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Targeting loss of the Hippo signaling pathway in NF2-deficient papillary kidney cancers.

Sourbier C, Liao PJ, Ricketts CJ, Wei D, Yang Y, Baranes SM, Gibbs BK, Ohanjanian L, Spencer Krane L, Scroggins BT, Keith Killian J, Wei MH, Kijima T, Meltzer PS, Citrin DE, Neckers L, Vocke CD, Marston Linehan W.

Oncotarget. 2018 Jan 10;9(12):10723-10733. doi: 10.18632/oncotarget.24112. eCollection 2018 Feb 13.


Methods to validate Hsp90 inhibitor specificity, to identify off-target effects, and to rethink approaches for further clinical development.

Neckers L, Blagg B, Haystead T, Trepel JB, Whitesell L, Picard D.

Cell Stress Chaperones. 2018 Feb 1. doi: 10.1007/s12192-018-0877-2. [Epub ahead of print]


Phosphorylation induced cochaperone unfolding promotes kinase recruitment and client class-specific Hsp90 phosphorylation.

Bachman AB, Keramisanou D, Xu W, Beebe K, Moses MA, Vasantha Kumar MV, Gray G, Noor RE, van der Vaart A, Neckers L, Gelis I.

Nat Commun. 2018 Jan 17;9(1):265. doi: 10.1038/s41467-017-02711-w.


Uncoupling tumor-stroma interactions in breast cancer patients.

Sourbier C, Neckers L.

Semin Oncol. 2017 Jun;44(3):235-236. doi: 10.1053/j.seminoncol.2017.10.008. Epub 2017 Oct 18. No abstract available.


Heat shock protein 90: its inhibition and function.

Zuehlke AD, Moses MA, Neckers L.

Philos Trans R Soc Lond B Biol Sci. 2018 Jan 19;373(1738). pii: 20160527. doi: 10.1098/rstb.2016.0527. Review.


Detecting Posttranslational Modifications of Hsp90.

Sager RA, Woodford MR, Neckers L, Mollapour M.

Methods Mol Biol. 2018;1709:209-219. doi: 10.1007/978-1-4939-7477-1_16.


Monitoring of the Heat Shock Response with a Real-Time Luciferase Reporter.

Kijima T, Eguchi T, Neckers L, Prince TL.

Methods Mol Biol. 2018;1709:35-45. doi: 10.1007/978-1-4939-7477-1_3.


Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH).

Rai G, Brimacombe KR, Mott BT, Urban DJ, Hu X, Yang SM, Lee TD, Cheff DM, Kouznetsova J, Benavides GA, Pohida K, Kuenstner EJ, Luci DK, Lukacs CM, Davies DR, Dranow DM, Zhu H, Sulikowski G, Moore WJ, Stott GM, Flint AJ, Hall MD, Darley-Usmar VM, Neckers LM, Dang CV, Waterson AG, Simeonov A, Jadhav A, Maloney DJ.

J Med Chem. 2017 Nov 22;60(22):9184-9204. doi: 10.1021/acs.jmedchem.7b00941. Epub 2017 Nov 9.


Out with the old: Hsp90 finds amino acid residue more useful than co-chaperone protein.

Zuehlke AD, Neckers L.

Microb Cell. 2017 Aug 1;4(8):273-274. doi: 10.15698/mic2017.08.586.


An Hsp90 co-chaperone protein in yeast is functionally replaced by site-specific posttranslational modification in humans.

Zuehlke AD, Reidy M, Lin C, LaPointe P, Alsomairy S, Lee DJ, Rivera-Marquez GM, Beebe K, Prince T, Lee S, Trepel JB, Xu W, Johnson J, Masison D, Neckers L.

Nat Commun. 2017 May 24;8:15328. doi: 10.1038/ncomms15328.


Proteomic analysis of proteome and histone post-translational modifications in heat shock protein 90 inhibition-mediated bladder cancer therapeutics.

Li QQ, Hao JJ, Zhang Z, Krane LS, Hammerich KH, Sanford T, Trepel JB, Neckers L, Agarwal PK.

Sci Rep. 2017 Mar 15;7(1):201. doi: 10.1038/s41598-017-00143-6.


A USE1ful Biomarker and Molecular Target in Lung Cancer?

Xu W, Neckers L.

J Natl Cancer Inst. 2016 Oct 21;109(3). pii: djw227. Print 2017 Mar. No abstract available.


STA-8666, a novel HSP90 inhibitor/SN-38 drug conjugate, causes complete tumor regression in preclinical mouse models of pediatric sarcoma.

Heske CM, Mendoza A, Edessa LD, Baumgart JT, Lee S, Trepel J, Proia DA, Neckers L, Helman LJ.

Oncotarget. 2016 Oct 4;7(40):65540-65552. doi: 10.18632/oncotarget.11869.


Gambogic acid identifies an isoform-specific druggable pocket in the middle domain of Hsp90β.

Yim KH, Prince TL, Qu S, Bai F, Jennings PA, Onuchic JN, Theodorakis EA, Neckers L.

Proc Natl Acad Sci U S A. 2016 Aug 16;113(33):E4801-9. doi: 10.1073/pnas.1606655113. Epub 2016 Jul 27.


Gr(i)p the ER to Stress Out Melanoma.

Xu W, Neckers L.

Cancer Cell. 2016 Jun 13;29(6):769-771. doi: 10.1016/j.ccell.2016.05.006.


Clients Place Unique Functional Constraints on Hsp90.

Zuehlke AD, Neckers L.

Trends Biochem Sci. 2016 Jul;41(7):562-564. doi: 10.1016/j.tibs.2016.05.011. Epub 2016 Jun 10.


Synthesis of a stable and orally bioavailable englerin analogue.

Fash DM, Peer CJ, Li Z, Talisman IJ, Hayavi S, Sulzmaier FJ, Ramos JW, Sourbier C, Neckers L, Figg WD, Beutler JA, Chain WJ.

Bioorg Med Chem Lett. 2016 Jun 1;26(11):2641-4. doi: 10.1016/j.bmcl.2016.04.016. Epub 2016 Apr 8.


Targeting Hsp90 in Non-Cancerous Maladies.

Woodford MR, Dunn DM, Ciciarelli JG, Beebe K, Neckers L, Mollapour M.

Curr Top Med Chem. 2016;16(25):2792-804. Review.


Hsp90 in Cancer: Transcriptional Roles in the Nucleus.

Calderwood SK, Neckers L.

Adv Cancer Res. 2016;129:89-106. doi: 10.1016/bs.acr.2015.08.002. Epub 2015 Oct 12. Review.


Impact of Posttranslational Modifications on the Anticancer Activity of Hsp90 Inhibitors.

Woodford MR, Dunn D, Miller JB, Jamal S, Neckers L, Mollapour M.

Adv Cancer Res. 2016;129:31-50. doi: 10.1016/bs.acr.2015.09.002. Epub 2015 Oct 23. Review.


Mps1 Mediated Phosphorylation of Hsp90 Confers Renal Cell Carcinoma Sensitivity and Selectivity to Hsp90 Inhibitors.

Woodford MR, Truman AW, Dunn DM, Jensen SM, Cotran R, Bullard R, Abouelleil M, Beebe K, Wolfgeher D, Wierzbicki S, Post DE, Caza T, Tsutsumi S, Panaretou B, Kron SJ, Trepel JB, Landas S, Prodromou C, Shapiro O, Stetler-Stevenson WG, Bourboulia D, Neckers L, Bratslavsky G, Mollapour M.

Cell Rep. 2016 Feb 2;14(4):872-884. doi: 10.1016/j.celrep.2015.12.084. Epub 2016 Jan 21.


Client Proteins and Small Molecule Inhibitors Display Distinct Binding Preferences for Constitutive and Stress-Induced HSP90 Isoforms and Their Conformationally Restricted Mutants.

Prince TL, Kijima T, Tatokoro M, Lee S, Tsutsumi S, Yim K, Rivas C, Alarcon S, Schwartz H, Khamit-Kush K, Scroggins BT, Beebe K, Trepel JB, Neckers L.

PLoS One. 2015 Oct 30;10(10):e0141786. doi: 10.1371/journal.pone.0141786. eCollection 2015.


Lack of mitochondrial topoisomerase I (TOP1mt) impairs liver regeneration.

Khiati S, Baechler SA, Factor VM, Zhang H, Huang SY, Dalla Rosa I, Sourbier C, Neckers L, Thorgeirsson SS, Pommier Y.

Proc Natl Acad Sci U S A. 2015 Sep 8;112(36):11282-7. doi: 10.1073/pnas.1511016112. Epub 2015 Aug 24.


Tonantzitlolone cytotoxicity toward renal cancer cells is PKCθ- and HSF1-dependent.

Sourbier C, Scroggins BT, Mannes PZ, Liao PJ, Siems K, Wolf D, Beutler JA, Linehan WM, Neckers L.

Oncotarget. 2015 Oct 6;6(30):29963-74. doi: 10.18632/oncotarget.4676.


Activation of Hsp90 Enzymatic Activity and Conformational Dynamics through Rationally Designed Allosteric Ligands.

Sattin S, Tao J, Vettoretti G, Moroni E, Pennati M, Lopergolo A, Morelli L, Bugatti A, Zuehlke A, Moses M, Prince T, Kijima T, Beebe K, Rusnati M, Neckers L, Zaffaroni N, Agard DA, Bernardi A, Colombo G.

Chemistry. 2015 Sep 21;21(39):13598-608. doi: 10.1002/chem.201502211. Epub 2015 Aug 18.


c-Abl Mediated Tyrosine Phosphorylation of Aha1 Activates Its Co-chaperone Function in Cancer Cells.

Dunn DM, Woodford MR, Truman AW, Jensen SM, Schulman J, Caza T, Remillard TC, Loiselle D, Wolfgeher D, Blagg BS, Franco L, Haystead TA, Daturpalli S, Mayer MP, Trepel JB, Morgan RM, Prodromou C, Kron SJ, Panaretou B, Stetler-Stevenson WG, Landas SK, Neckers L, Bratslavsky G, Bourboulia D, Mollapour M.

Cell Rep. 2015 Aug 11;12(6):1006-18. doi: 10.1016/j.celrep.2015.07.004. Epub 2015 Jul 30.


Phase 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. 2015 Aug;33(4):921-30. doi: 10.1007/s10637-015-0255-1. Epub 2015 Jun 18.


Regulation and function of the human HSP90AA1 gene.

Zuehlke AD, Beebe K, Neckers L, Prince T.

Gene. 2015 Oct 1;570(1):8-16. doi: 10.1016/j.gene.2015.06.018. Epub 2015 Jun 10. Review.


Combined HSP90 and kinase inhibitor therapy: Insights from The Cancer Genome Atlas.

Schwartz H, Scroggins B, Zuehlke A, Kijima T, Beebe K, Mishra A, Neckers L, Prince T.

Cell Stress Chaperones. 2015 Sep;20(5):729-41. doi: 10.1007/s12192-015-0604-1. Epub 2015 Jun 13. Review.


Alternative splicing of the cell fate determinant Numb in hepatocellular carcinoma.

Lu Y, Xu W, Ji J, Feng D, Sourbier C, Yang Y, Qu J, Zeng Z, Wang C, Chang X, Chen Y, Mishra A, Xu M, Lee MJ, Lee S, Trepel J, Linehan WM, Wang X, Yang Y, Neckers L.

Hepatology. 2015 Oct;62(4):1122-31. doi: 10.1002/hep.27923. Epub 2015 Jul 3.


The GLU that holds cancer together: targeting GLUtamine transporters in breast cancer.

Moses MA, Neckers L.

Cancer Cell. 2015 Mar 9;27(3):317-9. doi: 10.1016/j.ccell.2015.02.010.


Computational polypharmacology analysis of the heat shock protein 90 interactome.

Anighoro A, Stumpfe D, Heikamp K, Beebe K, Neckers LM, Bajorath J, Rastelli G.

J Chem Inf Model. 2015 Mar 23;55(3):676-86. doi: 10.1021/ci5006959. Epub 2015 Feb 23.


Targeting ABL1-mediated oxidative stress adaptation in fumarate hydratase-deficient cancer.

Sourbier C, Ricketts CJ, Matsumoto S, Crooks DR, Liao PJ, Mannes PZ, Yang Y, Wei MH, Srivastava G, Ghosh S, Chen V, Vocke CD, Merino M, Srinivasan R, Krishna MC, Mitchell JB, Pendergast AM, Rouault TA, Neckers L, Linehan WM.

Cancer Cell. 2014 Dec 8;26(6):840-850. doi: 10.1016/j.ccell.2014.10.005.


Solution formulation development and efficacy of MJC13 in a preclinical model of castration-resistant prostate cancer.

Liang S, Bian X, Liang D, Sivils JC, Neckers LM, Cox MB, Xie H.

Pharm Dev Technol. 2016;21(1):121-6. doi: 10.3109/10837450.2014.979946. Epub 2014 Nov 7.


Chaperoning parasitism: the importance of molecular chaperones in pathogen virulence.

Tatu U, Neckers L.

Parasitology. 2014 Aug;141(9):1123-6. doi: 10.1017/S0031182014000778. No abstract available.


Mitochondrial oxidative phosphorylation TRAP(1)ped in tumor cells.

Rasola A, Neckers L, Picard D.

Trends Cell Biol. 2014 Aug;24(8):455-63. doi: 10.1016/j.tcb.2014.03.005. Epub 2014 Apr 11. Review.


Mitochondrial topoisomerase I (top1mt) is a novel limiting factor of doxorubicin cardiotoxicity.

Khiati S, Dalla Rosa I, Sourbier C, Ma X, Rao VA, Neckers LM, Zhang H, Pommier Y.

Clin Cancer Res. 2014 Sep 15;20(18):4873-81. doi: 10.1158/1078-0432.CCR-13-3373. Epub 2014 Apr 8.


Asymmetric Hsp90 N domain SUMOylation recruits Aha1 and ATP-competitive inhibitors.

Mollapour M, Bourboulia D, Beebe K, Woodford MR, Polier S, Hoang A, Chelluri R, Li Y, Guo A, Lee MJ, Fotooh-Abadi E, Khan S, Prince T, Miyajima N, Yoshida S, Tsutsumi S, Xu W, Panaretou B, Stetler-Stevenson WG, Bratslavsky G, Trepel JB, Prodromou C, Neckers L.

Mol Cell. 2014 Jan 23;53(2):317-29. doi: 10.1016/j.molcel.2013.12.007.


Coordinated regulation of serum- and glucocorticoid-inducible kinase 3 by a C-terminal hydrophobic motif and Hsp90-Cdc37 chaperone complex.

Wang Y, Xu W, Zhou D, Neckers L, Chen S.

J Biol Chem. 2014 Feb 21;289(8):4815-26. doi: 10.1074/jbc.M113.518480. Epub 2013 Dec 30.


Stressing the development of small molecules targeting HSP90.

Neckers L, Trepel JB.

Clin Cancer Res. 2014 Jan 15;20(2):275-7. doi: 10.1158/1078-0432.CCR-13-2571. Epub 2013 Oct 28.


The HSP90 inhibitor ganetespib synergizes with the MET kinase inhibitor crizotinib in both crizotinib-sensitive and -resistant MET-driven tumor models.

Miyajima N, Tsutsumi S, Sourbier C, Beebe K, Mollapour M, Rivas C, Yoshida S, Trepel JB, Huang Y, Tatokoro M, Shinohara N, Nonomura K, Neckers L.

Cancer Res. 2013 Dec 1;73(23):7022-33. doi: 10.1158/0008-5472.CAN-13-1156. Epub 2013 Oct 11.


Synthesis and structure-activity relationship studies of novel dihydropyridones as androgen receptor modulators.

Pepe A, Pamment M, Kim YS, Lee S, Lee MJ, Beebe K, Filikov A, Neckers L, Trepel JB, Malhotra SV.

J Med Chem. 2013 Nov 14;56(21):8280-97. doi: 10.1021/jm301714s. Epub 2013 Oct 30.


Optical and radioiodinated tethered Hsp90 inhibitors reveal selective internalization of ectopic Hsp90 in malignant breast tumor cells.

Barrott JJ, Hughes PF, Osada T, Yang XY, Hartman ZC, Loiselle DR, Spector NL, Neckers L, Rajaram N, Hu F, Ramanujam N, Vaidyanathan G, Zalutsky MR, Lyerly HK, Haystead TA.

Chem Biol. 2013 Sep 19;20(9):1187-97. doi: 10.1016/j.chembiol.2013.08.004. Epub 2013 Sep 12.


New insights into von Hippel-Lindau function highlighted by investigation of the trichloroethylene-induced p.P81S hotspot mutation.

Neckers L, Ricketts CJ, Marston Linehan W.

J Natl Cancer Inst. 2013 Sep 18;105(18):1339-40. doi: 10.1093/jnci/djt240. Epub 2013 Aug 29. No abstract available.


Posttranslational modification and conformational state of heat shock protein 90 differentially affect binding of chemically diverse small molecule inhibitors.

Beebe K, Mollapour M, Scroggins B, Prodromou C, Xu W, Tokita M, Taldone T, Pullen L, Zierer BK, Lee MJ, Trepel J, Buchner J, Bolon D, Chiosis G, Neckers L.

Oncotarget. 2013 Jul;4(7):1065-74.


Contributions of co-chaperones and post-translational modifications towards Hsp90 drug sensitivity.

Walton-Diaz A, Khan S, Bourboulia D, Trepel JB, Neckers L, Mollapour M.

Future Med Chem. 2013 Jun;5(9):1059-71. doi: 10.4155/fmc.13.88. Review.


Molecular chaperone TRAP1 regulates a metabolic switch between mitochondrial respiration and aerobic glycolysis.

Yoshida S, Tsutsumi S, Muhlebach G, Sourbier C, Lee MJ, Lee S, Vartholomaiou E, Tatokoro M, Beebe K, Miyajima N, Mohney RP, Chen Y, Hasumi H, Xu W, Fukushima H, Nakamura K, Koga F, Kihara K, Trepel J, Picard D, Neckers L.

Proc Natl Acad Sci U S A. 2013 Apr 23;110(17):E1604-12. doi: 10.1073/pnas.1220659110. Epub 2013 Apr 5.


Targeting heat shock protein 90 for the treatment of malignant pheochromocytoma.

Giubellino A, Sourbier C, Lee MJ, Scroggins B, Bullova P, Landau M, Ying W, Neckers L, Trepel JB, Pacak K.

PLoS One. 2013;8(2):e56083. doi: 10.1371/journal.pone.0056083. Epub 2013 Feb 14.


TIMP-2 modulates cancer cell transcriptional profile and enhances E-cadherin/beta-catenin complex expression in A549 lung cancer cells.

Bourboulia D, Han H, Jensen-Taubman S, Gavil N, Isaac B, Wei B, Neckers L, Stetler-Stevenson WG.

Oncotarget. 2013 Jan;4(1):166-76.

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