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Items: 1 to 50 of 177

1.

The SERM/SERD bazedoxifene disrupts ESR1 helix 12 to overcome acquired hormone resistance in breast cancer cells.

Fanning SW, Jeselsohn R, Dharmarajan V, Mayne CG, Karimi M, Buchwalter G, Houtman R, Toy W, Fowler CE, Han R, Lainé M, Carlson KE, Martin TA, Nowak J, Nwachukwu JC, Hosfield DJ, Chandarlapaty S, Tajkhorshid E, Nettles KW, Griffin PR, Shen Y, Katzenellenbogen JA, Brown M, Greene GL.

Elife. 2018 Nov 29;7. pii: e37161. doi: 10.7554/eLife.37161.

2.

Antagonists for Constitutively Active Mutant Estrogen Receptors: Insights into the Roles of Antiestrogen-Core and Side-Chain.

Sharma A, Toy W, Guillen VS, Sharma N, Min J, Carlson KE, Mayne CG, Lin S, Sabio M, Greene G, Katzenellenbogen BS, Chandarlapaty S, Katzenellenbogen JA.

ACS Chem Biol. 2018 Dec 21;13(12):3374-3384. doi: 10.1021/acschembio.8b00877. Epub 2018 Nov 26.

PMID:
30404440
3.

Discovery of long-chain salicylketoxime derivatives as monoacylglycerol lipase (MAGL) inhibitors.

Bononi G, Granchi C, Lapillo M, Giannotti M, Nieri D, Fortunato S, Boustani ME, Caligiuri I, Poli G, Carlson KE, Kim SH, Macchia M, Martinelli A, Rizzolio F, Chicca A, Katzenellenbogen JA, Minutolo F, Tuccinardi T.

Eur J Med Chem. 2018 Sep 5;157:817-836. doi: 10.1016/j.ejmech.2018.08.038. Epub 2018 Aug 16.

PMID:
30144699
4.

New Class of Selective Estrogen Receptor Degraders (SERDs): Expanding the Toolbox of PROTAC Degrons.

Wang L, Guillen VS, Sharma N, Flessa K, Min J, Carlson KE, Toy W, Braqi S, Katzenellenbogen BS, Katzenellenbogen JA, Chandarlapaty S, Sharma A.

ACS Med Chem Lett. 2018 Jul 5;9(8):803-808. doi: 10.1021/acsmedchemlett.8b00106. eCollection 2018 Aug 9.

5.
6.

Long-Term Administration of Conjugated Estrogen and Bazedoxifene Decreased Murine Fecal β-Glucuronidase Activity Without Impacting Overall Microbiome Community.

Chen KLA, Liu X, Zhao YC, Hieronymi K, Rossi G, Auvil LS, Welge M, Bushell C, Smith RL, Carlson KE, Kim SH, Katzenellenbogen JA, Miller MJ, Madak-Erdogan Z.

Sci Rep. 2018 May 25;8(1):8166. doi: 10.1038/s41598-018-26506-1.

7.

Adamantyl Antiestrogens with Novel Side Chains Reveal a Spectrum of Activities in Suppressing Estrogen Receptor Mediated Activities in Breast Cancer Cells.

Min J, Guillen VS, Sharma A, Zhao Y, Ziegler Y, Gong P, Mayne CG, Srinivasan S, Kim SH, Carlson KE, Nettles KW, Katzenellenbogen BS, Katzenellenbogen JA.

J Med Chem. 2017 Jul 27;60(14):6321-6336. doi: 10.1021/acs.jmedchem.7b00585. Epub 2017 Jul 14.

8.

Structural and Molecular Mechanisms of Cytokine-Mediated Endocrine Resistance in Human Breast Cancer Cells.

Stender JD, Nwachukwu JC, Kastrati I, Kim Y, Strid T, Yakir M, Srinivasan S, Nowak J, Izard T, Rangarajan ES, Carlson KE, Katzenellenbogen JA, Yao XQ, Grant BJ, Leong HS, Lin CY, Frasor J, Nettles KW, Glass CK.

Mol Cell. 2017 Mar 16;65(6):1122-1135.e5. doi: 10.1016/j.molcel.2017.02.008.

9.

Exploring the Structural Compliancy versus Specificity of the Estrogen Receptor Using Isomeric Three-Dimensional Ligands.

Sharma N, Carlson KE, Nwachukwu JC, Srinivasan S, Sharma A, Nettles KW, Katzenellenbogen JA.

ACS Chem Biol. 2017 Feb 17;12(2):494-503. doi: 10.1021/acschembio.6b00918. Epub 2016 Dec 29.

10.

Activating ESR1 Mutations Differentially Affect the Efficacy of ER Antagonists.

Toy W, Weir H, Razavi P, Lawson M, Goeppert AU, Mazzola AM, Smith A, Wilson J, Morrow C, Wong WL, De Stanchina E, Carlson KE, Martin TS, Uddin S, Li Z, Fanning S, Katzenellenbogen JA, Greene G, Baselga J, Chandarlapaty S.

Cancer Discov. 2017 Mar;7(3):277-287. doi: 10.1158/2159-8290.CD-15-1523. Epub 2016 Dec 16.

11.

Selenophenes: Introducing a New Element into the Core of Non-Steroidal Estrogen Receptor Ligands.

Zhang S, Wang Z, Hu Z, Li C, Tang C, Carlson KE, Luo J, Dong C, Katzenellenbogen JA, Huang J, Zhou HB.

ChemMedChem. 2017 Feb 3;12(3):235-249. doi: 10.1002/cmdc.201600593. Epub 2017 Jan 9.

12.

Design of pathway preferential estrogens that provide beneficial metabolic and vascular effects without stimulating reproductive tissues.

Madak-Erdogan Z, Kim SH, Gong P, Zhao YC, Zhang H, Chambliss KL, Carlson KE, Mayne CG, Shaul PW, Korach KS, Katzenellenbogen JA, Katzenellenbogen BS.

Sci Signal. 2016 May 24;9(429):ra53. doi: 10.1126/scisignal.aad8170.

13.

Cyclic Ketoximes as Estrogen Receptor β Selective Agonists.

Granchi C, Lapillo M, Spena CR, Rizzolio F, Tuccinardi T, Martin TA, Carlson KE, Katzenellenbogen JA, Minutolo F.

ChemMedChem. 2016 Aug 19;11(16):1752-61. doi: 10.1002/cmdc.201600140. Epub 2016 May 2.

14.

Predictive features of ligand-specific signaling through the estrogen receptor.

Nwachukwu JC, Srinivasan S, Zheng Y, Wang S, Min J, Dong C, Liao Z, Nowak J, Wright NJ, Houtman R, Carlson KE, Josan JS, Elemento O, Katzenellenbogen JA, Zhou HB, Nettles KW.

Mol Syst Biol. 2016 Apr 22;12(4):864. doi: 10.15252/msb.20156701.

15.

Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation.

Fanning SW, Mayne CG, Dharmarajan V, Carlson KE, Martin TA, Novick SJ, Toy W, Green B, Panchamukhi S, Katzenellenbogen BS, Tajkhorshid E, Griffin PR, Shen Y, Chandarlapaty S, Katzenellenbogen JA, Greene GL.

Elife. 2016 Feb 2;5. pii: e12792. doi: 10.7554/eLife.12792.

16.

Licorice root components in dietary supplements are selective estrogen receptor modulators with a spectrum of estrogenic and anti-estrogenic activities.

Boonmuen N, Gong P, Ali Z, Chittiboyina AG, Khan I, Doerge DR, Helferich WG, Carlson KE, Martin T, Piyachaturawat P, Katzenellenbogen JA, Katzenellenbogen BS.

Steroids. 2016 Jan;105:42-9. doi: 10.1016/j.steroids.2015.11.006. Epub 2015 Nov 26.

17.

Discovery and Characterization of a Potent Interleukin-6 Binding Peptide with Neutralizing Activity In Vivo.

Ranganath S, Bhandari A, Avitahl-Curtis N, McMahon J, Wachtel D, Zhang J, Leitheiser C, Bernier SG, Liu G, Tran TT, Celino H, Tobin J, Jung J, Zhao H, Glen KE, Graul C, Griffin A, Schairer WC, Higgins C, Reza TL, Mowe E, Rivers S, Scott S, Monreal A, Shea C, Bourne G, Coons C, Smith A, Tang K, Mandyam RA, Masferrer J, Liu D, Patel DV, Fretzen A, Murphy CA, Milne GT, Smythe ML, Carlson KE.

PLoS One. 2015 Nov 10;10(11):e0141330. doi: 10.1371/journal.pone.0141330. eCollection 2015.

18.

Salicylketoximes That Target Glucose Transporter 1 Restrict Energy Supply to Lung Cancer Cells.

Granchi C, Qian Y, Lee HY, Paterni I, Pasero C, Iegre J, Carlson KE, Tuccinardi T, Chen X, Katzenellenbogen JA, Hergenrother PJ, Minutolo F.

ChemMedChem. 2015 Nov;10(11):1892-900. doi: 10.1002/cmdc.201500320. Epub 2015 Sep 1.

19.

Neural-Network Scoring Functions Identify Structurally Novel Estrogen-Receptor Ligands.

Durrant JD, Carlson KE, Martin TA, Offutt TL, Mayne CG, Katzenellenbogen JA, Amaro RE.

J Chem Inf Model. 2015 Sep 28;55(9):1953-61. doi: 10.1021/acs.jcim.5b00241. Epub 2015 Sep 4.

20.

Ligand Accessibility and Bioactivity of a Hormone-Dendrimer Conjugate Depend on pH and pH History.

Kim SH, Madak-Erdogan Z, Bae SC, Carlson KE, Mayne CG, Granick S, Katzenellenbogen BS, Katzenellenbogen JA.

J Am Chem Soc. 2015 Aug 19;137(32):10326-35. doi: 10.1021/jacs.5b05952. Epub 2015 Aug 10.

21.

Highly selective salicylketoxime-based estrogen receptor β agonists display antiproliferative activities in a glioma model.

Paterni I, Bertini S, Granchi C, Tuccinardi T, Macchia M, Martinelli A, Caligiuri I, Toffoli G, Rizzolio F, Carlson KE, Katzenellenbogen BS, Katzenellenbogen JA, Minutolo F.

J Med Chem. 2015 Feb 12;58(3):1184-94. doi: 10.1021/jm501829f. Epub 2015 Jan 14.

22.

The ecology of prescription opioid abuse in the USA: geographic variation in patients' use of multiple prescribers ("doctor shopping").

McDonald DC, Carlson KE.

Pharmacoepidemiol Drug Saf. 2014 Dec;23(12):1258-67. doi: 10.1002/pds.3690. Epub 2014 Aug 11.

23.

Synthesis and receptor binding in trans-CD ring-fused A-CD estrogens: comparison with the cis-fused isomers.

Dabrota C, Asim M, Choueiri C, Gargaun A, Korobkov I, Butt A, Carlson KE, Katzenellenbogen JA, Wright JS, Durst T.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3841-4. doi: 10.1016/j.bmcl.2014.06.066. Epub 2014 Jun 27.

24.

VAV3 mediates resistance to breast cancer endocrine therapy.

Aguilar H, Urruticoechea A, Halonen P, Kiyotani K, Mushiroda T, Barril X, Serra-Musach J, Islam A, Caizzi L, Di Croce L, Nevedomskaya E, Zwart W, Bostner J, Karlsson E, Pérez Tenorio G, Fornander T, Sgroi DC, Garcia-Mata R, Jansen MP, García N, Bonifaci N, Climent F, Soler MT, Rodríguez-Vida A, Gil M, Brunet J, Martrat G, Gómez-Baldó L, Extremera AI, Figueras A, Balart J, Clarke R, Burnstein KL, Carlson KE, Katzenellenbogen JA, Vizoso M, Esteller M, Villanueva A, Rodríguez-Peña AB, Bustelo XR, Nakamura Y, Zembutsu H, Stål O, Beijersbergen RL, Pujana MA.

Breast Cancer Res. 2014 May 28;16(3):R53. doi: 10.1186/bcr3664.

25.

Triaryl-substituted Schiff bases are high-affinity subtype-selective ligands for the estrogen receptor.

Liao ZQ, Dong C, Carlson KE, Srinivasan S, Nwachukwu JC, Chesnut RW, Sharma A, Nettles KW, Katzenellenbogen JA, Zhou HB.

J Med Chem. 2014 Apr 24;57(8):3532-45. doi: 10.1021/jm500268j. Epub 2014 Apr 7.

26.

Pepducin targeting the C-X-C chemokine receptor type 4 acts as a biased agonist favoring activation of the inhibitory G protein.

Quoyer J, Janz JM, Luo J, Ren Y, Armando S, Lukashova V, Benovic JL, Carlson KE, Hunt SW 3rd, Bouvier M.

Proc Natl Acad Sci U S A. 2013 Dec 24;110(52):E5088-97. doi: 10.1073/pnas.1312515110. Epub 2013 Dec 5.

27.

Reductions in log P improved protein binding and clearance predictions enabling the prospective design of cannabinoid receptor (CB1) antagonists with desired pharmacokinetic properties.

Ellsworth BA, Sher PM, Wu X, Wu G, Sulsky RB, Gu Z, Murugesan N, Zhu Y, Yu G, Sitkoff DF, Carlson KE, Kang L, Yang Y, Lee N, Baska RA, Keim WJ, Cullen MJ, Azzara AV, Zuvich E, Thomas MA, Rohrbach KW, Devenny JJ, Godonis HE, Harvey SJ, Murphy BJ, Everlof GG, Stetsko PI, Gudmundsson O, Johnghar S, Ranasinghe A, Behnia K, Pelleymounter MA, Ewing WR.

J Med Chem. 2013 Dec 12;56(23):9586-600. doi: 10.1021/jm4010835. Epub 2013 Nov 20.

PMID:
24182233
28.

Estimating the prevalence of opioid diversion by "doctor shoppers" in the United States.

McDonald DC, Carlson KE.

PLoS One. 2013 Jul 17;8(7):e69241. doi: 10.1371/journal.pone.0069241. Print 2013.

29.

Thiophene-core estrogen receptor ligands having superagonist activity.

Min J, Wang P, Srinivasan S, Nwachukwu JC, Guo P, Huang M, Carlson KE, Katzenellenbogen JA, Nettles KW, Zhou HB.

J Med Chem. 2013 Apr 25;56(8):3346-66. doi: 10.1021/jm400157e. Epub 2013 Apr 15.

30.

Nonsteroidal bivalent estrogen ligands: an application of the bivalent concept to the estrogen receptor.

Shan M, Carlson KE, Bujotzek A, Wellner A, Gust R, Weber M, Katzenellenbogen JA, Haag R.

ACS Chem Biol. 2013 Apr 19;8(4):707-15. doi: 10.1021/cb3006243. Epub 2013 Jan 30.

31.

Bicyclic core estrogens as full antagonists: synthesis, biological evaluation and structure-activity relationships of estrogen receptor ligands based on bridged oxabicyclic core arylsulfonamides.

Zhu M, Zhang C, Nwachukwu JC, Srinivasan S, Cavett V, Zheng Y, Carlson KE, Dong C, Katzenellenbogen JA, Nettles KW, Zhou HB.

Org Biomol Chem. 2012 Nov 21;10(43):8692-700. doi: 10.1039/c2ob26531a.

32.

Cannabinoid receptor antagonist-induced striated muscle toxicity and ethylmalonic-adipic aciduria in beagle dogs.

Tomlinson L, Tirmenstein MA, Janovitz EB, Aranibar N, Ott KH, Kozlosky JC, Patrone LM, Achanzar WE, Augustine KA, Brannen KC, Carlson KE, Charlap JH, Dubrow KM, Kang L, Rosini LT, Panzica-Kelly JM, Flint OP, Moulin FJ, Megill JR, Zhang H, Bennett MJ, Horvath JJ.

Toxicol Sci. 2012 Oct;129(2):268-79. doi: 10.1093/toxsci/kfs217. Epub 2012 Jul 21.

PMID:
22821849
33.

Synthesis and biological evaluation of two agents for imaging estrogen receptor β by positron emission tomography: challenges in PET imaging of a low abundance target.

Lee JH, Peters O, Lehmann L, Dence CS, Sharp TL, Carlson KE, Zhou D, Jeyakumar M, Welch MJ, Katzenellenbogen JA.

Nucl Med Biol. 2012 Nov;39(8):1105-16. doi: 10.1016/j.nucmedbio.2012.05.011. Epub 2012 Jun 30.

34.

Small-animal PET of steroid hormone receptors predicts tumor response to endocrine therapy using a preclinical model of breast cancer.

Fowler AM, Chan SR, Sharp TL, Fettig NM, Zhou D, Dence CS, Carlson KE, Jeyakumar M, Katzenellenbogen JA, Schreiber RD, Welch MJ.

J Nucl Med. 2012 Jul;53(7):1119-26. doi: 10.2967/jnumed.112.103465. Epub 2012 Jun 5.

35.

BC-spiro-estradiols. Synthesis and estrogen receptor binding affinity of four new estradiol isomers.

Asim M, Klonowska D, Choueiri C, Korobkov I, Carlson KE, Katzenellenbogen JA, Durst T.

Bioorg Med Chem Lett. 2012 Jun 1;22(11):3713-7. doi: 10.1016/j.bmcl.2012.04.022. Epub 2012 Apr 11.

PMID:
22546676
36.

Development of selective estrogen receptor modulator (SERM)-like activity through an indirect mechanism of estrogen receptor antagonism: defining the binding mode of 7-oxabicyclo[2.2.1]hept-5-ene scaffold core ligands.

Zheng Y, Zhu M, Srinivasan S, Nwachukwu JC, Cavett V, Min J, Carlson KE, Wang P, Dong C, Katzenellenbogen JA, Nettles KW, Zhou HB.

ChemMedChem. 2012 Jun;7(6):1094-100. doi: 10.1002/cmdc.201200048. Epub 2012 Apr 19.

37.

Solid phase synthesis of 1,5-diarylpyrazole-4-carboxamides: discovery of antagonists of the CB-1 receptor.

Pendri A, Dodd DS, Chen J, Cvijic ME, Kang L, Baska RA, Carlson KE, Burford NT, Sun C, Ewing WR, Gerritz SW.

ACS Comb Sci. 2012 Mar 12;14(3):197-204. doi: 10.1021/co200147y. Epub 2012 Feb 16.

PMID:
22340081
38.

Identification and structure-activity relationships of a novel series of estrogen receptor ligands based on 7-thiabicyclo[2.2.1]hept-2-ene-7-oxide.

Wang P, Min J, Nwachukwu JC, Cavett V, Carlson KE, Guo P, Zhu M, Zheng Y, Dong C, Katzenellenbogen JA, Nettles KW, Zhou HB.

J Med Chem. 2012 Mar 8;55(5):2324-41. doi: 10.1021/jm201556r. Epub 2012 Feb 21.

39.

Diarylpropionitrile (DPN) enantiomers: synthesis and evaluation of estrogen receptor β-selective ligands.

Carroll VM, Jeyakumar M, Carlson KE, Katzenellenbogen JA.

J Med Chem. 2012 Jan 12;55(1):528-37. doi: 10.1021/jm201436k. Epub 2011 Dec 14.

40.

Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studies.

Yang Y, Miller KJ, Zhu Y, Hong Y, Tian Y, Murugesan N, Gu Z, O'Tanyi E, Keim WJ, Rohrbach KW, Johnghar S, Behnia K, Pelleymounter MA, Carlson KE, Ewing WR.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6856-60. doi: 10.1016/j.bmcl.2011.09.016. Epub 2011 Sep 13.

PMID:
21962575
41.

Direct interaction between an allosteric agonist pepducin and the chemokine receptor CXCR4.

Janz JM, Ren Y, Looby R, Kazmi MA, Sachdev P, Grunbeck A, Haggis L, Chinnapen D, Lin AY, Seibert C, McMurry T, Carlson KE, Muir TW, Hunt S 3rd, Sakmar TP.

J Am Chem Soc. 2011 Oct 12;133(40):15878-81. doi: 10.1021/ja206661w. Epub 2011 Sep 21.

PMID:
21905700
42.

Selective and potent agonists for estrogen receptor beta derived from molecular refinements of salicylaldoximes.

Bertini S, De Cupertinis A, Granchi C, Bargagli B, Tuccinardi T, Martinelli A, Macchia M, Gunther JR, Carlson KE, Katzenellenbogen JA, Minutolo F.

Eur J Med Chem. 2011 Jun;46(6):2453-62. doi: 10.1016/j.ejmech.2011.03.030. Epub 2011 Mar 23.

43.

Exploration of dimensions of estrogen potency: parsing ligand binding and coactivator binding affinities.

Jeyakumar M, Carlson KE, Gunther JR, Katzenellenbogen JA.

J Biol Chem. 2011 Apr 15;286(15):12971-82. doi: 10.1074/jbc.M110.205112. Epub 2011 Feb 14.

44.

A-CD estrogens. I. Substituent effects, hormone potency, and receptor subtype selectivity in a new family of flexible estrogenic compounds.

Wright JS, Shadnia H, Anderson JM, Durst T, Asim M, El-Salfiti M, Choueiri C, Pratt MA, Ruddy SC, Lau R, Carlson KE, Katzenellenbogen JA, O'Brien PJ, Wan L.

J Med Chem. 2011 Jan 27;54(2):433-48. doi: 10.1021/jm100513m. Epub 2010 Dec 29.

PMID:
21190382
45.

Discovery of a CXCR4 agonist pepducin that mobilizes bone marrow hematopoietic cells.

Tchernychev B, Ren Y, Sachdev P, Janz JM, Haggis L, O'Shea A, McBride E, Looby R, Deng Q, McMurry T, Kazmi MA, Sakmar TP, Hunt S 3rd, Carlson KE.

Proc Natl Acad Sci U S A. 2010 Dec 21;107(51):22255-9. doi: 10.1073/pnas.1009633108. Epub 2010 Dec 7.

46.

Cannabinoid CB(1) receptor ligand binding and function examined through mutagenesis studies of F200 and S383.

Sitkoff DF, Lee N, Ellsworth BA, Huang Q, Kang L, Baska R, Huang Y, Sun C, Pendri A, Malley MF, Scaringe RP, Gougoutas JZ, Reggio PH, Ewing WR, Pelleymounter MA, Carlson KE.

Eur J Pharmacol. 2011 Jan 25;651(1-3):9-17. doi: 10.1016/j.ejphar.2010.10.056. Epub 2010 Oct 31.

PMID:
21044623
47.

Development of [F-18]fluorine-substituted Tanaproget as a progesterone receptor imaging agent for positron emission tomography.

Lee JH, Zhou HB, Dence CS, Carlson KE, Welch MJ, Katzenellenbogen JA.

Bioconjug Chem. 2010 Jun 16;21(6):1096-104. doi: 10.1021/bc1001054.

PMID:
20496889
48.

Imaging progesterone receptor in breast tumors: synthesis and receptor binding affinity of fluoroalkyl-substituted analogues of tanaproget.

Zhou HB, Lee JH, Mayne CG, Carlson KE, Katzenellenbogen JA.

J Med Chem. 2010 Apr 22;53(8):3349-60. doi: 10.1021/jm100052k.

49.

Characterization of the pharmacophore properties of novel selective estrogen receptor downregulators (SERDs).

Kieser KJ, Kim DW, Carlson KE, Katzenellenbogen BS, Katzenellenbogen JA.

J Med Chem. 2010 Apr 22;53(8):3320-9. doi: 10.1021/jm100047k.

50.

Steroidal bivalent ligands for the estrogen receptor: design, synthesis, characterization and binding affinities.

LaFrate AL, Carlson KE, Katzenellenbogen JA.

Bioorg Med Chem. 2009 May 15;17(10):3528-35. doi: 10.1016/j.bmc.2009.04.016. Epub 2009 Apr 12.

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