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Items: 1 to 50 of 147

1.

A 3-(4-nitronaphthen-1-yl) amino-benzoate analog as a bifunctional AKR1C3 inhibitor and AR antagonist: Head to head comparison with other advanced AKR1C3 targeted therapeutics.

Wangtrakuldee P, Adeniji AO, Zang T, Duan L, Khatri B, Twenter BM, Estrada MA, Higgins TF, Winkler JD, Penning TM.

J Steroid Biochem Mol Biol. 2019 Jan 11. pii: S0960-0760(18)30720-9. doi: 10.1016/j.jsbmb.2019.01.001. [Epub ahead of print]

PMID:
30641225
2.

PPT1 Promotes Tumor Growth and Is the Molecular Target of Chloroquine Derivatives in Cancer.

Rebecca VW, Nicastri MC, Fennelly C, Chude CI, Barber-Rotenberg JS, Ronghe A, McAfee Q, McLaughlin NP, Zhang G, Goldman AR, Ojha R, Piao S, Noguera-Ortega E, Martorella A, Alicea GM, Lee JJ, Schuchter LM, Xu X, Herlyn M, Marmorstein R, Gimotty PA, Speicher DW, Winkler JD, Amaravadi RK.

Cancer Discov. 2019 Feb;9(2):220-229. doi: 10.1158/2159-8290.CD-18-0706. Epub 2018 Nov 15.

PMID:
30442709
3.

Targeting quiescent leukemic stem cells using second generation autophagy inhibitors.

Baquero P, Dawson A, Mukhopadhyay A, Kuntz EM, Mitchell R, Olivares O, Ianniciello A, Scott MT, Dunn K, Nicastri MC, Winkler JD, Michie AM, Ryan KM, Halsey C, Gottlieb E, Keaney EP, Murphy LO, Amaravadi RK, Holyoake TL, Helgason GV.

Leukemia. 2018 Sep 5. doi: 10.1038/s41375-018-0252-4. [Epub ahead of print]

PMID:
30185934
4.

Design, Synthesis, and Biological Evaluation of Allosteric Effectors That Enhance CO Release from Carboxyhemoglobin.

Goldstein SR, Liu C, Safo MK, Nakagawa A, Zapol WM, Winkler JD.

ACS Med Chem Lett. 2018 May 11;9(7):714-718. doi: 10.1021/acsmedchemlett.8b00166. eCollection 2018 Jul 12.

PMID:
30034606
5.

N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[d]thiazol-2-yl)cyclopropanecarboxamide (TAK632) Promotes Inhibition of BRAF through the Induction of Inhibited Dimers.

Grasso M, Estrada MA, Berrios KN, Winkler JD, Marmorstein R.

J Med Chem. 2018 Jun 14;61(11):5034-5046. doi: 10.1021/acs.jmedchem.8b00499. Epub 2018 May 18.

PMID:
29727562
6.

Dimeric quinacrines as chemical tools to identify PPT1, a new regulator of autophagy in cancer cells.

Nicastri MC, Rebecca VW, Amaravadi RK, Winkler JD.

Mol Cell Oncol. 2017 Nov 30;5(1):e1395504. doi: 10.1080/23723556.2017.1395504. eCollection 2018.

7.

Synthesis and Structure-Activity Relationship Study of Biliatresone, a Plant Isoflavonoid That Causes Biliary Atresia.

Estrada MA, Zhao X, Lorent K, Kriegermeier A, Nagao SA, Berritt S, Wells RG, Pack M, Winkler JD.

ACS Med Chem Lett. 2017 Dec 14;9(1):61-64. doi: 10.1021/acsmedchemlett.7b00479. eCollection 2018 Jan 11.

8.

Gilbert Stork (1921-2017).

Nakamura E, Winkler JD, Aggarwal VK.

Angew Chem Int Ed Engl. 2018 Jan 2;57(1):36. doi: 10.1002/anie.201711474. Epub 2017 Nov 29.

PMID:
29193592
9.

Refactoring the Genetic Code for Increased Evolvability.

Pines G, Winkler JD, Pines A, Gill RT.

MBio. 2017 Nov 14;8(6). pii: e01654-17. doi: 10.1128/mBio.01654-17.

10.

The Tolerome: A Database of Transcriptome-Level Contributions to Diverse Escherichia coli Resistance and Tolerance Phenotypes.

Erickson KE, Winkler JD, Nguyen DT, Gill RT, Chatterjee A.

ACS Synth Biol. 2017 Dec 15;6(12):2302-2315. doi: 10.1021/acssynbio.7b00235. Epub 2017 Oct 19.

PMID:
29017328
11.

ALDH1A1 and HLTF modulate the activity of lysosomal autophagy inhibitors in cancer cells.

Piao S, Ojha R, Rebecca VW, Samanta A, Ma XH, Mcafee Q, Nicastri MC, Buckley M, Brown E, Winkler JD, Gimotty PA, Amaravadi RK.

Autophagy. 2017;13(12):2056-2071. doi: 10.1080/15548627.2017.1377377. Epub 2017 Oct 5.

12.

A Unified Approach to Targeting the Lysosome's Degradative and Growth Signaling Roles.

Rebecca VW, Nicastri MC, McLaughlin N, Fennelly C, McAfee Q, Ronghe A, Nofal M, Lim CY, Witze E, Chude CI, Zhang G, Alicea GM, Piao S, Murugan S, Ojha R, Levi SM, Wei Z, Barber-Rotenberg JS, Murphy ME, Mills GB, Lu Y, Rabinowitz J, Marmorstein R, Liu Q, Liu S, Xu X, Herlyn M, Zoncu R, Brady DC, Speicher DW, Winkler JD, Amaravadi RK.

Cancer Discov. 2017 Nov;7(11):1266-1283. doi: 10.1158/2159-8290.CD-17-0741. Epub 2017 Sep 12.

13.

ATG5 Mediates a Positive Feedback Loop between Wnt Signaling and Autophagy in Melanoma.

Ndoye A, Budina-Kolomets A, Kugel CH 3rd, Webster MR, Kaur A, Behera R, Rebecca VW, Li L, Brafford PA, Liu Q, Gopal YNV, Davies MA, Mills GB, Xu X, Wu H, Herlyn M, Nicastri MC, Winkler JD, Soengas MS, Amaravadi RK, Murphy ME, Weeraratna AT.

Cancer Res. 2017 Nov 1;77(21):5873-5885. doi: 10.1158/0008-5472.CAN-17-0907. Epub 2017 Sep 8.

14.

Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1.

Crew AP, Raina K, Dong H, Qian Y, Wang J, Vigil D, Serebrenik YV, Hamman BD, Morgan A, Ferraro C, Siu K, Neklesa TK, Winkler JD, Coleman KG, Crews CM.

J Med Chem. 2018 Jan 25;61(2):583-598. doi: 10.1021/acs.jmedchem.7b00635. Epub 2017 Jul 10.

PMID:
28692295
15.

CDK4/6 and autophagy inhibitors synergistically induce senescence in Rb positive cytoplasmic cyclin E negative cancers.

Vijayaraghavan S, Karakas C, Doostan I, Chen X, Bui T, Yi M, Raghavendra AS, Zhao Y, Bashour SI, Ibrahim NK, Karuturi M, Wang J, Winkler JD, Amaravadi RK, Hunt KK, Tripathy D, Keyomarsi K.

Nat Commun. 2017 Jun 27;8:15916. doi: 10.1038/ncomms15916.

16.

Autophagy supports generation of cells with high CD44 expression via modulation of oxidative stress and Parkin-mediated mitochondrial clearance.

Whelan KA, Chandramouleeswaran PM, Tanaka K, Natsuizaka M, Guha M, Srinivasan S, Darling DS, Kita Y, Natsugoe S, Winkler JD, Klein-Szanto AJ, Amaravadi RK, Avadhani NG, Rustgi AK, Nakagawa H.

Oncogene. 2017 Aug 24;36(34):4843-4858. doi: 10.1038/onc.2017.102. Epub 2017 Apr 17.

17.

Ischemia Induces Quiescence and Autophagy Dependence in Hepatocellular Carcinoma.

Gade TPF, Tucker E, Nakazawa MS, Hunt SJ, Wong W, Krock B, Weber CN, Nadolski GJ, Clark TWI, Soulen MC, Furth EE, Winkler JD, Amaravadi RK, Simon MC.

Radiology. 2017 Jun;283(3):702-710. doi: 10.1148/radiol.2017160728. Epub 2017 Mar 2.

18.

Targeted protein degradation by PROTACs.

Neklesa TK, Winkler JD, Crews CM.

Pharmacol Ther. 2017 Jun;174:138-144. doi: 10.1016/j.pharmthera.2017.02.027. Epub 2017 Feb 14. Review.

PMID:
28223226
19.

Autophagy Inhibition Enhances Sunitinib Efficacy in Clear Cell Ovarian Carcinoma.

DeVorkin L, Hattersley M, Kim P, Ries J, Spowart J, Anglesio MS, Levi SM, Huntsman DG, Amaravadi RK, Winkler JD, Tinker AV, Lum JJ.

Mol Cancer Res. 2017 Mar;15(3):250-258. doi: 10.1158/1541-7786.MCR-16-0132. Epub 2017 Feb 9.

20.

Chemically Linked Vemurafenib Inhibitors Promote an Inactive BRAFV600E Conformation.

Grasso M, Estrada MA, Ventocilla C, Samanta M, Maksimoska J, Villanueva J, Winkler JD, Marmorstein R.

ACS Chem Biol. 2016 Oct 21;11(10):2876-2888. Epub 2016 Sep 6.

21.

PUMA-dependent apoptosis in NSCLC cancer cells by a dimeric β-carboline.

Chatwichien J, Basu S, Budina-Kolomets A, Murphy ME, Winkler JD.

Bioorg Med Chem Lett. 2016 Oct 15;26(20):4884-4887. doi: 10.1016/j.bmcl.2016.09.030. Epub 2016 Sep 13.

22.

The Resistome: A Comprehensive Database of Escherichia coli Resistance Phenotypes.

Winkler JD, Halweg-Edwards AL, Erickson KE, Choudhury A, Pines G, Gill RT.

ACS Synth Biol. 2016 Dec 16;5(12):1566-1577. Epub 2016 Aug 2.

PMID:
27438180
23.

Quantifying complexity in metabolic engineering using the LASER database.

Winkler JD, Halweg-Edwards AL, Gill RT.

Metab Eng Commun. 2016 Jul 7;3:227-233. doi: 10.1016/j.meteno.2016.07.002. eCollection 2016 Dec.

24.

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer.

Raina K, Lu J, Qian Y, Altieri M, Gordon D, Rossi AM, Wang J, Chen X, Dong H, Siu K, Winkler JD, Crew AP, Crews CM, Coleman KG.

Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9. doi: 10.1073/pnas.1521738113. Epub 2016 Jun 6.

25.

A Web Interface for Codon Compression.

Halweg-Edwards AL, Pines G, Winkler JD, Pines A, Gill RT.

ACS Synth Biol. 2016 Sep 16;5(9):1021-3. doi: 10.1021/acssynbio.6b00026. Epub 2016 May 19.

PMID:
27169595
26.

Sex steroids regulate skin pigmentation through nonclassical membrane-bound receptors.

Natale CA, Duperret EK, Zhang J, Sadeghi R, Dahal A, O'Brien KT, Cookson R, Winkler JD, Ridky TW.

Elife. 2016 Apr 26;5. pii: e15104. doi: 10.7554/eLife.15104.

27.

Genome-Wide Tuning of Protein Expression Levels to Rapidly Engineer Microbial Traits.

Freed EF, Winkler JD, Weiss SJ, Garst AD, Mutalik VK, Arkin AP, Knight R, Gill RT.

ACS Synth Biol. 2015 Nov 20;4(11):1244-53. doi: 10.1021/acssynbio.5b00133. Epub 2015 Nov 5.

PMID:
26478262
28.

The Suramin Derivative NF449 Interacts with the 5-fold Vertex of the Enterovirus A71 Capsid to Prevent Virus Attachment to PSGL-1 and Heparan Sulfate.

Nishimura Y, McLaughlin NP, Pan J, Goldstein S, Hafenstein S, Shimizu H, Winkler JD, Bergelson JM.

PLoS Pathog. 2015 Oct 2;11(10):e1005184. doi: 10.1371/journal.ppat.1005184. eCollection 2015 Oct.

29.

Complex systems in metabolic engineering.

Winkler JD, Erickson K, Choudhury A, Halweg-Edwards AL, Gill RT.

Curr Opin Biotechnol. 2015 Dec;36:107-14. doi: 10.1016/j.copbio.2015.08.002. Epub 2015 Aug 28. Review.

PMID:
26319897
30.

The emergence of commodity-scale genetic manipulation.

Halweg-Edwards AL, Grau WC, Winkler JD, Garst AD, Gill RT.

Curr Opin Chem Biol. 2015 Oct;28:150-5. doi: 10.1016/j.cbpa.2015.07.009. Epub 2015 Aug 22. Review.

PMID:
26302383
31.

Design, Synthesis and Biological Evaluation of β-Carboline Dimers Based on the Structure of Neokauluamine.

Chatwichien J, Basu S, Murphy ME, Hamann MT, Winkler JD.

Tetrahedron Lett. 2015 Jun 3;56(23):3515-3517.

32.

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.

Lu J, Qian Y, Altieri M, Dong H, Wang J, Raina K, Hines J, Winkler JD, Crew AP, Coleman K, Crews CM.

Chem Biol. 2015 Jun 18;22(6):755-63. doi: 10.1016/j.chembiol.2015.05.009. Epub 2015 Jun 4.

33.

Inhibition of JNK Sensitizes Hypoxic Colon Cancer Cells to DNA-Damaging Agents.

Vasilevskaya IA, Selvakumaran M, Hierro LC, Goldstein SR, Winkler JD, O'Dwyer PJ.

Clin Cancer Res. 2015 Sep 15;21(18):4143-52. doi: 10.1158/1078-0432.CCR-15-0352. Epub 2015 May 28.

34.

Bacterial Recombineering: Genome Engineering via Phage-Based Homologous Recombination.

Pines G, Freed EF, Winkler JD, Gill RT.

ACS Synth Biol. 2015 Nov 20;4(11):1176-85. doi: 10.1021/acssynbio.5b00009. Epub 2015 Apr 27. Review.

PMID:
25856528
35.

Autophagy gene Atg16L1 prevents lethal T cell alloreactivity mediated by dendritic cells.

Hubbard-Lucey VM, Shono Y, Maurer K, West ML, Singer NV, Ziegler CG, Lezcano C, Motta AC, Schmid K, Levi SM, Murphy GF, Liu C, Winkler JD, Amaravadi RK, Rogler G, Dickinson AM, Holler E, van den Brink MR, Cadwell K.

Immunity. 2014 Oct 16;41(4):579-91. doi: 10.1016/j.immuni.2014.09.011. Epub 2014 Oct 9.

36.

Recent advances in the evolutionary engineering of industrial biocatalysts.

Winkler JD, Kao KC.

Genomics. 2014 Dec;104(6 Pt A):406-11. doi: 10.1016/j.ygeno.2014.09.006. Epub 2014 Sep 28. Review.

37.

Evolved osmotolerant Escherichia coli mutants frequently exhibit defective N-acetylglucosamine catabolism and point mutations in cell shape-regulating protein MreB.

Winkler JD, Garcia C, Olson M, Callaway E, Kao KC.

Appl Environ Microbiol. 2014 Jun;80(12):3729-40. doi: 10.1128/AEM.00499-14. Epub 2014 Apr 11.

38.

Lys05: a new lysosomal autophagy inhibitor.

Amaravadi RK, Winkler JD.

Autophagy. 2012 Sep;8(9):1383-4. doi: 10.4161/auto.20958. Epub 2012 Aug 10.

39.

Autophagy inhibitor Lys05 has single-agent antitumor activity and reproduces the phenotype of a genetic autophagy deficiency.

McAfee Q, Zhang Z, Samanta A, Levi SM, Ma XH, Piao S, Lynch JP, Uehara T, Sepulveda AR, Davis LE, Winkler JD, Amaravadi RK.

Proc Natl Acad Sci U S A. 2012 May 22;109(21):8253-8. doi: 10.1073/pnas.1118193109. Epub 2012 May 7.

40.

Crystal structures of AKR1C3 containing an N-(aryl)amino-benzoate inhibitor and a bifunctional AKR1C3 inhibitor and androgen receptor antagonist. Therapeutic leads for castrate resistant prostate cancer.

Chen M, Adeniji AO, Twenter BM, Winkler JD, Christianson DW, Penning TM.

Bioorg Med Chem Lett. 2012 May 15;22(10):3492-7. doi: 10.1016/j.bmcl.2012.03.085. Epub 2012 Mar 29.

41.

Development of potent and selective inhibitors of aldo-keto reductase 1C3 (type 5 17β-hydroxysteroid dehydrogenase) based on N-phenyl-aminobenzoates and their structure-activity relationships.

Adeniji AO, Twenter BM, Byrns MC, Jin Y, Chen M, Winkler JD, Penning TM.

J Med Chem. 2012 Mar 8;55(5):2311-23. doi: 10.1021/jm201547v. Epub 2012 Feb 15.

42.

A NEW APPROACH TO THE SYNTHESIS OF SUBSTITUTED PHENAZINES VIA PALLADIUM-CATALYZED ARYL LIGATIONi.

Winkler JD, Twenter BM, Gendrineau T.

Heterocycles. 2012;84(2). doi: 10.3987/COM-11-S(P)76.

43.

Design, synthesis, and biological evaluation of estrone-derived hedgehog signaling inhibitors.

Winkler JD, Isaacs AK, Xiang C, Baubet V, Dahmane N.

Tetrahedron. 2011 Dec 30;67(52):10261-10266.

44.

STUDIES DIRECTED TOWARD THE SYNTHESIS OF NAKADOMARIN A.

Haimowitz T, Fitzgerald ME, Winkler JD.

Tetrahedron Lett. 2011 Apr 27;52(17):2162-2164.

45.

Studies directed toward the elucidation of the pharmacophore of steroid-based Sonic Hedgehog signaling inhibitors.

Isaacs AK, Xiang C, Baubet V, Dahmane N, Winkler JD.

Org Lett. 2011 Oct 7;13(19):5140-3. doi: 10.1021/ol202020c. Epub 2011 Sep 9.

46.

Stereoselective synthesis of F-ring saturated estrone-derived inhibitors of Hedgehog signaling based on cyclopamine.

Zhang Z, Baubet V, Ventocilla C, Xiang C, Dahmane N, Winkler JD.

Org Lett. 2011 Sep 16;13(18):4786-9. doi: 10.1021/ol2017966. Epub 2011 Aug 15.

47.

Discovery of substituted 3-(phenylamino)benzoic acids as potent and selective inhibitors of type 5 17β-hydroxysteroid dehydrogenase (AKR1C3).

Adeniji AO, Twenter BM, Byrns MC, Jin Y, Winkler JD, Penning TM.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1464-8. doi: 10.1016/j.bmcl.2011.01.010. Epub 2011 Jan 7.

48.

Design and synthesis of inhibitors of Hedgehog signaling based on the alkaloid cyclopamine.

Winkler JD, Isaacs A, Holderbaum L, Tatard V, Dahmane N.

Org Lett. 2009 Jul 2;11(13):2824-7. doi: 10.1021/ol900974u.

PMID:
19552464
49.

De novo design and in vivo activity of conformationally restrained antimicrobial arylamide foldamers.

Choi S, Isaacs A, Clements D, Liu D, Kim H, Scott RW, Winkler JD, DeGrado WF.

Proc Natl Acad Sci U S A. 2009 Apr 28;106(17):6968-73. doi: 10.1073/pnas.0811818106. Epub 2009 Apr 9.

50.

An unusual pathway to cyclobutane formation via desulfurative intramolecular photocycloaddition of an enone benzothiazoline pair.

Jo H, Fitzgerald ME, Winkler JD.

Org Lett. 2009 Apr 16;11(8):1685-7. doi: 10.1021/ol900186y.

PMID:
19301922

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