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Novel Neurotensin Analogues for Radioisotope Targeting to Neurotensin Receptor-Positive Tumors Vrije Universiteit Brussel

Faisal Alshoukr, Cedric Rosant, Veronique Maes, Jallane Abdelhak, Olivier Raguin, Samuel Burg, Laure Sarda, Jacques Barbet, Dirk Tourwe, Didier Pelaprat, et al.
The increased expression of the neurotensin (NT) receptor NTS1 by different cancer cells, such as pancreatic adenocarcinoma and ductal breast cancer cells, as compared to normal epithelium. offers the opportunity to target these tumors with radiolabeled neurotensin analogues for diagnostic or therapeutic purposes. The aim of the present study was to design and synthesize new neurotensin radioligands and to Select a lead molecule with high in ...

A stable neurotensin-based radiopharmaceutical for targeted imaging and therapy of neurotensin receptor-positive tumours Vrije Universiteit Brussel

Elisa Garcia-Garayoa, P. Blaüenstein, A. Blanc, Veronique Maes, Dirk Tourwe, P.a. Schubiger
Purpose Neurotensin (NT) and its high affinity receptor (NTR1) are involved in several neoplastic processes. Thus, NT-based radiopharmaceuticals are potential tracers for targeted diagnosis and therapy of NTR-positive tumours. A new analogue based on NT(8-13), NT-XIX, with the three enzymatic cleavage sites stabilised, was synthesised and tested.
Methods The synthesis was performed by Boc strategy. Labelling with Tc-99m/Re-188 was performed ...

Neurotensin Analogues Containing Cyclic Surrogates of Tyrosine at Position 11 Improve NTS2 Selectivity Leading to Analgesia without Hypotension and Hypothermia Vrije Universiteit Brussel

Emilie Eiselt, Simon Gonzalez, Charlotte Martin, Magali Chartier, Cecilia Betti, Jean-Michel Longpre, Dirk Tourwe, Louis Gendron, Steven Ballet

Selective activation of the δ-opioid receptor (DOP) has great potential for the treatment of chronic pain, benefitting from ancillary anxiolytic and antidepressant-like effects. Moreover, DOP agonists show reduced adverse effects as compared to μ-opioid receptor (MOP) agonists that are in the spotlight of the current "opioid crisis." Here, we report the first crystal structures of the DOP in an activated state, in complex with two relevant ...

Novel DOTA-Neurotensin Analogues for In-111 Scintigraphy and Ga-68 PET Imaging of Neurotensin Receptor-Positive Tumors Vrije Universiteit Brussel

Faisal Alshoukr, Aurelie Prignon, Luc Brans, Abdelhak Jallane, Sandra Mendes, Jean-Noel Talbot, Dirk Tourwe, Jacques Barbet, Anne Gruaz-Guyon
Abstract: 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) ...

Insightful Backbone Modifications Preventing Proteolytic Degradation of Neurotensin Analogs Improve NT S1-Induced Protective Hypothermia. Vrije Universiteit Brussel

Santo Previti, Melanie Vivancoe, Emmanuelle Remand, Sabrina Beaulieu, Jean-Michel Longpre, Steven Ballet, Philippe Sarret

Therapeutic hypothermia represents a brain-protective strategy for multiple emergency situations, such as stroke or traumatic injury. Neurotensin (NT), which exerts its effects through activation of two G protein-coupled receptors, namely NTS1 and NTS2, induces a strong and long-lasting decrease in core body temperature after its central administration. Growing evidence demonstrates that NTS1 is the receptor subtype mediating the hypothermic ...

The Drosophila neurogenin Tap functionally interacts with the Wnt-PCP pathway to regulate neuronal extension and guidance KU Leuven

Natalie De Geest, Bassem Hassan
The neurogenin (Ngn) transcription factors control early neurogenesis and neurite outgrowth in mammalian cortex. In contrast to their proneural activity, their function in neurite growth is poorly understood. Drosophila has a single predicted Ngn homolog, Tap, of unknown function. Here we show that Tap is not a proneural protein in Drosophila but is required for proper axonal growth and guidance of neurons of the mushroom body, a neuropile ...

Neurogenin 3+ cells contribute to β-cell neogenesis and proliferation in injured adult mouse pancreas Universiteit Antwerpen Vrije Universiteit Brussel

M Van de Casteele, G Leuckx, L Baeyens, Y Cai, Y Yuchi, Violette Coppens, S De Groef, M Eriksson, C Svensson, U Ahlgren, et al.
We previously showed that injury by partial duct ligation (PDL) in adult mouse pancreas activates Neurogenin 3 (Ngn3)(+) progenitor cells that can differentiate to beta cells ex vivo. Here we evaluate the role of Ngn3(+) cells in beta cell expansion in situ. PDL not only induced doubling of the beta cell volume but also increased the total number of islets. beta cells proliferated without extended delay (the so-called 'refractory' period), their ...

The basic helix-loop-helix region of human neurogenin 1 is a monomeric natively unfolded protein which forms a "fuzzy" complex upon DNA binding KU Leuven

Natalie De Geest, Bassem Hassan
Neuronal specification is regulated by the activity of transcription factors containing the basic helix-loop-helix motif (bHLH); these regulating proteins include, among others, the neurogenin (Ngn) family, related to the atonal family of genes. Neurogenin 1 (NGN1) is a 237-residue protein that contains a bHLH domain and is involved in neuronal differentiation. In this work, we synthesized the bHLH region of NGN1 (bHLHN) comprising residues ...