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Items: 1 to 50 of 142

1.

Design and Synthesis of Fungal-Selective Resorcylate Aminopyrazole Hsp90 Inhibitors.

Huang DS, LeBlanc EV, Shekhar-Guturja T, Robbins N, Krysan DJ, Pizarro J, Whitesell L, Cowen LE, Brown LE.

J Med Chem. 2019 Sep 26. doi: 10.1021/acs.jmedchem.9b00826. [Epub ahead of print]

PMID:
31513387
2.

Rebalancing Protein Homeostasis Enhances Tumor Antigen Presentation.

Jaeger AM, Stopfer L, Lee S, Gaglia G, Sandel D, Santagata S, Lin NU, Trepel JB, White F, Jacks T, Lindquist S, Whitesell L.

Clin Cancer Res. 2019 Nov 1;25(21):6392-6405. doi: 10.1158/1078-0432.CCR-19-0596. Epub 2019 Jun 18.

PMID:
31213460
3.

Author Correction: Mitochondrial metabolism promotes adaptation to proteotoxic stress.

Tsvetkov P, Detappe A, Cai K, Keys HR, Brune Z, Ying W, Thiru P, Reidy M, Kugener G, Rossen J, Kocak M, Kory N, Tsherniak A, Santagata S, Whitesell L, Ghobrial IM, Markley JL, Lindquist S, Golub TR.

Nat Chem Biol. 2019 Jul;15(7):757. doi: 10.1038/s41589-019-0315-5.

PMID:
31164776
4.

Mitochondrial metabolism promotes adaptation to proteotoxic stress.

Tsvetkov P, Detappe A, Cai K, Keys HR, Brune Z, Ying W, Thiru P, Reidy M, Kugener G, Rossen J, Kocak M, Kory N, Tsherniak A, Santagata S, Whitesell L, Ghobrial IM, Markley JL, Lindquist S, Golub TR.

Nat Chem Biol. 2019 Jul;15(7):681-689. doi: 10.1038/s41589-019-0291-9. Epub 2019 May 27. Erratum in: Nat Chem Biol. 2019 Jun 4;:.

PMID:
31133756
5.

Structural basis for species-selective targeting of Hsp90 in a pathogenic fungus.

Whitesell L, Robbins N, Huang DS, McLellan CA, Shekhar-Guturja T, LeBlanc EV, Nation CS, Hui R, Hutchinson A, Collins C, Chatterjee S, Trilles R, Xie JL, Krysan DJ, Lindquist S, Porco JA Jr, Tatu U, Brown LE, Pizarro J, Cowen LE.

Nat Commun. 2019 Jan 24;10(1):402. doi: 10.1038/s41467-018-08248-w.

6.

Withaferin A and Withanolide D Analogues with Dual Heat-Shock-Inducing and Cytotoxic Activities: Semisynthesis and Biological Evaluation.

Wijeratne EMK, Oliveira MCF, Mafezoli J, Xu YM, Minguzzi S, Batista PHJ, Pessoa ODL, Whitesell L, Gunatilaka AAL.

J Nat Prod. 2018 Apr 27;81(4):825-837. doi: 10.1021/acs.jnatprod.7b00918. Epub 2018 Mar 14.

PMID:
29537263
7.

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 Jul;23(4):467-482. doi: 10.1007/s12192-018-0877-2. Epub 2018 Feb 1. Review.

8.

FKBP12 contributes to α-synuclein toxicity by regulating the calcineurin-dependent phosphoproteome.

Caraveo G, Soste M, Cappelleti V, Fanning S, van Rossum DB, Whitesell L, Huang Y, Chung CY, Baru V, Zaichick S, Picotti P, Lindquist S.

Proc Natl Acad Sci U S A. 2017 Dec 26;114(52):E11313-E11322. doi: 10.1073/pnas.1711926115. Epub 2017 Dec 11.

9.

Inhibiting mitochondrial phosphate transport as an unexploited antifungal strategy.

McLellan CA, Vincent BM, Solis NV, Lancaster AK, Sullivan LB, Hartland CL, Youngsaye W, Filler SG, Whitesell L, Lindquist S.

Nat Chem Biol. 2018 Feb;14(2):135-141. doi: 10.1038/nchembio.2534. Epub 2017 Dec 11.

10.

Inhibiting the oncogenic translation program is an effective therapeutic strategy in multiple myeloma.

Manier S, Huynh D, Shen YJ, Zhou J, Yusufzai T, Salem KZ, Ebright RY, Shi J, Park J, Glavey SV, Devine WG, Liu CJ, Leleu X, Quesnel B, Roche-Lestienne C, Snyder JK, Brown LE, Gray N, Bradner J, Whitesell L, Porco JA Jr, Ghobrial IM.

Sci Transl Med. 2017 May 10;9(389). pii: eaal2668. doi: 10.1126/scitranslmed.aal2668.

11.

HSP90 Shapes the Consequences of Human Genetic Variation.

Karras GI, Yi S, Sahni N, Fischer M, Xie J, Vidal M, D'Andrea AD, Whitesell L, Lindquist S.

Cell. 2017 Feb 23;168(5):856-866.e12. doi: 10.1016/j.cell.2017.01.023. Epub 2017 Feb 16.

12.

Suppression of 19S proteasome subunits marks emergence of an altered cell state in diverse cancers.

Tsvetkov P, Sokol E, Jin D, Brune Z, Thiru P, Ghandi M, Garraway LA, Gupta PB, Santagata S, Whitesell L, Lindquist S.

Proc Natl Acad Sci U S A. 2017 Jan 10;114(2):382-387. doi: 10.1073/pnas.1619067114. Epub 2016 Dec 27.

13.

Susan Lindquist (1949-2016).

Whitesell L, Santagata S.

Science. 2016 Nov 25;354(6315):974. No abstract available.

PMID:
27884995
14.

A Fungal-Selective Cytochrome bc1 Inhibitor Impairs Virulence and Prevents the Evolution of Drug Resistance.

Vincent BM, Langlois JB, Srinivas R, Lancaster AK, Scherz-Shouval R, Whitesell L, Tidor B, Buchwald SL, Lindquist S.

Cell Chem Biol. 2016 Aug 18;23(8):978-991. doi: 10.1016/j.chembiol.2016.06.016. Epub 2016 Aug 11.

15.

Synthesis of Aza-Rocaglates via ESIPT-Mediated (3+2) Photocycloaddition.

Wang W, Cencic R, Whitesell L, Pelletier J, Porco JA Jr.

Chemistry. 2016 Aug 16;22(34):12006-10. doi: 10.1002/chem.201602953. Epub 2016 Jul 15.

16.

Preface.

Isaacs J, Whitesell L.

Adv Cancer Res. 2016;129:xiii-xv. doi: 10.1016/S0065-230X(16)30016-1. No abstract available.

PMID:
26916008
17.

Endothelial Thermotolerance Impairs Nanoparticle Transport in Tumors.

Bagley AF, Scherz-Shouval R, Galie PA, Zhang AQ, Wyckoff J, Whitesell L, Chen CS, Lindquist S, Bhatia SN.

Cancer Res. 2015 Aug 15;75(16):3255-67. doi: 10.1158/0008-5472.CAN-15-0325. Epub 2015 Jun 29.

18.

Nontoxic antimicrobials that evade drug resistance.

Davis SA, Vincent BM, Endo MM, Whitesell L, Marchillo K, Andes DR, Lindquist S, Burke MD.

Nat Chem Biol. 2015 Jul;11(7):481-7. doi: 10.1038/nchembio.1821. Epub 2015 Jun 1.

19.

Widespread macromolecular interaction perturbations in human genetic disorders.

Sahni N, Yi S, Taipale M, Fuxman Bass JI, Coulombe-Huntington J, Yang F, Peng J, Weile J, Karras GI, Wang Y, Kovács IA, Kamburov A, Krykbaeva I, Lam MH, Tucker G, Khurana V, Sharma A, Liu YY, Yachie N, Zhong Q, Shen Y, Palagi A, San-Miguel A, Fan C, Balcha D, Dricot A, Jordan DM, Walsh JM, Shah AA, Yang X, Stoyanova AK, Leighton A, Calderwood MA, Jacob Y, Cusick ME, Salehi-Ashtiani K, Whitesell LJ, Sunyaev S, Berger B, Barabási AL, Charloteaux B, Hill DE, Hao T, Roth FP, Xia Y, Walhout AJM, Lindquist S, Vidal M.

Cell. 2015 Apr 23;161(3):647-660. doi: 10.1016/j.cell.2015.04.013.

20.

Biomimetic kinetic resolution: highly enantio- and diastereoselective transfer hydrogenation of aglain ketones to access flavagline natural products.

Stone SD, Lajkiewicz NJ, Whitesell L, Hilmy A, Porco JA Jr.

J Am Chem Soc. 2015 Jan 14;137(1):525-30. doi: 10.1021/ja511728b. Epub 2014 Dec 29.

21.

HSP90 empowers evolution of resistance to hormonal therapy in human breast cancer models.

Whitesell L, Santagata S, Mendillo ML, Lin NU, Proia DA, Lindquist S.

Proc Natl Acad Sci U S A. 2014 Dec 23;111(51):18297-302. doi: 10.1073/pnas.1421323111. Epub 2014 Dec 8.

22.

Calcineurin determines toxic versus beneficial responses to α-synuclein.

Caraveo G, Auluck PK, Whitesell L, Chung CY, Baru V, Mosharov EV, Yan X, Ben-Johny M, Soste M, Picotti P, Kim H, Caldwell KA, Caldwell GA, Sulzer D, Yue DT, Lindquist S.

Proc Natl Acad Sci U S A. 2014 Aug 26;111(34):E3544-52. doi: 10.1073/pnas.1413201111. Epub 2014 Aug 13.

23.

The reprogramming of tumor stroma by HSF1 is a potent enabler of malignancy.

Scherz-Shouval R, Santagata S, Mendillo ML, Sholl LM, Ben-Aharon I, Beck AH, Dias-Santagata D, Koeva M, Stemmer SM, Whitesell L, Lindquist S.

Cell. 2014 Jul 31;158(3):564-78. doi: 10.1016/j.cell.2014.05.045.

24.
25.

Probing Metabolic Requirements for Fungal Virulence — Probe 1.

Hartland CL, Youngsaye W, Pu J, Vincent B, Mosher CM, Anthoine T, Johnston S, Whitesell L, Dandapani S, Perez J, Munoz B, Palmer M, Lindquist S, Schreiber SL.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Apr 16 [updated 2014 May 14].

26.

Structure-activity relationships for withanolides as inducers of the cellular heat-shock response.

Wijeratne EM, Xu YM, Scherz-Shouval R, Marron MT, Rocha DD, Liu MX, Costa-Lotufo LV, Santagata S, Lindquist S, Whitesell L, Gunatilaka AA.

J Med Chem. 2014 Apr 10;57(7):2851-63. doi: 10.1021/jm401279n. Epub 2014 Mar 25.

PMID:
24625088
27.

Fitness trade-offs restrict the evolution of resistance to amphotericin B.

Vincent BM, Lancaster AK, Scherz-Shouval R, Whitesell L, Lindquist S.

PLoS Biol. 2013 Oct;11(10):e1001692. doi: 10.1371/journal.pbio.1001692. Epub 2013 Oct 29.

28.

ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans.

Youngsaye W, Hartland CL, Morgan BJ, Ting A, Nag PP, Vincent B, Mosher CA, Bittker JA, Dandapani S, Palmer M, Whitesell L, Lindquist S, Schreiber SL, Munoz B.

Beilstein J Org Chem. 2013 Jul 26;9:1501-7. doi: 10.3762/bjoc.9.171. eCollection 2013.

29.

Tight coordination of protein translation and HSF1 activation supports the anabolic malignant state.

Santagata S, Mendillo ML, Tang YC, Subramanian A, Perley CC, Roche SP, Wong B, Narayan R, Kwon H, Koeva M, Amon A, Golub TR, Porco JA Jr, Whitesell L, Lindquist S.

Science. 2013 Jul 19;341(6143):1238303. doi: 10.1126/science.1238303.

30.

Synthesis and biological evaluation of novobiocin analogues as potential heat shock protein 90 inhibitors.

Gunaherath GM, Marron MT, Wijeratne EM, Whitesell L, Gunatilaka AA.

Bioorg Med Chem. 2013 Sep 1;21(17):5118-29. doi: 10.1016/j.bmc.2013.06.042. Epub 2013 Jun 27.

PMID:
23859777
31.

Chaperones as thermodynamic sensors of drug-target interactions reveal kinase inhibitor specificities in living cells.

Taipale M, Krykbaeva I, Whitesell L, Santagata S, Zhang J, Liu Q, Gray NS, Lindquist S.

Nat Biotechnol. 2013 Jul;31(7):630-7. doi: 10.1038/nbt.2620. Epub 2013 Jun 30.

32.

Identification of small molecules that selectively inhibit fluconazole-resistant Candida albicans in the presence of fluconazole but not in its absence.

Hartland CL, Youngsaye W, Morgan B, Buhrlage S, Bittker J, Johnston S, Lindquist S, Whitesell L, Vincent B, MacPherson L, Munoz B, Palmer M, Schreiber SL.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Oct 29 [updated 2012 Nov 7].

33.

Loss of tumor suppressor NF1 activates HSF1 to promote carcinogenesis.

Dai C, Santagata S, Tang Z, Shi J, Cao J, Kwon H, Bronson RT, Whitesell L, Lindquist S.

J Clin Invest. 2012 Oct;122(10):3742-54. doi: 10.1172/JCI62727. Epub 2012 Sep 4.

34.

HSF1 drives a transcriptional program distinct from heat shock to support highly malignant human cancers.

Mendillo ML, Santagata S, Koeva M, Bell GW, Hu R, Tamimi RM, Fraenkel E, Ince TA, Whitesell L, Lindquist S.

Cell. 2012 Aug 3;150(3):549-62. doi: 10.1016/j.cell.2012.06.031.

35.

Identification of small molecules that selectively inhibit fluconazole-resistant Candida albicans in the presence of fluconazole but not in its absence - Probe 2.

Hartland CL, Youngsaye W, Morgan B, Ting A, Nag P, Buhrlage S, Johnston S, Bittker J, Vincent B, Whitesell L, Dandapani S, MacPherson L, Munoz B, Palmer M, Lindquist S, Schreiber SL.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Mar 24 [updated 2011 Dec 12].

36.

Identification of Small Molecules that Selectively Inhibit Fluconazole-Resistant Candida Albicans in the Presence of Fluconazole but not in its Absence - Probe 3.

Hartland CL, Youngsaye W, Dockendorff C, Johnston S, Bittker J, Vincent B, Whitesell L, Dandapani S, MacPherson L, Munoz B, Palmer M, Lindquist S, Schreiber SL.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Mar 31 [updated 2011 Nov 21].

37.

Inhibiting HSP90 to treat cancer: a strategy in evolution.

Whitesell L, Santagata S, Lin NU.

Curr Mol Med. 2012 Nov 1;12(9):1108-24. Review.

PMID:
22804235
38.

Inhibiting GPI anchor biosynthesis in fungi stresses the endoplasmic reticulum and enhances immunogenicity.

McLellan CA, Whitesell L, King OD, Lancaster AK, Mazitschek R, Lindquist S.

ACS Chem Biol. 2012 Sep 21;7(9):1520-8. Epub 2012 Jun 22.

PMID:
22724584
39.

Overcoming fluconazole resistance in Candida albicans clinical isolates with tetracyclic indoles.

Youngsaye W, Dockendorff C, Vincent B, Hartland CL, Bittker JA, Dandapani S, Palmer M, Whitesell L, Lindquist S, Schreiber SL, Munoz B.

Bioorg Med Chem Lett. 2012 May 1;22(9):3362-5. doi: 10.1016/j.bmcl.2012.02.035. Epub 2012 Feb 22.

40.

Geopyxins A-E, ent-kaurane diterpenoids from endolichenic fungal strains Geopyxis aff. majalis and Geopyxis sp. AZ0066: structure-activity relationships of geopyxins and their analogues.

Wijeratne EM, Bashyal BP, Liu MX, Rocha DD, Gunaherath GM, U'Ren JM, Gunatilaka MK, Arnold AE, Whitesell L, Gunatilaka AA.

J Nat Prod. 2012 Mar 23;75(3):361-9. doi: 10.1021/np200769q. Epub 2012 Jan 20.

41.

HSP90 as a platform for the assembly of more effective cancer chemotherapy.

Whitesell L, Lin NU.

Biochim Biophys Acta. 2012 Mar;1823(3):756-66. doi: 10.1016/j.bbamcr.2011.12.006. Epub 2011 Dec 24. Review.

42.

Using the heat-shock response to discover anticancer compounds that target protein homeostasis.

Santagata S, Xu YM, Wijeratne EM, Kontnik R, Rooney C, Perley CC, Kwon H, Clardy J, Kesari S, Whitesell L, Lindquist S, Gunatilaka AA.

ACS Chem Biol. 2012 Feb 17;7(2):340-9. doi: 10.1021/cb200353m. Epub 2011 Nov 30.

43.

High levels of nuclear heat-shock factor 1 (HSF1) are associated with poor prognosis in breast cancer.

Santagata S, Hu R, Lin NU, Mendillo ML, Collins LC, Hankinson SE, Schnitt SJ, Whitesell L, Tamimi RM, Lindquist S, Ince TA.

Proc Natl Acad Sci U S A. 2011 Nov 8;108(45):18378-83. doi: 10.1073/pnas.1115031108. Epub 2011 Oct 31.

44.

Piperazinyl quinolines as chemosensitizers to increase fluconazole susceptibility of Candida albicans clinical isolates.

Youngsaye W, Vincent B, Hartland CL, Morgan BJ, Buhrlage SJ, Johnston S, Bittker JA, MacPherson L, Dandapani S, Palmer M, Whitesell L, Lindquist S, Schreiber SL, Munoz B.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5502-5. doi: 10.1016/j.bmcl.2011.06.105. Epub 2011 Jun 30.

45.

Autoantibodies to villin occur frequently in IPEX, a severe immune dysregulation, syndrome caused by mutation of FOXP3.

Kobayashi I, Kubota M, Yamada M, Tanaka H, Itoh S, Sasahara Y, Whitesell L, Ariga T.

Clin Immunol. 2011 Oct;141(1):83-9. doi: 10.1016/j.clim.2011.05.010. Epub 2011 Jun 13.

PMID:
21741320
46.

Accuracy of cardiac magnetic resonance of absolute myocardial blood flow with a high-field system: comparison with conventional field strength.

Christian TF, Bell SP, Whitesell L, Jerosch-Herold M.

JACC Cardiovasc Imaging. 2009 Sep;2(9):1103-10. doi: 10.1016/j.jcmg.2009.06.009.

47.

Inhibiting the transcription factor HSF1 as an anticancer strategy.

Whitesell L, Lindquist S.

Expert Opin Ther Targets. 2009 Apr;13(4):469-78. doi: 10.1517/14728220902832697 . Review.

PMID:
19335068
48.

Harnessing Hsp90 function as a powerful, broadly effective therapeutic strategy for fungal infectious disease.

Cowen LE, Singh SD, Köhler JR, Collins C, Zaas AK, Schell WA, Aziz H, Mylonakis E, Perfect JR, Whitesell L, Lindquist S.

Proc Natl Acad Sci U S A. 2009 Feb 24;106(8):2818-23. doi: 10.1073/pnas.0813394106. Epub 2009 Feb 5.

49.

2,3-Dihydrowithaferin A-3beta-O-sulfate, a new potential prodrug of withaferin A from aeroponically grown Withania somnifera.

Xu YM, Marron MT, Seddon E, McLaughlin SP, Ray DT, Whitesell L, Gunatilaka AA.

Bioorg Med Chem. 2009 Mar 15;17(6):2210-4. doi: 10.1016/j.bmc.2008.10.091. Epub 2008 Nov 12.

PMID:
19056281
50.

Discovery of quinolinediones exhibiting a heat shock response and angiogenesis inhibition.

Hargreaves RH, David CL, Whitesell LJ, Labarbera DV, Jamil A, Chapuis JC, Skibo EB.

J Med Chem. 2008 Apr 24;51(8):2492-501. doi: 10.1021/jm7014099. Epub 2008 Mar 26.

PMID:
18363347

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