Molecular and Cellular Oncogenesis Program, The Wistar Institute, Philadelphia, PA 19104, USA.
Department of Biomedical Engineering, Northwestern University, Evanston, IL 60208, USA.
Sci Transl Med. 2015 Jun 3;7(290):290ra92. doi: 10.1126/scitranslmed.3010228.
Whereas amphibians regenerate lost appendages spontaneously, mammals generally form scars over the injury site through the process of wound repair. The MRL mouse strain is an exception among mammals because it shows a spontaneous regenerative healing trait and so can be used to investigate proregenerative interventions in mammals. We report that hypoxia-inducible factor 1α (HIF-1α) is a central molecule in the process of regeneration in adult MRL mice. The degradation of HIF-1α protein, which occurs under normoxic conditions, is mediated by prolyl hydroxylases (PHDs). We used the drug 1,4-dihydrophenonthrolin-4-one-3-carboxylic acid (1,4-DPCA), a PHD inhibitor, to stabilize constitutive expression of HIF-1α protein. A locally injectable hydrogel containing 1,4-DPCA was designed to achieve controlled delivery of the drug over 4 to 10 days. Subcutaneous injection of the 1,4-DPCA/hydrogel into Swiss Webster mice that do not show a regenerative phenotype increased stable expression of HIF-1α protein over 5 days, providing a functional measure of drug release in vivo. Multiple peripheral subcutaneous injections of the 1,4-DPCA/hydrogel over a 10-day period led to regenerative wound healing in Swiss Webster mice after ear hole punch injury. Increased expression of the HIF-1α protein may provide a starting point for future studies on regeneration in mammals.
虽然两栖动物会自发地再生失去的附肢,但哺乳动物通常会通过伤口修复过程在受伤部位形成疤痕。MRL 小鼠品系是哺乳动物中的一个例外,因为它表现出自发的再生愈合特性,因此可用于研究哺乳动物中的促再生干预措施。我们报告称,缺氧诱导因子 1α(HIF-1α)是成年 MRL 小鼠再生过程中的一个核心分子。在正常氧条件下,HIF-1α 蛋白的降解是由脯氨酰羟化酶(PHD)介导的。我们使用了一种名为 1,4-二氢苯并噻吩-4-酮-3-羧酸(1,4-DPCA)的 PHD 抑制剂,以稳定 HIF-1α 蛋白的组成型表达。设计了一种局部可注射的含有 1,4-DPCA 的水凝胶,以实现药物在 4 至 10 天内的控制释放。将 1,4-DPCA/水凝胶皮下注射到不表现出生殖表型的瑞士 Webster 小鼠中,可在 5 天内稳定地增加 HIF-1α 蛋白的表达,从而提供了体内药物释放的功能衡量标准。在 10 天内多次进行外周皮下注射 1,4-DPCA/水凝胶,可导致瑞士 Webster 小鼠在耳孔穿孔损伤后实现再生性伤口愈合。HIF-1α 蛋白的表达增加可能为哺乳动物再生的未来研究提供一个起点。