An Active Insect Kinin Analog with 4-Aminopyroglutamate, A Novel cis-Peptide Bond, Type VI beta-Turn Motif
Abstract
The insect kinins are potent diuretic peptides that preferentially form a cis-Pro, type VI beta-turn. An insect kinin analog containing (2S,4S)-4-aminopyroglutamate, a novel cis-peptide bond, type VI beta-turn motif, demonstrates significant activity in the physiological range in a cricket diuretic assay. This is the first instance of a 4-aminopyroglutamate analog of a peptide with a preference for a type VI turn that demonstrates significant bioactivity. The results provide further confirmatory evidence for the active conformation of the insect kinins, and a new scaffold with which to design biostable, peptidomimetic analogs capable of disrupting critical insect kinin-regulated processes in insects.
Document Details
- Document Type
- Technical Report
- Publication Date
- Jan 01, 2004
- Accession Number
- ADA512080
Entities
People
- Geoffrey M. Coast
- Howard J. Williams
- Janusz Zabrocki
- Krzysztof Kaczmarek
- Ronald J. Nachman