Bioactive analogs of neurotensin: Focus on CNS effects

Boules, Mona; Fredrickson, Paul A.; Richelson, Elliott

doi:10.1016/j.peptides.2005.12.018

Cited by 58 publications

(74 citation statements)

References 137 publications

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“…2 and Table 2). Specificity of NTR1-mediated uptake was verified in each case by blocking experiments in the presence of 1000-fold excess NT (8)(9)(10)(11)(12)(13). showed specific cell internalization rates of approx.…”

Section: Resultsmentioning

confidence: 91%

Section: Introductionmentioning

confidence: 99%

“…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]. The NT receptor (NTR) family consists of the three subtypes, NTR1-3 [10], of which NTR1 is of particular interest for radiotracer development because of its over-expression in various tumours including colon [11], lung [12], prostate [13], and breast cancer [14].…”

Section: Introductionmentioning

confidence: 99%

“…vector (NT (8)(9)(10)(11)(12)(13)) from the radioactive reporter probe (e.g. a radiometal complex), has been reported.…”

Section: Introductionmentioning

confidence: 99%

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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: Resultsmentioning

confidence: 91%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

“…vector (NT (8)(9)(10)(11)(12)(13)) from the radioactive reporter probe (e.g. a radiometal complex), has been reported.…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Effect of a spacer moiety on radiometal labelled Neurotensin derivatives

Mascarin¹,

Valverde²,

Mindt³

2013

Radiochimica Acta

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“…In this sense, neurotensin has long been known to include analgesia among its actions. 9,16,23 The analgesic actions of neurotensin are readily distinct from those of the opioids, based on their insensitivity to the highly opioid-selective antagonist naloxone, thus ruling out an opioid mechanism. 55 Neurotensin acts as part of the peripheral and central mechanisms of pain modulation, 23 because the antinociceptive effect of neurotensin has been reported after the injection of the peptide in many brain areas.…”

Section: Discussionmentioning

confidence: 99%

Changes in Biochemical Markers of Pain Perception and Stress Response After Spinal Manipulation

Plaza-Manzano

Molina²,

Lomas‐Vega³

et al. 2014

J Orthop Sports Phys Ther

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A proopiomelanocortin‐derived peptide sequence enhances plasma stability of peptide drugs

2020

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Bioactive peptide drugs hold promise for therapeutic application due to their high potency and selectivity but display short plasma half‐life. Examination of selected naturally occurring peptide hormones derived from proteolytic cleavage of the proopiomelanocortin (POMC) precursor lead to the identification of significant plasma‐stabilizing properties of a 12‐amino acid serine‐rich orphan sequence NSSSSGSSGAGQ in human γ3‐melanocyte‐stimulating hormone (MSH) that is homologous to previously discovered NSnGGH (n = 4–24) sequences in owls. Notably, transfer of this sequence to des‐acetyl‐α‐MSH and the therapeutically relevant peptide hormones neurotensin and glucagon‐like peptide‐1 likewise enhance their plasma stability without affecting receptor signaling. The stabilizing effect of the sequence module is independent of plasma components, suggesting a direct effect in cis. This natural sequence module may provide a possible strategy to enhance plasma stability, complementing existing methods of chemical modification.

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Bioactive analogs of neurotensin: Focus on CNS effects

Cited by 58 publications

References 137 publications

Effect of a spacer moiety on radiometal labelled Neurotensin derivatives

Effect of a spacer moiety on radiometal labelled Neurotensin derivatives

Changes in Biochemical Markers of Pain Perception and Stress Response After Spinal Manipulation

A proopiomelanocortin‐derived peptide sequence enhances plasma stability of peptide drugs

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