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Bioconjug Chem. 2006 Mar-Apr;17(2):267-74.

Amphiphilic conjugates of human brain natriuretic peptide designed for oral delivery: in vitro activity screening.

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1
Nobex Corporation, 617 Davis Drive, Suite 100, Durham, North Carolina 27713, USA.

Abstract

Congestive heart failure (CHF) is a complex syndrome involving altered neurohormonal levels and impaired cardiac and renal function. In recent years, intravenous administration of exogenous human brain-type natriuretic peptide (hBNP) has become an important therapy in treating patients with acutely decompensated CHF. However, reports during the past year suggest that hBNP could play a prominent role in the chronic treatment of CHF patients as well. We are currently developing conjugates of hBNP suitable for oral delivery to provide a patient-friendly treatment option for chronic heart failure patients. In this report, we present in vitro activity results obtained from hBNP conjugates featuring a variety of rationally designed amphiphilic oligomers. Mapping studies revealed that the hydrophobic/hydrophilic balance of the oligomer impacted the regioselectivity of conjugation. Additionally, the regiochemistry and extent of conjugation had a significant impact on activity. Many monoconjugates retained activity comparable to native peptide and are currently under evaluation in subsequent in vivo screens.

PMID:
16536455
DOI:
10.1021/bc0501000
[Indexed for MEDLINE]

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