PIKfyve, a FYVE finger -containing phosphoinositide kinase, is an enzyme that in humans is encoded by the PIKFYVE gene. [5][6] The principal enzymatic activity of PIKfyve is to phosphorylate PtdIns3P to PtdIns (3,5)P2.

2021年9月9日 · PIKfyve plays a critical role in the endosomal and lysosomal system, regulating membrane homeostasis, endosomal trafficking and autophagy (Toxicol. Appl. Pharmacol. 383, 114771; 2019), and is...

2024年12月25日 · This gene encodes an enzyme (PIKfyve; also known as phosphatidylinositol-3-phosphate 5-kinase type III or PIPKIII) that phosphorylates the D-5 position in PtdIns and phosphatidylinositol-3-phosphate (PtdIns3P) to make PtdIns5P and PtdIns (3,5)biphosphate.

2022年1月18日 · We show that PIKfyve controls recycling of cargoes including integrins, receptors that control cell migration. Furthermore, endogenous PIKfyve colocalizes with SNX17, Retriever, WASH, and CCC complexes on endosomes. Importantly, PIKfyve inhibition results in displacement of Retriever and CCC from endosomes.

2021年11月5日 · PIK001 is a novel chemical entity with demonstrable PIKfyve inhibition and cellular cytotoxicity on the same scale as APY0201. The specificity of PIK-001 was demonstrated against all tested kinases, GPCRs, ion channels, and enzymes.

2017年12月7日 · Introduction: PIKfyve is an endosomal lipid kinase that phosphorylates P1(3)P to phosphatidylinositol 3,5-bisphosphate (PI[3,5]P2). Unlike PI3Kδ-related signaling, PIKfyve regulates endosomal membrane trafficking and has a critical role in autophagy, which exposes damaged proteins to proteases (cathepsins) in autophagolysosomes.

2023年6月29日 · PI (3,5)P 2 is generated by the phosphoinositide 5-kinase PIKfyve, which is critical for phagosomal digestion and antimicrobial activity. However PI (3,5)P 2 dynamics and regulation remain unclear due to lack of reliable reporters.

2016年3月8日 · PIKFYVE is the PtdIns (3,5)P2-producing component of a trimolecular complex that tightly regulates the level of PtdIns (3,5)P2. Other components of this complex are the PIKFYVE activator VAC14 (604632) and the PtdIns (3,5)P2 phosphatase FIG4 …

2023年2月13日 · More recent interest in PIKfyve has surged due to some evidence showing efficacy of a PIKfyve inhibitor, Apilimod, against SARS-CoV-2 entry into cells. Here we will briefly summarize PIKfyve function and how inhibiting its activity may be …

2024年3月2日 · In immune cells, high PIKFYVE expression in DCs was associated with worse response to ICB. Genetic and pharmacological studies demonstrated that PIKfyve ablation enhanced DC function via selectively altering the alternate/non-canonical NF-κB pathway.