Initial testing (stage 1) of ganetespib, an Hsp90 inhibitor, by the Pediatric Preclinical Testing Program.
Initial testing (stage 1) of ganetespib, an Hsp90 inhibitor, by the Pediatric Preclinical Testing Program.
复制标题
DOI：
10.1002/pbc.24451
复制
发表时间：
2013-07
影响因子：
3.2
通讯作者：
Smith, Malcolm A.
中科院分区：
文献类型：
--
作者：
Lock, Richard B.;Carol, Hernan;Maris, John M.;Kang, Min H.;Reynolds, C. Patrick;Kolb, E. Anders;Gorlick, Richard;Keir, Stephen T.;Billups, Catherine A.;Kurmasheva, Raushan T.;Houghton, Peter J.;Smith, Malcolm A.
针对PPTP体外细胞系组和选定的体内异种移植物（包括JAK 2和BRAF突变模型）测试了Ganetespib（一种Hsp 90抑制剂）。Ganetespib显示出强效的体外细胞毒性活性（中位rIC 50 8.8 nM，范围4.4-27.1 nM）。在体内，ganetespib诱导了11种异种移植物中4种的EFS分布的显著差异。仅在MV 4;11异种移植物中观察到中间活性（EFS T/C > 2），并且没有客观反应。作为单一药物给药，PPTP检查的Hsp 90抑制剂显示出对实体瘤和白血病儿科临床前模型的治疗窗口的有限证据。
Ganetespib, an Hsp90 inhibitor, was tested against the PPTP in vitro cell line panel and selected xenografts in vivo, including JAK2- and BRAF-mutated models. Ganetespib demonstrated potent in vitro cytotoxic activity (median rIC50 8.8 nM, range 4.4–27.1 nM). In vivo, ganetespib induced significant differences in EFS distribution for 4 of 11 xenografts. Intermediate activity (EFS T/C > 2) was noted only for the MV4;11 xenograft, and there were no objective responses. Administered as single agents, Hsp90 inhibitors examined by the PPTP have shown limited evidence for a therapeutic window against both solid tumor and leukemia pediatric preclinical models.
登录
查看更多内容
DOI：
10.1084/jem.20111694
发表时间：
2012-02-13
期刊：
The Journal of experimental medicine
影响因子：
--
作者：
Weigert O;Lane AA;Bird L;Kopp N;Chapuy B;van Bodegom D;Toms AV;Marubayashi S;Christie AL;McKeown M;Paranal RM;Bradner JE;Yoda A;Gaul C;Vangrevelinghe E;Romanet V;Murakami M;Tiedt R;Ebel N;Evrot E;De Pover A;Régnier CH;Erdmann D;Hofmann F;Eck MJ;Sallan SE;Levine RL;Kung AL;Baffert F;Radimerski T;Weinstock DM
通讯作者：
Weinstock DM
影响因子：
3.2
作者：
Houghton, Peter J.;Morton, Christopher L.;Smith, Malcolm A.
通讯作者：
Smith, Malcolm A.
影响因子：
20.3
作者：
Chen, I. Ming;Harvey, Richard C.;Willman, Cheryl L.
通讯作者：
Willman, Cheryl L.
影响因子：
8
作者：
Normant, E.;Paez, G.;Fritz, C. C.
通讯作者：
Fritz, C. C.
影响因子：
64.8
作者：
Mosse, Yael P.;Laudenslager, Marci;Longo, Luca;Cole, Kristina A.;Wood, Andrew;Attiyeh, Edward F.;Laquaglia, Michael J.;Sennett, Rachel;Lynch, Jill E.;Perri, Patrizia;Laureys, Genevieve;Speleman, Frank;Kim, Cecilia;Hou, Cuiping;Hakonarson, Hakon;Torkamani, Ali;Schork, Nicholas J.;Brodeur, Garrett M.;Tonini, Gian P.;Rappaport, Eric;Devoto, Marcella;Maris, John M.
通讯作者：
Maris, John M.