The NK-1 Receptor is Involved in the Antitumoural Action of L-733,060 and in the Mitogenic Action of Substance P on Human Pancreatic Cancer Cell Lines

Muñoz, Miguel; Rosso, Marisa; Coveñas, Rafael

doi:10.2174/157018006777574168

Cited by 34 publications

(49 citation statements)

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“…10,12,15,16,24 We show the presence of several NK-1 receptor isoforms (33, 58 and 75 kDa) in MEL HO, COLO 858 and COLO 679 human malignant melanoma cell lines, although the functional roles of these NK-1 receptor isoforms are currently unknown. Until now, the expression of NK-1 receptors in human primary invasive malignant melanomas and metastatic melanomas was unknown.…”

Section: Nk-1 Receptor and Aprepitant In Melanomas M Muñ Oz Et Almentioning

confidence: 86%

“…21 Thus, using immunohistochemical methods, NK-1 receptor visualization should facilitate the identification of tumors with a sufficient NK-1 receptor overexpression for diagnostic and therapeutic intervention (administering NK-1 receptor antagonists). 4,23 It is known that the activation of the NK-1 receptor by SP at nanomolar concentrations induces mitogenesis in human malignant melanoma cell lines 6 and in several cancer cell lines, 8,[10][11][12][13]15,16 and also that SP is expressed in primary invasive malignant melanomas and metastatic melanomas. 5 We showed that treatment of the three melanoma cell lines studied herein with the NK-1 receptor antagonist aprepitant causes growth inhibition and cell death.…”

Section: Nk-1 Receptor and Aprepitant In Melanomas M Muñ Oz Et Almentioning

confidence: 99%

“…5 It has also been shown that activation of NK-1 receptors by SP induces mitogenesis in several melanoma cell lines 6,7 and others tumor cell lines. [8][9][10][11][12][13][14][15][16] SP is also a main mediator in the growth of capillary vessels in vivo and in the proliferation of cultured endothelial cells in vitro, and it has also been shown that NK-1 receptor agonists induced neoangiogenesis. 17 Moreover, the active migration of tumor cells, a crucial requirement for invasion and metastasis, is regulated by SP signals.…”

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confidence: 99%

“…4,7,16,[19][20][21][22][23][24] Moreover, the expression of NK-1 receptors has also been reported in human glioma, neuroblastoma, pancreatic carcinoma, retinoblastoma, laryngeal carcinoma, as well as in gastric and colon carcinoma cell lines. 10,12,15,16,21,24 The NK-1 receptor antagonist L-733060 (a piperidine derivative) shows a high affinity for the human NK-1 receptor in vitro. 25 Moreover, we have previously shown that L-733060 shows antitumor activity against human malignant melanoma cell lines 6 and neuroblastoma, glioma, retinoblastoma, pancreas, larynx, gastric and colon carcinoma cell lines.…”

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confidence: 99%

“…25 Moreover, we have previously shown that L-733060 shows antitumor activity against human malignant melanoma cell lines 6 and neuroblastoma, glioma, retinoblastoma, pancreas, larynx, gastric and colon carcinoma cell lines. 11,12,15,16,26 Aprepitant is a selective high-affinity antagonist of the human NK-1 receptor. Until now, this drug has been used as an antidepressant, anxiolytic and antiemetic.…”

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confidence: 99%

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The NK-1 receptor is expressed in human melanoma and is involved in the antitumor action of the NK-1 receptor antagonist aprepitant on melanoma cell lines

Muñoz

Rosso

Robles‐Frías

et al. 2010

Laboratory Investigation

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Melanoma, the most deadly form of skin cancer, is aggressive and resistant to current therapies. It has been previously reported that the substance P and neurokinin-1 (NK-1) receptor antagonists induce cell proliferation and cell inhibition, respectively, in human melanoma cell lines. Aprepitant is a selective high-affinity antagonist of the human NK-1 receptor. Until now, this drug has been used as an anxiolytic, antidepressant and antiemetic. Moreover, the antitumor action of aprepitant has been previously reported. However, the presence of NK-1 receptors in human melanomas and whether the antitumor action of the NK-1 receptor antagonist aprepitant is exerted on human malignant melanomas have not been previously described. The aims of this study are to show the presence of NK-1 receptors in human malignant melanomas and the antitumoral action of aprepitant against several human melanoma cell lines. Immunoblot analysis was used to determine the presence of NK-1 receptors in human melanoma cell lines, and immunohistochemistry was used to demonstrate NK-1 receptors in human melanoma samples. We performed an in vitro study of the cytotoxicity of the NK-1 receptor antagonist aprepitant on human melanoma cell lines. A coulter counter was used to determine viable cell numbers, followed by application of the tetrazolium compound MTS. The DAPI method was applied to demonstrate apoptosis. We observed that NK-1 receptors were present in all the melanoma samples studied as well as in human melanoma cell lines. We also showed that melanoma cell lines expressed mRNA for the NK-1 receptor. Moreover, after using a knockdown method, we showed that NK-1 receptors are involved in the viability of tumor cells. In this study, we also report that aprepitant, at 10-60 mM concentrations, elicits cell growth inhibition in a concentration-dependent manner in all melanoma cell lines studied, that the specific antitumor action of aprepitant occurs through the NK-1 receptor and that melanoma cell death is due to apoptosis. These findings show for the first time that the NK-1 receptor may be a promising new target and that the NK-1 receptor antagonist aprepitant could be a candidate as a new antitumor drug in the treatment of human melanoma.

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Section: Nk-1 Receptor and Aprepitant In Melanomas M Muñ Oz Et Almentioning

confidence: 86%

Section: Nk-1 Receptor and Aprepitant In Melanomas M Muñ Oz Et Almentioning

confidence: 99%

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confidence: 99%

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confidence: 99%

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confidence: 99%

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The NK-1 receptor is expressed in human melanoma and is involved in the antitumor action of the NK-1 receptor antagonist aprepitant on melanoma cell lines

Muñoz

Rosso

Robles‐Frías

et al. 2010

Laboratory Investigation

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The Orthoester Johnson–Claisen Rearrangement in the Synthesis of Bioactive Molecules, Natural Products, and Synthetic Intermediates – Recent Advances

2013

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The orthoester Johnson–Claisen rearrangement, an important C–C bond forming reaction, has been used enormously in the past four decades in the synthesis of bioactive molecules, natural products, synthetic intermediates, analogues, and useful building blocks. The method has also featured in chemical modification of materials. This review covers developments in this rearrangement since 2003. Unlike many other forms of Claisen rearrangement, this reaction is generally a one‐pot, one‐step process. It is compatible with numerous functional groups, despite its use of acid catalysis, and offers chirality transfer to produce stereoselective products. The method also offers opportunities for rapid modifications to various functionalized compounds and building blocks for further synthetic exploration.

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Fighting Cancer Using Selective Antagonists Targeting the Substance P/Neurokinin-1 Receptor System

Coveñas,

Rodríguez,

Muñoz

2024

Interdisciplinary Cancer Research

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The NK-1 Receptor is Involved in the Antitumoural Action of L-733,060 and in the Mitogenic Action of Substance P on Human Pancreatic Cancer Cell Lines

Cited by 34 publications

References 0 publications

The NK-1 receptor is expressed in human melanoma and is involved in the antitumor action of the NK-1 receptor antagonist aprepitant on melanoma cell lines

The NK-1 receptor is expressed in human melanoma and is involved in the antitumor action of the NK-1 receptor antagonist aprepitant on melanoma cell lines

The Orthoester Johnson–Claisen Rearrangement in the Synthesis of Bioactive Molecules, Natural Products, and Synthetic Intermediates – Recent Advances

Fighting Cancer Using Selective Antagonists Targeting the Substance P/Neurokinin-1 Receptor System

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