Document Detail


Incretin analogues that have been developed to treat type 2 diabetes hold promise as a novel treatment strategy for Alzheimer's disease.
MedLine Citation:
PMID:  20337586     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Analogues of the incretins Glucagon-like peptide 1 (GLP-1) and Glucose-dependent insulinotropic peptide (GIP) have been developed to treat type 2 diabetes mellitus. They are protease resistant and have a longer biological half life than the native peptides. Some of these novel analogues can cross the blood-brain barrier, have neuroprotective effects, activate neuronal stem cells in the brain, and can improve cognition. The receptors for GIP and GLP-1 are expressed in neurons, and both GIP and GLP-1 are expressed and released as transmitters by neurons. GIP analogues such as DAla(2)GIP and GLP-1 analogues such as liraglutide enhance synaptic plasticity in the brain and also reverse the betaamyloid induced impairment of synaptic plasticity. In mouse models of Alzheimer's disease, GLP-1 analogues Val(8)GLP-1 and liraglutide prevent memory impairment and the block of synaptic plasticity in the brain. Since two GLP- 1 analogues exendin-4 (Exenatide, Byetta) and liraglutide (Victoza) are already on the market as treatments for Type 2 diabetes, and others are in late stage clinical trials, these drugs show promise as treatments for neurodegenerative diseases such as Alzheimer's disease. Currently, there are three patents covering native GLP-1 and different GLP-1 analogues and one patent for the use of GIP and different GIP analogues for the treatment of neurodegenerative diseases.
Authors:
Christian Holscher
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  Recent patents on CNS drug discovery     Volume:  5     ISSN:  2212-3954     ISO Abbreviation:  Recent Pat CNS Drug Discov     Publication Date:  2010 Jun 
Date Detail:
Created Date:  2010-06-03     Completed Date:  2010-09-07     Revised Date:  2011-11-10    
Medline Journal Info:
Nlm Unique ID:  101265656     Medline TA:  Recent Pat CNS Drug Discov     Country:  United Arab Emirates    
Other Details:
Languages:  eng     Pagination:  109-17     Citation Subset:  IM    
Affiliation:
School of Biomedical Sciences, Ulster University, Cromore road, Coleraine BT52 1SA, UK. c.holscher@ulster.ac.uk
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MeSH Terms
Descriptor/Qualifier:
Alzheimer Disease / drug therapy*
Amino Acid Sequence
Animals
Blood-Brain Barrier / metabolism
Diabetes Mellitus, Type 2 / drug therapy*
Gastric Inhibitory Polypeptide / analogs & derivatives,  pharmacology,  therapeutic use*
Glucagon-Like Peptide 1 / analogs & derivatives,  pharmacology,  therapeutic use*
Humans
Incretins / therapeutic use*
Models, Neurological
Molecular Sequence Data
Neuroprotective Agents / pharmacology,  therapeutic use*
Patents as Topic
Chemical
Reg. No./Substance:
0/Incretins; 0/Neuroprotective Agents; 59392-49-3/Gastric Inhibitory Polypeptide; 89750-14-1/Glucagon-Like Peptide 1

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