“Click to chelate”: synthesis and installation of metal chelates into biomolecules in a single step

…, C Schweinsberg, V Maes, D Tourwé… - Journal of the …, 2006 - ACS Publications
Click chemistry has been employed for the assembly of novel and efficient triazole-based
multidentate chelating systems while simultaneously attaching them to molecules of biological …

Structural basis for bifunctional peptide recognition at human δ-opioid receptor

…, CE Conrad, R Fromme, P Fromme, D Tourwé… - Nature structural & …, 2015 - nature.com
Bifunctional μ- and δ-opioid receptor (OR) ligands are potential therapeutic alternatives, with
diminished side effects, to alkaloid opiate analgesics. We solved the structure of human δ-…

Comprehensive overview of biased pharmacology at the opioid receptors: biased ligands and bias factors

J De Neve, TMA Barlow, D Tourwé, F Bihel… - RSC Medicinal …, 2021 - pubs.rsc.org
… Dirk Tourwé (inset) obtained his PhD degree at the VUB in 1974. He became director of the
… Notably, they all contain the L,D,L,D stereochemical pattern. SAR studies proved that this L,D

[PDF][PDF] Organometallic 99mTc-aquaion labels peptide to an unprecedented high specific activity

…, A Schaffland, R Waibel, D Tourwé… - Journal of Nuclear …, 1999 - Soc Nuclear Med
A new peptide labeling method that uses the Organometallic aquaion [99rnTc (H2O) 3 (CO)
3]+ has been developed. Methods: A selection of amino acids was labeled at different …

Influence of the Molecular Charge on the Biodistribution of Bombesin Analogues Labeled with the [99mTc(CO)3]-Core

…, L Brans, P Bläuenstein, DA Tourwé… - Bioconjugate …, 2008 - ACS Publications
… The new analogues showed a shift in hydrophilicity from a Log D = 0.9 to Log D values …
with Log D values between +1 and −1 showed the highest binding affinities with K d values …

Side chain cyclized aromatic amino acids: great tools as local constraints in peptide and peptidomimetic design

…, D Sejer Pedersen, S Ballet, D Tourwé - Journal of Medicinal …, 2016 - ACS Publications
… In summary, when the four C-terminal amino acids of 62 are constrained by the d-Tic-Oic
dipeptide motif which produces 63, excellent affinity and potency toward the B 2 receptors are …

Radiolabeled neurotensin analog, 99mTc-NT-XI, evaluated in ductal pancreatic adenocarcinoma patients

…, JC Reubi, P Bläuenstein, D Tourwé… - Journal of Nuclear …, 2003 - Soc Nuclear Med
… Neoplastic pancreatic ducts (arrows) are strongly labeled in C but not in D. (E and F)
Autoradiograms show absence of nonspecific binding in presence of 10 −6 mol/L NT. …

A 99mTc(I)-Postlabeled High Affinity Bombesin Analogue as a Potential Tumor Imaging Agent

…, R Schibli, P Conrath, D Tourwe… - Bioconjugate …, 2002 - ACS Publications
The overexpression of neuropeptide receptors observed in many cancers provides an attractive
target for tumor imaging and therapy. Bombesin is a peptide exhibiting a high affinity for …

Preclinical evaluation of a new, stabilized neurotensin (8–13) pseudopeptide radiolabeled with 99mTc

…, A Blanc, K Iterbeke, P Conrath, D Tourwé… - Journal of Nuclear …, 2002 - Soc Nuclear Med
… xenograft (A), liver (B), kidneys (C), and human prostate carcinoma PC-3 xenograft (D).
Tumors were induced by subcutaneous injection of 8 × 10 6 cells of each type 10 d before assay. …

Chemical and biological characterization of new Re (CO) 3/[99mTc](CO) 3 bombesin analogues

…, A Blanc, AG Beck-Sickinger, DA Tourwé… - Nuclear medicine and …, 2007 - Elsevier
… The receptor affinity of the new technetium 99m ([ 99m Tc])-labeled BBS analogues was
similar to the unmodified compound with K d <1 nM. Uptake in the pancreas and in PC-3 tumor …