Results 31 to 40 of about 815 (149)

Synthesis of Insulin-Regulated Aminopeptidase (IRAP) inhibitors

, 2015
The need for alternative cognitive enhancers has risen due to the fact that clinical trial results of the drugs currently approved for treating these disorders have not been satisfactory. IRAP has become a possible drug target for treating cognitive impairment brought about by Alzheimer’s disease, head trauma or cerebral ischemia, among others.
Agalo, Faith
openaire   +2 more sources

Discovery of Selective Inhibitor Leads by Targeting an Allosteric Site in Insulin-Regulated Aminopeptidase

Pharmaceuticals, 2021
Insulin-Regulated aminopeptidase (IRAP) is a zinc-dependent aminopeptidase with several important biological functions and is an emerging pharmaceutical target for cognitive enhancement and immune system regulation.
Ioannis Temponeras, Lykourgos Chiniadis, Athanasios Papakyriakou, Efstratios Stratikos   +3 more
doaj   +1 more source

Stabilization of the open conformation οf insulin-regulated aminopeptidase by a novel substrate-selective small-molecule inhibitor. [PDF]

Protein Sci
Abstract Insulin‐regulated aminopeptidase (IRAP) is an enzyme with important biological functions and the target of drug‐discovery efforts. We combined in silico screening with a medicinal chemistry optimization campaign to discover a nanomolar inhibitor of IRAP based on a pyrazolylpyrimidine scaffold.
Mpakali A, Georgaki G, Buson A, Findlay AD, Foot JS, Mauvais FX, van Endert P, Giastas P, Hamprecht DW, Stratikos E.   +9 more
europepmc   +2 more sources

Discovery of Lomitapide as a Novel Mast Cell Regulatory Agent Through Chemical Library Screening. [PDF]

Eur J Immunol
Chemical library screening identified lomitapide as a novel mast cell (MC) regulatory agent. Lomitapide selectively inhibits IgE/Ag‐ or phorbol 12‐myristate 13‐acetate (PMA)/ionomycin‐mediated MC degranulation by altering plasma membrane dynamics, including endocytosis and membrane fusion. ABSTRACT Allergic diseases are a global health concern, and new
Mamorita S, Furukawa A, Nagata Y, Suzuki R.   +3 more
europepmc   +2 more sources

Phosphoproteomics for studying signaling pathways evoked by hormones of the renin-angiotensin system: A source of untapped potential. [PDF]

Acta Physiol (Oxf)
Abstract The Renin‐Angiotensin System (RAS) is a complex neuroendocrine system consisting of a single precursor protein, angiotensinogen (AGT), which is processed into various peptide hormones, including the angiotensins [Ang I, Ang II, Ang III, Ang IV, Ang‐(1–9), Ang‐(1–7), Ang‐(1–5), etc] and Alamandine‐related peptides [Ang A, Alamandine, Ala‐(1–5)],
Souza-Silva IM, Carregari VC, Steckelings UM, Verano-Braga T.   +3 more
europepmc   +2 more sources

Design and Synthesis of Angiotensin IV Peptidomimetics Targeting the Insulin-Regulated Aminopeptidase (IRAP)

, 2010
Peptidomimetics derived from the bioactive hexapeptide angiotensin IV (Ang IV, Val1-Tyr2-Ile3-His4-Pro5-Phe6) have been designed and synthesized. These peptidomimetics are aimed at inhibiting the insulin-regulated amino peptidase (IRAP), also known as the AT4 receptor. This membrane-bound zinc-metallopeptidase is currently under investigation regarding
Andersson, Hanna
openaire   +2 more sources

The Role of Insulin Regulated Aminopeptidase in Endocytic Trafficking and Receptor Signaling in Immune Cells

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   +1 more source

The intracellular helical bundle of human glucose transporter GLUT4 is important for complex formation with ASPL

FEBS Open Bio, Volume 13, Issue 11, Page 2094-2107, November 2023., 2023
Blood glucose levels must be tightly controlled. In fat cells, insulin enhances glucose uptake by stimulating exocytosis of GLUT4 from intracellular compartments resulting in increased GLUT4 levels at the plasma membrane. Here, we show that human GLUT4 binds to ASPL via its intercellular domain to control glucose uptake.
Peng Huang, Hannah Åbacka, Daniel Varela, Raminta Venskutonytė, Lotta Happonen, Jonathan S. Bogan, Pontus Gourdon, Mahmood R. Amiry‐Moghaddam, Ingmar André, Karin Lindkvist‐Petersson   +9 more
wiley   +1 more source

Up‐regulation of oxytocin receptors on peripheral sensory neurons mediates analgesia in chemotherapy‐induced neuropathic pain

British Journal of Pharmacology, Volume 180, Issue 13, Page 1730-1747, July 2023., 2023
Background and Purpose Chemotherapy‐induced neuropathic pain (CINP) currently has limited effective treatment. Although the roles of oxytocin (OXT) and the oxytocin receptor (OXTR) in central analgesia have been well documented, the expression and function of OXTR in the peripheral nervous system remain unclear.
Lixuan Li, Pupu Li, Jing Guo, Yifei Wu, Qian Zeng, Nan Li, Xiaoting Huang, Yongshen He, Wen Ai, Wuping Sun, Tao Liu, Donglin Xiong, Lizu Xiao, Yanyan Sun, Qiming Zhou, Haixia Kuang, Zilong Wang, Changyu Jiang   +17 more
wiley   +1 more source

Insulin-Regulated Aminopeptidase Inhibition Ameliorates Metabolism in Obese Zucker Rats

Frontiers in Molecular Biosciences, 2020
The aim of our study was to determine the influence of inhibition of insulin-regulated aminopeptidase/oxytocinase (IRAP) on glucose tolerance and metabolism of skeletal muscle and visceral adipose tissue in obese Zucker rats.
Katarina Krskova, Lucia Balazova, Viktoria Dobrocsyova, Rafal Olszanecki, Maciej Suski, Siew Yeen Chai, Štefan Zorad   +6 more
doaj   +1 more source