Lu Zhen, Baquero Maria T, Yang Hailing, Yang Maojie, Reger Albert S, Kim Choel, Levine Douglas A, Clarke Charlotte H, Liao Warren S-L, Bast Robert C
Department of Experimental Therapeutics; The University of Texas MD Anderson Cancer Center; Houston, TX USA.
Department of Pharmacology; Baylor College of Medicine; Houston, TX USA.
Autophagy. 2014 Jun;10(6):1071-92. doi: 10.4161/auto.28577.
DIRAS3 is an imprinted tumor suppressor gene that is downregulated in 60% of human ovarian cancers. Re-expression of DIRAS3 at physiological levels inhibits proliferation, decreases motility, induces autophagy, and regulates tumor dormancy. Functional inhibition of autophagy with choroquine in dormant xenografts that express DIRAS3 significantly delays tumor regrowth after DIRAS3 levels are reduced, suggesting that autophagy sustains dormant ovarian cancer cells. This study documents a newly discovered role for DIRAS3 in forming the autophagosome initiation complex (AIC) that contains BECN1, PIK3C3, PIK3R4, ATG14, and DIRAS3. Participation of BECN1 in the AIC is inhibited by binding of BECN1 homodimers to BCL2. DIRAS3 binds BECN1, disrupting BECN1 homodimers and displacing BCL2. Binding of DIRAS3 to BECN1 increases the association of BECN1 with PIK3C3 and ATG14, facilitating AIC activation. Amino acid starvation of cells induces DIRAS3 expression, reduces BECN1-BCL2 interaction and promotes autophagy, whereas DIRAS3 depletion blocks amino acid starvation-induced autophagy. In primary ovarian cancers, punctate expression of DIRAS3, BECN1, and the autophagic biomarker MAP1LC3 are highly correlated (P<0.0001), underlining the clinical relevance of these mechanistic studies. Punctate expression of DIRAS3 and MAP1LC3 was detected in only 21-23% of primary ovarian cancers but in 81-84% of tumor nodules found on the peritoneal surface at second-look operations following primary chemotherapy. This reflects a 4-fold increase (P<0.0001) in autophagy between primary disease and post-treatment recurrence. We suggest that DIRAS3 not only regulates the AIC, but induces autophagy in dormant, nutrient-deprived ovarian cancer cells that remain after conventional chemotherapy, facilitating their survival.
DIRAS3是一种印记肿瘤抑制基因,在60%的人类卵巢癌中表达下调。DIRAS3在生理水平的重新表达可抑制增殖、降低迁移能力、诱导自噬并调节肿瘤休眠。在表达DIRAS3的休眠异种移植瘤中,用氯喹对自噬进行功能抑制可在DIRAS3水平降低后显著延迟肿瘤再生长,这表明自噬维持着休眠的卵巢癌细胞。本研究记录了DIRAS3在形成包含BECN1、PIK3C3、PIK3R4、ATG14和DIRAS3的自噬体起始复合物(AIC)中的新发现作用。BECN1同二聚体与BCL2结合会抑制BECN1参与AIC。DIRAS3与BECN1结合,破坏BECN1同二聚体并取代BCL2。DIRAS3与BECN1的结合增加了BECN1与PIK3C3和ATG14的关联,促进AIC激活。细胞的氨基酸饥饿诱导DIRAS3表达,减少BECN1 - BCL2相互作用并促进自噬,而DIRAS3缺失则阻断氨基酸饥饿诱导的自噬。在原发性卵巢癌中,DIRAS3、BECN1和自噬生物标志物MAP1LC3的点状表达高度相关(P<0.0001),突出了这些机制研究的临床相关性。在原发性卵巢癌中仅21 - 23%检测到DIRAS3和MAP1LC3的点状表达,但在初次化疗后二次探查手术时在腹膜表面发现的肿瘤结节中81 - 84%检测到。这反映了原发性疾病与治疗后复发之间自噬增加了4倍(P<0.0001)。我们认为DIRAS3不仅调节AIC,还在常规化疗后残留的休眠、营养缺乏的卵巢癌细胞中诱导自噬,促进其存活。