Results 11 to 20 of about 3,708 (156)

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
doaj   +7 more sources

Benzylhydroxamic acids as inhibitors of insulin regulated aminopeptidase (IRAP)

European Journal of Medicinal Chemistry Reports
With 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, Marcus Söderström, Rubén Prieto-Díaz, Hugo Gutierrez-de-Teran, Luke R. Odell, Mathias Hallberg, Mats Larhed, Johan Gising   +7 more
doaj   +6 more sources

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, Johan Åqvist, Anders Hallberg, Hugo Gutiérrez-de-Terán, Hugo Gutiérrez-de-Terán   +4 more
doaj   +3 more sources

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
doaj   +5 more sources

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, Vanga SR, Sävmarker J, Sandström A, Burns P, Hallberg A, Åqvist J, Gutiérrez-de-Terán H, Hallberg M, Larhed M, Chai SY, Thompson PE.   +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, Jonas Sävmarker, Thomas Lundbäck   +2 more
exaly   +7 more sources

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, Jonas Sävmarker, Leelee Ng, Mats Larhed, Mathias Hallberg, Johan Åqvist, Anders Hallberg, Siew Yeen Chai, Hugo Gutiérrez-de-Terán   +8 more
doaj   +5 more sources

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, Irini Evnouchidou, Irini Evnouchidou, Vivien Caillens, Carole Drajac, Sabine Riffault, Peter van Endert, Peter van Endert, Peter van Endert, Loredana Saveanu   +9 more
doaj   +2 more sources

The Role of GABA and Insulin Regulated Aminopeptidase on Insulin Resistance and GLUT4 in Prediabetes and Type 2 Diabetes Mellitus

مجله كليه طب الكندي
Background: Different proposed mechanisms for insulin resistance have been put forth to understand the relationship and changes in insulin resistance. Looking at the levels of insulin, the neurotransmitter gamma-aminobutyric acid, glucose transport type
Ismael Sadeq Khashan, Maysaa Jalal Majeed   +1 more
doaj   +3 more sources

Structural Basis of Inhibition of Insulin-Regulated Aminopeptidase by a Macrocyclic Peptidic Inhibitor. [PDF]

ACS Med Chem Lett, 2020
Insulin-regulated aminopeptidase (IRAP) is a transmembrane zinc metallopeptidase with many important biological functions and an emerging pharmacological target. Although previous structural studies have given insight on how IRAP recognizes linear peptides, how it recognizes its physiological cyclic ligands remains elusive.
Mpakali A, Saridakis E, Giastas P, Maben Z, Stern LJ, Larhed M, Hallberg M, Stratikos E.   +7 more
europepmc   +6 more sources