Majuelos-Melguizo Jara, Rodríguez-Vargas José Manuel, Martínez-López Nuria, Delgado-Bellido Daniel, García-Díaz Ángel, Yuste Víctor J, García-Macía Marina, López Laura M, Singh Rajat, Oliver F J
Department of Immunology and Cell Biology, Institute of Parasitology and Biomedicine "López-Neyra", IPBLN, CSIC, CIBERONC, 18016 Granada, Spain.
Department of Biochemistry, Autonomous University of Madrid (UAM), 'Alberto Sols' Biomedical Research Institute (CSIC-UAM), 28029 Madrid, Spain.
Cancers (Basel). 2022 Jan 30;14(3):726. doi: 10.3390/cancers14030726.
Glioblastoma multiforme (GBM) is the most common and aggressive primary brain tumor in adults. Poly (ADP-ribose) polymerase inhibitors (PARPi) represent a new class of anti-neoplastic drugs. In the current study, we have characterized the mechanism by which glioblastoma cells evade the effect of PARPi as anti-tumor agents. We have found that suppression of PARP activity exerts an anti-stemness effect and has a dual impact on autophagy, inducing its activation in the first 24 h (together with down-regulation of the pro-survival mTOR pathway) and preventing autophagosomes fusion to lysosomes at later time-points, in primary glioma cells. In parallel, PARPi triggered the synthesis of lipid droplets (LDs) through ACC-dependent activation of de novo fatty acids (FA) synthesis. Notably, inhibiting β-oxidation and blocking FA utilization, increased PARPi-induced glioma cell death while treatment with oleic acid (OA) prevented the anti-glioma effect of PARPi. Moreover, LDs fuel glioma cells by inducing pro-survival lipid consumption as confirmed by quantitation of oxygen consumption rates using Seahorse respirometry in presence or absence of OA. In summary, we uncover a novel mechanism by which glioblastoma escapes to anti-tumor agents through metabolic reprogramming, inducing the synthesis and utilization of LDs as a pro-survival strategy in response to PARP inhibition.
多形性胶质母细胞瘤(GBM)是成人中最常见且侵袭性最强的原发性脑肿瘤。聚(ADP - 核糖)聚合酶抑制剂(PARPi)代表了一类新型抗肿瘤药物。在当前研究中,我们已阐明胶质母细胞瘤细胞逃避PARPi作为抗肿瘤药物作用的机制。我们发现,抑制PARP活性具有抗干性作用,并且对自噬有双重影响,在原发性胶质瘤细胞中,它在最初24小时诱导自噬激活(同时下调促生存的mTOR途径),而在随后的时间点阻止自噬体与溶酶体融合。同时,PARPi通过ACC依赖的从头脂肪酸(FA)合成激活触发脂滴(LDs)的合成。值得注意的是,抑制β - 氧化并阻断FA利用,会增加PARPi诱导的胶质瘤细胞死亡,而用油酸(OA)处理可防止PARPi的抗胶质瘤作用。此外,通过在有或没有OA的情况下使用海马呼吸测定法对氧消耗率进行定量证实,LDs通过诱导促生存的脂质消耗为胶质瘤细胞提供能量。总之,我们揭示了一种新机制,即胶质母细胞瘤通过代谢重编程逃避抗肿瘤药物,诱导LDs 的合成和利用作为对PARP抑制的一种促生存策略。