Literature DB >> 7714762

Superactive lipophilic peptides discriminate multiple vasoactive intestinal peptide receptors.

I Gozes1, G Lilling, R Glazer, A Ticher, I E Ashkenazi, A Davidson, S Rubinraut, M Fridkin, D E Brenneman.   

Abstract

To distinguish vasoactive intestinal peptide (VIP) receptors in the brain-mediating neurotransmission and neurotrophism, potent VIP analogues were designed. Using a single amino acid substitution and the addition of a fatty acyl moiety, an analogue was devised that exhibited both a 100-fold greater potency than VIP and specificity for a VIP receptor associated with neuronal survival. This VIP agonist increased neuronal survival via a cAMP-independent mechanism. Identical chemical modification of a prototype VIP antagonist (Met-Hybrid, Neurotensin6-11-VIP7-28) also resulted in a 100-fold greater potency in blocking VIP-mediated increases in neuronal survival. Blockade of circadian activity rhythms was limited to VIP antagonists that could inhibit VIP-mediated increases in cAMP. These lipophilic peptides provide novel tools in receptor discrimination and drug design.

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Year:  1995        PMID： 7714762

Source DB:  PubMed          Journal:  J Pharmacol Exp Ther        ISSN： 0022-3565            Impact factor:   4.030


  32 in total

1.  (N-stearyl, norleucine17)VIPhybrid is a broad spectrum vasoactive intestinal peptide receptor antagonist.

Authors:  Terry W Moody; Robert T Jensen; Mati Fridkin; Illana Gozes
Journal:  J Mol Neurosci       Date:  2002 Feb-Apr       Impact factor: 3.444

2.  Overexpression of the human VPAC2 receptor in the suprachiasmatic nucleus alters the circadian phenotype of mice.

Authors:  S Shen; C Spratt; W J Sheward; I Kallo; K West; C F Morrison; C W Coen; H M Marston; A J Harmar
Journal:  Proc Natl Acad Sci U S A       Date:  2000-10-10       Impact factor: 11.205

3.  VIP-PACAP 2010: my own perspective on modulation of cognitive and emotional behavior.

Authors:  Illana Gozes
Journal:  J Mol Neurosci       Date:  2010-11       Impact factor: 3.444

4.  VIP, from gene to behavior and back: summarizing my 25 years of research.

Authors:  Illana Gozes
Journal:  J Mol Neurosci       Date:  2008-07-08       Impact factor: 3.444

Review 5.  Neuroprotection in experimental stroke with targeted neurotrophins.

Authors:  Dafang Wu
Journal:  NeuroRx       Date:  2005-01

6.  Lipophilization of somatostatin analog RC-160 improves its bioactivity and stability.

Authors:  P Dasgupta; A T Singh; R Mukherjee
Journal:  Pharm Res       Date:  1999-07       Impact factor: 4.200

7.  A femtomolar-acting neuroprotective peptide.

Authors:  D E Brenneman; I Gozes
Journal:  J Clin Invest       Date:  1996-05-15       Impact factor: 14.808

Review 8.  A VIP hybrid antagonist: from developmental neurobiology to clinical applications.

Authors:  I Gozes; M Fridkin; D E Brenneman
Journal:  Cell Mol Neurobiol       Date:  1995-12       Impact factor: 5.046

9.  Protection against developmental deficiencies by a lipophilic VIP analogue.

Authors:  I Gozes; M Bachar; A Bardea; A Davidson; S Rubinraut; M Fridkin
Journal:  Neurochem Res       Date:  1998-05       Impact factor: 3.996

10.  Vasoactive intestinal peptide (VIP) regulates activity-dependent neuroprotective protein (ADNP) expression in vivo.

Authors:  Eliezer Giladi; Joanna M Hill; Efrat Dresner; Conor M Stack; Illana Gozes
Journal:  J Mol Neurosci       Date:  2007-10-02       Impact factor: 3.444
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