PTEN antagonist多肽 (PAP4)

TVEEPSNPEASSSTSVTPGRKKRRQRRRPQ

Thr-Val-Glu-Glu-Pro-Ser-Asn-Pro-Glu-Ala-Ser-Ser-Ser-Thr-Ser-Val-Thr-Pro-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Pro-Gln

30

95.4

C₁₃₉H₂₄₁N₅₃O₄₈

3422.78

固相合成

PTEN antagonist peptide (PAP4) is a 30-amino acid peptide designed to inhibit phosphatase and tensin homolog (PTEN), a central neuron-intrinsic inhibitor of axon growth potential that operates via the phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin (mTOR) pathway. PAP4 binds to the C-terminal portion of PTEN, resulting in PTEN inhibition and can cross the blood-brain barrier. In a chronic model of cervical contusion spinal cord injury, systemic administration of PAP4 promoted robust growth of descending bulbospinal rVRG axons within the denervated portion of the phrenic motor neuron (PhMN) pool located caudal to the injury site.

PAP4 treatment led to a significant increase in both the number and total length of rVRG axon profiles in the phrenic nucleus region, with a 5-8 fold increase in axon numbers compared to control conditions. This axonal growth was associated with partial recovery of diaphragm motor activity, as measured by electromyography (EMG) amplitude, though this functional effect depended on the anesthetic regimen used during recording. The observed axon growth occurred in a region critical for controlling diaphragmatic respiratory function, suggesting PAP4 can stimulate significant re-growth of damaged respiratory neural circuitry in a chronic injury setting.

一般情况下， PTEN antagonist多肽 (PAP4) 粉末应该保存在-20甚至-70摄氏度. PTEN antagonist多肽 (PAP4) 溶解后应该-70摄氏度分装保存，避免反复冻融. 了解更多细节，请查阅手册:多肽溶解及保存指南

• Ohtake Y, Park D, Muneer PMA, Li H, Xu B, Sharma K, Smith GM, Selzer ME, Li S. The effect of systemic PTEN antagonist peptides on axon growth and functional recovery after spinal cord injury. Biomaterials. 2014 May;35(16):4610-26. doi: 10.1016/j.biomaterials.2014.02.037. Epub 2014 Mar 12. PMID: 24630093; PMCID: PMC4195449.
• Michel-Flutot P, Cheng L, Thomas SJ, Lisi B, Schwartz H, Lam S, Lyttle M, Jaffe DA, Smith G, Li S, Wright MC, Lepore AC. PTEN inhibition promotes robust growth of bulbospinal respiratory axons and partial recovery of diaphragm function in a chronic model of cervical contusion spinal cord injury. bioRxiv [Preprint]. 2024 Jan 11:2024.01.10.575021. doi: 10.1101/2024.01.10.575021. Update in: Exp Neurol. 2024 Aug;378:114816. doi: 10.1016/j.expneurol.2024.114816. PMID: 38260313; PMCID: PMC10802567.

三氟乙酸（Trifluoroacetic acid，简称 TFA）是高效液相色谱（简称 HPLC）纯化过程中常用的反离子。TFA 的存在可能会对肽的净重量、外观及溶解度产生影响，具体如下：

对净重量的影响：TFA 盐会增加产物的总质量。在大多数情况下，肽的含量占总重量的 80% 以上，剩余部分则为 TFA。

对溶解度的影响：TFA 盐通常能提高肽在水溶液中的溶解度。

在生物检测中的影响：对于大多数标准的体外检测，残留的 TFA 水平一般不会造成干扰。但需注意，在高灵敏度的细胞研究或生化研究中，需关注其存在可能带来的影响。

干品多肽的重量中不仅仅包含多肽，还包含有一些非肽的组份，如水、被吸收的溶剂、配位离子和盐等。肽的净含量是指肽在其中的重量百分比，这个百分比的数值范围很大，可能从50%到90%，取决于纯度、序列以及合成和纯化的方法，不要将肽的净含量和肽的纯度混为一谈，他们是两个完全不同的概念。纯度通常是通过HPLC测定的。纯度定义的是多肽样品中含正确序列的组分的百分比，而肽的净含量是指样品中肽类物质相对于总物质所占的百分比，肽的净含量通常是氨基酸组分分析或紫外分光法测定的，这个信息主要是在一些对肽的浓度很敏感的实验中，对计算肽的浓度是很重要的。