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Ref Type Journal Article
PMID (27325686)
Authors Cherry AE, Haas BR, Naydenov AV, Fung S, Xu C, Swinney K, Wagenbach M, Freeling J, Canton DA, Coy J, Horne EA, Rickman B, Vicente JJ, Scott JD, Ho RJ, Liggitt D, Wordeman L, Stella N
Title ST-11: A New Brain-Penetrant Microtubule-Destabilizing Agent with Therapeutic Potential for Glioblastoma Multiforme.
Journal Vol Issue Date Pages Journal Short Title
Molecular cancer therapeutics 15 9 2016 Sep 2018-29 Mol Cancer Ther
URL
Abstract Text Glioblastoma multiforme is a devastating and intractable type of cancer. Current antineoplastic drugs do not improve the median survival of patients diagnosed with glioblastoma multiforme beyond 14 to 15 months, in part because the blood-brain barrier is generally impermeable to many therapeutic agents. Drugs that target microtubules (MT) have shown remarkable efficacy in a variety of cancers, yet their use as glioblastoma multiforme treatments has also been hindered by the scarcity of brain-penetrant MT-targeting compounds. We have discovered a new alkylindole compound, ST-11, that acts directly on MTs and rapidly attenuates their rate of assembly. Accordingly, ST-11 arrests glioblastoma multiforme cells in prometaphase and triggers apoptosis. In vivo analyses reveal that unlike current antitubulin agents, ST-11 readily crosses the blood-brain barrier. Further investigation in a syngeneic orthotopic mouse model of glioblastoma multiforme shows that ST-11 activates caspase-3 in tumors to reduce tumor volume without overt toxicity. Thus, ST-11 represents the first member of a new class of brain-penetrant antitubulin therapeutic agents. Mol Cancer Ther; 15(9); 2018-29. ©2016 AACR.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
ST-11 ST-11 0 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
ST-11 Antimicrotubule Agent 14 ST-11 targets tubulin to destabilize microtubules, and is capable of crossing the blood-brain barrier, potentially resulting increased death of tumor cells (PMID: 27325686).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References