ArticleProceedings of the National Academy of Sciences of the United States of America2000
Antagonistic actions of analogs related to growth hormone-releasing hormone (GHRH) on receptors for GHRH and vasoactive intestinal peptide on rat pituitary and pineal cells in vitro.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2000. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 33 citations in OpenAlex.
- A Molecular Dynamics Study of Vasoactive Intestinal Peptide Receptor 1 and the Basis of Its Therapeutic Antagonism.International journal of molecular sciences · 2019Article
- Atrazine binds to the growth hormone-releasing hormone receptor and affects growth hormone gene expression.Environmental health perspectives · 2010Article
- Growth hormone-releasing hormone as an agonist of the ghrelin receptor GHS-R1a.Proceedings of the National Academy of Sciences of the United States of America · 2008Article
- Circadian expression of Bmal1 and serotonin-N-acetyltransferase mRNAs in chicken retina cells and pinealocytes in vivo and in vitro.Journal of molecular neuroscience : MN · 2006Article
- Two tyrosine residues in the first transmembrane helix of the human vasoactive intestinal peptide receptors play a role in supporting the active conformation.British journal of pharmacology · 2002Article
- Expression of a splice variant of the receptor for GHRH in 3T3 fibroblasts activates cell proliferation responses to GHRH analogs.Proceedings of the National Academy of Sciences of the United States of America · 2002Article
- Human renal cell carcinoma expresses distinct binding sites for growth hormone-releasing hormone.Proceedings of the National Academy of Sciences of the United States of America · 2000Article
- Isolation and sequencing of cDNAs for splice variants of growth hormone-releasing hormone receptors from human cancers.Proceedings of the National Academy of Sciences of the United States of America · 2000Article
- Growth hormone-releasing hormone antagonists counteract hydrogen peroxide - induced paracellular hyperpermeability in endothelial cells.Growth hormone & IGF research : official journal of the Growth Hormone Research Society and the International IGF Research SocietyArticle
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Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Peptide analogs of growth hormone-releasing hormone (GHRH) can potentially interact with vasoactive intestinal peptide (VIP) receptors (VPAC(1)-R and VPAC(2)-R) because of the structural similarities of these two hormones and their receptors. We synthesized four new analogs related to GHRH (JV-1-50, JV-1-51, JV-1-52, and JV-1-53) with decreased GHRH antagonistic activity and increased VIP antagonistic potency. To characterize various peptide analogs for their antagonistic activity on receptors for GHRH and VIP, we developed assay systems based on superfusion of rat pituitary and pineal cells. Receptor-binding affinities of peptides to the membranes of these cells were also evaluated by radioligand competition assays. Previously reported GHRH antagonists JV-1-36, JV-1-38, and JV-1-42 proved to be selective for GHRH receptors, because they did not influence VIP-stimulated VPAC(2) receptor-dependent prolactin release from pituitary cells or VPAC(1) receptor-dependent cAMP efflux from pinealocytes but strongly inhibited GHRH-stimulated growth hormone (GH) release. Analogs JV-1-50, JV-1-51, and JV-1-52 showed various degrees of VPAC(1)-R and VPAC(2)-R antagonistic potency, although also preserving a substantial GHRH antagonistic effect. Analog JV-1-53 proved to be a highly potent VPAC(1) and VPAC(2) receptor antagonist, devoid of inhibitory effects on GHRH-evoked GH release. The antagonistic activity of these peptide analogs on processes mediated by receptors for GHRH and VIP was consistent with the binding affinity. The analogs with antagonistic effects on different types of receptors expressed on tumor cells could be utilized for the development of new approaches to treatment of various human cancers.
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