Results 1 to 10 of about 815 (149)

The Discovery of Insulin-Regulated Aminopeptidase (IRAP) Inhibitors: A Literature Review [PDF]

Frontiers in Pharmacology, 2020
Insulin-Regulated Aminopeptidase (IRAP, EC 3.4.11.3) is a multi-tasking member of the M1 family of zinc aminopeptidases. Among its diverse biological functions, IRAP is a regulator of oxytocin levels during late stages of pregnancy, it affects cellular ...
Dimitris Georgiadis, Angeliki Ziotopoulou, Eleni Kaloumenou, Angelos Lelis, Antonia Papasava   +4 more
doaj   +9 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 inhibitors, improves cognition in several rodent models.
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   +9 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   +6 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

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

Comparative study of Dapagliflozin versus Glimepiride effect on insulin regulated aminopeptidase (IRAP) and interleukin-34 (IL-34) in patient with type 2 diabetes mellitus [PDF]

Scientific Reports, 2023
Type 2 diabetes mellitus (T2DM) is one of the most common diseases, that managed by several medications such as Glimepiride and Dapagliflozin. This study aims to compare the effects of Dapagliflozin versus Glimepiride on glycemic control, insulin ...
Rania Zekry, Gamal A. Omran, Nashwa M. El-Gharbawy, Rehab H. Werida   +3 more
doaj   +4 more sources

Sex- and time-dependent role of insulin regulated aminopeptidase in lipopolysaccharide-induced inflammation [PDF]

Frontiers in Immunology
The enzyme, insulin regulated aminopeptidase (IRAP), is expressed in multiple immune cells such as macrophages, dendritic cells and T cells, where it plays a role in regulating the innate and adaptive immune response.
Anika Vear, Anika Vear, Amlan Chakraborty, Amlan Chakraborty, Farnaz Fahimi, Dorota Ferens, Robert Widdop, Chrishan S. Samuel, Tracey Gaspari, Peter M. van Endert, Peter M. van Endert, Siew Yeen Chai   +11 more
doaj   +4 more sources

Author Correction: Comparative study of Dapagliflozin versus Glimepiride effect on insulin regulated aminopeptidase (IRAP) and interleukin-34 (IL-34) in patient with type 2 diabetes mellitus [PDF]

Scientific Reports, 2023
Rania Zekry, Gamal A. Omran, Nashwa M. El-Gharbawy, Rehab H. Werida   +3 more
doaj   +3 more sources

Vasopressin is a physiological substrate for the insulin-regulated aminopeptidase IRAP [PDF]

American Journal of Physiology - Endocrinology and Metabolism, 2007
Insulin-regulated aminopeptidase (IRAP) is a membrane aminopeptidase and is homologous to the placental leucine aminopeptidase, P-LAP. IRAP has a wide distribution but has been best characterized in adipocytes and myocytes. In these cells, IRAP colocalizes with the glucose transporter GLUT4 to intracellular vesicles and, like GLUT4, translocates from ...
Susanna R Keller
exaly   +3 more sources