J C Reubi

Summary

Affiliation: University of Bern
Country: Switzerland

Publications

  1. pmc Illuminating somatostatin analog action at neuroendocrine tumor receptors
    Jean Claude Reubi
    Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Berne, Switzerland Electronic address
    Trends Pharmacol Sci 34:676-88. 2013
  2. doi request reprint Old and new peptide receptor targets in cancer: future directions
    Jean Claude Reubi
    University of Berne, Berne, Switzerland
    Recent Results Cancer Res 194:567-76. 2013
  3. doi request reprint Glucose-dependent insulinotropic polypeptide receptors in most gastroenteropancreatic and bronchial neuroendocrine tumors
    Beatrice Waser
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, CH 3010 Berne, Switzerland
    J Clin Endocrinol Metab 97:482-8. 2012
  4. pmc Novel dimeric DOTA-coupled peptidic Y1-receptor antagonists for targeting of neuropeptide Y receptor-expressing cancers
    David Chatenet
    The Clayton Foundation Laboratories for Peptide Biology, The Salk Institute for Biological Studies, 10010 N, Torrey Pines Rd, La Jolla, CA, USA
    EJNMMI Res 1:21. 2011
  5. doi request reprint Concomitant vascular GRP-receptor and VEGF-receptor expression in human tumors: molecular basis for dual targeting of tumoral vasculature
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Bern, PO Box 62, Murtenstrasse 31, CH 3010 Bern, Switzerland
    Peptides 32:1457-62. 2011
  6. ncbi request reprint Concomitant expression of several peptide receptors in neuroendocrine tumours: molecular basis for in vivo multireceptor tumour targeting
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Berne, Switzerland
    Eur J Nucl Med Mol Imaging 30:781-93. 2003
  7. doi request reprint Glucagon-like peptide-1 (GLP-1) receptors are not overexpressed in pancreatic islets from patients with severe hyperinsulinaemic hypoglycaemia following gastric bypass
    J C Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, PO Box 62, Murtenstrasse 31, CH 3010 Berne, Switzerland
    Diabetologia 53:2641-5. 2010
  8. ncbi request reprint Expression of CRF1 and CRF2 receptors in human cancers
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, CH 3010 Berne, Switzerland
    J Clin Endocrinol Metab 88:3312-20. 2003
  9. ncbi request reprint Distribution of CCK1 and CCK2 receptors in normal and diseased human pancreatic tissue
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Switzerland
    Gastroenterology 125:98-106. 2003
  10. pmc Switch from antagonist to agonist after addition of a DOTA chelator to a somatostatin analog
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, PO Box 62, Murtenstrasse 31, 3010 Berne, Switzerland
    Eur J Nucl Med Mol Imaging 37:1551-8. 2010

Collaborators

Detail Information

Publications100

  1. pmc Illuminating somatostatin analog action at neuroendocrine tumor receptors
    Jean Claude Reubi
    Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Berne, Switzerland Electronic address
    Trends Pharmacol Sci 34:676-88. 2013
    ..The increased understanding of somatostatin receptor pharmacology provides new opportunities to design more sophisticated assays to aid the future development of somatostatin analogs with increased efficacy. ..
  2. doi request reprint Old and new peptide receptor targets in cancer: future directions
    Jean Claude Reubi
    University of Berne, Berne, Switzerland
    Recent Results Cancer Res 194:567-76. 2013
    ..Due to the abundance of peptide receptors in various cancers, it may be possible in the future to define for each tumor type a corresponding overexpressed peptide receptor suitable for targeting...
  3. doi request reprint Glucose-dependent insulinotropic polypeptide receptors in most gastroenteropancreatic and bronchial neuroendocrine tumors
    Beatrice Waser
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, CH 3010 Berne, Switzerland
    J Clin Endocrinol Metab 97:482-8. 2012
    ..Unfortunately, not all NET express these receptors sufficiently...
  4. pmc Novel dimeric DOTA-coupled peptidic Y1-receptor antagonists for targeting of neuropeptide Y receptor-expressing cancers
    David Chatenet
    The Clayton Foundation Laboratories for Peptide Biology, The Salk Institute for Biological Studies, 10010 N, Torrey Pines Rd, La Jolla, CA, USA
    EJNMMI Res 1:21. 2011
    ..abstract:..
  5. doi request reprint Concomitant vascular GRP-receptor and VEGF-receptor expression in human tumors: molecular basis for dual targeting of tumoral vasculature
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Bern, PO Box 62, Murtenstrasse 31, CH 3010 Bern, Switzerland
    Peptides 32:1457-62. 2011
    ....
  6. ncbi request reprint Concomitant expression of several peptide receptors in neuroendocrine tumours: molecular basis for in vivo multireceptor tumour targeting
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Berne, Switzerland
    Eur J Nucl Med Mol Imaging 30:781-93. 2003
    ..Finally, the data strongly encourage concomitant application of several radiopeptides to permit more efficient targeting of these tumours...
  7. doi request reprint Glucagon-like peptide-1 (GLP-1) receptors are not overexpressed in pancreatic islets from patients with severe hyperinsulinaemic hypoglycaemia following gastric bypass
    J C Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, PO Box 62, Murtenstrasse 31, CH 3010 Berne, Switzerland
    Diabetologia 53:2641-5. 2010
    ..The present study sought to evaluate the GLP-1 receptor status in vitro in other pancreatic disorders leading to hyperinsulinaemic hypoglycaemia, specifically after gastric bypass surgery...
  8. ncbi request reprint Expression of CRF1 and CRF2 receptors in human cancers
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, CH 3010 Berne, Switzerland
    J Clin Endocrinol Metab 88:3312-20. 2003
    ....
  9. ncbi request reprint Distribution of CCK1 and CCK2 receptors in normal and diseased human pancreatic tissue
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Switzerland
    Gastroenterology 125:98-106. 2003
    ..The localization and functional role of cholecystokinin (CCK) receptor proteins in normal and diseased human pancreas, particularly in ductal pancreatic carcinomas, remain unclear...
  10. pmc Switch from antagonist to agonist after addition of a DOTA chelator to a somatostatin analog
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, PO Box 62, Murtenstrasse 31, 3010 Berne, Switzerland
    Eur J Nucl Med Mol Imaging 37:1551-8. 2010
    ..They have, however, rarely been tested for their agonistic or antagonistic properties. We report here on a somatostatin antagonist that switched to an agonist upon coupling to a DOTA chelator...
  11. pmc Internalized somatostatin receptor subtype 2 in neuroendocrine tumors of octreotide-treated patients
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, P O Box 62, Murtenstrasse 31, CH 3010 Berne, Switzerland
    J Clin Endocrinol Metab 95:2343-50. 2010
    ..Recently, it has been demonstrated in animal sst(2) tumor models in vivo that somatostatin analog treatment was able to induce a complete internalization of the tumor sst(2)...
  12. ncbi request reprint High expression of peptide receptors as a novel target in gastrointestinal stromal tumours
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Murtenstrasse 31, PO Box 62, 3010 Bern, Switzerland
    Eur J Nucl Med Mol Imaging 31:803-10. 2004
    ....
  13. doi request reprint Peptide-based probes for cancer imaging
    Jean Claude Reubi
    University of Berne, Berne, Switzerland
    J Nucl Med 49:1735-8. 2008
    ..Application fields include both SPECT/CT and PET/CT...
  14. ncbi request reprint Somatostatin and other Peptide receptors as tools for tumor diagnosis and treatment
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Berne, Switzerland
    Neuroendocrinology 80:51-6. 2004
    ..Often, several of these peptide receptors are expressed simultaneously in GEP NET, providing a molecular basis for in vivo multireceptor targeting of those tumors...
  15. ncbi request reprint Candidates for peptide receptor radiotherapy today and in the future
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Berne, Switzerland
    J Nucl Med 46:67S-75S. 2005
    ..Improved somatostatin or CCK(2) analogs as well as newly designed bombesin, neurotensin, substance P, neuropeptide Y, and glucagon-like peptide-1 analogs offer promise for future PRRT...
  16. ncbi request reprint Targeting CCK receptors in human cancers
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Berne, Switzerland
    Curr Top Med Chem 7:1239-42. 2007
    ....
  17. ncbi request reprint Peptide receptor expression in GEP-NET
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, P O Box 62, Murtenstrasse 31, CH 3010, Berne, Switzerland
    Virchows Arch 451:S47-50. 2007
    ..Often, several of these peptide receptors are expressed simultaneously in GEP-NET, providing a molecular basis for in vivo multireceptor targeting of those tumors...
  18. ncbi request reprint A new peptidic somatostatin agonist with high affinity to all five somatostatin receptors
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Switzerland
    Eur J Pharmacol 456:45-9. 2002
    ....
  19. ncbi request reprint Subcellular distribution of somatostatin sst2A receptors in human tumors of the nervous and neuroendocrine systems: membranous versus intracellular location
    J C Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Switzerland
    J Clin Endocrinol Metab 85:3882-91. 2000
    ....
  20. ncbi request reprint Vasoactive intestinal peptide/pituitary adenylate cyclase-activating peptide receptor subtypes in human tumors and their tissues of origin
    J C Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Switzerland
    Cancer Res 60:3105-12. 2000
    ....
  21. pmc SST3-selective potent peptidic somatostatin receptor antagonists
    J C Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Switzerland
    Proc Natl Acad Sci U S A 97:13973-8. 2000
    ....
  22. ncbi request reprint Potent somatostatin undecapeptide agonists selective for somatostatin receptor 1 (sst1)
    J E Rivier
    The Salk Institute, The Clayton Foundation Laboratories for Peptide Biology, 10010 N Torrey Pines Road, La Jolla, CA 92037, USA
    J Med Chem 44:2238-46. 2001
    ....
  23. pmc Distribution of somatostatin receptors in normal and neoplastic human tissues: recent advances and potential relevance
    J C Reubi
    Division of Cell Biology and Experimental Cancer Research, University of Berne, Switzerland
    Yale J Biol Med 70:471-9. 1997
    ..The multiple somatostatin targets in normal and pathological human tissues represents the basis for potential diagnostic and clinical applications of somatostatin analogs...
  24. ncbi request reprint Potent and long-acting corticotropin releasing factor (CRF) receptor 2 selective peptide competitive antagonists
    J Rivier
    The Clayton Foundation Laboratories for Peptide Biology, The Salk Institute for Biological Studies, 10010 North Torrey Pines Road, La Jolla, California 92037, USA
    J Med Chem 45:4737-47. 2002
    ....
  25. ncbi request reprint Receptor autoradiographic evaluation of cholecystokinin, neurotensin, somatostatin and vasoactive intestinal peptide receptors in gastro-intestinal adenocarcinoma samples: where are they really located?
    J C Reubi
    Institute of Pathology, University of Berne, Switzerland
    Int J Cancer 81:376-86. 1999
    ....
  26. pmc Immunohistochemical localization of somatostatin receptors sst2A in human tumors
    J C Reubi
    Institute of Pathology, University of Berne, Switzerland
    Am J Pathol 153:233-45. 1998
    ..The sst2A receptor identification and visualization in tumors with simple immunohistochemical methods in formalin-fixed, paraffin-embedded material will open new diagnostic opportunities for pathologists...
  27. pmc Cellular detection of sst2A receptors in human gastrointestinal tissue
    M Gugger
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, PO Box 62, Murtenstrasse 31, CH 3010 Berne, Switzerland
    Gut 53:1431-6. 2004
    ..However, little information is available about the cellular location of sst2A in corresponding non-neoplastic epithelial tissues...
  28. ncbi request reprint Neurotensin receptors in human neoplasms: high incidence in Ewing's sarcomas
    J C Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Switzerland
    Int J Cancer 82:213-8. 1999
    ....
  29. ncbi request reprint Somatostatin receptor sst1-sst5 expression in normal and neoplastic human tissues using receptor autoradiography with subtype-selective ligands
    J C Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Switzerland
    Eur J Nucl Med 28:836-46. 2001
    ..This information is of importance with regard to the clinical applications and development of somatostatin analogues with distinct receptor subtype selectivities...
  30. ncbi request reprint Y(1)-mediated effect of neuropeptide Y in cancer: breast carcinomas as targets
    J C Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Murtenstrasse 31, CH 3010 Berne, Switzerland
    Cancer Res 61:4636-41. 2001
    ..The high incidence of Y(1) in in situ, invasive, and metastatic breast cancers allows for the possibility to target them for diagnosis and therapy with NPY analogues...
  31. ncbi request reprint Immunohistochemical detection of somatostatin sst2a receptors in the lymphatic, smooth muscular, and peripheral nervous systems of the human gastrointestinal tract: facts and artifacts
    J C Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Switzerland
    J Clin Endocrinol Metab 84:2942-50. 1999
    ....
  32. ncbi request reprint Internalization of sst2, sst3, and sst5 receptors: effects of somatostatin agonists and antagonists
    Renzo Cescato
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Berne, Switzerland
    J Nucl Med 47:502-11. 2006
    ....
  33. pmc Somatostatin receptors in the gastrointestinal tract in health and disease
    J C Reubi
    Division of Cell Biology and Experimental Cancer Research, University of Berne, Switzerland
    Yale J Biol Med 65:493-503; discussion 531-6. 1992
    ..Since somatostatin receptors in gastroenteropancreatic tumors are functional, their identification can be used to assess the therapeutic efficacy of octreotide to inhibit excessive hormone release in the patients...
  34. ncbi request reprint Neurotensin receptor-1 mRNA analysis in normal pancreas and pancreatic disease
    L Wang
    Department of Visceral and Transplantation Surgery, University of Bern, Inselspital, Switzerland
    Clin Cancer Res 6:566-71. 2000
    ..However, its relatively high levels in CP excludes NTR-1 mRNA as a specific parameter for pancreatic cancer and for the differentiation of pancreatic cancer from CP...
  35. ncbi request reprint CCK receptors in human neuroendocrine tumors: clinical implications
    J C Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Switzerland
    Scand J Clin Lab Invest Suppl 234:101-4. 2001
    ....
  36. doi request reprint Bombesin receptor antagonists may be preferable to agonists for tumor targeting
    Renzo Cescato
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Berne, Switzerland
    J Nucl Med 49:318-26. 2008
    ....
  37. pmc Secretin receptors in normal and diseased human pancreas: marked reduction of receptor binding in ductal neoplasia
    Meike Korner
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology of the University of Bern, Murtenstrasse 31, PO Box 62, CH 3010 Bern, Switzerland
    Am J Pathol 167:959-68. 2005
    ..Reduced secretin binding in pancreatic ductal tumors may relate to (alternatively spliced) secretin receptor isoforms. Thus, secretin receptors in pancreatic tumors may represent potential clinical targets...
  38. ncbi request reprint Somatostatin receptors in human prostate and prostate cancer
    J C Reubi
    Division of Cell Biology and Experimental Cancer Research, University of Berne, Switzerland
    J Clin Endocrinol Metab 80:2806-14. 1995
    ..These data suggest that the human prostate as well as prostate cancers may be targets for SRIH therapy; however, SRIH analogs with different selectivities for SRIH-R subtypes are required in each case...
  39. ncbi request reprint In vitro evaluation of VIP/PACAP receptors in healthy and diseased human tissues. Clinical implications
    J C Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, P O Box 62, Murtenstrasse 31, CH 3010 Berne, Switzerland
    Ann N Y Acad Sci 921:1-25. 2000
    ..Moreover, the receptor expression in tumors is the molecular basis for clinical applications of VIP/PACAP such as in vivo scintigraphy and radiotherapy of tumors as well as VIP/PACAP analog treatment for tumor growth inhibition...
  40. ncbi request reprint Immunohistochemical localization of somatostatin receptor sst2A in human gut and lung tissue: possible implications for physiology and carcinogenesis
    M Gugger
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Berne, Switzerland
    Ann N Y Acad Sci 1014:132-6. 2004
    ..It is currently not clear whether and which of the identified sst2A cells are at the origin of sst2A-positive neuroendocrine gut or lung tumors...
  41. pmc Cholecystokinin-B/gastrin receptors enhance wound healing in the rat gastric mucosa
    A Schmassmann
    Gastrointestinal Unit, Inselspital, University Hospital, University of Berne, Berne, Switzerland
    J Clin Invest 106:1021-9. 2000
    ..These effects were completely reversed by cotherapy with YF-476. These in vivo and vitro data suggest that CCK-B/gastrin receptors in regenerative rat gastric oxyntic mucosa enhance trophic effects during wound healing...
  42. doi request reprint Neuropeptide Y receptors in primary human brain tumors: overexpression in high-grade tumors
    Meike Korner
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology of the University of Berne, Berne, Switzerland
    J Neuropathol Exp Neurol 67:741-9. 2008
    ..Moreover, identification of the high expression of NPY receptors in high-grade gliomas and embryonal brain tumors provides the basis for in vivo targeting...
  43. ncbi request reprint Bombesin receptor subtypes in human cancers: detection with the universal radioligand (125)I-[D-TYR(6), beta-ALA(11), PHE(13), NLE(14)] bombesin(6-14)
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, CH 3010 Berne, Switzerland
    Clin Cancer Res 8:1139-46. 2002
    ..Whereas the gastrin-releasing peptide (GRP) receptor is a bombesin receptor subtype frequently expressed by tumors, the other three subtypes, the neuromedin B (NMB), BB3, and BB4 receptors, have been poorly investigated in human tissues...
  44. pmc CCK(2) receptor splice variant with intron 4 retention in human gastrointestinal and lung tumours
    Meike Korner
    Mayo Clinic, Cancer Center and Department of Molecular Pharmacology and Experimental Therapeutics, Scottsdale, Arizona, USA
    J Cell Mol Med 14:933-43. 2010
    ..In conclusion, the CCK(2)Ri4sv is a marker of specific gastrointestinal and lung tumours. With its high selectivity for and high incidence in SCLC and GIST, it may represent an attractive clinical target...
  45. ncbi request reprint Neuropeptide Y receptor expression in human primary ovarian neoplasms
    Meike Korner
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Bern, Bern, Switzerland
    Lab Invest 84:71-80. 2004
    ..Moreover, the high incidence and density of NPY receptors in sex cord-stromal tumors suggest that these receptors represent a new potential target for the diagnostic and therapeutic administration of NPY analogs in these tumors...
  46. doi request reprint Absence of somatostatin SST(2) receptor internalization in vivo after intravenous SOM230 application in the AR42J animal tumor model
    Beatrice Waser
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Berne, Switzerland
    Eur J Pharmacol 644:257-62. 2010
    ..These characteristics may point towards different tumor targeting but also to different desensitization properties of clinically applied SOM230...
  47. ncbi request reprint Selective in vitro targeting of GRP and NMB receptors in human tumours with the new bombesin tracer 177Lu-AMBA
    Beatrice Waser
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, P O Box 62, Murtenstrasse 31, 3010, Bern, Switzerland
    Eur J Nucl Med Mol Imaging 34:95-100. 2007
    ..To investigate the in vitro binding properties of a novel radiolabelled bombesin analogue, (177)Lu-AMBA, in human neoplastic and non-neoplastic tissues selected for their expression of the bombesin receptor subtypes GRP-R, NMB-R and BRS-3...
  48. ncbi request reprint Value of immunohistochemistry for somatostatin receptor subtype sst2A in cancer tissues: lessons from the comparison of anti-sst2A antibodies with somatostatin receptor autoradiography
    Meike Korner
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Bern, Bern, Switzerland
    Am J Surg Pathol 29:1642-51. 2005
    ..In conclusion, the commercially available SS-800 antibody promises to be useful for the routine immunohistochemical assessment of sst2A in formalin-fixed human tumors...
  49. pmc Agonist-biased signaling at the sst2A receptor: the multi-somatostatin analogs KE108 and SOM230 activate and antagonize distinct signaling pathways
    Renzo Cescato
    Division of Cell Biology, Institute of Pathology, University of Berne, Berne, Switzerland
    Mol Endocrinol 24:240-9. 2010
    ..Thus, SOM230 and KE108 are not somatostatin mimics, and their functional selectivity at sst2A receptors must be considered in clinical applications where it may have important consequences for therapy...
  50. ncbi request reprint GLP-1 receptor expression in human tumors and human normal tissues: potential for in vivo targeting
    Meike Korner
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Bern, Bern, Switzerland
    J Nucl Med 48:736-43. 2007
    ..Anticipating a major development of GLP-1 receptor targeting in nuclear medicine, our aim was to evaluate in vitro the GLP-1 receptor expression in a large variety of other tumors and to compare it with that in nonneoplastic tissues...
  51. ncbi request reprint Peptide receptors as molecular targets for cancer diagnosis and therapy
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, CH 3010 Berne, Switzerland
    Endocr Rev 24:389-427. 2003
    ..Other emerging and promising peptides and their respective receptors, including neurotensin, substance P, and neuropeptide Y, are introduced. This information relates to established and potential clinical applications in oncology...
  52. ncbi request reprint Procholecystokinin as marker of human Ewing sarcomas
    Jean Claude Reubi
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Switzerland
    Clin Cancer Res 10:5523-30. 2004
    ....
  53. doi request reprint High expression of gastrin-releasing peptide receptors in the vascular bed of urinary tract cancers: promising candidates for vascular targeting applications
    Achim Fleischmann
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Bern, CH 3010 Bern, Switzerland
    Endocr Relat Cancer 16:623-33. 2009
    ..Urinary tract cancers express vascular GRP-receptors so abundantly, that they are promising candidates for vascular targeting applications...
  54. ncbi request reprint Localization and characterization of neuropeptide receptors in human colon
    M Rettenbacher
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Bern, Switzerland
    Naunyn Schmiedebergs Arch Pharmacol 364:291-304. 2001
    ....
  55. doi request reprint High expression of neuropeptide Y1 receptors in ewing sarcoma tumors
    Meike Korner
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology of the University of Berne, Murtenstrasse 31, Berne, Switzerland
    Clin Cancer Res 14:5043-9. 2008
    ..Because NPY receptors are expressed in selected sarcoma cell lines and because novel treatment options are needed for sarcomas, this study assessed the NPY receptor in primary human sarcomas...
  56. ncbi request reprint Secretin receptors in the human liver: expression in biliary tract and cholangiocarcinoma, but not in hepatocytes or hepatocellular carcinoma
    Meike Korner
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Bern, Murtenstrasse 31, P O Box 62, CH 3010 Bern, Switzerland
    J Hepatol 45:825-35. 2006
    ..The secretin receptor expression was investigated in the human liver because the liver is a physiological secretin target and because novel diagnostic and treatment modalities are needed for liver cancer...
  57. ncbi request reprint Overexpression of gastrin-releasing peptide receptors in tumor-associated blood vessels of human ovarian neoplasms
    Achim Fleischmann
    Institute of Pathology, University of Berne, Switzerland
    Cell Oncol 29:421-33. 2007
    ..In this study, receptors for the gastrin-releasing peptide (GRP), and other members of the bombesin-family of peptides, were evaluated in ovarian neoplasms...
  58. doi request reprint Highly efficient in vivo agonist-induced internalization of sst2 receptors in somatostatin target tissues
    Bea Waser
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Berne, Switzerland
    J Nucl Med 50:936-41. 2009
    ..Although in vitro studies have shown ample evidence that the ligand-receptor complex is internalized, in vivo evidence of agonist-induced internalization of peptide receptors, such as somatostatin receptors, is missing...
  59. ncbi request reprint Expression of functional neurokinin-1 receptors in regenerative glands during gastric wound healing in rodents
    Adrian Schmassmann
    Gastrointestinal Unit, University Hospital, University of Berne, Switzerland
    Gastroenterology 126:784-95. 2004
    ..The aim of this study was to assess whether neurokinin-1 receptors play a role in gastric wound healing...
  60. ncbi request reprint Gastrin-releasing peptide receptors in normal and neoplastic human uterus: involvement of multiple tissue compartments
    Achim Fleischmann
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Murtenstrasse 31, P O Box 62, CH 3010 Berne, Switzerland
    J Clin Endocrinol Metab 90:4722-9. 2005
    ..However, information about the function of these neuropeptides and the incidence, distribution, density, and subtype of their receptors in human uterine tissues is scarce...
  61. pmc Design and in vitro characterization of highly sst2-selective somatostatin antagonists suitable for radiotargeting
    Renzo Cescato
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Berne, Switzerland
    J Med Chem 51:4030-7. 2008
    ....
  62. pmc GPR87 is an overexpressed G-protein coupled receptor in squamous cell carcinoma of the lung
    Mathias Gugger
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Bern, Murtenstrasse 31, 3010 Bern, Switzerland
    Dis Markers 24:41-50. 2008
    ..GPR87, LGR4 and CMKOR1 are orphan receptors. GPR87 stands out as a candidate for further target validation due to its marked overexpression and correlation on a mutation-based level to squamous cell carcinoma...
  63. ncbi request reprint High expression of neuropeptide y receptors in tumors of the human adrenal gland and extra-adrenal paraganglia
    Meike Korner
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology of the University of Bern, Bern, Switzerland
    Clin Cancer Res 10:8426-33. 2004
    ....
  64. ncbi request reprint Neuropeptide Y receptors in renal cell carcinomas and nephroblastomas
    Meike Korner
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Bern, Bern, Switzerland
    Int J Cancer 115:734-41. 2005
    ..With regard to clinical applications, NPY receptors may act as in vivo targets for receptor-directed therapy of RCCs and nephroblastomas for which alternative therapeutic approaches are still required...
  65. ncbi request reprint NPY receptors in human cancer: a review of current knowledge
    Meike Korner
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Bern, Murtenstrasse 31, PO Box 62, CH 3010 Bern, Switzerland
    Peptides 28:419-25. 2007
    ..Clinically, tumoral NPY receptors may be targeted with NPY analogs coupled with adequate radionuclides or cytotoxic agents for a scintigraphic tumor imaging and/or tumor therapy...
  66. ncbi request reprint CRF receptors in the rodent and human cardiovascular systems: species differences
    Beatrice Waser
    Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, PO Box 62, Murtenstrasse 31, CH 3010 Bern, Switzerland
    Peptides 27:3029-38. 2006
    ....
  67. ncbi request reprint Distribution of the VPAC2 receptor in peripheral tissues of the mouse
    Anthony J Harmar
    Division of Neuroscience, School of Biomedical and Clinical Laboratory Sciences, University of Edinburgh, United Kingdom EH8 9JZ
    Endocrinology 145:1203-10. 2004
    ....
  68. ncbi request reprint Biodistribution and catabolism of (18)F-labeled neurotensin(8-13) analogs
    Ralf Bergmann
    Institut fuer Bioanorganische und Radiopharmazeutische Chemie, Forschungszentrum Rossendorf, Germany
    Nucl Med Biol 29:61-72. 2002
    ..The catabolic pathways of the radiofluorinated peptides were elucidated. The results suggest that the high binding affinity to NTR1 and the stabilization against proteolytic degradation are not yet sufficient for tumor imaging by PET...
  69. doi request reprint Novel sst5-selective somatostatin dicarba-analogues: synthesis and conformation-affinity relationships
    Debora D'Addona
    Laboratory of Peptides and Proteins, Chemistry and Biology, Department of Organic Chemistry, University of Firenze, Via Lastruccia 13 I 50019, Sesto Fiorentino, Italy
    J Med Chem 51:512-20. 2008
    ..The presence of the bulky aromatic side chain of Tyr(Bzl)(10) favored the formation of a 3(10)-helix and enhanced the sst5 selectivity suppressing the sst2 affinity. Finally, a new pharmacophore model for the sst5 was developed...
  70. ncbi request reprint NODAGATOC, a new chelator-coupled somatostatin analogue labeled with [67/68Ga] and [111In] for SPECT, PET, and targeted therapeutic applications of somatostatin receptor (hsst2) expressing tumors
    Klaus Peter Eisenwiener
    Division of Radiological Chemistry, Institute of Nuclear Medicine, Department of Radiology, University Hospital, Petersgraben 4, CH 4031 Basel, Switzerland
    Bioconjug Chem 13:530-41. 2002
    ..The results indicate an improved biological behavior which is likely due to the fact that an additional spacer group separates the chelate from the pharmacophoric part of the somatostatin analogue...
  71. doi request reprint Glucagon-like peptide 1-receptor scans to localize occult insulinomas
    Damian Wild
    N Engl J Med 359:766-8. 2008
  72. ncbi request reprint Synthesis and evaluation of bombesin derivatives on the basis of pan-bombesin peptides labeled with indium-111, lutetium-177, and yttrium-90 for targeting bombesin receptor-expressing tumors
    Hanwen Zhang
    Division of Radiological Chemistry, Institute of Nuclear Medicine, Department of Radiology, University Hospital, Basel
    Cancer Res 64:6707-15. 2004
    ....
  73. ncbi request reprint Improvement of pharmacokinetics of radioiodinated Tyr(3)-octreotide by conjugation with carbohydrates
    Margret Schottelius
    Nuklearmedizinische Klinik und Poliklinik, Klinikum rechts der Isar, Technische Universitat Munchen, 81675 Munchen, Germany
    Bioconjug Chem 13:1021-30. 2002
    ..8 mg TOC/kg and gamma-camera imaging. Glycosylation proved to be a powerful tool for the development of high affinity sst ligands with excellent excretion profiles and improved tumor accumulation...
  74. ncbi request reprint [99mTc]Demobesin 1, a novel potent bombesin analogue for GRP receptor-targeted tumour imaging
    Berthold Nock
    Institute of Radioisotopes Radiodiagnostic Products, National Center for Scientific Research Demokritos, 15310 Ag Paraskevi, Attikis, Athens, Greece
    Eur J Nucl Med Mol Imaging 30:247-58. 2003
    ..24+/-0.67%ID/g was still observed in the tumour. The high and prolonged localization of [(99m)Tc]Demobesin 1 at the tumour site and its rapid background clearance are very promising qualities for GRP-R-targeted tumour imaging in man...
  75. ncbi request reprint Neurokinin-1 receptor expression and its potential effects on tumor growth in human pancreatic cancer
    Helmut Friess
    Department of General Surgery, University of Heidelberg, Germany
    Lab Invest 83:731-42. 2003
    ..These findings illustrate that the NK-1R pathway is activated in human pancreatic cancer and has the potential to contribute to cancer cell growth, thus suggesting the existence of a neuro-cancer cell interaction in vivo...
  76. ncbi request reprint Novel sst(4)-selective somatostatin (SRIF) agonists. 4. Three-dimensional consensus structure by NMR
    Christy Rani R Grace
    Structural Biology Laboratory and The Clayton Foundation Laboratories for Peptide Biology, The Salk Institute for Biological Studies, 10010 North Torrey Pines Road, La Jolla, CA 92037, USA
    J Med Chem 46:5606-18. 2003
    ..This motif is necessary and sufficient to explain the binding affinities of all of the analogues studied and is distinct from the existing model suggested for sst(2)/sst(5) selectivity...
  77. ncbi request reprint Novel sst(4)-selective somatostatin (SRIF) agonists. 3. Analogues amenable to radiolabeling
    Judit Erchegyi
    The Clayton Foundation Laboratories for Peptide Biology, The Salk Institute for Biological Studies, 10010 North Torrey Pines Road, La Jolla, CA 92037, USA
    J Med Chem 46:5597-605. 2003
    ..5 nM). (125)Iodinated 19 selectively binds to sst(4)-transfected cells but not to sst(1-3)- or sst(5)-transfected cells. Binding in sst(4)-transfected cells was completely displaced by SRIF-28 or the sst(4)-selective L-803,087...
  78. ncbi request reprint Novel sst(4)-selective somatostatin (SRIF) agonists. 2. Analogues with beta-methyl-3-(2-naphthyl)alanine substitutions at position 8
    Judit Erchegyi
    The Clayton Foundation Laboratories for Peptide Biology, The Salk Institute for Biological Studies, 10010 North Torrey Pines Road, La Jolla, CA 92037, USA
    J Med Chem 46:5587-96. 2003
    ..On the other hand, some of the diastereomers identified in this study, such as 5, 11, 17, and 19, are very potent ligands at all receptors but sst(1)...
  79. ncbi request reprint Novel sst(4)-selective somatostatin (SRIF) agonists. 1. Lead identification using a betide scan
    Jean Rivier
    The Clayton Foundation Laboratories for Peptide Biology, The Salk Institute for Biological Studies, 10010 North Torrey Pines Road, La Jolla, CA 92037, USA
    J Med Chem 46:5579-86. 2003
    ..These results suggested that the orientation of side chains at position 6, 7, or 11 with respect to the side chains of residues 8 and 9 may be independently responsible for sst(4) selectivity...
  80. pmc Ring size of somatostatin analogues (ODT-8) modulates receptor selectivity and binding affinity
    Judit Erchegyi
    The Clayton Foundation Laboratories for Peptide Biology and Structural Biology Laboratory, The Salk Institute for Biological Studies, 10010 North Torrey Pines Road, La Jolla, California 92037, USA
    J Med Chem 51:2668-75. 2008
    ..Interestingly and not unexpectedly, the 3D structures of these analogues comprised the pharmacophore for which the analogues had the highest binding affinities (i.e., sst 4 in all cases)...
  81. ncbi request reprint DOTA-PESIN, a DOTA-conjugated bombesin derivative designed for the imaging and targeted radionuclide treatment of bombesin receptor-positive tumours
    Hanwen Zhang
    Division of Radiological Chemistry, Department of Radiology, University Hospital Basel, Petersgraben 4, 4031 Basel, Switzerland
    Eur J Nucl Med Mol Imaging 34:1198-208. 2007
    ....
  82. ncbi request reprint Somatostatin receptor imaging in vivo by planar scintigraphy facilitates the diagnosis of canine insulinomas
    Oliver A Garden
    Department of Clinical Sciences, College of Veterinary Medicine, Cornell University, Ithaca, NY 14853, USA
    J Vet Intern Med 19:168-76. 2005
    ..111In-pentetreotide scintigraphy is a useful diagnostic adjunct to the clinical evaluation of the insulinoma patient, but is unable to localize the tumor in some cases...
  83. ncbi request reprint Modulation of pharmacokinetics of radioiodinated sugar-conjugated somatostatin analogues by variation of peptide net charge and carbohydration chemistry
    Margret Schottelius
    Nuklearmedizinische Klinik und Poliklinik, Klinikum rechts der Isar, Technische Universitat Munchen, 81675 Munchen, Germany
    Bioconjug Chem 16:429-37. 2005
    ..Taking into account the combined effects of the Gluc-S-moiety both on kidney and on tumor accumulation, this group seems to be a promising synthon for the synthesis of other radiolabeled peptide analogues with improved pharmacokinetics...
  84. pmc Radiolabeled somatostatin receptor antagonists are preferable to agonists for in vivo peptide receptor targeting of tumors
    Mihaela Ginj
    Division of Radiological Chemistry, Institute of Nuclear Medicine, Department of Radiology, University Hospital Basel, Petersgraben 4, CH 4031 Basel, Switzerland
    Proc Natl Acad Sci U S A 103:16436-41. 2006
    ..Antagonist radioligands for other peptide receptors need to be evaluated in nuclear oncology as a result of this paradigm shift...
  85. ncbi request reprint Ectopic growth hormone-releasing hormone secretion by a metastatic bronchial carcinoid tumor: a case with a non hypophysial intracranial tumor that shrank during long acting octreotide treatment
    Patricia Fainstein Day
    Department of Endocrinology and Nuclear Medicine, Hospital Italiano, Gascón 450 1187, Buenos Aires, Argentina
    Pituitary 10:311-9. 2007
    ..Total regression of pituitary enlargement was also observed. No changes were observed in lung and liver metastases. After 24 months of therapy the patient is asymptomatic and living a full and active life...
  86. ncbi request reprint Preclinical evaluation of new and highly potent analogues of octreotide for predictive imaging and targeted radiotherapy
    Mihaela Ginj
    Division of Radiological Chemistry, Department of Radiology, University Hospital Basel, Petersgraben 4, CH 4031 Basel, Switzerland
    Clin Cancer Res 11:1136-45. 2005
    ..The aim of this study was to develop novel analogues with a broader sstr profile for diagnostic (positron emission tomography and single-photon emission computed tomography) and radiotherapeutic applications...
  87. ncbi request reprint New sst4/5-selective somatostatin peptidomimetics based on a constrained tryptophan scaffold
    Debby Feytens
    Department of Organic Chemistry, Vrije Universiteit Brussel, Pleinlaan 2, B 1050, Brussels, Belgium
    J Med Chem 50:3397-401. 2007
    ..This study allowed us to identify a new highly potent sst5 agonist with good selectivity over the other receptors, except versus sst4...
  88. ncbi request reprint Somatostatin receptor 1 selective analogues: 4. Three-dimensional consensus structure by NMR
    Christy Rani R Grace
    Structural Biology Laboratory, The Salk Institute for Biological Studies, 10010 North Torrey Pines Road, La Jolla, California 92037, USA
    J Med Chem 48:523-33. 2005
    ..This motif is necessary and sufficient to explain the binding affinities of all of the analogues studied and is distinct from the existing models suggested for sst(4) as well as sst(2)/sst(5) selectivity...
  89. ncbi request reprint Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides
    Jean E Rivier
    The Clayton Foundation Laboratories for Peptide Biology, The Salk Institute, 10010 N Torrey Pines Road, La Jolla, California 92037, USA
    J Med Chem 48:515-22. 2005
    ..Binding affinity was decreased in all other cases with alternate bridging constraints such as cyclo (6-11), cyclo (6-12), and cyclo (7-11). Compound 45 is an agonist (EC(50) = 8.8 nM) in the adenylate cyclase assay...
  90. ncbi request reprint N-terminal sugar conjugation and C-terminal Thr-for-Thr(ol) exchange in radioiodinated Tyr3-octreotide: effect on cellular ligand trafficking in vitro and tumor accumulation in vivo
    Margret Schottelius
    Nuklearmedizinische Klinik und Poliklinik, Klinikum rechts der Isar, Technische Universitat Munchen, 81675 Munchen, Germany
    J Med Chem 48:2778-89. 2005
    ....
  91. ncbi request reprint Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan
    Judit Erchegyi
    The Clayton Foundation Laboratories for Peptide Biology, The Salk Institute, 10010 North Torrey Pines Road, La Jolla, California, 92037, USA
    J Med Chem 48:507-14. 2005
    ....
  92. ncbi request reprint [Lys40(Ahx-DTPA-111In)NH2]exendin-4, a very promising ligand for glucagon-like peptide-1 (GLP-1) receptor targeting
    Damian Wild
    Clinic and Institute of Nuclear Medicine, University Hospital Basel, Basel, Switzerland
    J Nucl Med 47:2025-33. 2006
    ..The goal of this study was to establish a tumor model for GLP-1 receptor targeting and to use a newly designed exendin-4-DTPA (DTPA is diethylenetriaminepentaacetic acid) conjugate for GLP-1 receptor targeting...
  93. doi request reprint New pansomatostatin ligands and their chelated versions: affinity profile, agonist activity, internalization, and tumor targeting
    Mihaela Ginj
    Division of Radiological Chemistry, University Hospital Basel, Basel, Switzerland
    Clin Cancer Res 14:2019-27. 2008
    ..Currently used targeting peptides mainly have sst2 affinity. We aimed at developing (radio)peptides that bind with high affinity to all receptor subtypes...
  94. ncbi request reprint 177Lu-AMBA: Synthesis and characterization of a selective 177Lu-labeled GRP-R agonist for systemic radiotherapy of prostate cancer
    Laura E Lantry
    Ernst Felder Laboratories, Bracco Research USA Inc, Princeton, New Jersey 08540 6608, USA
    J Nucl Med 47:1144-52. 2006
    ..We describe a new radiolabeled bombesin (BBN) analog for imaging and systemic radiotherapy that has improved pharmacokinetics (PK) and better retention of radioactivity in the tumor...
  95. ncbi request reprint Local targeting of malignant gliomas by the diffusible peptidic vector 1,4,7,10-tetraazacyclododecane-1-glutaric acid-4,7,10-triacetic acid-substance p
    Stefan Kneifel
    Clinic and Institute of Nuclear Medicine, University Hospitals, Basel, Switzerland
    Clin Cancer Res 12:3843-50. 2006
    ..The complex geometry of rapidly proliferating high-grade gliomas requires a diffusible system targeting tumor-associated surface structures to saturate the tumor, including its margins...
  96. ncbi request reprint Somatostatin receptors in nasopharyngeal carcinoma
    Kwok Seng Loh
    Department of Otolaryngology, Head and Neck Tumour Clinic, National University Hospital, Singapore
    Virchows Arch 441:444-8. 2002
    ..This study demonstrates for the first time the presence of type 2 SS-R in NPC. These receptors may play a role in the management of NPC, as is the case for other somatostatin-expressing tumours...
  97. pmc Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR
    Christy Rani R Grace
    Structural Biology Laboratory, The Clayton Foundation Laboratories for Peptide Biology, The Salk Institute for Biological Studies, 10010 N Torrey Pines Road, La Jolla, California 92037, USA
    J Med Chem 49:4487-96. 2006
    ..This pharmacophore is, therefore, different from that proposed by others for sst2/3/5 analogues...
  98. pmc Ring size in octreotide amide modulates differently agonist versus antagonist binding affinity and selectivity
    Christy Rani R Grace
    Structural Biology Laboratory, The Salk Institute for Biological Studies, 10010 North Torrey Pines Road, La Jolla, California 92037, USA
    J Med Chem 51:2676-81. 2008
    ..The 3D NMR structures of the analogues in dimethylsulfoxide are consistent with the observed binding affinities...
  99. ncbi request reprint 68Ga-DOTANOC: a first compound for PET imaging with high affinity for somatostatin receptor subtypes 2 and 5
    Damian Wild
    Clinic and Institute of Nuclear Medicine, University Hospital Basel, Petersgraben 4, 4031, Basel, Switzerland
    Eur J Nucl Med Mol Imaging 32:724. 2005
  100. ncbi request reprint Conformational analysis of a potent SSTR3-selective somatostatin analogue by NMR in water solution
    Margarida Gairi
    NMR Facility, Serveis Cientificotecnics, University of Barcelona, Barcelona Science Park, Josep Samitier 1 5, 08028 Barcelona, Spain
    J Pept Sci 12:82-91. 2006
    ..The structural determinant factors that could explain selectivity of peptide 1 for SSTR3 receptors are discussed...