Furthermore, an overview is given of the clinically approved medications, the potential naturally isolated inhibitors, and the synthesised candidates which were tested either in-vitro, in-vivo and/or clinically. Finally, we outline the in-silico attempts which were carried out using virtual screening...
Mechanism of Action Receptor Pharmacology Receptors Transport receptors Data availability No datasets were generated or analysed during the current study. Abbreviations AR-C 69931: 2-(Propylthio)adenosine-5’-O-(β,γ-difluoromethylene)triphosphate tetrasodium salt ATP: adenosine triphosphate cAMP...
P. Inflammasomes: mechanism of action, role in disease, and therapeutics. Nat. Med. 21, 677–687 (2015). PubMed PubMed Central Google Scholar Lamkanfi, M. & Dixit, V. M. Mechanisms and functions of inflammasomes. Cell 157, 1013–1022 (2014). CAS PubMed Google Scholar Swanson, K...
Mechanistically, P2Y12 expression was induced by transforming growth factor β1 (TGF-β1) and promoted MMT via the Smad3-dependent mechanism. Thus, silencing or pharmacological inhibition of P2Y12 was capable of inhibiting TGF-β/Smad3-mediated MMT and progressive renal fibrosis in vivo and in ...
3. Purinergic Receptors’ Mechanism of Action: Thienopyridine vs. Nonthienopyridine P2Y12 Inhibitors One of the fundamental tenets of contemporary antiplatelet therapy is the inhibition of ADP-mediated platelet activation and aggregation via the P2Y12 receptor. A significant obstacle to the efficacy of ...
As P2Y12 inhibitors are now used routinely in the clinic, our data suggests that this class of anti- platelet agent may be a therapeutic option to prevent tumour metastasis in specific cancers. Abbreviations CTCs: Circulating tumour cells; EMT: Epithelial-mesenchymal transition; TGF-β: ...
onset of action than clopidogrel. The objectives of this review are to discuss the limitations of clopidogrel, and describe alternative P2Y12 inhibitors and the clinical implications of the introduction of these new medicines. Pharmacology of P2Y12 inhibitors...
The depressant action of extracellular ATP was significantly reduced by diphenyleneiodonium chloride and 4-(2-aminoethyl)-benzenesulfonyl fluoride hydrochloride, two structurally different inhibitors of NADPH oxidase, indicating that this enzyme indeed mediates the action of ATP. Since the location and ...
It inhibits platelet aggregation by irreversibly blocking the adenosine diphosphate P2Y12 receptor. Ticagrelor, Cangrelor and Enilogrel represent the last generation of thienopyridines. This review is focused on the effects of adenosine diphosphate P2Y12 inhibitors. 展开 ...
Understanding the pharmacodynamic effects of platelet inhibitors is standard for developing more effective antithrombotic therapies. An example is the antithrombotic treatment of acute coronary syndrome (ACS), in particular ST-elevated myocardial infarction (STEMI) patients who are in need for rapid acting...