ArticleProceedings of the National Academy of Sciences of the United States of America1999
Mapping the active site in vasoactive intestinal peptide to a core of four amino acids: neuroprotective drug design.
Article in Proceedings of the National Academy of Sciences of the United States of America, 1999. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
17 citing papers in PubMed, 60 citations in OpenAlex.
- Therapeutic Potential of Vasoactive Intestinal Peptide and its Derivative Stearyl-Norleucine-VIP in Inflammation-Induced Osteolysis.Frontiers in pharmacology · 2021Article
- Protective Effects of Pituitary Adenylate Cyclase-Activating Polypeptide and Vasoactive Intestinal Peptide Against Cognitive Decline in Neurodegenerative Diseases.Frontiers in cellular neuroscience · 2020Article
- ADNP Regulates Cognition: A Multitasking Protein.Frontiers in neuroscience · 2018Article
- Adenylyl cyclase activating polypeptide reduces phosphorylation and toxicity of the polyglutamine-expanded androgen receptor in spinobulbar muscular atrophy.Science translational medicine · 2016Article
- Agnathan VIP, PACAP and their receptors: ancestral origins of today's highly diversified forms.PloS one · 2012Article
- Neuropeptide GPCRs in neuroendocrinology: the case of activity-dependent neuroprotective protein (ADNP).Frontiers in endocrinology · 2012Article
- VIP-PACAP 2010: my own perspective on modulation of cognitive and emotional behavior.Journal of molecular neuroscience : MN · 2010Article
- VIP, from gene to behavior and back: summarizing my 25 years of research.Journal of molecular neuroscience : MN · 2008Article
- Select cognitive deficits in vasoactive intestinal peptide deficient mice.BMC neuroscience · 2008Article
- Structure-activity relationship of vasoactive intestinal peptide (VIP): potent agonists and potential clinical applications.Naunyn-Schmiedeberg's archives of pharmacology · 2008Review
- Neonatal mice of the Down syndrome model, Ts65Dn, exhibit upregulated VIP measures and reduced responsiveness of cortical astrocytes to VIP stimulation.Journal of molecular neuroscience : MN · 2006Article
- NAP: research and development of a peptide derived from activity-dependent neuroprotective protein (ADNP).CNS drug reviews · 2005Review
- Apolipoprotein E knockout mice as a model of behavioral dysfunction.Journal of molecular neuroscience : MN · 2004Article
- From vasoactive intestinal peptide (VIP) through activity-dependent neuroprotective protein (ADNP) to NAP: a view of neuroprotection and cell division.Journal of molecular neuroscience : MN · 2003Review
- VIP and peptides related to activity-dependent neurotrophic factor protect PC12 cells against oxidative stress.Journal of molecular neuroscience : MN · 2000Article
- VIP-Related protection against lodoacetate toxicity in pheochromocytoma (PC12) cells: a model for ischemic/hypoxic injury.Journal of molecular neuroscience : MN · 2000Article
- A new concept in the pharmacology of neuroprotection.Journal of molecular neuroscience : MNReview
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The understanding of the molecular mechanisms leading to peptide action entails the identification of a core active site. The major 28-aa neuropeptide, vasoactive intestinal peptide (VIP), provides neuroprotection. A lipophilic derivative with a stearyl moiety at the N-terminal and norleucine residue replacing the Met-17 was 100-fold more potent than VIP in promoting neuronal survival, acting at femtomolar-picomolar concentration. To identify the active site in VIP, over 50 related fragments containing an N-terminal stearic acid attachment and an amidated C terminus were designed, synthesized, and tested for neuroprotective properties. Stearyl-Lys-Lys-Tyr-Leu-NH2 (derived from the C terminus of VIP and the related peptide, pituitary adenylate cyclase activating peptide) captured the neurotrophic effects offered by the entire 28-aa parent lipophilic derivative and protected against beta-amyloid toxicity in vitro. Furthermore, the 4-aa lipophilic peptide recognized VIP-binding sites and enhanced choline acetyltransferase activity as well as cognitive functions in Alzheimer's disease-related in vivo models. Biodistribution studies following intranasal administration of radiolabeled peptide demonstrated intact peptide in the brain 30 min after administration. Thus, lipophilic peptide fragments offer bioavailability and stability, providing lead compounds for drug design against neurodegenerative diseases.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.