Publications by authors named "L M BRANS"

Article Synopsis
  • The study investigates the effectiveness of a PEGylated radiotracer, 177Lu-DOTA-PEG5k-Lys-B, for targeting breast and prostate tumors, assessing its therapeutic impact compared to a non-PEGylated version.
  • PEGylation slightly decreased receptor binding affinity but significantly improved stability, tumor uptake, and retention over time in animal models, indicating enhanced in vivo performance.
  • Results showed that the PEGylated analogue achieved higher tumor accumulation and better tumor-to-organ ratios, suggesting it may be more effective for imaging and therapy of cancers overexpressing bombesin receptors.
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Introduction: Radiolabeled bombesin (BN) conjugates are promising radiotracers for imaging and therapy of breast and prostate tumors in which BN(2)/gastrin-releasing peptide (GRP) receptors are overexpressed. However, the low in vivo stability of BN conjugates may limit their clinical application. In an attempt to improve their pharmacokinetics and counteract their rapid enzymatic degradation, we prepared a series of polyethylene glycol (PEG)-ylated BN(7-14) analogues for radiolabeling with (99m)Tc(CO)(3) and evaluated them in vitro and in vivo.

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Overexpression of the high affinity neurotensin receptor 1 (NTSR1), demonstrated in several human cancers, has been proposed as a new marker for human ductal pancreatic carcinoma and as an independent factor for poor prognosis for ductal breast cancer, head and neck squamous cell carcinoma, and non-small cell lung cancer. The aim of the present study was to develop new DOTA-neurotensin analogues for positron emission tomography (PET) imaging with (68)Ga and for targeted radiotherapy with (90)Y or (177)Lu. We synthesized a DOTA-neurotensin analogue series.

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Synthetic strategies that enable the efficient and selective combination of different biologically active entities hold great promise for the development of multifunctional hybrid conjugates useful for biochemical and medical applications. Starting from side-chain-functionalized N(α)-propargyl lysine derivatives, conjugates containing a ⁹⁹(m)Tc-based imaging probe for SPECT and two different moieties (e.g.

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Article Synopsis
  • Researchers are exploring overexpressed gastrin-releasing peptide receptors (GRPRs) in cancer for improved diagnosis and treatment.
  • A novel peptide analogue has shown high affinity for GRPR and its distribution in the body is enhanced through glycation techniques.
  • New triazole-based chelating systems have been synthesized to label peptides, with glycation still being the more significant factor for better tumor visibility compared to the type of chelator used.
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