword(s):  
Androgen Receptors ◽  
Design And Synthesis ◽  
Chimeric Molecules

267: Effects of Steroidal and Non-Steroidal Antiandrogens on Wild-Type and Mutant Androgen Receptors

2007 ◽  
Vol 177 (4S) ◽  
pp. 89-90
Author(s):  
Masayasu Urushibara ◽  
Yukio Kageyama ◽  
Junichiro Ishioka ◽  
Yotsuo Higashi ◽  
Shuntaro Hara ◽  
...  
Keyword(s):  
Androgen Receptors ◽  
Wild Type

Expression of Urokinase and Its Receptor in Invasive and Non-Invasive Prostate Cancer Cell Lines

1992 ◽  
Vol 68 (06) ◽  
pp. 662-666 ◽  
Author(s):  
W Hollas ◽  
N Hoosein ◽  
L W K Chung ◽  
A Mazar ◽  
J Henkin ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Steady State ◽  
Cell Surface ◽  
Cell Lines ◽  
Cancer Cell ◽  
Prostate Cancer Cell ◽  
Cancer Cell Lines ◽  
Lncap Cells ◽  
Prostate Cancer Cell Lines ◽  
Non Invasive

SummaryWe previously reported that extracellular matrix invasion by the prostate cancer cell lines, PC-3 and DU-145 was contingent on endogenous urokinase being bound to a specific cell surface receptor. The present study was undertaken to characterize the expression of both urokinase and its receptor in the non-invasive LNCaP and the invasive PC-3 and DU-145 prostate cells. Northern blotting indicated that the invasive PC-3 cells, which secreted 10 times more urokinase (680 ng/ml per 106 cells per 48 h) than DU-145 cells (63 ng/ml per 106 cells per 48 h), had the most abundant transcript for the plasminogen activator. This, at least, partly reflected a 3 fold amplification of the urokinase gene in the PC-3 cells. In contrast, urokinase-specific transcript could not be detected in the non-invasive LNCaP cells previously characterized as being negative for urokinase protein. Southern blotting indicated that this was not a consequence of deletion of the urokinase gene. Crosslinking of radiolabelled aminoterminal fragment of urokinase to the cell surface indicated the presence of a 51 kDa receptor in extracts of the invasive PC-3 and DU-145 cells but not in extracts of the non-invasive LNCaP cells. The amount of binding protein correlated well with binding capacities calculated by Scatchard analysis. In contrast, the steady state level of urokinase receptor transcript was a poor predictor of receptor display. PC-3 cells, which were equipped with 25,000 receptors per cell had 2.5 fold more steady state transcript than DU-145 cells which displayed 93,000 binding sites per cell.

ZUM WIRKUNGSMECHANISMUS VON AN FETEN ANTIMASKULIN WIRKSAMEN GESTAGENEN

1964 ◽  
Vol 45 (4_Suppl) ◽  
pp. S139-S153 ◽  
Author(s):  
K. Junkmann ◽  
F. Neumann
Keyword(s):  
Pituitary Gland ◽  
Mechanism Of Action ◽  
Androgen Receptors ◽  
Male Rat ◽  
Pregnant Rats ◽  
Target Organs ◽  
Causative Factors ◽  
Competitive Action ◽  
Androgenic Effect

ABSTRACT Experiments are described dealing with the mechanism of action of 6-chloro-Δ6-1,2α-methylene-17α-hydroxyprogesterone-acetate with regard to its anti-masculine effect on male rat foetuses, when administered to pregnant rats. It was shown that a marked direct anti-androgenic effect due to a competitive action on androgen receptors within the target organs, is probably the explanation of the mechanism of action. It was further shown that an oestrogenic effect or an appreciable inhibition of the pituitary gland respectively, can be ruled out as causative factors in the mechanism of action.

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