scholarly journals The cytotoxic and pro-apoptotic activities of the novel fluoropyrimidine F10 towards prostate cancer cells are enhanced by Zn2+ -chelation and inhibiting the serine protease Omi/HtrA2

The Prostate ◽  
2014 ◽  
Vol 75 (4) ◽  
pp. 360-369 ◽  
Author(s):  
William H. Gmeiner ◽  
Olcay Boyacioglu ◽  
Christopher H. Stuart ◽  
Jamie Jennings-Gee ◽  
K.C. Balaji
Keyword(s):  
Prostate Cancer ◽  
Cancer Cells ◽  
Serine Protease ◽  
The Novel ◽  
Prostate Cancer Cells

scholarly journals The membrane-anchored serine protease, TMPRSS2, activates PAR-2 in prostate cancer cells

2005 ◽  
Vol 388 (3) ◽  
pp. 967-972 ◽  
Author(s):  
Susan WILSON ◽  
Brett GREER ◽  
John HOOPER ◽  
Andries ZIJLSTRA ◽  
Brian WALKER ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cancer Cells ◽  
Serine Protease ◽  
G Protein ◽  
Calcium Mobilization ◽  
Prostate Cancer Cells ◽  
Protease Domain ◽  
Serine Protease Domain ◽  
Pre Treatment ◽  
G Protein Coupled

TMPRSS2 is a type II transmembrane-bound serine protease that has gained interest owing to its highly localized expression in the prostate and its overexpression in neoplastic prostate epithelium. Once activated, the serine protease domain of TMPRSS2 is released from the cell surface into the extracellular space. PAR (protease-activated receptor)-2 belongs to a family of G-protein-coupled receptors (PAR-1–4) that are activated by specific serine proteases, which are expressed in many normal and malignant cell types. Previous in vitro studies on prostate cancer cells suggest a role for PAR-2 in prostate cancer metastasis. A polyclonal anti-human TMPRSS2 antibody was generated against the TMPRSS2 serine protease domain. The antibody showed specific reactivity with recombinant expressed TMPRSS2, and so was used to extract and purify the cleaved active TMPRSS2 protease from prostate cancer cells. Reverse transcriptase PCR and Western blot analysis were used to show the expression of both TMPRSS2 and PAR-2 in the androgen-dependent LNCaP prostate cancer cell line. Treatment of LNCaP cells with the cellular immunopurified TMPRSS2 protease induced a transient increase in intracellular calcium, which is indicative of G-protein-coupled-receptor activation. This calcium mobilization was inhibited by cellular pre-treatment with a specific PAR-2 antagonist, but not with a PAR-1 antagonist; inhibition of the protease activity also failed to mobilize calcium, suggesting that TMPRSS2 is capable of cleaving and thereby activating the PAR-2 receptor. The calcium mobilization was also inhibited by cellular pre-treatment with suramin or 2-APB (2-aminoethoxydiphenyl borate), indicating that a G-protein pathway is involved and that subsequent calcium release is mainly from intracellular stores. The present study describes how TMPRSS2 may contribute to prostate tumour metastasis via the activation of PAR-2.

scholarly journals The Novel PIM1 Inhibitor NMS-P645 Reverses PIM1-Dependent Effects on TMPRSS2/ERG Positive Prostate Cancer Cells And Shows Anti-Proliferative Activity in Combination with PI3K Inhibition

2017 ◽  
Vol 8 (1) ◽  
pp. 140-145 ◽  
Author(s):  
Luca Mologni ◽  
Vera Magistroni ◽  
Francesco Casuscelli ◽  
Marisa Montemartini ◽  
Carlo Gambacorti-Passerini
Keyword(s):  
Prostate Cancer ◽  
Cancer Cells ◽  
Proliferative Activity ◽  
The Novel ◽  
Prostate Cancer Cells ◽  
Pi3k Inhibition

scholarly journals miRNA-205 Nanoformulation Sensitizes Prostate Cancer Cells to Chemotherapy

Cancers ◽  
2018 ◽  
Vol 10 (9) ◽  
pp. 289 ◽  
Author(s):  
Prashanth Nagesh ◽  
Pallabita Chowdhury ◽  
Elham Hatami ◽  
Vijaya Boya ◽  
Vivek Kashyap ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cancer Cells ◽  
Confocal Imaging ◽  
The Novel ◽  
Prostate Cancer Cells ◽  
Study Results ◽  
Docetaxel Treatment ◽  
Iron Oxide Core ◽  
Poly Ethylene ◽  
Microrna Delivery

The therapeutic application of microRNA(s) in the field of cancer has generated significant attention in research. Previous studies have shown that miR-205 negatively regulates prostate cancer cell proliferation, metastasis, and drug resistance. However, the delivery of miR-205 is an unmet clinical need. Thus, the development of a viable nanoparticle platform to deliver miR-205 is highly sought. A novel magnetic nanoparticle (MNP)-based nanoplatform composed of an iron oxide core with poly(ethyleneimine)-poly(ethylene glycol) layer(s) was developed. An optimized nanoplatform composition was confirmed by examining the binding profiles of MNPs with miR-205 using agarose gel and fluorescence methods. The novel formulation was applied to prostate cancer cells for evaluating cellular uptake, miR-205 delivery, and anticancer, antimetastasis, and chemosensitization potentials against docetaxel treatment. The improved uptake and efficacy of formulations were studied with confocal imaging, flow cytometry, proliferation, clonogenicity, Western blot, q-RT-PCR, and chemosensitization assays. Our findings demonstrated that the miR-205 nanoplatform induces significant apoptosis and enhancing chemotherapeutic effects in prostate cancer cells. Overall, these study results provide a strong proof-of-concept for a novel nonviral-based nanoparticle protocol for effective microRNA delivery to prostate cancer cells.

scholarly journals MP51-09 THE NOVEL ROLE OF SPOP IN REGULATING TOPOISOMERASE 2A IN PROSTATE CANCER CELLS AS A POTENTIAL THERAPEUTIC MARKER FOR DNA REPAIR TARGETED THERAPY

2020 ◽  
Vol 203 ◽  
pp. e767
Author(s):  
Ryuta Watanabe* ◽  
Masashi Maekawa ◽  
Miki Hieda ◽  
Tomohiko Taguchi ◽  
Noriyoshi Miura ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Dna Repair ◽  
Targeted Therapy ◽  
Cancer Cells ◽  
The Novel ◽  
Prostate Cancer Cells ◽  
Topoisomerase 2A
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