Role of peroxisome proliferator-activated receptor-gamma in hematologic malignancies.
Role of peroxisome proliferator-activated receptor-gamma in hematologic malignancies.
复制标题
过氧化物酶体增殖物激活受体-γ在血液恶性肿瘤中的作用。
DOI：
10.1097/00062752-200207000-00006
复制
发表时间：
2002
影响因子：
3.2
通讯作者：
Andreeff,Michael
中科院分区：
文献类型：
--
作者：
Konopleva,Marina;Andreeff,Michael
核受体超家族的成员，包括视黄酸受体 (RAR)、类视黄醇 X 受体 (RXR) 和维生素 D 受体 (VDR)，是控制许多重要细胞功能的转录因子，其配体广泛用于多种临床适应症。最新的家族成员是过氧化物酶体增殖物激活受体-γ (PPARγ)，它在正常单核细胞、不同的白血病和上皮恶性肿瘤中高表达。 PPARγ 配体已被开发出来并发出分化、生长停滞和细胞凋亡信号。 PPARγ 与 RXR 形成异二聚体，并且两个受体的连接是最大信号传导所必需的。讨论了 PPARγ 信号传导、其在血液恶性肿瘤中的表达以及在分化中的作用。 PPARγ 与 X-RARα、蛋白激酶 R (PKR)、PTEN 和丝裂原激活蛋白激酶 (MAPK) 的相互作用已有描述。 PPARγ配体已被开发用于治疗糖尿病，但新的、更有效的配体（包括三萜类化合物）正在研究作为上皮和血液恶性肿瘤的治疗剂。
Members of the nuclear receptor superfamily, including retinoic acid receptors (RARs), retinoid X receptors (RXRs), and vitamin D receptors (VDRs), are transcription factors that control many important cellular functions, and their ligands are widely used in several clinical indications. The latest family member is the peroxisome proliferator-activated receptor-γ (PPARγ), which is highly expressed in normal monocytes, different leukemias, and epithelial malignancies. PPARγ ligands have been developed and signal differentiation, growth arrest, and apoptosis. PPARγ forms heterodimers with RXR, and ligation of both receptors is required for maximal signaling. PPARγ signaling, its expression in hematologic malignancies, and role in differentiation are discussed. Interactions of PPARγ with X-RARα, protein kinase R (PKR), PTEN, and mitogen-activated protein kinase (MAPK) have been described. PPARγ ligands have been developed for the management of diabetes, but new and more potent ligands, including triterpenoids, are being investigated as therapeutic agents for epithelial and hematologic malignancies.