Paul O'Gorman Leukaemia Research Centre, College of Medical, Veterinary and Life Sciences, University of Glasgow, United Kingdom.
Blood. 2012 Mar 8;119(10):2196-204. doi: 10.1182/blood-2011-10-383752. Epub 2012 Jan 5.
The Hedgehog pathway is a critical mediator of embryonic patterning and organ development, including hematopoiesis. It influences stem cell fate, differentiation, proliferation, and apoptosis in responsive tissues. In adult organisms, hedgehog pathway activity is required for aspects of tissue maintenance and regeneration; however, there is increasing awareness that abnormal hedgehog signaling is associated with malignancy. Hedgehog signaling is critical for early hematopoietic development, but there is controversy over its role in normal hematopoiesis in adult organisms where it may be dispensable. Conversely, hedgehog signaling appears to be an important survival and proliferation signal for a spectrum of hematologic malignancies. Furthermore, hedgehog signaling may be critical for the maintenance and expansion of leukemic stem cells and therefore provides a possible mechanism to selectively target these primitive cell subpopulations, which are resistant to conventional chemotherapy. Indeed, phase 1 clinical trials of hedgehog pathway inhibitors are currently underway to test this hypothesis in myeloid leukemias. This review covers: (1) the hedgehog pathway and its role in normal and malignant hematopoiesis, (2) the recent development of clinical grade small molecule inhibitors of the pathway, and (3) the potential utility of hedgehog pathway inhibition as a therapeutic strategy in hemato-oncology.
刺猬通路是胚胎模式形成和器官发育(包括造血)的关键介质。它影响响应组织中的干细胞命运、分化、增殖和凋亡。在成年生物体中,刺猬通路活性对于组织维持和再生的某些方面是必需的;然而,越来越多的人意识到异常的刺猬信号与恶性肿瘤有关。刺猬信号对于早期造血发育至关重要,但在成年生物体中,它在正常造血中的作用存在争议,在那里它可能是可有可无的。相反,刺猬信号似乎是一系列血液恶性肿瘤的重要存活和增殖信号。此外,刺猬信号对于白血病干细胞的维持和扩增可能是至关重要的,因此为选择性靶向这些对常规化疗有抵抗力的原始细胞亚群提供了一种可能的机制。事实上,目前正在进行针对髓性白血病的刺猬通路抑制剂的 1 期临床试验,以检验这一假设。本综述涵盖了:(1)刺猬通路及其在正常和恶性造血中的作用,(2)该通路的临床级小分子抑制剂的最新发展,以及(3)作为血液肿瘤学中一种治疗策略的刺猬通路抑制的潜在效用。