2‐D gel electrophoresis‐based proteomic analysis reveals that ormeloxifen induces G0–G1 growth arrest and ERK‐mediated apoptosis in chronic myeloid leukemia cells K562

Pal, Pooja; Kanaujiya, Jitendra Kumar; Lochab, Savita; Tripathi, Shashi B.; Bhatt, Madan Lal Brahma; Singh, Pradhyumna Kumar; Sanyal, Sabyasachi; Trivedi, Arun Kumar

doi:10.1002/pmic.201000720

Cited by 36 publications

(36 citation statements)

References 42 publications

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“…Sustained ERK phosphorylation may act as a compensatory mechanism, mediating the block in G 0 /G 1 progression in MCF-7 cells treated with BAD-NE. Accordingly, sustained ERK activation can lead to cell cycle arrest at G 0 /G 1 or G 2 /M [109–115]. More recently, the nuclear translocation of ERK1/2 has been suggested to be an anticancer drug target [116].…”

Section: Resultsmentioning

confidence: 99%

H2S-releasing nanoemulsions: a new formulation to inhibit tumor cells proliferation and improve tissue repair

et al. 2016

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The improvement of solubility and/or dissolution rate of poorly soluble natural compounds is an ideal strategy to make them optimal candidates as new potential drugs. Accordingly, the allyl sulfur compounds and omega-3 fatty acids are natural hydrophobic compounds that exhibit two important combined properties: cardiovascular protection and antitumor activity. Here, we have synthesized and characterized a novel formulation of diallyl disulfide (DADS) and α-linolenic acid (ALA) as protein-nanoemulsions (BAD-NEs), using ultrasounds. BAD-NEs are stable over time at room temperature and show antioxidant and radical scavenging property. These NEs are also optimal H2S slow-release donors and show a significant anti-proliferative effect on different human cancer cell lines: MCF-7 breast cancer and HuT 78 T-cell lymphoma cells. BAD-NEs are able to regulate the ERK1/2 pathway, inducing apoptosis and cell cycle arrest at the G0/G1 phase. We have also investigated their effect on cell proliferation of human adult stem/progenitor cells. Interestingly, BAD-NEs are able to improve the Lin– Sca1+ human cardiac progenitor cells (hCPC) proliferation. This stem cell growth stimulation is combined with the expression and activation of proteins involved in tissue-repair, such as P-AKT, α-sma and connexin 43. Altogether, our results suggest that these antioxidant nanoemulsions might have potential application in selective cancer therapy and for promoting the muscle tissue repair.

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Section: Resultsmentioning

confidence: 99%

H2S-releasing nanoemulsions: a new formulation to inhibit tumor cells proliferation and improve tissue repair

et al. 2016

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“…Ormeloxifene has demonstrated excellent anti-proliferative activity not only in several solid tumors, but also in hematological tumors like chronic myeloid leukemia (CML) [56]. Ormeloxifene induced a concentration dependent increase in apoptosis in multiple CML cells lines (U937, HL60, and K562), with the most prominent effect in K562 CML cells [56].…”

Section: Ormeloxifene As An Anti-cancer Agentmentioning

confidence: 99%

“…Ormeloxifene induced a concentration dependent increase in apoptosis in multiple CML cells lines (U937, HL60, and K562), with the most prominent effect in K562 CML cells [56]. Ormeloxifene arrested the cells in G0–G1 growth phase and induced ERK mediated apoptosis in CML K562 cells.…”

Section: Ormeloxifene As An Anti-cancer Agentmentioning

confidence: 99%

“…The induction of apoptosis by ormeloxifene was associated with the ERK pathway and loss of mitochondrial membrane potential. Importantly, the results obtained from ormeloxifene treatment in the K562 cell line were translatable to mononuclear cells isolated from CML patients [56]. Ormeloxifene treatment of mononuclear cells isolated from patients showed apoptotic phenotypes, including nuclear condensation and membrane blebbing.…”

Section: Ormeloxifene As An Anti-cancer Agentmentioning

confidence: 99%

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Anti-Cancer Potential of a Novel SERM Ormeloxifene

Gara¹,

Sundram²,

Chauhan³

et al. 2013

CMC

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Ormeloxifene is a non-steroidal Selective Estrogen Receptor Modulator (SERM) that is used as an oral contraceptive. Recent studies have shown its potent anti-cancer activities in breast, head and neck, and chronic myeloid leukemia cells. Several in vivo and clinical studies have reported that ormeloxifene possesses an excellent therapeutic index and has been well-tolerated, without any haematological, biochemical or histopathological toxicity, even with chronic administration. A reasonably long period of time and an enormous financial commitment are required to develop a lead compound into a clinically approved anti-cancer drug. For these reasons and to circumvent these obstacles, ormeloxifene is a promising candidate on a fast track for the development or repurposing established drugs as anti-cancer agents for cancer treatment. The current review summarizes recent findings on ormeloxifene as an anti-cancer agent and future prospects of this clinically safe pharmacophore.

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“…Furthermore, the drug has been shown to have anti-cancer activities (40). Thomas et al (41) demonstrated that ormeloxifene significantly increased the levels of serum immunoglobulins in mice.…”

Section: Ormeloxifenementioning

confidence: 99%

Immunomodulatory effects of anti-estrogenic drugs

Ray¹,

M²

2012

Acta Pharmaceutica

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Immunomodulatory effects of anti-estrogenic drugsThere are substantial experimental, epidemiological and clinical evidences that show that breast cancer pathology is influenced by endogenous estrogens. This knowledge is the foundation upon which endocrine deprivation therapy has been developed as a major modality for the management of breast cancer. Tamoxifen, which functions as a competitive partial agonist-inhibitor of estrogen at its receptor, has been widely used for more than three decades for adjuvant endocrine treatment in breast cancer. Currently, other effective drugs for endocrine therapy include raloxifene, different aromatase inhibitors (particularly third-generation agents) and luteinizing hormone-releasing hormone agonists. In recent years, a growing body of evidence suggests that these drugs can also act as immune modulators by altering the function of various leukocytes and the release of different cytokines. Moreover, there is evidence that anti-estrogens may prove to be beneficial in the treatment or prevention of some autoimmune diseases due to their effects on immune function. However, their immunopharmacological aspects in the present state of knowledge are not precisely comprehensible. Only a clear pathophysiological understanding could lead to an efficient strategy for breast cancer prevention and decrease in the mortality due to this disease.

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2‐D gel electrophoresis‐based proteomic analysis reveals that ormeloxifen induces G0–G1 growth arrest and ERK‐mediated apoptosis in chronic myeloid leukemia cells K562

Cited by 36 publications

References 42 publications

H2S-releasing nanoemulsions: a new formulation to inhibit tumor cells proliferation and improve tissue repair

H2S-releasing nanoemulsions: a new formulation to inhibit tumor cells proliferation and improve tissue repair

Anti-Cancer Potential of a Novel SERM Ormeloxifene

Immunomodulatory effects of anti-estrogenic drugs

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