Differential Effects of Endomorphin-1, Endomorphin-2, and Tyr-W-MIF-1 on Activation of G-Proteins in SH-SY5Y Human Neuroblastoma Membranes

Differential Effects of Endomorphin-1, Endomorphin-2, and Tyr-W-MIF-1 on Activation of G-Proteins... Endomorphin-1 (Tyr-Pro-Trp-Phe-NH 2 ) and endomorphin-2 (Tyr-Pro-Phe-Phe-NH 2 ), peptides recently isolated from bovine and human brain, have high affinity and selectivity for μ opiate receptors. They share sequence similarity with the endogenous opiate-modulating peptide Tyr-W-MIF-1 (Tyr-Pro-Trp-Gly-NH 2 ). The efficacies of these endogenous peptides and of the enkephalin analog DAMGO were compared by measuring their effects on the binding of guanosine-5′- O -(γ-( 35 S)thio)triphosphate (( 35 S)GTPγS) to G-proteins in membranes from SH-SY5Y human neuroblastoma cells. DAMGO, endomorphin-1, and endomorphin-2 stimulated ( 35 S)GTPγS binding dose dependently, with maximal effects of 60 ± 9%, 47 ± 9%, and 43 ± 6% stimulation above basal and ED 50 of 49 ± 8 n M , 38 ± 8 n M , and 64 ± 13 n M , respectively. Tyr-W-MIF-1 showed only a small stimulation of binding (5% stimulation above basal, ED 50 = 2 μ M ). When given in combination with the other opioids, however, Tyr-W-MIF-1 attenuated their ability to activate G-proteins. Thus, the endogenous opioids endomorphin-1 and endomorphin-2 activate G-proteins similarly to the synthetic agonist DAMGO, but the structurally similar peptide Tyr-W-MIF-1 produces only minimal stimulation of G-proteins. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Peptides Elsevier

Differential Effects of Endomorphin-1, Endomorphin-2, and Tyr-W-MIF-1 on Activation of G-Proteins in SH-SY5Y Human Neuroblastoma Membranes

Loading next page...
 
/lp/elsevier/differential-effects-of-endomorphin-1-endomorphin-2-and-tyr-w-mif-1-on-4gpQznOcxQ
Publisher site
See Article on Publisher Site

Abstract

Endomorphin-1 (Tyr-Pro-Trp-Phe-NH 2 ) and endomorphin-2 (Tyr-Pro-Phe-Phe-NH 2 ), peptides recently isolated from bovine and human brain, have high affinity and selectivity for μ opiate receptors. They share sequence similarity with the endogenous opiate-modulating peptide Tyr-W-MIF-1 (Tyr-Pro-Trp-Gly-NH 2 ). The efficacies of these endogenous peptides and of the enkephalin analog DAMGO were compared by measuring their effects on the binding of guanosine-5′- O -(γ-( 35 S)thio)triphosphate (( 35 S)GTPγS) to G-proteins in membranes from SH-SY5Y human neuroblastoma cells. DAMGO, endomorphin-1, and endomorphin-2 stimulated ( 35 S)GTPγS binding dose dependently, with maximal effects of 60 ± 9%, 47 ± 9%, and 43 ± 6% stimulation above basal and ED 50 of 49 ± 8 n M , 38 ± 8 n M , and 64 ± 13 n M , respectively. Tyr-W-MIF-1 showed only a small stimulation of binding (5% stimulation above basal, ED 50 = 2 μ M ). When given in combination with the other opioids, however, Tyr-W-MIF-1 attenuated their ability to activate G-proteins. Thus, the endogenous opioids endomorphin-1 and endomorphin-2 activate G-proteins similarly to the synthetic agonist DAMGO, but the structurally similar peptide Tyr-W-MIF-1 produces only minimal stimulation of G-proteins.

Journal

PeptidesElsevier

Published: Apr 1, 1998

References

  • Analgesic effects of Tyr-W-MIF-1
    Gergen, K.A.; Zadina, J.E.; Paul, D.

You’re reading a free preview. Subscribe to read the entire article.


DeepDyve is your
personal research library

It’s your single place to instantly
discover and read the research
that matters to you.

Enjoy affordable access to
over 18 million articles from more than
15,000 peer-reviewed journals.

All for just $49/month

Explore the DeepDyve Library

Search

Query the DeepDyve database, plus search all of PubMed and Google Scholar seamlessly

Organize

Save any article or search result from DeepDyve, PubMed, and Google Scholar... all in one place.

Access

Get unlimited, online access to over 18 million full-text articles from more than 15,000 scientific journals.

Your journals are on DeepDyve

Read from thousands of the leading scholarly journals from SpringerNature, Elsevier, Wiley-Blackwell, Oxford University Press and more.

All the latest content is available, no embargo periods.

See the journals in your area

DeepDyve

Freelancer

DeepDyve

Pro

Price

FREE

$49/month
$360/year

Save searches from
Google Scholar,
PubMed

Create folders to
organize your research

Export folders, citations

Read DeepDyve articles

Abstract access only

Unlimited access to over
18 million full-text articles

Print

20 pages / month

PDF Discount

20% off