The HSP90 inhibitor onalespib potentiates 177Lu‑DOTATATE therapy in neuroendocrine tumor cells.
Lundsten S, Spiegelberg D, Stenerlöw B, Nestor M.
Int J Oncol · research-article; journal article · DOI 10.3892/ijo.2019.4888 PUBLICATION REGISTRY
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18 hitsEfficacy 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 · research-article; journal article · DOI 10.1158/1078-0432.ccr-16-3151Emergence of resistance to tyrosine kinase inhibitors in non-small-cell lung cancer can be delayed by an upfront combination with the HSP90 inhibitor onalespib.
Courtin A, Smyth T, Hearn K, Saini HK, Thompson NT, Lyons JF, Wallis NG.
Br J Cancer · research-article; journal article · DOI 10.1038/bjc.2016.294Dose-escalation study of a second-generation non-ansamycin HSP90 inhibitor, onalespib (AT13387), in combination with imatinib in patients with metastatic gastrointestinal stromal tumour.
Wagner AJ, Agulnik M, Heinrich MC, Mahadevan D, Riedel RF, von Mehren M, Trent J, Demetri GD, Corless CL, Yule M, Lyons JF, Oganesian A, Keer H.
Eur J Cancer · research support, non-u.s. gov't; clinical trial, phase i; journal article · DOI 10.1016/j.ejca.2016.03.076Second-Generation HSP90 Inhibitor Onalespib Blocks mRNA Splicing of Androgen Receptor Variant 7 in Prostate Cancer Cells.
Ferraldeschi R, Welti J, Powers MV, Yuan W, Smyth T, Seed G, Riisnaes R, Hedayat S, Wang H, Crespo M, Nava Rodrigues D, Figueiredo I, Miranda S, Carreira S, Lyons JF, Sharp S, Plymate SR, Attard G, Wallis N, Workman P, de Bono JS.
Cancer Res · research-article; journal article · DOI 10.1158/0008-5472.can-15-2186Re: First-in-Human Phase I Dose Escalation Study of a Second-Generation Non-Ansamycin HSP90 Inhibitor, AT13387, in Patients with Advanced Solid Tumors.
Chang SS.
J Urol · comment; journal article · DOI 10.1016/j.juro.2016.03.162Molecular imaging of EGFR and CD44v6 for prediction and response monitoring of HSP90 inhibition in an in vivo squamous cell carcinoma model.
Spiegelberg D, Mortensen AC, Selvaraju RK, Eriksson O, Stenerlöw B, Nestor M.
Eur J Nucl Med Mol Imaging · research support, non-u.s. gov't; research-article; journal article · DOI 10.1007/s00259-015-3260-xThe novel HSP90 inhibitor AT13387 potentiates radiation effects in squamous cell carcinoma and adenocarcinoma cells.
Spiegelberg D, Dascalu A, Mortensen AC, Abramenkovs A, Kuku G, Nestor M, Stenerlöw B.
Oncotarget · research support, non-u.s. gov't; research-article; journal article · DOI 10.18632/oncotarget.5363Heat shock protein 90 inhibition abrogates TLR4-mediated NF-κB activity and reduces renal ischemia-reperfusion injury.
O'Neill S, Humphries D, Tse G, Marson LP, Dhaliwal K, Hughes J, Ross JA, Wigmore SJ, Harrison EM.
Sci Rep · research support, non-u.s. gov't; research-article; journal article · DOI 10.1038/srep12958Phase I study of the heat shock protein 90 (Hsp90) inhibitor onalespib (AT13387) administered on a daily for 2 consecutive days per week dosing schedule in patients with advanced solid tumors.
Do K, Speranza G, Chang LC, Polley EC, Bishop R, Zhu W, Trepel JB, Lee S, Lee MJ, Kinders RJ, Phillips L, Collins J, Lyons J, Jeong W, Antony R, Chen AP, Neckers L, Doroshow JH, Kummar S.
Invest New Drugs · research-article; clinical trial, phase i; journal article; research support, n.i.h., extramural · DOI 10.1007/s10637-015-0255-1Inhibition of HSP90 by AT13387 delays the emergence of resistance to BRAF inhibitors and overcomes resistance to dual BRAF and MEK inhibition in melanoma models.
Smyth T, Paraiso KHT, Hearn K, Rodriguez-Lopez AM, Munck JM, Haarberg HE, Sondak VK, Thompson NT, Azab M, Lyons JF, Smalley KSM, Wallis NG.
Mol Cancer Ther · research-article; journal article; research support, n.i.h., extramural · DOI 10.1158/1535-7163.mct-14-0452First-in-human phase I dose escalation study of a second-generation non-ansamycin HSP90 inhibitor, AT13387, in patients with advanced solid tumors.
Shapiro GI, Kwak E, Dezube BJ, Yule M, Ayrton J, Lyons J, Mahadevan D.
Clin Cancer Res · research support, non-u.s. gov't; clinical trial, phase i; journal article · DOI 10.1158/1078-0432.ccr-14-0979A novel Hsp90 inhibitor AT13387 induces senescence in EBV-positive nasopharyngeal carcinoma cells and suppresses tumor formation.
Chan KC, Ting CM, Chan PS, Lo MC, Lo KW, Curry JE, Smyth T, Lee AW, Ng WT, Tsao GS, Wong RN, Lung ML, Mak NK.
Mol Cancer · research support, non-u.s. gov't; research-article; journal article · DOI 10.1186/1476-4598-12-128Total synthesis of resorcinol amide Hsp90 inhibitor AT13387.
Patel BH, Barrett AG.
J Org Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jo302406wThe HSP90 inhibitor, AT13387, is effective against imatinib-sensitive and -resistant gastrointestinal stromal tumor models.
Smyth T, Van Looy T, Curry JE, Rodriguez-Lopez AM, Wozniak A, Zhu M, Donsky R, Morgan JG, Mayeda M, Fletcher JA, Schöffski P, Lyons J, Thompson NT, Wallis NG.
Mol Cancer Ther · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1158/1535-7163.mct-11-1046The heat shock protein 90 inhibitor, AT13387, displays a long duration of action in vitro and in vivo in non-small cell lung cancer.
Graham B, Curry J, Smyth T, Fazal L, Feltell R, Harada I, Coyle J, Williams B, Reule M, Angove H, Cross DM, Lyons J, Wallis NG, Thompson NT.
Cancer Sci · research-article; journal article · DOI 10.1111/j.1349-7006.2011.02191.xInitial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric preclinical testing program.
Kang MH, Reynolds CP, Houghton PJ, Alexander D, Morton CL, Kolb EA, Gorlick R, Keir ST, Carol H, Lock R, Maris JM, Wozniak A, Smith MA.
Pediatr Blood Cancer · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1002/pbc.23154Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design.
Woodhead AJ, Angove H, Carr MG, Chessari G, Congreve M, Coyle JE, Cosme J, Graham B, Day PJ, Downham R, Fazal L, Feltell R, Figueroa E, Frederickson M, Lewis J, McMenamin R, Murray CW, O'Brien MA, Parra L, Patel S, Phillips T, Rees DC, Rich S, Smith DM, Trewartha G, Vinkovic M, Williams B, Woolford AJ.
J Med Chem · journal article · DOI 10.1021/jm100060b