Cancer, Chemistry, and the Cell: Molecules that Interact with the Neurotensin Receptors

Myers, R. M.; Shearman, James W.; Kitching, Matthew O.; Ramos-Montoya, Antonio; Neal, David E.; Ley, Steven V.

doi:10.1021/cb900038e

Cited by 71 publications

(106 citation statements)

References 192 publications

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“…Among other peptides investigated, Neurotensin (NT), or its binding sequence NT (8)(9)(10)(11)(12)(13) respectively, has been the subject of radiotracer development for application in nuclear oncology [3][4][5][6]. NT is a regulatory peptide present as a hormone in the gastrointestinal tract [7] and as a neurotransmitter in the central nervous system [8,9].…”

Section: Introductionmentioning

confidence: 99%

Effect of a spacer moiety on radiometal labelled Neurotensin derivatives

Mascarin¹,

Valverde²,

Mindt³

2013

Radiochimica Acta

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Neurotensin / NT(8-13) / Radiotracer / Lu-177 / DOTA / Spacer moietySummary. The binding sequence of the regulatory peptide Neurotensin, NT(8-13), represents a promising tumourspecific vector for the development of radiopeptides useful in nuclear oncology for the diagnosis (imaging) and therapy of cancer. A number of radiometal-labelled NT(8-13) derivatives have been reported, however, the effect of the spacer which connects the vector with the radiometal complex has yet not been investigated systematically. Because a spacer moiety can influence potentially important biological characteristics of radiopeptides, we synthesized three [DOTA( 177 Lu)]-X-NT(8-13) derivatives and evaluated the effect of a spacer (X) on the physico-chemical properties of the conjugate including lipophilicity, stability, and in vitro receptor affinity and cell internalization.

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Section: Introductionmentioning

confidence: 99%

Effect of a spacer moiety on radiometal labelled Neurotensin derivatives

Mascarin¹,

Valverde²,

Mindt³

2013

Radiochimica Acta

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“…They stimulate cancer cell growth (21), mainly through binding to NTSR1, that is overexpressed in many cancer cell lines (51). NTSR1 expression is also associated with a poor prognosis in human lung cancer (8,9).…”

Section: Discussionmentioning

confidence: 99%

Differential Expression of Neurotensin and Specific Receptors, NTSR1 and NTSR2, in Normal and Malignant Human B Lymphocytes

Saada

Marget

Fauchais

et al. 2012

The Journal of Immunology

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Neurotensin, a neuropeptide growth factor, and its two specific neurotensin receptors, NTSR1 and NTSR2, were shown to be expressed by human B cell lines. Another NTSR, sortilin, which is common to neurotensin and neurotrophins, was also detected as we have previously described. Neurotensin was functional in B cell lines; it induced their proliferation and inhibited apoptosis induced by serum deprivation or Fas activation. Quantitative study of gene expression in two malignant B cell diseases showed that NTSR2 was overexpressed, NTSR1 decreased, and neurotensin was unexpressed in B cell leukemia patient’s cells, as compared with healthy B cells. However, these expressions did not significantly change in large diffuse B cell lymphoma lymph nodes compared with benign ones. This study points out that neurotensin and its two specific receptors are expressed in human B lymphocytes. Such expressions were not described, and their relationship in B cell diseases, especially in chronic B cell leukemia, needs to be considered further in regard to these findings.

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“…The purinoreceptors stimulated by ATP, are known as P2 receptors and are subdivided into P2X (P2X 1-7 ) and P2Y (P2Y 1 , P2Y 2 , P2Y 4 , P2Y [11][12][13][14] receptors [10][11][12]. The P2X receptors are Ca 2+ permeable ion channels that promote the opening of voltage-dependent Ca 2+ channels [13 36].…”

Section: Introductionmentioning

confidence: 99%

“…P2Y receptors include G-protein-coupled receptors (GPCRs) that increase intracellular calcium by activation of phospholipase C, formation of IP 3 and the subsequent release of Ca 2+ from intracellular stores [9,12]. Three neurotensin receptors have been identified, of which neurotensin receptor 1 (NTS1) and neurotensin receptor 2 (NTS2) are G-protein coupled receptors (GPCR) and induce Ca 2+ release from internal stores [14] while neurotensin receptor 3 (NTS3) is a non GPCR which modulates NT signaling in HT-29 cells by forming a functional interaction with NTS1 [15].…”

Section: Introductionmentioning

confidence: 99%

Effects of differentiation on purinergic and neurotensin-mediated calcium signaling in human HT-29 colon cancer cells

Chowdhury

Peters

Roberts‐Thomson

et al. 2013

Biochemical and Biophysical Research Communications

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Calcium signaling is a key regulator of processes important in differentiation. In colon cancer cells differentiation is associated with altered expression of specific isoforms of calcium pumps of the endoplasmic reticulum and the plasma membrane, suggesting that differentiation of colon cancer cells is associated with a major remodeling of calcium homeostasis. Purinergic and neurotensin receptor activation are known regulators of cytosolic free Ca 2+ levels in colon cancer cells. This study aimed to assess changes in cytosolic free Ca 2+ levels in response to ATP and neurotensin with differentiation induced by sodium butyrate or culturing post-confluence.Parameters assessed included peak cytosolic free Ca 2+ level after activation; time to reach peak cytosolic free Ca 2+ and the EC 50 of dose response curves. Our results demonstrate that differentiation of HT-29 colon cancer cells is associated with a remodeling of both ATP and neurotensin mediated Ca 2+ signaling. Neurotensin-mediated calcium signaling appeared more sensitive to differentiation than ATP-mediated Ca 2+ signaling.

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Cancer, Chemistry, and the Cell: Molecules that Interact with the Neurotensin Receptors

Cited by 71 publications

References 192 publications

Effect of a spacer moiety on radiometal labelled Neurotensin derivatives

Effect of a spacer moiety on radiometal labelled Neurotensin derivatives

Differential Expression of Neurotensin and Specific Receptors, NTSR1 and NTSR2, in Normal and Malignant Human B Lymphocytes

Effects of differentiation on purinergic and neurotensin-mediated calcium signaling in human HT-29 colon cancer cells

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