Discovery of Inhibitors of Insulin-Regulated Aminopeptidase as Cognitive Enhancers [PDF]
International Journal of Hypertension, 2012 The hexapeptide angiotensin IV (Ang IV) is a metabolite of angiotensin II (Ang II) and plays a central role in the brain. It was reported more than two decades ago that intracerebroventricular injection of Ang IV improved memory and learning in the rat ...
Hanna Andersson, Mathias Hallberg
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The role of insulin-regulated aminopeptidase in MHC class I antigen presentation [PDF]
Frontiers in Immunology, 2012 Production of MHC I ligands from antigenic proteins generally requires multiple proteolytic events. While the proteolytic steps required for antigen processing in the endogenous pathway are clearly established, persisting gaps of knowledge regarding ...
Peter M Van Endert, Loredana eSaveanu
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Benzylhydroxamic acids as inhibitors of insulin regulated aminopeptidase (IRAP)
European Journal of Medicinal Chemistry ReportsWith the objective of finding new classes of cognitive enhancers with potential for the treatment of neurodegenerative disorders, such as Alzheimer's disease, small molecule inhibitors of insulin-regulated aminopeptidase (IRAP) were designed and ...
Julia Beveridge +2 more
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The Role of Insulin Regulated Aminopeptidase in Endocytic Trafficking and Receptor Signaling in Immune Cells [PDF]
Frontiers in Molecular Biosciences, 2020 Insulin regulated aminopeptidase (IRAP) is a type II transmembrane protein with broad tissue distribution initially identified as a major component of Glut4 storage vesicles (GSV) in adipocytes.
Delphyne Descamps +9 more
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Structural Basis of Inhibition of Human Insulin-Regulated Aminopeptidase (IRAP) by Benzopyran-Based Inhibitors [PDF]
Frontiers in Molecular Biosciences, 2021 Inhibition of the insulin-regulated aminopeptidase (IRAP) improves memory and cognition in animal models. The enzyme has recently been crystallized and several series of inhibitors reported.
Sudarsana Reddy Vanga +4 more
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Macrocyclic peptidomimetics as inhibitors of insulin-regulated aminopeptidase (IRAP). [PDF]
RSC Med Chem, 2020 The IRAP inhibition of the macrocyclic peptide, HA-08 has been explored by analogue design coupled to molecular dynamics analysis.
Barlow N +11 more
europepmc +5 more sources
Inhibition of Insulin‐Regulated Aminopeptidase (IRAP) by Arylsulfonamides [PDF]
ChemistryOpen, 2014 AbstractThe inhibition of insulin‐regulated aminopeptidase (IRAP, EC 3.4.11.3) by angiotenesin IV is known to improve memory and learning in rats. Screening 10 500 low‐molecular‐weight compounds in an enzyme inhibition assay with IRAP from Chinese Hamster Ovary (CHO) cells provided an arylsulfonamide (N‐(3‐(1H‐tetrazol‐5‐yl)phenyl)‐4‐bromo‐5 ...
Ulrika Rosenström +2 more
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Structural Basis of Inhibition of Human Insulin-Regulated Aminopeptidase (IRAP) by Aryl Sulfonamides [PDF]
ACS Omega, 2018 The insulin-regulated aminopeptidase (IRAP) is a membrane-bound zinc metallopeptidase with many important regulatory functions. It has been demonstrated that inhibition of IRAP by angiotensin IV (Ang IV) and other peptides, as well as more druglike ...
Sudarsana Reddy Vanga +8 more
doaj +4 more sources
Development of cognitive enhancers based on inhibition of insulin-regulated aminopeptidase. [PDF]
BMC Neurosci, 2008 The peptides angiotensin IV and LVV-hemorphin 7 were found to enhance memory in a number of memory tasks and reverse the performance deficits in animals with experimentally induced memory loss. These peptides bound specifically to the enzyme insulin-regulated aminopeptidase (IRAP), which is proposed to be the site in the brain that mediates the memory ...
Chai SY +6 more
europepmc +9 more sources
Inhibition of Insulin-Regulated Aminopeptidase by Imidazo [1,5-α]pyridines—Synthesis and Evaluation [PDF]
International Journal of Molecular SciencesInhibition of Insulin-regulated Aminopeptidase (IRAP) has been shown to improve cognitive functions in several animal models. Recently, we performed a screening campaign identifying novel small-molecule based compounds acting as inhibitors of the ...
Karin Engen +2 more
exaly +3 more sources