Absence of binding of targeted analogs of somatostatin carrying cytotoxic radicals or radionuclides to growth hormone secretagogue receptors on human myocardium

Gabor Halmos, Andrew V. Schally, Ana Maria Comaru-Schally, Attila Nagy, Anand Irimpen

Research output: Contribution to journalArticle

2 Scopus citations

Abstract

Various peripheral human tissues express receptors for growth hormone secretagogue (GHS), the highest density being in the myocardium. It was also reported that some octapeptide analogs of somatostatin (SRIH) can displace radiolabeled Tyr-Ala-hexarelin from GHS receptors on the human pituitary and heart. Thus, it is possible that radionuclide analogs of SRIH such as OctreoScan® and recently developed cytotoxic SRIH analogs containing doxorubicin (DOX) intended for targeted tumor therapy, could bind to these GHS receptors, compromising the safety of compounds of this type. Therefore, we determined the binding of OctreoScan® and two cytotoxic SRIH analogs consisting of octapeptide carrier RC-121 and DOX (AN-162) or 2-pyrrolino-DOX (AN-238) to human myocardium specimens. None of these compounds displayed specific binding to the human heart indicating that the clinical use of SRIH analogs linked to anthracyclines or radionuclides should not be associated with increased cardiac side effects.

Original languageEnglish (US)
Pages (from-to)2669-2674
Number of pages6
JournalLife Sciences
Volume72
Issue number23
DOIs
StatePublished - Apr 25 2003
Externally publishedYes

Keywords

  • Growth hormone secretagogue receptors
  • Human myocardium
  • Targeted somatostatin analogs

ASJC Scopus subject areas

  • Pharmacology

Fingerprint Dive into the research topics of 'Absence of binding of targeted analogs of somatostatin carrying cytotoxic radicals or radionuclides to growth hormone secretagogue receptors on human myocardium'. Together they form a unique fingerprint.

  • Cite this