Piekarz R L, Robey R, Sandor V, Bakke S, Wilson W H, Dahmoush L, Kingma D M, Turner M L, Altemus R, Bates S E
Medicine Branch, National Cancer Institute, National Institutes of Health, Bethesda, MD, USA.
Blood. 2001 Nov 1;98(9):2865-8. doi: 10.1182/blood.v98.9.2865.
Depsipeptide, FR901228, has demonstrated potent in vitro and in vivo cytotoxic activity against murine and human tumor cell lines. In the laboratory, it has been shown to be a histone deacetylase (HDAC) inhibitor. In a phase I trial of depsipeptide conducted at the National Cancer Institute, 3 patients with cutaneous T-cell lymphoma had a partial response, and 1 patient with peripheral T-cell lymphoma, unspecified, had a complete response. Sézary cells isolated from patients after treatment had increased histone acetylation. These results suggest that inhibition of HDAC is a novel and potentially effective therapy for patients with T-cell lymphoma.
缩肽环肽（FR901228）已显示出对鼠类和人类肿瘤细胞系具有强大的体外和体内细胞毒性活性。在实验室中，它已被证明是一种组蛋白去乙酰化酶（HDAC）抑制剂。在国立癌症研究所进行的缩肽环肽I期试验中，3例皮肤T细胞淋巴瘤患者出现部分缓解，1例未明确类型的外周T细胞淋巴瘤患者出现完全缓解。治疗后从患者体内分离出的Sezary细胞的组蛋白乙酰化增加。这些结果表明，抑制HDAC对T细胞淋巴瘤患者是一种新颖且可能有效的治疗方法。
