Results 71 to 80 of about 815 (149)

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

, 2016
Macrocyclic analogues of angiotensin IV (Ang IV, Val1-Tyr2-Ile3-His4-Pro5-Phe6) targeting the insulin-regulated aminopeptidase (IRAP) have been designed, synthesized, and evaluated biologically.
Hanna Andersson (1408987), Mathias Hallberg (1656958), Anders Karlén (1281249), Gunnar Lindeberg (492163), Anders Johnsson (2193301), Anders Hallberg (585061), Heidi Demaegdt (470499), Georges Vauquelin (2136157), Máté Erdélyi (1364241)   +8 more
core   +1 more source

Structure‐guided discovery of aminopeptidase ERAP1 variants capable of processing antigens with novel PC anchor specificities

Immunology, Volume 171, Issue 1, Page 131-145, January 2024.
Altering a single amino acid at the SC specificity site of ERAP1, such as the V737R mutant, results in a change of substrate preference from a hydrophobic to a negatively charged PC anchor residue; the latter is presumed to be a poor substrate for WT ERAP1.
Suchita Pande, Hwai‐Chen Guo
wiley   +1 more source

The clinical course and pathophysiological investigation of adolescent gestational diabetes insipidus: a case report

BMC Endocrine Disorders, 2018
Background Gestational diabetes insipidus (GDI) is a rare endocrine complication during pregnancy that is associated with vasopressinase overproduction from the placenta.
Tatsuya Kondo, Miwa Nakamura, Sayaka Kitano, Junji Kawashima, Takeshi Matsumura, Takashi Ohba, Munekage Yamaguchi, Hidetaka Katabuchi, Eiichi Araki   +8 more
doaj   +1 more source

Binding to and Inhibition of Insulin-Regulated Aminopeptidase (IRAP) by Macrocyclic Disulfides Enhances Spine Density

, 2016
Angiotensin IV (Ang IV) and related peptide analogues, as well as non-peptide inhibitors of insulin-regulated aminopeptidase (IRAP), have previously been shown to enhance memory and cognition in animal models.
Lundback, Thomas, Hallberg, Mathias,, Nylander, Erik,, Pham, Vi, Engen, Karin,, Larhed, Mats,, Diwakarla, Shanti,, Sävmarker, Jonas,, Åqvist, Johan,, Grönbladh, Alfhild,, Andersson, Hanna,, Rosenström, Ulrika,, Gutierrez-de-Teran, Hugo,, Shamsudin Khan, Yasmin,, Jenmalm-Jensen, Annika, Reddy Vanga, Sudarsana,, Ng, Leelee, Yeen Chai, Siew   +17 more
core   +1 more source

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

, 2016
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.
Hanna Andersson (1408987), Mathias Hallberg (1656958), Anders Karlén (1281249), Gunnar Lindeberg (492163), Anders Hallberg (585061), Heidi Demaegdt (470499), Georges Vauquelin (2136157), Máté Erdélyi (1364241)   +7 more
core   +1 more source

Discovery of Inhibitors of Insulin-Regulated Aminopeptidase as Cognitive Enhancers

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   +1 more source

Hypothalamus–pituitary–thyroid axis disruption in rats with breast cancer is related to an altered endogenous oxytocin/insulin-regulated aminopeptidase (IRAP) system

Tumor Biology, 2011
Associations of breast cancer with diseases of the thyroid have been repeatedly reported, but the mechanism underlying this association remains to be elucidated. It has been reported that oxytocin (OXT) attenuates the thyroid-stimulating hormone (TSH) release in response to thyrotrophin-releasing hormone (TRH) and decreased plasma levels of TSH as well
María Pilar, Carrera-González, María Jesús, Ramírez-Expósito, Jose Manuel Arias, de Saavedra, Rafael, Sánchez-Agesta, María Dolores, Mayas, Jose Manuel, Martínez-Martos   +5 more
openaire   +2 more sources

Angiotensin II type 1 receptor blocker losartan prevents and rescues cerebrovascular, neuropathological and cognitive deficits in an Alzheimer’s disease model

Neurobiology of Disease, 2014
Angiotensin II (AngII) receptor blockers that bind selectively AngII type 1 (AT1) receptors may protect from Alzheimer’s disease (AD). We studied the ability of the AT1 receptor antagonist losartan to cure or prevent AD hallmarks in aged (~18 months at ...
Brice Ongali, Nektaria Nicolakakis, Xin-Kang Tong, Tahar Aboulkassim, Panayiota Papadopoulos, Pedro Rosa-Neto, Clotilde Lecrux, Hans Imboden, Edith Hamel   +8 more
doaj   +1 more source

Microwave Heated Flow Synthesis of Spiro-oxindole Dihydroquinazolinone Based IRAP Inhibitors

, 2014
A fast and convenient synthetic route towards spiro-oxindole dihydroquinazolinones as novel and drug-like insulin-regulated aminopeptidase (IRAP) inhibitors is reported. The synthesis is performed using a MW heated continuous flow system employing 200 mm
Lundbäck, Thomas, Wannberg, Johan,, Savmarker, J, Engen, Karin,, Larhed, Mats,, Sävmarker, Jonas,, Larhed, M, Rosenström, Ulrika,, Engen, K, Wannberg, J, Jenmalm-Jensen, A, Lundback, T, Jenmalm-Jensen, Annika, Rosenstrom, U   +13 more
core   +1 more source

Characterisation of the paradigms used to assess IRAP inhibitors as novel cognitive enhancing agents

, 2019
There are few effective cognitive enhancing agents available. Insulin-regulated aminopeptidase (IRAP, a protein in the brain) is an attractive target and IRAP inhibitors have already been shown to improve memory, however the mechanism remains unknown ...
BENJAMIN SEYER (5070041)
core   +1 more source