Literature DB >> 16509599

Novel 99mTc-labeled neurotensin analogues with optimized biodistribution properties.

Veronique Maes1, Elisa Garcia-Garayoa, Peter Bläuenstein, Dirk Tourwé.   

Abstract

Two new 99mTc-labeled neurotensin(8-13) analogues containing the retro-N(alpha)-carboxymethyl-histidine ((N(alpha)His)Ac) chelator were synthesized as potential radiopharmaceuticals for visualization of pancreatic carcinoma. To improve the pharmacokinetic properties, (N(alpha)His)Ac-Arg-NMeArg-Pro-Tyr-Tle-Leu (NT-XII), which is metabolically stabilized at two positions, was further modified. Shikimic acid (3,4,5-trihydroxy-1-cyclohexene-1-carboxylic acid) was introduced to obtain a more hydrophilic peptide (NT-XVIII), or Tyr11 was replaced by 2,6-dimethyltyrosine (Dmt) resulting in a triple-stabilized NT(8-13) analogue (NT-XIX). The latter has the best biodistribution profile.

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Year:  2006        PMID: 16509599     DOI: 10.1021/jm051172f

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  10 in total

1.  Modifications at Arg and Ile Give Neurotensin(8-13) Derivatives with High Stability and Retained NTS1 Receptor Affinity.

Authors:  Lisa Schindler; Günther Bernhardt; Max Keller
Journal:  ACS Med Chem Lett       Date:  2019-05-10       Impact factor: 4.345

Review 2.  Peptides and peptide hormones for molecular imaging and disease diagnosis.

Authors:  Seulki Lee; Jin Xie; Xiaoyuan Chen
Journal:  Chem Rev       Date:  2010-05-12       Impact factor: 60.622

3.  Investigation of the Biological Impact of Charge Distribution on a NTR1-Targeted Peptide.

Authors:  Yinnong Jia; Wenting Zhang; Wei Fan; Susan Brusnahan; Jered Garrison
Journal:  Bioconjug Chem       Date:  2016-10-21       Impact factor: 4.774

4.  A stable neurotensin-based radiopharmaceutical for targeted imaging and therapy of neurotensin receptor-positive tumours.

Authors:  Elisa García-Garayoa; Peter Bläuenstein; Alain Blanc; Veronique Maes; Dirk Tourwé; P August Schubiger
Journal:  Eur J Nucl Med Mol Imaging       Date:  2008-08-09       Impact factor: 9.236

5.  [99mTc]Demotensin 5 and 6 in the NTS1-R-targeted imaging of tumours: synthesis and preclinical results.

Authors:  Theodosia Maina; Anastasia Nikolopoulou; Eleni Stathopoulou; Athanassios S Galanis; Paul Cordopatis; Berthold A Nock
Journal:  Eur J Nucl Med Mol Imaging       Date:  2007-06-27       Impact factor: 9.236

6.  Evaluation of DOTA-chelated neurotensin analogs with spacer-enhanced biological performance for neurotensin-receptor-1-positive tumor targeting.

Authors:  Yinnong Jia; Wen Shi; Zhengyuan Zhou; Nilesh K Wagh; Wei Fan; Susan K Brusnahan; Jered C Garrison
Journal:  Nucl Med Biol       Date:  2015-07-29       Impact factor: 2.408

Review 7.  Peptide-based probes for targeted molecular imaging.

Authors:  Seulki Lee; Jin Xie; Xiaoyuan Chen
Journal:  Biochemistry       Date:  2010-02-23       Impact factor: 3.162

8.  Development of a Neurotensin-Derived 68Ga-Labeled PET Ligand with High In Vivo Stability for Imaging of NTS1 Receptor-Expressing Tumors.

Authors:  Lisa Schindler; Jutta Moosbauer; Daniel Schmidt; Thilo Spruss; Lukas Grätz; Steffen Lüdeke; Frank Hofheinz; Sebastian Meister; Bernd Echtenacher; Günther Bernhardt; Jens Pietzsch; Dirk Hellwig; Max Keller
Journal:  Cancers (Basel)       Date:  2022-10-08       Impact factor: 6.575

9.  Synthesis, Characterization, and Interaction with Biomolecules of Platinum(II) Complexes with Shikimic Acid-Based Ligands.

Authors:  Yan Peng; Min-Min Zhang; Zhen-Feng Chen; Kun Hu; Yan-Cheng Liu; Xia Chen; Hong Liang
Journal:  Bioinorg Chem Appl       Date:  2013-03-05       Impact factor: 7.778

10.  Optimizing the Profile of [99mTc]Tc-NT(7-13) Tracers in Pancreatic Cancer Models by Means of Protease Inhibitors.

Authors:  Panagiotis Kanellopoulos; Berthold A Nock; Eric P Krenning; Theodosia Maina
Journal:  Int J Mol Sci       Date:  2020-10-26       Impact factor: 5.923

  10 in total

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