Deininger Michael W N, Druker Brian J
Oregon Health & Science University Cancer Institute, Center for Hematologic Malignancies, L592, 3181 SW Sam Jackson Park Road, Portland, OR 97239, USA.
Cancer Cell. 2004 Aug;6(2):108-10. doi: 10.1016/j.ccr.2004.08.006.
The ABL inhibitor imatinib is a highly effective therapy for patients with chronic myeloid leukemia. Relapses after an initial response have been observed in some patients, and mutations of the BCR-ABL gene are the most common mechanism driving these relapses. Alternative ABL inhibitors have been identified that inhibit most of the common BCR-ABL mutations, and one has entered clinical trials. The structural basis for these results has yielded significant insights into the mechanism of action of these compounds, mechanisms of resistance, and their ability to inhibit the BCR-ABL mutants. These studies demonstrate the importance and impact of conducting scientific studies as part of clinical trials.
ABL抑制剂伊马替尼是治疗慢性髓性白血病患者的一种高效疗法。在一些患者中观察到初始缓解后出现复发,而BCR-ABL基因突变是导致这些复发的最常见机制。已鉴定出可抑制大多数常见BCR-ABL突变的替代ABL抑制剂,其中一种已进入临床试验。这些结果的结构基础为这些化合物的作用机制、耐药机制以及它们抑制BCR-ABL突变体的能力提供了重要见解。这些研究证明了作为临床试验一部分开展科学研究的重要性和影响。