Efficacy of Onalespib, a Long-Acting Second-Generation HSP90 Inhibitor, as a Single Agent and in Combination with Temozolomide against Malignant Gliomas.

Canella A, Welker AM, Yoo JY, Xu J, Abas FS, Kesanakurti D, Nagarajan P, Beattie CE, Sulman EP, Liu J, Gumin J, Lang FF, Gurcan MN, Kaur B, Sampath D, Puduvalli VK
Clin Cancer Res 23 6215-6226 10/15/2017

Abstract

HSP90, a highly conserved molecular chaperone that regulates the function of several oncogenic client proteins, is altered in glioblastoma. However, HSP90 inhibitors currently in clinical trials are short-acting, have unacceptable toxicities, or are unable to cross the blood-brain barrier (BBB). We examined the efficacy of onalespib, a potent, long-acting novel HSP90 inhibitor as a single agent and in combination with temozolomide (TMZ) against gliomas

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