NFAT Inhibitor is a cell-permeable peptide inhibitor of nuclear factor of activated T cells (NFAT) that selectively inhibits calcineurin-mediated dephosphorylation of NFAT[1]. NFAT inhibitors inhibit the transcriptional activity of NFAT by directly binding to the NFAT protein and interfering with its binding to DNA, thereby affecting the expression of related genes[2]. The NFAT protein family plays a key role in immune responses, primarily regulating the transcription of cytokine genes and other genes that are important to immune responses[3][4]. NFAT Inhibitor is commonly used in immunology and cardiovascular-related research[5][6].
In vitro, NFAT inhibitor (1µM; 48h) significantly decreased NFAT-driven transcriptional activity and inhibited the expression of endogenous NFAT-target genes such as COX2, c-MYC, and CCND1 in LN229 glioma cells[7].
References:
[1] Aramburu J, Yaffe MB, López-Rodríguez C, Cantley LC, Hogan PG, Rao A. Affinity-driven peptide selection of an NFAT inhibitor more selective than cyclosporin A. Science. 1999;285(5436):2129-2133.
[2] Ma JD, Jing J, Wang JW, et al. Activation of the Peroxisome Proliferator-Activated Receptor γ Coactivator 1β/NFATc1 Pathway in Circulating Osteoclast Precursors Associated With Bone Destruction in Rheumatoid Arthritis. Arthritis Rheumatol. 2019;71(8):1252-1264.
[3] Macian F. NFAT proteins: key regulators of T-cell development and function. Nat Rev Immunol. 2005;5(6):472-484.
[4] Martínez-Martínez S, Redondo JM. Inhibitors of the calcineurin/NFAT pathway. Curr Med Chem. 2004;11(8):997-1007.
[5] Yu H, van Berkel TJ, Biessen EA. Therapeutic potential of VIVIT, a selective peptide inhibitor of nuclear factor of activated T cells, in cardiovascular disorders. Cardiovasc Drug Rev. 2007;25(2):175-187.
[6] Samuelsson AM, Bayer AL, Li J, et al. Targeting of CIP4-Calcineurin Signalosomes Improves Cardiac Structure and Function After Myocardial Infarction. Preprint. bioRxiv. 2025;2025.05.12.653597.
[7] Ellert-Miklaszewska A, Szymczyk A, Poleszak K, Kaminska B. Delivery of the VIVIT Peptide to Human Glioma Cells to Interfere with Calcineurin-NFAT Signaling. Molecules. 2021;26(16):4785.
NFAT inhibitor是活化T细胞核因子（NFAT）的细胞渗透性肽抑制剂，选择性抑制钙调磷酸酶介导的NFAT的去磷酸化[1]。NFAT Inhibitor通过直接结合NFAT蛋白，干扰其与DNA的结合，从而抑制NFAT的转录活性，进而影响相关基因的表达[2]。NFAT蛋白家族在免疫反应中起着关键作用，主要调节细胞因子基因和其他对免疫反应至关重要的基因的转录[3][4]。NFAT Inhibitor通常用于免疫和心血管相关研究[5][6]。
在体外实验中，NFAT inhibitor（1μM；48小时）显著降低了LN229胶质瘤细胞中NFAT驱动的转录活性，并抑制了内源性NFAT靶基因（如COX2、c-MYC和CCND1）的表达[7]。