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Receptors | Angiotensin Receptors
The renin-angiotensin-aldosterone system (RAS) is a vital hormone-receptor system that regulates cardiovascular and renal functions. In this article, we discuss exciting new findings in the RAS field. Recently solved active state crystal structures of Angiotensin II type 1 (AT1R) and type 2 receptor (AT2R) helped in understanding receptor activation ...
Triveni R. Pardhi, Sadashiva S. Karnik
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An Introduction to Receptors and Receptor Disorders
SummaryIn the last decade reliable methods have been introduced to quantitate and characterize receptors for hormones and other biologically interesting ligands. Applied initially to hormone receptors on malignant cells and to androgen-resistant and insulin-resistant states, these methods have led to the identification of many disease processes where ...
J. Roth+8 more
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Of the established Ca2+-mobilizing messengers, NAADP is arguably the most tantalizing. It is the most potent, often efficacious at low nanomolar concentrations, and its receptors undergo dramatic desensitization. Recent studies have identified a new class of calcium-release channel, the two-pore channels (TPCs), as the likely targets for NAADP ...
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Pyruvate kinase M2 (PKM2) mainly catalyzes glycolysis, but it also exerts non-glycolytic functions in several cancers. While it has been shown to interact with the human papillomavirus 16 (HPV16) E7 oncoprotein, the functional significance of PKM2 in HPV-
Seoung-Ae Lee+4 more
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Exploring the kinetic selectivity of drugs targeting the β1‐adrenoceptor
In this study, we report the β1‐adrenoceptor binding kinetics of several clinically relevant β1/2‐adrenoceptor (β1/2AR) agonists and antagonists. [3H]‐DHA was used to label CHO‐β1AR for binding studies. The kinetics of ligand binding was assessed using a
David A. Sykes+5 more
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Lipoxins (LXs) represent a class of arachidonic acid (AA) metabolites that carry potent immunoregulatory and anti-inflammatory properties, LXA4and LXB4being the main components of this series. LXs are generated by cooperation between 5-lipoxygenase (LO) and 12- or 15-LO during cell-cell interactions or by single cell types. LX epimers at carbon 15, the
ROMANO, Mario+2 more
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Current strategies in engaging oncolytic viruses with antitumor immunity
Oncolytic virotherapy has produced promising yet limited results in preclinical and clinical studies. Besides direct oncolytic activity, a significant therapeutic mechanism of oncolytic virotherapy is the induction of tumor-specific immunity ...
Drew Ashton Boagni+2 more
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Perspectives on the Trypanosoma cruzi-host cell receptor interaction [PDF]
Chagas disease is caused by the parasite Trypanosoma cruzi. The critical initial event is the interaction of the trypomastigote form of the parasite with host receptors. This review highlights recent observations concerning these interactions.
A Belley+108 more
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Hearing relies on the transduction of sound-evoked vibrations into electrical signals, occurring in the stereocilia bundle of inner ear hair cells. The G protein-coupled receptor (GPCR) ADGRV1 and the multi-PDZ protein PDZD7 play a critical role in the ...
Baptiste Colcombet-Cazenave+11 more
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Synthesis, biological evaluation, and SAR studies of 14β-phenylacetyl substituted 17-cyclopropylmethyl-7, 8-dihydronoroxymorphinones derivatives : Ligands with mixed NOP and opioid receptor profile [PDF]
© 2018 Kumar, Polgar, Cami-Kobeci, Thomas, Khroyan, Toll and Husbands.A series of 14β-acyl substituted 17-cyclopropylmethyl-7,8-dihydronoroxymorphinone compounds has been synthesized and evaluated for affinity and efficacy for mu (MOP), kappa (KOP), and ...
Cami-Kobeci+47 more
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