bpV (phen), a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50 s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV (phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV (phen) strongly induces the secretion of a large number of chemokines and pro...

BpV (HOpic) 是一种有效的和选择性的 PTEN 抑制剂， IC50 值为 14 nM。 Nanocarrier-BpV (HOpic) 具有神经保护作用。

2021年1月18日 · Phosphatase and Tensin Homolog on chromosome 10 (PTEN) antagonizes PI3K activity by dephosphorylating PIP3, thus suppressing PI3K/AKT signaling that could prevent IR induced cytotoxicity. The...

2025年1月15日 · Our study highlights the complexity of PTEN inhibition by first-generation compounds and their limitations, such as low specificity, adverse effects and non-specific mechanisms of action, and emphasizes the need for developing more selective and potent PTEN inhibitors with improved efficacy and well-defined mechanisms of actions.

2015年1月1日 · Here we investigate the inhibition of PTEN by four available PTEN inhibitors, bpV (phen), bpV (pic), VO-OHpic and SF1670 and compared this inhibition with that of only 3 other related enzymes, the tyrosine phosphatase SHP1 and the phosphoinositide phosphatases INPP4A and INPP4B.

2024年7月29日 · Mxene-bpV, through PTEN inhibition and Akt activation, was more effective than bpV (HOpic) alone in reducing cerebral infarct sizes and promoting brain function recovery after MCAO/R injury in mice.

2004年5月21日 · The tumour suppressor phosphatase and tensin homologue deleted on chromosome 10 (PTEN) shares homology with protein tyrosine phosphatases (PTPases). Similarly, bisperoxovanadium (bpV) molecules that are well-established PTPase inhibitors were shown to inhibit PTEN, but at up to 100-fold lower concentrations.

2024年7月3日 · 生物活性： BpV (HOpic) 是一种 有效的 选择性 PTEN 抑制剂， IC50 为 14 nM。 Nanocarrier-BpV (HOpic)具有神经保护活性 [1] [2]。 IC50 和靶标：IC50：14 nM (PTEN)。 体外： BpV (HOpic) (1 µM) 处理在接受顺铂处理的 MG63 细胞中增加细胞增殖并降低凋亡率 [3]。

在具有肾缺血/再灌注损伤的小鼠模型中，通过bpV (HOpic)抑制PTEN可加速其肾功能不全以及促进肾小管损伤。 PTEN的抑制可加强肾小管细胞的凋亡，这一过程与caspase-3的过度激活相关。 此外，抑制PTEN可加强中性粒细胞和巨噬细胞浸润入缺血/再灌注损伤的肾脏中，同时促炎性分子的表达增强 [3]。 [1] Schmid AC, et al. FEBS Lett. 2004, 566 (1-3):35-8. [2] Dimchev GA, et al. J Muscle Res Cell Motil. 2013 May;34 (2):125-36. [3] Jun Zhou, et al. Sci Rep. 2017, 7: 9503.

Our study highlights the complexity of PTEN inhibition by first-generation compounds and their limitations, such as low specificity, adverse effects and non-specific mechanisms of action, and emphasizes the need for developing more selective and potent PTEN inhibitors with improved efficacy and well-defined mechanisms of actions.