Results 131 to 140 of about 815 (149)

Potent Macrocyclic Inhibitors of Insulin-Regulated Aminopeptidase (IRAP) by Olefin Ring-Closing Metathesis

Journal of Medicinal Chemistry, 2011
Macrocyclic analogues of angiotensin IV (Ang IV, Val(1)-Tyr(2)-Ile(3)-His(4)-Pro(5)-Phe(6)) targeting the insulin-regulated aminopeptidase (IRAP) have been designed, synthesized, and evaluated biologically. Replacement of His(4)-Pro(5)-Phe(6) by a 2-(aminomethyl)phenylacetic acid (AMPAA) moiety and of Val(1) and Ile(3) by amino acids bearing olefinic ...
Andersson, H, Demaegdt, Heidi, Johnsson, A., Vauquelin, Georges, Lindeberg, G., Hallberg, M., Erdélyi, M., Karlen, A., Hallberg, A.   +8 more
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Reproduction and maternal behavior in insulin-regulated aminopeptidase (IRAP) knockout mice

Peptides, 2009
During human pregnancy, a circulating form of insulin-regulated aminopeptidase (IRAP EC 3.4.11.3), often termed oxytocinase or placental leucine aminopeptidase (PLAP), is present in plasma. It is proposed that circulating IRAP plays an important role in regulating the circulating levels of oxytocin and/or vasopressin during pregnancy.
Vi Pham, Anthony L Albiston, Holly R Yeatman   +2 more
exaly   +3 more sources

Disulfide Cyclized Tripeptide Analogues of Angiotensin IV as Potent and Selective Inhibitors of Insulin-Regulated Aminopeptidase (IRAP)

Journal of Medicinal Chemistry, 2010
The insulin-regulated aminopeptidase (IRAP) localized in areas of the brain associated with memory and learning is emerging as a new promising therapeutic target for the treatment of memory dysfunctions. The angiotensin II metabolite angiotensin IV (Ang IV, Val(1)-Tyr(2)-Ile(3)-His(4)-Pro(5)-Phe(6)) binds with high affinity to IRAP and inhibits this ...
Andersson, H, Demaegdt, Heidi, Vauquelin, Georges, Lindeberg, G., Karlen, A., Hallberg, M., Erdélyi, M., Hallberg, A.   +7 more
openaire   +4 more sources

Identification of insulin-regulated aminopeptidase (IRAP) in the rat pineal gland and the modulation of melatonin synthesis by angiotensin IV

Brain Research, 2019
A local renin-angiotensin system (RAS) has been postulated in the pineal gland. In addition to angiotensin II (Ang II), other active metabolites have been described. In this study, we aimed to investigate a role for Ang IV in melatonin synthesis and the presence of its proposed (IRAP)/AT4 receptor (insulin-regulated aminopeptidase) in the pineal gland.
Wilson Mitsuo Tatagiba Kuwabara, Fernanda Gaspar do Amaral, Rafael Peres   +2 more
exaly   +3 more sources

The insulin‐regulated aminopeptidase IRAP is colocalised with GLUT4 in the mouse hippocampus – potential role in modulation of glucose uptake in neurones?

European Journal of Neuroscience, 2008
AbstractIt is proposed that insulin‐regulated aminopeptidase (IRAP) is the site of action of two peptides, angiotensin IV and LVV‐hemorphin 7, which have facilitatory effects on learning and memory. In fat and muscles, IRAP codistributes with the insulin‐responsive glucose transporter GLUT4 in specialised vesicles, where it plays a role in the ...
Ruani N Fernando, Anthony L Albiston
exaly   +4 more sources

Cyclic insulin‐regulated aminopeptidase (IRAP)/AT₄ receptor ligands

Journal of Peptide Science, 2006
AbstractThe angiotensin IV receptor (AT4 receptor) is the insulin‐regulated aminopeptidase enzyme (IRAP, EC 3.4.11.3). This membrane‐spanning enzyme belongs to the M1 family of zinc‐dependent metallo‐peptidases. It has been proposed that AT4 receptor ligands exert their physiological effects by binding to the active site of IRAP and thereby inhibiting ...
Axen, A., Lindberg, G., Demaegdt, Heidi, Vauquelin, Georges, Karlen, A., Hallberg, M.   +5 more
openaire   +3 more sources

Insulin-regulated aminopeptidase (IRAP) is required for appropriate dilution of urine after an acute water load

Physiology, 2023
Study Objective: Understand the response to acute water load in mice lacking the insulin-regulated aminopeptidase (IRAP). Hypothesis: IRAP degrades vasopressin in vivo, therefore, mice lacking IRAP would have impaired ability to dilute urine and to excrete water. Methods: Age matched 8–10-week-old IRAP WT and KO male mice were used for all experiments.
Yvonne Zuchowski, Joshua Carty, Jonathan Trapani, Fabian Bock, Andrew Terker, Mingzhi Zhang, Raymond Harris, Juan Pablo Arroyo   +7 more
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Alpha-1-Adrenergic Receptor Blockade Modifies Insulin-Regulated Aminopeptidase (IRAP) Activity in Rat Prostate and Modulates Oxytocin Functions

Drug Metabolism Letters, 2011
Oxytocin (OT) is one of the important paracrine factors that prostate synthesizes. OT maintains its resting tone and stimulates its contractile activity. However, the involvement of OT in modulating cell proliferation of the prostate is being investigated. In fact, alterations in OT concentrations accompany both benign prostatic hyperplasia/hypertrophy
Marcela Arrazola, Saníger, María Jesús, Ramírez-Expósito, Susana, de la Chica, María Pilar, Carrera-González, María Dolores, Mayas, José, Manuel Martínez-Martos   +5 more
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Insulin-regulated aminopeptidase/placental leucil Aminopeptidase (IRAP/P-lAP) and angiotensin IV-forming activities are modified in serum of rats with breast cancer induced by N-methyl-nitrosourea.

Anticancer research, 2006
In previous reports, changes in oxytocinase activity in human breast cancer tissue and in the serum of N-methyl-nitrosourea (NMU)-induced rat mammary tumors were described. Insulin-regulated aminopeptidase (IRAP) has been identified with oxytocinase and has also been referred to as placental leucine aminopeptidase (P-LAP).The IRAP/P-LAP activity in rat
María, Pilar Carrera, María Jesús, Ramírez-Expósito, Basilio, Dueñas, María, Dolores Mayas, María, Jesús García, Susana, De la Chica, Pedro, Cortés, María, Ruíz-Sanjuan, José Manuel, Martínez-Martos   +8 more
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Insulin regulated aminopeptidase (IRAP) – A novel target to combat diabetes-induced cardiovascular and renal disease.

New strategies are needed to combat diabetes-induced heart and kidney disease. We have identified a novel target, called insulin regulated aminopeptidase (IRAP), and have developed new drugs that inhibit the action of IRAP. This study demonstrated that treatment with our novel drugs was more effective than use of a current gold standard of care ...
openaire   +1 more source