Hemolymph and tissue-bound peptidase-resistant analogs of the insect allatostatins.

Abstract:

:While neuropeptides of the allatostatin family inhibit in vitro production of juvenile hormone, which modulates aspects of development and reproduction in the cockroach, Diploptera punctata, they are susceptible to inactivation by peptidases in the hemolymph, gut, and bound to internal tissues. Patterns of peptidase cleavage were investigated in two allatostatin analogs in which sterically bulky components were incorporated into the active core region to block peptidase attack. The results were used to design and synthesize the first pseudopeptide analog of an insect neuropeptide resistant to degradation by both hemolymph and tissue-bound peptidases. This pseudotetrapeptide allatostatin mimetic analog represents a valuable tool to neuroendocrinologists studying mechanisms by which the natural peptides operate and the physiological consequences of challenging an insect with an allatostatin that is not readily degraded via peptidase enzymes. Disruption of critical physiological processes modulated by neuropeptides such as the allatostatins via peptidase-resistant mimetic analogs could form the basis for novel pest insect management strategies in the future.

journal_name

Peptides

journal_title

Peptides

authors

Nachman RJ,Garside CS,Tobe SS

doi

10.1016/s0196-9781(98)00149-1

subject

Has Abstract

pub_date

1999-01-01 00:00:00

pages

23-9

issue

1

eissn

0196-9781

issn

1873-5169

pii

S0196978198001491

journal_volume

20

pub_type

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