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Activation of Nrf2 and Hypoxic Adaptive Response Contribute to Neuroprotection Elicited by Phenylhydroxamic Acid Selective HDAC6 Inhibitors.

Gaisina IN, Lee SH, Kaidery NA, Ben Aissa M, Ahuja M, Smirnova NN, Wakade S, Gaisin A, Bourassa MW, Ratan RR, Nikulin SV, Poloznikov AA, Thomas B, Thatcher GRJ, Gazaryan IG.

ACS Chem Neurosci. 2018 Jan 17. doi: 10.1021/acschemneuro.7b00435. [Epub ahead of print]


Time-Gated Luminescence Detection of Enzymatically Produced Hydrogen Sulfide: Design, Synthesis, and Application of a Lanthanide-Based Probe.

Yao Y, Delgado-Rivera L, Samareh Afsari H, Yin L, Thatcher GRJ, Moore TW, Miller LW.

Inorg Chem. 2018 Jan 16;57(2):681-688. doi: 10.1021/acs.inorgchem.7b02533. Epub 2017 Dec 27.


2-Arylidene Hydrazinecarbodithioates as Potent, Selective Inhibitors of Cystathionine γ-Lyase (CSE).

Bhattacharjee A, Sinha A, Ratia K, Yin L, Delgado-Rivera L, Petukhov PA, Thatcher GRJ, Wardrop DJ.

ACS Med Chem Lett. 2017 Nov 21;8(12):1241-1245. doi: 10.1021/acsmedchemlett.7b00313. eCollection 2017 Dec 14.


Design, Synthesis, Molecular Modeling, and Biological Evaluation of Novel Amine-based Histone Deacetylase Inhibitors.

Abdelkarim H, Neelarapu R, Madriaga A, Vaidya AS, Kastrati I, Karumudi B, Wang YT, Taha TY, Thatcher GRJ, Frasor J, Petukhov PA.

ChemMedChem. 2017 Dec 19;12(24):2030-2043. doi: 10.1002/cmdc.201700449. Epub 2017 Nov 30.


Soluble guanylyl cyclase is a critical regulator of migraine-associated pain.

Ben Aissa M, Tipton AF, Bertels Z, Gandhi R, Moye LS, Novack M, Bennett BM, Wang Y, Litosh V, Lee SH, Gaisina IN, Thatcher GR, Pradhan AA.

Cephalalgia. 2017 Jan 1:333102417737778. doi: 10.1177/0333102417737778. [Epub ahead of print]


Design, Synthesis, and Biological Evaluation of Tetrahydroisoquinoline-Based Histone Deacetylase 8 Selective Inhibitors.

Taha TY, Aboukhatwa SM, Knopp RC, Ikegaki N, Abdelkarim H, Neerasa J, Lu Y, Neelarapu R, Hanigan TW, Thatcher GRJ, Petukhov PA.

ACS Med Chem Lett. 2017 Aug 1;8(8):824-829. doi: 10.1021/acsmedchemlett.7b00126. eCollection 2017 Aug 10.


A Novel Strategy to Co-target Estrogen Receptor and Nuclear Factor κB Pathways with Hybrid Drugs for Breast Cancer Therapy.

Kastrati I, Siklos MI, Brovkovych SD, Thatcher GRJ, Frasor J.

Horm Cancer. 2017 Jun;8(3):135-142. doi: 10.1007/s12672-017-0294-5. Epub 2017 Apr 10.


Synthesis and Characterization of an Aspirin-fumarate Prodrug that Inhibits NFκB Activity and Breast Cancer Stem Cells.

Kastrati I, Delgado-Rivera L, Georgieva G, Thatcher GR, Frasor J.

J Vis Exp. 2017 Jan 18;(119). doi: 10.3791/54798.


Novel Selective Estrogen Receptor Downregulators (SERDs) Developed against Treatment-Resistant Breast Cancer.

Xiong R, Zhao J, Gutgesell LM, Wang Y, Lee S, Karumudi B, Zhao H, Lu Y, Tonetti DA, Thatcher GR.

J Med Chem. 2017 Feb 23;60(4):1325-1342. doi: 10.1021/acs.jmedchem.6b01355. Epub 2017 Feb 10.


Targeting NO/cGMP Signaling in the CNS for Neurodegeneration and Alzheimer's Disease.

Ben Aissa M, Lee SH, Bennett BM, Thatcher GR.

Curr Med Chem. 2016;23(24):2770-2788. Review.


Time-Gated Detection of Cystathionine γ-Lyase Activity and Inhibition with a Selective, Luminogenic Hydrogen Sulfide Sensor.

Yao Y, Kong C, Yin L, Jain AD, Ratia K, Thatcher GR, Moore TW, Driver TG, Miller LW.

Chemistry. 2017 Jan 18;23(4):752-756. doi: 10.1002/chem.201604786. Epub 2016 Nov 25.


Rexinoids as Therapeutics for Alzheimer's Disease: Role of APOE.

Koster KP, Smith C, Valencia-Olvera AC, Thatcher GR, Tai LM, LaDu MJ.

Curr Top Med Chem. 2017;17(6):708-720. Review.


Prodrugs Bioactivated to Quinones Target NF-κB and Multiple Protein Networks: Identification of the Quinonome.

Pierce EN, Piyankarage SC, Dunlap T, Litosh V, Siklos MI, Wang YT, Thatcher GR.

Chem Res Toxicol. 2016 Jul 18;29(7):1151-9. doi: 10.1021/acs.chemrestox.6b00115. Epub 2016 Jun 13.


Erratum to: A multifunctional therapeutic approach to disease modification in multiple familial mouse models and a novel sporadic model of Alzheimer's disease.

Luo J, Lee SH, VandeVrede L, Qin Z, Aissa MB, Larson J, Teich AF, Arancio O, D'Souza Y, Elharram A, Koster K, Tai LM, LaDu MJ, Bennett BM, Thatcher GR.

Mol Neurodegener. 2016 May 18;11(1):40. No abstract available.


A multifunctional therapeutic approach to disease modification in multiple familial mouse models and a novel sporadic model of Alzheimer's disease.

Luo J, Lee SH, VandeVrede L, Qin Z, Ben Aissa M, Larson J, Teich AF, Arancio O, D'Souza Y, Elharram A, Koster K, Tai LM, LaDu MJ, Bennett BM, Thatcher GR.

Mol Neurodegener. 2016 Apr 29;11:35. doi: 10.1186/s13024-016-0103-6. Erratum in: Mol Neurodegener. 2016;11(1):40.


Correction: The Schistosoma mansoni Cytochrome P450 (CYP3050A1) Is Essential for Worm Survival and Egg Development.

Ziniel PD, Karumudi B, Barnard AH, Fisher EM, Thatcher GR, Podust LM, Williams DL.

PLoS Negl Trop Dis. 2016 Feb 1;10(2):e0004439. doi: 10.1371/journal.pntd.0004439. eCollection 2016 Feb. No abstract available.


The Schistosoma mansoni Cytochrome P450 (CYP3050A1) Is Essential for Worm Survival and Egg Development.

Ziniel PD, Karumudi B, Barnard AH, Fisher EM, Thatcher GR, Podust LM, Williams DL.

PLoS Negl Trop Dis. 2015 Dec 29;9(12):e0004279. doi: 10.1371/journal.pntd.0004279. eCollection 2015 Dec. Erratum in: PLoS Negl Trop Dis. 2016 Feb;10(2):e0004439.


Cysteine proteases as therapeutic targets: does selectivity matter? A systematic review of calpain and cathepsin inhibitors.

Siklos M, BenAissa M, Thatcher GR.

Acta Pharm Sin B. 2015 Nov;5(6):506-19. doi: 10.1016/j.apsb.2015.08.001. Epub 2015 Sep 26. Review.


Dimethyl Fumarate Inhibits the Nuclear Factor κB Pathway in Breast Cancer Cells by Covalent Modification of p65 Protein.

Kastrati I, Siklos MI, Calderon-Gierszal EL, El-Shennawy L, Georgieva G, Thayer EN, Thatcher GR, Frasor J.

J Biol Chem. 2016 Feb 12;291(7):3639-47. doi: 10.1074/jbc.M115.679704. Epub 2015 Dec 18.


Selective Human Estrogen Receptor Partial Agonists (ShERPAs) for Tamoxifen-Resistant Breast Cancer.

Xiong R, Patel HK, Gutgesell LM, Zhao J, Delgado-Rivera L, Pham TND, Zhao H, Carlson K, Martin T, Katzenellenbogen JA, Moore TW, Tonetti DA, Thatcher GRJ.

J Med Chem. 2016 Jan 14;59(1):219-237. doi: 10.1021/acs.jmedchem.5b01276. Epub 2015 Dec 30.


A novel aspirin prodrug inhibits NFκB activity and breast cancer stem cell properties.

Kastrati I, Litosh VA, Zhao S, Alvarez M, Thatcher GR, Frasor J.

BMC Cancer. 2015 Nov 4;15:845. doi: 10.1186/s12885-015-1868-7.


Novel Selective Calpain 1 Inhibitors as Potential Therapeutics in Alzheimer's Disease.

Fà M, Zhang H, Staniszewski A, Saeed F, Shen LW, Schiefer IT, Siklos MI, Tapadar S, Litosh VA, Libien J, Petukhov PA, Teich AF, Thatcher GR, Arancio O.

J Alzheimers Dis. 2016;49(3):707-21. doi: 10.3233/JAD-150618.


Re-engineering a neuroprotective, clinical drug as a procognitive agent with high in vivo potency and with GABAA potentiating activity for use in dementia.

Luo J, Lee SH, VandeVrede L, Qin Z, Piyankarage S, Tavassoli E, Asghodom RT, Ben Aissa M, Fà M, Arancio O, Yue L, Pepperberg DR, Thatcher GR.

BMC Neurosci. 2015 Oct 19;16:67. doi: 10.1186/s12868-015-0208-9.


Amyloid-β pathology and APOE genotype modulate retinoid X receptor agonist activity in vivo.

Tai LM, Koster KP, Luo J, Lee SH, Wang YT, Collins NC, Ben Aissa M, Thatcher GR, LaDu MJ.

J Biol Chem. 2014 Oct 31;289(44):30538-55. doi: 10.1074/jbc.M114.600833. Epub 2014 Sep 12.


Novel selective estrogen mimics for the treatment of tamoxifen-resistant breast cancer.

Molloy ME, White BE, Gherezghiher T, Michalsen BT, Xiong R, Patel H, Zhao H, Maximov PY, Jordan VC, Thatcher GR, Tonetti DA.

Mol Cancer Ther. 2014 Nov;13(11):2515-26. doi: 10.1158/1535-7163.MCT-14-0319. Epub 2014 Sep 9.


SERMs attenuate estrogen-induced malignant transformation of human mammary epithelial cells by upregulating detoxification of oxidative metabolites.

Hemachandra LP, Patel H, Chandrasena RE, Choi J, Piyankarage SC, Wang S, Wang Y, Thayer EN, Scism RA, Michalsen BT, Xiong R, Siklos MI, Bolton JL, Thatcher GR.

Cancer Prev Res (Phila). 2014 May;7(5):505-15. doi: 10.1158/1940-6207.CAPR-13-0296. Epub 2014 Mar 5.


Proteomic profiling of nitrosative stress: protein S-oxidation accompanies S-nitrosylation.

Wang YT, Piyankarage SC, Williams DL, Thatcher GR.

ACS Chem Biol. 2014 Mar 21;9(3):821-30. doi: 10.1021/cb400547u. Epub 2014 Jan 21.


Novel analogues of chlormethiazole are neuroprotective in four cellular models of neurodegeneration by a mechanism with variable dependence on GABA(A) receptor potentiation.

Vandevrede L, Tavassoli E, Luo J, Qin Z, Yue L, Pepperberg DR, Thatcher GR.

Br J Pharmacol. 2014 Jan;171(2):389-402. doi: 10.1111/bph.12454.


An NO donor approach to neuroprotective and procognitive estrogen therapy overcomes loss of NO synthase function and potentially thrombotic risk.

VandeVrede L, Abdelhamid R, Qin Z, Choi J, Piyankarage S, Luo J, Larson J, Bennett BM, Thatcher GR.

PLoS One. 2013 Aug 16;8(8):e70740. doi: 10.1371/journal.pone.0070740. eCollection 2013.


A chimeric SERM-histone deacetylase inhibitor approach to breast cancer therapy.

Patel HK, Siklos MI, Abdelkarim H, Mendonca EL, Vaidya A, Petukhov PA, Thatcher GR.

ChemMedChem. 2014 Mar;9(3):602-13. doi: 10.1002/cmdc.201300270. Epub 2013 Aug 16.


Design, synthesis, and optimization of novel epoxide incorporating peptidomimetics as selective calpain inhibitors.

Schiefer IT, Tapadar S, Litosh V, Siklos M, Scism R, Wijewickrama GT, Chandrasena EP, Sinha V, Tavassoli E, Brunsteiner M, Fa' M, Arancio O, Petukhov P, Thatcher GR.

J Med Chem. 2013 Aug 8;56(15):6054-68. doi: 10.1021/jm4006719. Epub 2013 Jul 22.


Quinone-induced activation of Keap1/Nrf2 signaling by aspirin prodrugs masquerading as nitric oxide.

Dunlap T, Piyankarage SC, Wijewickrama GT, Abdul-Hay S, Vanni M, Litosh V, Luo J, Thatcher GR.

Chem Res Toxicol. 2012 Dec 17;25(12):2725-36. doi: 10.1021/tx3003609. Epub 2012 Oct 18.


Design and synthesis of neuroprotective methylthiazoles and modification as NO-chimeras for neurodegenerative therapy.

Qin Z, Luo J, VandeVrede L, Tavassoli E, Fa' M, Teich AF, Arancio O, Thatcher GR.

J Med Chem. 2012 Aug 9;55(15):6784-801. doi: 10.1021/jm300353r. Epub 2012 Jul 24.


Selective estrogen receptor modulator (SERM) lasofoxifene forms reactive quinones similar to estradiol.

Michalsen BT, Gherezghiher TB, Choi J, Chandrasena RE, Qin Z, Thatcher GR, Bolton JL.

Chem Res Toxicol. 2012 Jul 16;25(7):1472-83. doi: 10.1021/tx300142h. Epub 2012 Jun 14.


Furoxans (1,2,5-oxadiazole-N-oxides) as novel NO mimetic neuroprotective and procognitive agents.

Schiefer IT, VandeVrede L, Fa' M, Arancio O, Thatcher GR.

J Med Chem. 2012 Apr 12;55(7):3076-87. doi: 10.1021/jm201504s. Epub 2012 Mar 30.


Is S-nitrosocysteine a true surrogate for nitric oxide?

Hickok JR, Vasudevan D, Thatcher GR, Thomas DD.

Antioxid Redox Signal. 2012 Oct 1;17(7):962-8. doi: 10.1089/ars.2012.4543. Epub 2012 Mar 12.


The naphthol selective estrogen receptor modulator (SERM), LY2066948, is oxidized to an o-quinone analogous to the naphthol equine estrogen, equilenin.

Gherezghiher TB, Michalsen B, Chandrasena RE, Qin Z, Sohn J, Thatcher GR, Bolton JL.

Chem Biol Interact. 2012 Mar 5;196(1-2):1-10. doi: 10.1016/j.cbi.2012.01.004. Epub 2012 Jan 28.


Raloxifene and desmethylarzoxifene block estrogen-induced malignant transformation of human breast epithelial cells.

Kastrati I, Edirisinghe PD, Hemachandra LP, Chandrasena ER, Choi J, Wang YT, Bolton JL, Thatcher GR.

PLoS One. 2011;6(11):e27876. doi: 10.1371/journal.pone.0027876. Epub 2011 Nov 29.


Hops (Humulus lupulus) inhibits oxidative estrogen metabolism and estrogen-induced malignant transformation in human mammary epithelial cells (MCF-10A).

Hemachandra LP, Madhubhani P, Chandrasena R, Esala P, Chen SN, Main M, Lankin DC, Scism RA, Dietz BM, Pauli GF, Thatcher GR, Bolton JL.

Cancer Prev Res (Phila). 2012 Jan;5(1):73-81. doi: 10.1158/1940-6207.CAPR-11-0348. Epub 2011 Oct 13.


Effects of aromatase inhibition versus gonadectomy on hippocampal complex amyloid pathology in triple transgenic mice.

Overk CR, Lu PY, Wang YT, Choi J, Shaw JW, Thatcher GR, Mufson EJ.

Neurobiol Dis. 2012 Jan;45(1):479-87. doi: 10.1016/j.nbd.2011.08.035. Epub 2011 Sep 16.


NO-SSRIs: Nitric Oxide Chimera Drugs Incorporating a Selective Serotonin Reuptake Inhibitor.

Abdul-Hay S, Schiefer IT, Chandrasena RE, Li M, Abdelhamid R, Wang YT, Tavassoli E, Michalsen B, Asghodom RT, Luo J, Thatcher GR.

ACS Med Chem Lett. 2011 Sep 8;2(9):656-661.


Benzothiophene Selective Estrogen Receptor Modulators Provide Neuroprotection by a novel GPR30-dependent Mechanism.

Abdelhamid R, Luo J, Vandevrede L, Kundu I, Michalsen B, Litosh VA, Schiefer IT, Gherezghiher T, Yao P, Qin Z, Thatcher GR.

ACS Chem Neurosci. 2011 May 18;2(5):256-268.


Inhibition of amyloidogenesis by nonsteroidal anti-inflammatory drugs and their hybrid nitrates.

Schiefer IT, Abdul-Hay S, Wang H, Vanni M, Qin Z, Thatcher GR.

J Med Chem. 2011 Apr 14;54(7):2293-306. doi: 10.1021/jm101450p. Epub 2011 Mar 15.


GT-094, a NO-NSAID, inhibits colon cancer cell growth by activation of a reactive oxygen species-microRNA-27a: ZBTB10-specificity protein pathway.

Pathi SS, Jutooru I, Chadalapaka G, Sreevalsan S, Anand S, Thatcher GR, Safe S.

Mol Cancer Res. 2011 Feb;9(2):195-202. doi: 10.1158/1541-7786.MCR-10-0363. Epub 2010 Dec 14.


Estrogen-induced apoptosis of breast epithelial cells is blocked by NO/cGMP and mediated by extranuclear estrogen receptors.

Kastrati I, Edirisinghe PD, Wijewickrama GT, Thatcher GR.

Endocrinology. 2010 Dec;151(12):5602-16. doi: 10.1210/en.2010-0378. Epub 2010 Oct 13.


Unexpected hormonal activity of a catechol equine estrogen metabolite reveals reversible glutathione conjugation.

Peng KW, Chang M, Wang YT, Wang Z, Qin Z, Bolton JL, Thatcher GR.

Chem Res Toxicol. 2010 Aug 16;23(8):1374-83. doi: 10.1021/tx100129h.


Proteomic and mass spectroscopic quantitation of protein S-nitrosation differentiates NO-donors.

Sinha V, Wijewickrama GT, Chandrasena RE, Xu H, Edirisinghe PD, Schiefer IT, Thatcher GR.

ACS Chem Biol. 2010 Jul 16;5(7):667-80. doi: 10.1021/cb100054m.


Redox cycling of catechol estrogens generating apurinic/apyrimidinic sites and 8-oxo-deoxyguanosine via reactive oxygen species differentiates equine and human estrogens.

Wang Z, Chandrasena ER, Yuan Y, Peng KW, van Breemen RB, Thatcher GR, Bolton JL.

Chem Res Toxicol. 2010 Aug 16;23(8):1365-73. doi: 10.1021/tx1001282.


Click synthesis of estradiol-cyclodextrin conjugates as cell compartment selective estrogens.

Kim HY, Sohn J, Wijewickrama GT, Edirisinghe P, Gherezghiher T, Hemachandra M, Lu PY, Chandrasena RE, Molloy ME, Tonetti DA, Thatcher GR.

Bioorg Med Chem. 2010 Jan 15;18(2):809-21. doi: 10.1016/j.bmc.2009.11.046. Epub 2009 Nov 27.


Selective estrogen receptor modulator delivery of quinone warheads to DNA triggering apoptosis in breast cancer cells.

Peng KW, Wang H, Qin Z, Wijewickrama GT, Lu M, Wang Z, Bolton JL, Thatcher GR.

ACS Chem Biol. 2009 Dec 18;4(12):1039-49. doi: 10.1021/cb9001848.

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