Our Publications

1. Dudek AZ, Liu LC, Fischer JH, Wiley EL, Sachdev JC, Bleeker J, Hurley RW, Tonetti DA, Thatcher GRJ, Venuti RP, O'Regan RM. Phase 1 study of TTC-352 in patients with metastatic breast cancer progressing on endocrine and CDK4/6 inhibitor therapy. Breast Cancer Res Treat. 2020;183(3):617-27. Epub 2020/07/23. doi: 10.1007/s10549-020-05787-z. PubMed PMID: 32696319.

2. Andreano KJ, Wardell SE, Baker JG, Desautels TK, Baldi R, Chao CA, Heetderks KA, Bae Y, Xiong R, Tonetti DA, Gutgesell LM, Zhao J, Sorrentino JA, Thompson DA, Bisi JE, Strum JC, Thatcher GRJ, Norris JD. G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer. Breast Cancer Res Treat. 2020;180(3):635-46. Epub 2020/03/05. doi: 10.1007/s10549-020-05575-9. PubMed PMID: 32130619; PMCID: PMC7103015.

3. Xiong R, Zhao J, Gutgesell LM, Wang Y, Lee S, Karumudi B, Zhao H, Lu Y, Tonetti DA, Thatcher GR. Novel Selective Estrogen Receptor Downregulators (SERDs) Developed against Treatment-Resistant Breast Cancer. J Med Chem. 2017;60(4):1325-42. Epub 2017/01/25. doi: 10.1021/acs.jmedchem.6b01355. PubMed PMID: 28117994; PMCID: PMC5786431.

4. 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. Selective Human Estrogen Receptor Partial Agonists (ShERPAs) for Tamoxifen-Resistant Breast Cancer. J Med Chem. 2016;59(1):219-37. Epub 2015/12/19. doi: 10.1021/acs.jmedchem.5b01276. PubMed PMID: 26681208; PMCID: PMC4779956.

5. Luo J, Lee SH, VandeVrede L, Qin Z, Piyankarage S, Tavassoli E, Asghodom RT, Ben Aissa M, Fa M, Arancio O, Yue L, Pepperberg DR, Thatcher GR. Re-engineering a neuroprotective, clinical drug as a procognitive agent with high in vivo potency and with GABAA potentiating activity for use in dementia. BMC Neurosci. 2015;16:67. doi: 10.1186/s12868-015-0208-9. PubMed PMID: 26480871; PMCID: 4612403.

6. Knopp RC, Jastaniah A, Dubrovskyi O, Gaisina I, Tai L, Thatcher GRJ. Extending the Calpain-Cathepsin Hypothesis to the Neurovasculature: Protection of Brain Endothelial Cells and Mice from Neurotrauma. ACS Pharmacol Transl Sci. 2021;4(1):372-85. Epub 2021/02/23. doi: 10.1021/acsptsci.0c00217. PubMed PMID: 33615187; PMCID: PMC7887848

7. Knopp RC, Lee SH, Hollas M, Nepomuceno E, Gonzalez D, Tam K, Aamir D, Wang Y, Pierce E, BenAissa M, Thatcher GRJ. Interaction of oxidative stress and neurotrauma in ALDH2(-/-) mice causes significant and persistent behavioral and pro-inflammatory effects in a tractable model of mild traumatic brain injury. Redox Biol. 2020;32:101486. Epub 2020/03/11. doi: 10.1016/j.redox.2020.101486. PubMed PMID: 32155582; PMCID: PMC7063127.

8. 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. A multifunctional therapeutic approach to disease modification in multiple familial mouse models and a novel sporadic model of Alzheimer's disease. Mol Neurodegener. 2016;11(1):35. doi: 10.1186/s13024-016-0103-6. PubMed PMID: 27129593; PMCID: PMC4850651.

9. Ben Aissa M, Lewandowski CT, Ratia KM, Lee SH, Layden BT, LaDu MJ, Thatcher GRJ. Discovery of Nonlipogenic ABCA1 Inducing Compounds with Potential in Alzheimer's Disease and Type 2 Diabetes. ACS Pharmacol Transl Sci. 2021;4(1):143-54. Epub 2021/02/23. doi: 10.1021/acsptsci.0c00149. PubMed PMID: 33615168; PMCID: PMC7887740.

10. Yu L, Tasaki S, Schneider JA, Arfanakis K, Duong DM, Wingo AP, Wingo TS, Kearns N, Thatcher GRJ, Seyfried NT, Levey AI, De Jager PL, Bennett DA. Cortical Proteins Associated With Cognitive Resilience in Community-Dwelling Older Persons. JAMA Psychiatry. 2020. Epub 2020/07/02. doi: 10.1001/jamapsychiatry.2020.1807. PubMed PMID: 32609320; PMCID: PMC7330835.

11. Jastaniah A, Gaisina IN, Knopp RC, Thatcher GRJ. Synthesis of alpha-Ketoamide-Based Stereoselective Calpain-1 Inhibitors as Neuroprotective Agents. ChemMedChem. 2020;15(23):2280-5. Epub 2020/08/26. doi: 10.1002/cmdc.202000385. PubMed PMID: 32840034.

12. Fa 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. Novel Selective Calpain 1 Inhibitors as Potential Therapeutics in Alzheimer's Disease. J Alzheimers Dis. 2016;49(3):707-21. Epub 2015/10/21. doi: 10.3233/JAD-150618. PubMed PMID: 26484927.

13. Siklos M, BenAissa M, Thatcher GR. Cysteine proteases as therapeutic targets: does selectivity matter? A systematic review of calpain and cathepsin inhibitors. Acta Pharm Sin B. 2015;5(6):506-19. doi: 10.1016/j.apsb.2015.08.001. PubMed PMID: 26713267; PMCID: 4675809.

14. 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. Design, synthesis, and optimization of novel epoxide incorporating peptidomimetics as selective calpain inhibitors. J Med Chem. 2013;56(15):6054-68. Epub 2013/07/10. doi: 10.1021/jm4006719. PubMed PMID: 23834438.

15. Scheinman SB, Zaldua S, Dada A, Krochmaliuk K, Dye K, Marottoli FM, Thatcher GRJ, Tai LM. Systemic Candesartan Treatment Modulates Behavior, Synaptic Protein Levels, and Neuroinflammation in Female Mice That Express Human APOE4. Frontiers in neuroscience. 2021;15:628403. Epub 2021/03/02. doi: 10.3389/fnins.2021.628403. PubMed PMID: 33642985; PMCID: PMC7902885.

16. Lewandowski CT, Khan MW, BenAissa M, Dubrovskyi O, Ackerman-Berrier M, LaDu MJ, Layden BT, Thatcher GRJ. Metabolomic analysis of a selective ABCA1 inducer in obesogenic challenge provides a rationale for therapeutic development. EBioMedicine. 2021;66:103287. Epub 2021/03/23. doi: 10.1016/j.ebiom.2021.103287. PubMed PMID: 33752129.

17. Tai LM, Koster KP, Luo J, Lee SH, Wang YT, Collins NC, Ben Aissa M, Thatcher GR, LaDu MJ. Amyloid-beta pathology and APOE genotype modulate retinoid X receptor agonist activity in vivo. J Biol Chem. 2014;289(44):30538-55. doi: 10.1074/jbc.M114.600833. PubMed PMID: 25217640; PMCID: 4215234.

18. Koster KP, Smith C, Valencia-Olvera AC, Thatcher GR, Tai LM, LaDu MJ. Rexinoids as Therapeutics for Alzheimer's Disease: Role of APOE. Curr Top Med Chem. 2017;17(6):708-20. PubMed PMID: 27320328. 19. Silvestri I, Lyu H, Fata F, Boumis G, Miele AE, Ardini M, Ippoliti R, Bellelli A, Jadhav A, Lea WA, Simeonov A, Cheng Q, Arner ESJ, Thatcher GRJ, Petukhov PA, Williams DL, Angelucci F. Fragment-Based Discovery of a Regulatory Site in Thioredoxin Glutathione Reductase Acting as "Doorstop" for NADPH Entry. ACS Chem Biol. 2018;13(8):2190-202. Epub 2018/05/26. doi: 10.1021/acschembio.8b00349. PubMed PMID: 29800515; PMCID: PMC6905387.

20. Silvestri I, Lyu H, Fata F, Banta PR, Mattei B, Ippoliti R, Bellelli A, Pitari G, Ardini M, Petukhova V, Thatcher GRJ, Petukhov PA, Williams DL, Angelucci F. Ectopic suicide inhibition of thioredoxin glutathione reductase. Free Radic Biol Med. 2020;147:200-11. Epub 2019/12/25. doi: 10.1016/j.freeradbiomed.2019.12.019. PubMed PMID: 31870799.

21. Lyu H, Petukhov PA, Banta PR, Jadhav A, Lea WA, Cheng Q, Arner ESJ, Simeonov A, Thatcher GRJ, Angelucci F, Williams DL. Characterization of Lead Compounds Targeting the Selenoprotein Thioredoxin Glutathione Reductase for Treatment of Schistosomiasis. ACS Infect Dis. 2020;6(3):393-405. Epub 2020/01/16. doi: 10.1021/acsinfecdis.9b00354. PubMed PMID: 31939288; PMCID: PMC7072008.

22. Ziniel PD, Karumudi B, Barnard AH, Fisher EM, Thatcher GR, Podust LM, Williams DL. The Schistosoma mansoni Cytochrome P450 (CYP3050A1) Is Essential for Worm Survival and Egg Development. PLoS Negl Trop Dis. 2015;9(12):e0004279. doi: 10.1371/journal.pntd.0004279. PubMed PMID: 26713732.

23. Wang YT, Piyankarage SC, Williams DL, Thatcher GR. Proteomic profiling of nitrosative stress: protein s-oxidation accompanies s-nitrosylation. ACS Chem Biol. 2014;9(3):821-30. Epub 2014/01/09. doi: 10.1021/cb400547u. PubMed PMID: 24397869.

24. Hollas MA, Ben Aissa M, Lee SH, Gordon-Blake JM, Thatcher GRJ. Pharmacological manipulation of cGMP and NO/cGMP in CNS drug discovery. Nitric Oxide. 2019;82:59-74. Epub 2018/11/06. doi: 10.1016/j.niox.2018.10.006. PubMed PMID: 30394348.

25. 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. Soluble guanylyl cyclase is a critical regulator of migraine-associated pain. Cephalalgia. 2018;38(8):1471-84. Epub 2017/10/13. doi: 10.1177/0333102417737778. PubMed PMID: 29022756; PMCID: PMC5916516.

26. Ben Aissa M, Lee SH, Bennett BM, Thatcher GR. Targeting NO/cGMP Signaling in the CNS for Neurodegeneration and Alzheimer's Disease. Curr Med Chem. 2016;23(24):2770-88. PubMed PMID: 27776476.

27. Hagos GK, Abdul-Hay SO, Sohn J, Edirisinghe PD, Chandrasena RE, Wang Z, Li Q, Thatcher GRJ. Anti-inflammatory, antiproliferative, and cytoprotective activity of NO chimera nitrates of use in cancer chemoprevention. Mol Pharmacol. 2008;74(5):1381-91. Epub 2008/08/05. doi: mol.108.046664 [pii] 10.1124/mol.108.046664. PubMed PMID: 18676677.

28. Dunlap T, Abdul-Hay SO, Chandrasena RE, Hagos GK, Sinha V, Wang Z, Wang H, Thatcher GRJ. Nitrates and NO-NSAIDs in cancer chemoprevention and therapy: in vitro evidence querying the NO donor functionality. Nitric Oxide. 2008;19(2):115-24. Epub 2008/05/20. doi: S1089-8603(08)00066-9 [pii] 10.1016/j.niox.2008.04.013. PubMed PMID: 18485921.

29. Thatcher GRJ. Organic nitrates and nitrites as stores of NO. In: van Fassen E, Vanin A, editors. Radicals for Life: the various forms of nitric oxide. Amsterdam: Elsevier Science; 2007.

30. Hagos GK, Carroll RE, Kouznetsova T, Li Q, Toader V, Fernandez PA, Swanson SM, Thatcher GRJ. Colon cancer chemoprevention by a novel NO chimera that shows anti-inflammatory and antiproliferative activity in vitro and in vivo. Mol Cancer Ther. 2007;6(8):2230-9. PubMed PMID: 17699720.

31. Thatcher GRJ, Bennett BM, Reynolds JN. NO chimeras as therapeutic agents in Alzheimer's disease. Curr Alzheimer Res. 2006;3(3):237-45. PubMed PMID: 16842101.

32. Nicolescu AC, Li Q, Brown L, Thatcher GRJ. Nitroxidation, nitration, and oxidation of a BODIPY fluorophore by RNOS and ROS. Nitric Oxide. 2006;15(2):163-76. PubMed PMID: 16549377.

33. Thatcher GRJ, Bennett BM, Reynolds JN. Nitric oxide mimetic molecules as therapeutic agents in Alzheimer's disease. Curr Alzheimer Res. 2005;2(2):171-82. PubMed PMID: 15974915.

34. Thatcher GR, Bennett BM, Reynolds JN. Nitric oxide mimetic molecules as therapeutic agents in Alzheimer's disease. Curr Alzheimer Res. 2005;2(2):171-82. Epub 2005/06/25. PubMed PMID: 15974915.

35. Thatcher G, Editor. Nitric Oxide. [In: Curr. Top. Med. Chemistry (Shar jah, United Arab Emirates)2005. 141 pp p.

36. Thatcher GRJ, Nicolescu AC, Bennett BM, Toader V. Nitrates and NO release: Contemporary aspects in biological and medicinal chemistry. Free Radic Biol Med. 2004;37(8):1122-43. PubMed PMID: AN 2004:792172.

37. Toader V, Xu X, Nicolescu A, Yu L, Bolton JL, Thatcher GRJ. Nitrosation, nitration, and autoxidation of the selective estrogen receptor modulator raloxifene by nitric oxide, peroxynitrite, and reactive nitrogen/oxygen species. Chem Res Toxicol. 2003;16(10):1264-76. PubMed PMID: 14565768.

38. Akhter S, Green JR, Root P, Thatcher GJ, Mutus B. Peroxynitrite and NO+ donors form colored nitrite adducts with sinapinic acid: potential applications. Nitric Oxide. 2003;8(4):214-21. PubMed PMID: 12895430.

39. Zavorin SI, Artz JD, Dumitrascu A, Nicolescu A, Scutaru D, Smith SV, Thatcher GR. Nitrate esters as nitric oxide donors: SS-nitrates. Org Lett. 2001;3(8):1113-6. Epub 2001/05/12. doi: 10.1021/ol007022a. PubMed PMID: 11348172.

40. Toong S, Xiong ZG, Zavorin SI, Bai D, Orser BA, Thatcher GR, Reynolds JN, MacDonald JF. Modulation of AMPA receptors by a novel organic nitrate. Can J Physiol Pharmacol. 2001;79(5):422-9. PubMed PMID: 11405246.

41. Murray J, Macartney D, Thatcher GR. Catalysis of NO production by a molybdoenzyme model. Org Lett. 2001;3(23):3635-8. PubMed PMID: 11700100.

42. Artz JD, Toader V, Zavorin SI, Bennett BM, Thatcher GR. In vitro activation of soluble guanylyl cyclase and nitric oxide release: a comparison of NO donors and NO mimetics. Biochemistry. 2001;40(31):9256-64. Epub 2001/08/02. doi: 10.1021/bi002885x. PubMed PMID: 11478893.

43. Thatcher GRJ, Weldon H. NO problem for nitroglycerin: organic nitrate chemistry and therapy. Chem Soc Rev. 1998;27(5):331-7. PubMed PMID: AN 1998:568552.

44. Artz JD, Thatcher GR. NO release from NO donors and nitrovasodilators: comparisons between oxyhemoglobin and potentiometric assays. Chem Res Toxicol. 1998;11(12):1393-7. Epub 1998/12/22. doi: 10.1021/tx980205+. PubMed PMID: 9860479.

45. Artz JD, Yang KX, Lock J, Sanchez C, Bennett BM, Thatcher GRJ. Reactivity of thionitrate esters: Putative intermediates in nitrovasodilator activity. Chem Commun. 1996(8):927-8. doi: DOI 10.1039/cc9960000927. PubMed PMID: WOS:A1996UJ31900018.

46. Artz JD, Yang K, Lock J, Sanchez C, Bennett BM, Thatcher GRJ. Reactivity of thionitrate esters: putative intermediates in nitrovasodilator activity. Chem Commun. 1996(8):927-8. PubMed PMID: AN 1996:281819.

47. Cameron DR, Borrajo AMP, Bennett BM, Thatcher GRJ. Organic nitrates, thionitrates, peroxynitrites, and nitric oxide: a molecular orbital study of the RXNO2 => RXONO (X=O,S) rearrangement, a reaction of potential bilogical significance. Canadian Journal of Chemistry. 1995;73:1627-38.

48. VandeVrede L, Abdelhamid R, Qin Z, Choi J, Piyankarage S, Luo J, Larson J, Bennett BM, Thatcher GR. An NO donor approach to neuroprotective and procognitive estrogen therapy overcomes loss of NO synthase function and potentially thrombotic risk. PLoS One. 2013;8(8):e70740. Epub 2013/08/27. doi: 10.1371/journal.pone.0070740 PONE-D-13-15498 [pii]. PubMed PMID: 23976955; PMCID: 3745399.

49. Hickok JR, Vasudevan D, Thatcher GR, Thomas DD. Is s-nitrosocysteine a true surrogate for nitric oxide? Antioxid Redox Signal. 2012;17(7):962-8. Epub 2012/02/07. doi: 10.1089/ars.2012.4543. PubMed PMID: 22304688; PMCID: 3411343.

50. Dunlap T, Piyankarage SC, Wijewickrama GT, Abdul-Hay S, Vanni M, Litosh V, Luo J, Thatcher GR. Quinone-induced activation of Keap1/Nrf2 signaling by aspirin prodrugs masquerading as nitric oxide. Chem Res Toxicol. 2012;25(12):2725-36. Epub 2012/10/06. doi: 10.1021/tx3003609. PubMed PMID: 23035985.

51. Pathi SS, Jutooru I, Chadalapaka G, Sreevalsan S, Anand S, Thatcher GR, Safe S. GT-094, a NO-NSAID, inhibits colon cancer cell growth by activation of a reactive oxygen species-microRNA-27a: ZBTB10-specificity protein pathway. Mol Cancer Res. 2011;9(2):195-202. Epub 2010/12/16. doi: 1541-7786.MCR-10-0363 [pii] 10.1158/1541-7786.MCR-10-0363. PubMed PMID: 21156786; PMCID: 3069691.

52. Abdul-Hay S, Schiefer IT, Chandrasena RE, Li M, Abdelhamid R, Wang YT, Tavassoli E, Michalsen B, Asghodom RT, Luo J, Thatcher GR. NO-SSRIs: Nitric Oxide Chimera Drugs Incorporating a Selective Serotonin Reuptake Inhibitor. ACS Med Chem Lett. 2011;2(9):656-61. Epub 2011/09/29. doi: 10.1021/ml2000033. PubMed PMID: 21927645; PMCID: 3171965.

53. Sinha V, Wijewickrama GT, Chandrasena RE, Xu H, Edirisinghe PD, Schiefer IT, Thatcher GR. Proteomic and mass spectroscopic quantitation of protein S-nitrosation differentiates NO-donors. ACS Chem Biol. 2010;5(7):667-80. Epub 2010/06/08. doi: 10.1021/cb100054m. PubMed PMID: 20524644; PMCID: PMC2941763.

54. Kastrati I, Edirisinghe PD, Wijewickrama GT, Thatcher GR. Estrogen-induced apoptosis of breast epithelial cells is blocked by NO/cGMP and mediated by extranuclear estrogen receptors. Endocrinology. 2010;151(12):5602-16. Epub 2010/10/15. doi: en.2010-0378 [pii] 10.1210/en.2010-0378. PubMed PMID: 20943808; PMCID: 2999489.

55. Anand S, Thatcher GRJ. Nitric oxide-releasing molecules for cancer therapy and chemoprevention. In: Bonavida B, editor. Nitric oxide (NO) and cancer : prognosis, prevention, and therapy. 1st ed. New York: Springer; 2010. p. 361-86.

56. Anand S, Schiefer IT, Thatcher GR. Nitric oxide donor and mimetic molecules in cancer chemotherapy and chemoprevention. Forum Immun Dis Ther. 2010;1(4):251-79.

57. Vandevrede L, Tavassoli E, Luo J, Qin Z, Yue L, Pepperberg DR, Thatcher GR. Novel analogues of chlormethiazole are neuroprotective in four cellular models of neurodegeneration by a mechanism with variable dependence on GABAA receptor potentiation. Br J Pharmacol. 2014;171(2):389-402. Epub 2013/10/15. doi: 10.1111/bph.12454. PubMed PMID: 24116891; PMCID: 3904259.

58. Nicolescu AC, Thatcher GRJ. Differential activation of soluble guanylate cyclase by a series of aryl disulfanyl dinitrate esters. Medchemcomm. 2014;5(1):51-6. doi: 10.1039/c3md00261f. PubMed PMID: WOS:000328886000007.

59. Schiefer IT, Vandevrede L, Fa M, Arancio O, Thatcher GR. Furoxans (1,2,5-Oxadiazole-N-Oxides) as Novel NO Mimetic Neuroprotective and Procognitive Agents. J Med Chem. 2012;55(7):3076-87. Epub 2012/03/21. doi: 10.1021/jm201504s. PubMed PMID: 22429006.

60. Qin Z, Luo J, VandeVrede L, Tavassoli E, Fa M, Teich AF, Arancio O, Thatcher GR. Design and synthesis of neuroprotective methylthiazoles and modification as NO-chimeras for neurodegenerative therapy. J Med Chem. 2012;55(15):6784-801. Epub 2012/07/12. doi: 10.1021/jm300353r. PubMed PMID: 22779770.

61. Abdul-Hay SO, Luo J, Ashghodom RT, Thatcher GR. NO-flurbiprofen reduces amyloid-beta, is neuroprotective in cell culture, and enhances cognition in response to cholinergic blockade. J Neurochem. 2009;111(3):766-76. Epub 2009/08/26. doi: JNC6353 [pii] 10.1111/j.1471-4159.2009.06353.x. PubMed PMID: 19702655; PMCID: 2792633.

62. Abdul-Hay SO, Edirisinghe P, Thatcher GR. Selective modulation of amyloid-beta peptide degradation by flurbiprofen, fenofibrate, and related compounds regulates Abeta levels. J Neurochem. 2009;111(3):683-95. Epub 2009/08/26. doi: JNC6355 [pii] 10.1111/j.1471-4159.2009.06355.x. PubMed PMID: 19702658.

63. 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. Activation of Nrf2 and Hypoxic Adaptive Response Contribute to Neuroprotection Elicited by Phenylhydroxamic Acid Selective HDAC6 Inhibitors. ACS Chem Neurosci. 2018;9(5):894-900. Epub 2018/01/18. doi: 10.1021/acschemneuro.7b00435. PubMed PMID: 29338172; PMCID: PMC5955769.

64. Pierce EN, Piyankarage SC, Dunlap T, Litosh V, Siklos MI, Wang YT, Thatcher GR. Prodrugs Bioactivated to Quinones Target NF-kappaB and Multiple Protein Networks: Identification of the Quinonome. Chem Res Toxicol. 2016;29(7):1151-9. doi: 10.1021/acs.chemrestox.6b00115. PubMed PMID: 27258437.

65. Abdelhamid R, Luo J, Vandevrede L, Kundu I, Michalsen B, Litosh VA, Schiefer IT, Gherezghiher T, Yao P, Qin Z, Thatcher GR. Benzothiophene Selective Estrogen Receptor Modulators Provide Neuroprotection by a novel GPR30-dependent Mechanism. ACS Chem Neurosci. 2011;2(5):256-68. Epub 2011/07/07. doi: 10.1021/cn100106a. PubMed PMID: 21731800; PMCID: 3124785.

66. Chirapu SR, Pachaiyappan B, Nural HF, Cheng X, Yuan H, Lankin DC, Abdul-Hay SO, Thatcher GRJ, Shen Y, Kozikowski AP, Petukhov PA. Molecular modeling, synthesis, and activity studies of novel biaryl and fused-ring BACE1 inhibitors. Bioorg Med Chem Lett. 2009;19(1):264-74. Epub 2008/11/18. doi: S0960-894X(08)01287-0 [pii] 10.1016/j.bmcl.2008.10.096. PubMed PMID: 19013792; PMCID: 2643073.

67. Taha TY, Aboukhatwa SM, Knopp RC, Ikegaki N, Abdelkarim H, Neerasa J, Lu Y, Neelarapu R, Hanigan TW, Thatcher GRJ, Petukhov PA. Design, Synthesis, and Biological Evaluation of Tetrahydroisoquinoline-Based Histone Deacetylase 8 Selective Inhibitors. ACS Med Chem Lett. 2017;8(8):824-9. Epub 2017/08/25. doi: 10.1021/acsmedchemlett.7b00126. PubMed PMID: 28835796; PMCID: PMC5554898.

68. Abdelkarim H, Neelarapu R, Madriaga A, Vaidya AS, Kastrati I, Karumudi B, Wang YT, Taha TY, Thatcher GRJ, Frasor J, Petukhov PA. Design, Synthesis, Molecular Modeling, and Biological Evaluation of Novel Amine-based Histone Deacetylase Inhibitors. ChemMedChem. 2017;12(24):2030-43. Epub 2017/10/29. doi: 10.1002/cmdc.201700449. PubMed PMID: 29080240; PMCID: PMC5881582.

69. Schiefer IT, Abdul-Hay S, Wang H, Vanni M, Qin Z, Thatcher GR. Inhibition of Amyloidogenesis by Nonsteroidal Anti-inflammatory Drugs and Their Hybrid Nitrates. J Med Chem. 2011;54(7):2293-306. Epub 2011/03/17. doi: 10.1021/jm101450p. PubMed PMID: 21405086; PMCID: 3072465.

70. Hemachandra LP, Madhubhani P, Chandrasena R, Esala P, Chen SN, Main M, Lankin DC, Scism RA, Dietz BM, Pauli GF, Thatcher GR, Bolton JL. Hops (Humulus lupulus) inhibits oxidative estrogen metabolism and estrogen-induced malignant transformation in human mammary epithelial cells (MCF-10A). Cancer Prev Res (Phila). 2012;5(1):73-81. Epub 2011/10/15. doi: 10.1158/1940-6207.CAPR-11-0348 1940-6207.CAPR-11-0348 [pii]. PubMed PMID: 21997247; PMCID: 3252489.

71. Overk CR, Lu PY, Wang YT, Choi J, Shaw JW, Thatcher GR, Mufson EJ. Effects of aromatase inhibition versus gonadectomy on hippocampal complex amyloid pathology in triple transgenic mice. Neurobiol Dis. 2012;45(1):479-87. Epub 2011/09/29. doi: S0969-9961(11)00305-6 [pii] 10.1016/j.nbd.2011.08.035. PubMed PMID: 21945538; PMCID: 3225601.

72. Lu Y, Gutgesell LM, Xiong R, Zhao J, Li Y, Rosales CI, Hollas M, Shen Z, Gordon-Blake J, Dye K, Wang Y, Lee S, Chen H, He D, Dubrovyskyii O, Zhao H, Huang F, Lasek AW, Tonetti DA, Thatcher GRJ. Design and Synthesis of Basic Selective Estrogen Receptor Degraders for Endocrine Therapy Resistant Breast Cancer. J Med Chem. 2019;62(24):11301-23. Epub 2019/11/21. doi: 10.1021/acs.jmedchem.9b01580. PubMed PMID: 31746603; PMCID: PMC7261373.

73. Liu H, Bolton JL, Thatcher GRJ. Chemical modification modulates estrogenic activity, oxidative reactivity, and metabolic stability in 4'F-DMA, a new benzothiophene selective estrogen receptor modulator. Chem Res Toxicol. 2006;19(6):779-87. PubMed PMID: 16780356; PMCID: 2570111.

74. Overk CR, Peng KW, Asghodom RT, Kastrati I, Lantvit DD, Qin Z, Frasor J, Bolton JL, Thatcher GRJ. Structure-activity relationships for a family of benzothiophene selective estrogen receptor modulators including raloxifene and arzoxifene. ChemMedChem. 2007;2(10):1520-6. PubMed PMID: 17654759.

75. Qin Z, Kastrati I, Chandrasena RE, Liu H, Yao P, Petukhov PA, Bolton JL, Thatcher GRJ. Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity. J Med Chem. 2007;50(11):2682-92. PubMed PMID: 17489582.

76. Yu B, Dietz BM, Dunlap T, Kastrati I, Lantvit DD, Overk CR, Yao P, Qin Z, Bolton JL, Thatcher GRJ. Structural modulation of reactivity/activity in design of improved benzothiophene selective estrogen receptor modulators: induction of chemopreventive mechanisms. Mol Cancer Ther. 2007;6(9):2418-28. PubMed PMID: 17876041.

77. Peng KW, Wang H, Qin Z, Wijewickrama GT, Lu M, Wang Z, Bolton JL, Thatcher GR. Selective estrogen receptor modulator delivery of quinone warheads to DNA triggering apoptosis in breast cancer cells. ACS Chem Biol. 2009;4(12):1039-49. Epub 2009/10/21. doi: 10.1021/cb9001848. PubMed PMID: 19839584; PMCID: 2814347.

78. Qin Z, Kastrati I, Ashgodom RT, Lantvit DD, Overk CR, Choi Y, van Breemen RB, Bolton JL, Thatcher GRJ. Structural modulation of oxidative metabolism in design of improved benzothiophene selective estrogen receptor modulators. Drug Metab Dispos. 2009;37(1):161-9. Epub 2008/10/22. doi: dmd.108.023408 [pii] 10.1124/dmd.108.023408. PubMed PMID: 18936111; PMCID: 2683656.

79. Kastrati I, Edirisinghe PD, Hemachandra LP, Chandrasena ER, Choi J, Wang YT, Bolton JL, Thatcher GR. Raloxifene and desmethylarzoxifene block estrogen-induced malignant transformation of human breast epithelial cells. PLoS One. 2011;6(11):e27876. Epub 2011/12/06. doi: 10.1371/journal.pone.0027876 PONE-D-11-13536 [pii]. PubMed PMID: 22140478; PMCID: 3226622.

80. 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. SERMs attenuate estrogen-induced malignant transformation of human mammary epithelial cells by upregulating detoxification of oxidative metabolites. Cancer Prev Res (Phila). 2014;7(5):505-15. Epub 2014/03/07. doi: 10.1158/1940-6207.CAPR-13-0296 1940-6207.CAPR-13-0296 [pii]. PubMed PMID: 24598415.

81. Patel HK, Siklos MI, Abdelkarim H, Mendonca EL, Vaidya A, Petukhov PA, Thatcher GR. A chimeric SERM-Histone deacetylase inhibitor approach to breast cancer therapy. ChemMedChem. 2014;9(3):602-13. Epub 2013/08/21. doi: 10.1002/cmdc.201300270. PubMed PMID: 23956109.

82. Kastrati I, Siklos MI, Brovkovych SD, Thatcher GRJ, Frasor J. A Novel Strategy to Co-target Estrogen Receptor and Nuclear Factor kappaB Pathways with Hybrid Drugs for Breast Cancer Therapy. Horm Cancer. 2017;8(3):135-42. Epub 2017/04/12. doi: 10.1007/s12672-017-0294-5. PubMed PMID: 28396978; PMCID: PMC5690576.

83. Abderrahman B, Maximov PY, Curpan RF, Hanspal JS, Fan P, Xiong R, Tonetti DA, Thatcher GRJ, Jordan VC. Pharmacology and Molecular Mechanisms of Clinically Relevant Estrogen Estetrol and Estrogen Mimic BMI-135 for the Treatment of Endocrine-Resistant Breast Cancer. Mol Pharmacol. 2020;98(4):364-81. Epub 2020/08/14. doi: 10.1124/molpharm.120.000054. PubMed PMID: 32788222.

84. Abderrahman B, Maximov PY, Curpan RF, Fanning SW, Hanspal JS, Fan P, Foulds CE, Chen Y, Malovannaya A, Jain A, Xiong R, Greene GL, Tonetti DA, Thatcher GRJ, Jordan VC. Rapid Induction of the Unfolded Protein Response and Apoptosis by Estrogen Mimic TTC-352 for the Treatment of Endocrine-Resistant Breast Cancer. Mol Cancer Ther. 2021;20(1):11-25. Epub 2020/11/13. doi: 10.1158/1535-7163.MCT-20-0563. PubMed PMID: 33177154; PMCID: PMC7790886.

85. Molloy ME, White BE, Gherezghiher T, Michalsen BT, Xiong R, Patel H, Zhao H, Maximov PY, Jordan VC, Thatcher GR, Tonetti DA. Novel selective estrogen mimics for the treatment of tamoxifen-resistant breast cancer. Mol Cancer Ther. 2014;13(11):2515-26. Epub 2014/09/11. doi: 10.1158/1535-7163.MCT-14-0319 1535-7163.MCT-14-0319 [pii]. PubMed PMID: 25205655; PMCID: 4221411.

86. Kim HY, Sohn J, Wijewickrama GT, Edirisinghe P, Gherezghiher T, Hemachandra M, Lu PY, Chandrasena RE, Molloy ME, Tonetti DA, Thatcher GR. Click synthesis of estradiol-cyclodextrin conjugates as cell compartment selective estrogens. Bioorg Med Chem. 2009;18(2):809-21. Epub 2009/12/25. doi: S0968-0896(09)01064-5 [pii] 10.1016/j.bmc.2009.11.046. PubMed PMID: 20031420; PMCID: 2906776.

87. Li Y, Zhao J, Gutgesell LM, Shen Z, Ratia K, Dye K, Dubrovskyi O, Zhao H, Huang F, Tonetti DA, Thatcher GRJ, Xiong R. Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib. J Med Chem. 2020;63(13):7186-210. Epub 2020/05/27. doi: 10.1021/acs.jmedchem.0c00456. PubMed PMID: 32453591.

88. Kumar S, Singh SK, Viswakarma N, Sondarva G, Nair RS, Sethupathi P, Sinha SC, Emmadi R, Hoskins K, Danciu O, Thatcher GRJ, Rana B, Rana A. Mixed lineage kinase 3 inhibition induces T cell activation and cytotoxicity. Proc Natl Acad Sci U S A. 2020;117(14):7961-70. Epub 2020/03/27. doi: 10.1073/pnas.1921325117. PubMed PMID: 32209667; PMCID: PMC7149389.

89. Kumar S, Singh SK, Viswakarma N, Sondarva G, Nair RS, Sethupathi P, Dorman M, Sinha SC, Hoskins K, Thatcher G, Rana B, Rana A. Rationalized inhibition of mixed lineage kinase 3 and CD70 enhances life span and antitumor efficacy of CD8(+) T cells. J Immunother Cancer. 2020;8(2). Epub 2020/08/08. doi: 10.1136/jitc-2019-000494. PubMed PMID: 32759234; PMCID: PMC7410077.

90. Schafer A, Cheng H, Xiong R, Soloveva V, Retterer C, Mo F, Bavari S, Thatcher G, Rong L. Repurposing potential of 1st generation H1-specific antihistamines as anti-filovirus therapeutics. Antiviral research. 2018;157:47-56. Epub 2018/07/08. doi: 10.1016/j.antiviral.2018.07.003. PubMed PMID: 29981374.

91. Cooper L, Schafer A, Li Y, Cheng H, Medegan Fagla B, Shen Z, Nowar R, Dye K, Anantpadma M, Davey RA, Thatcher GRJ, Rong L, Xiong R. Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. J Med Chem. 2020;63(19):11085-99. Epub 2020/09/05. doi: 10.1021/acs.jmedchem.0c01001. PubMed PMID: 32886512.

92. Gaisina IN, Peet NP, Cheng H, Li P, Du R, Cui Q, Furlong K, Manicassamy B, Caffrey M, Thatcher GRJ, Rong L. Optimization of 4-Aminopiperidines as Inhibitors of Influenza A Viral Entry That Are Synergistic with Oseltamivir. J Med Chem. 2020;63(6):3120-30. Epub 2020/02/19. doi: 10.1021/acs.jmedchem.9b01900. PubMed PMID: 32069052.

93. Gaisina IN, Peet NP, Wong L, Schafer AM, Cheng H, Anantpadma M, Davey RA, Thatcher GRJ, Rong L. Discovery and Structural Optimization of 4-(Aminomethyl)benzamides as Potent Entry Inhibitors of Ebola and Marburg Virus Infections. J Med Chem. 2020;63(13):7211-25. Epub 2020/06/04. doi: 10.1021/acs.jmedchem.0c00463. PubMed PMID: 32490678.

94. Schafer A, Xiong R, Cooper L, Nowar R, Lee H, Li Y, Ramirez BE, Peet NP, Caffrey M, Thatcher GRJ, Saphire EO, Cheng H, Rong L. Evidence for distinct mechanisms of small molecule inhibitors of filovirus entry. PLoS pathogens. 2021;17(2):e1009312. Epub 2021/02/05. doi: 10.1371/journal.ppat.1009312. PubMed PMID: 33539432.

95. Shen Z, Ratia K, Cooper L, Kong D, Lee H, Kwon Y, Li Y, Alqarni S, Huang F, Dubrovskyi O, Rong L, Thatcher GR, Xiong R. Potent, Novel SARS-CoV-2 PLpro Inhibitors Block Viral Replication in Monkey and Human Cell Cultures. bioRxiv. 2021. Epub 2021/02/18. doi: 10.1101/2021.02.13.431008. PubMed PMID: 33594371; PMCID: PMC7885923.

96. Bolton JL, Yu L, Thatcher GR. Quinoids formed from estrogens and antiestrogens. Methods Enzymol. 2004;378:110-23. Epub 2004/03/25. doi: 10.1016/S0076-6879(04)78006-4. PubMed PMID: 15038960.

97. Yu L, Liu H, Li W, Zhang F, Luckie C, van Breemen RB, Thatcher GR, Bolton JL. Oxidation of raloxifene to quinoids: potential toxic pathways via a diquinone methide and o-quinones. Chem Res Toxicol. 2004;17(7):879-88. PubMed PMID: 15257612.

98. Liu H, Liu J, van Breemen RB, Thatcher GRJ, Bolton JL. Bioactivation of the selective estrogen receptor modulator desmethylated arzoxifene to quinoids: 4'-fluoro substitution prevents quinoid formation. Chem Res Toxicol. 2005;18(2):162-73. PubMed PMID: 15720120.

99. Liu J, Liu H, van Breemen RB, Thatcher GRJ, Bolton JL. Bioactivation of the selective estrogen receptor modulator acolbifene to quinone methides. Chem Res Toxicol. 2005;18(2):174-82. PubMed PMID: 15720121.

100. Chang M, Peng KW, Kastrati I, Overk CR, Qin ZH, Yao P, Bolton JL, Thatcher GRJ. Activation of estrogen receptor-mediated gene transcription by the equine estrogen metabolite, 4-methoxyequilenin, in human breast cancer cells. Endocrinology. 2007;148(10):4793-802. PubMed PMID: 17584965.

101. Dunlap T, Chandrasena RE, Wang Z, Sinha V, Thatcher GRJ. Quinone formation as a chemoprevention strategy for hybrid drugs: balancing cytotoxicity and cytoprotection. Chem Res Toxicol. 2007;20(12):1903-12. Epub 2007/11/03. doi: 10.1021/tx7002257. PubMed PMID: 17975886.

102. Liu H, Qin Z, Thatcher GRJ, Bolton JL. Uterine peroxidase-catalyzed formation of diquinone methides from the selective estrogen receptor modulators raloxifene and desmethylated arzoxifene. Chem Res Toxicol. 2007;20(11):1676-84. Epub 2007/07/17. doi: 10.1021/tx7001367. PubMed PMID: 17630709; PMCID: 2507766.

103. Bolton JL, Thatcher GRJ. Potential mechanisms of estrogen quinone carcinogenesis. Chem Res Toxicol. 2008;21(1):93-101. Epub 2007/12/07. doi: 10.1021/tx700191p. PubMed PMID: 18052105; PMCID: 2556295.

104. Chandrasena RE, Edirisinghe PD, Bolton JL, Thatcher GR. Problematic detoxification of estrogen quinones by NAD(P)H-dependent quinone oxidoreductase and glutathione-S-transferase. Chem Res Toxicol. 2008;21(7):1324-9. Epub 2008/07/01. doi: 10.1021/tx8000797. PubMed PMID: 18588320.

105. Chang M, Overk CR, Kastrati I, Peng KW, Yao P, Qin ZH, Petukhov P, Bolton JL, Thatcher GRJ. Estrogenic activity of the equine estrogen metabolite, 4-methoxyequilenin. Adv Exp Med Biol. 2008;617:601-7. Epub 2008/05/24. PubMed PMID: 18497087.

106. Wang Z, Edirisinghe P, Sohn J, Qin Z, Geacintov NE, Thatcher GRJ, Bolton JL. Development of a liquid chromatography electrospray ionization tandem mass spectrometry method for analysis of stable 4-hydroxyequilenin-DNA adducts in human breast cancer cells. Chem Res Toxicol. 2009;22(6):1129-36. Epub 2009/04/17. doi: 10.1021/tx900063g. PubMed PMID: 19368368; PMCID: 2714912.

107. Wang Z, Wijewickrama GT, Peng KW, Dietz BM, Yuan L, van Breemen RB, Bolton JL, Thatcher GRJ. Estrogen Receptor {alpha} Enhances the Rate of Oxidative DNA Damage by Targeting an Equine Estrogen Catechol Metabolite to the Nucleus. J Biol Chem. 2009;284(13):8633-42. Epub 2009/01/23. doi: M807860200 [pii] 10.1074/jbc.M807860200. PubMed PMID: 19158089; PMCID: 2659222.

108. Peng KW, Chang M, Wang YT, Wang Z, Qin Z, Bolton JL, Thatcher GR. Unexpected hormonal activity of a catechol equine estrogen metabolite reveals reversible glutathione conjugation. Chem Res Toxicol. 2010;23(8):1374-83. Epub 2010/06/15. doi: 10.1021/tx100129h. PubMed PMID: 20540524; PMCID: 2941764.

109. Wang Z, Chandrasena ER, Yuan Y, Peng KW, van Breemen RB, Thatcher GR, Bolton JL. Redox cycling of catechol estrogens generating apurinic/apyrimidinic sites and 8-oxo-deoxyguanosine via reactive oxygen species differentiates equine and human estrogens. Chem Res Toxicol. 2010;23(8):1365-73. Epub 2010/06/01. doi: 10.1021/tx1001282. PubMed PMID: 20509668; PMCID: 2922465.

110. Gherezghiher TB, Michalsen B, Chandrasena RE, Qin Z, Sohn J, Thatcher GR, Bolton JL. The naphthol selective estrogen receptor modulator (SERM), LY2066948, is oxidized to an o-quinone analogous to the naphthol equine estrogen, equilenin. Chem Biol Interact. 2012;196(1-2):1-10. Epub 2012/02/01. doi: S0009-2797(12)00014-2 [pii] 10.1016/j.cbi.2012.01.004. PubMed PMID: 22290292; PMCID: 3319273.

111. Michalsen BT, Gherezghiher TB, Choi J, Chandrasena RE, Qin Z, Thatcher GR, Bolton JL. Selective estrogen receptor modulator (SERM) lasofoxifene forms reactive quinones similar to estradiol. Chem Res Toxicol. 2012;25(7):1472-83. Epub 2012/05/31. doi: 10.1021/tx300142h. PubMed PMID: 22642258; PMCID: 3398215.

112. Yao Y, Delgado-Rivera L, Samareh Afsari H, Yin L, Thatcher GRJ, Moore TW, Miller LW. Time-Gated Luminescence Detection of Enzymatically Produced Hydrogen Sulfide: Design, Synthesis, and Application of a Lanthanide-Based Probe. Inorg Chem. 2018;57(2):681-8. Epub 2017/12/28. doi: 10.1021/acs.inorgchem.7b02533. PubMed PMID: 29281273; PMCID: PMC5791759.

113. Yao Y, Kong C, Yin L, Jain AD, Ratia K, Thatcher GR, Moore TW, Driver TG, Miller LW. Time-Gated Detection of Cystathionine gamma-Lyase Activity and Inhibition with a Selective, Luminogenic Hydrogen Sulfide Sensor. Chemistry. 2017;23(4):752-6. doi: 10.1002/chem.201604786. PubMed PMID: 27734530; PMCID: PMC5250566.

114. Kastrati I, Delgado-Rivera L, Georgieva G, Thatcher GR, Frasor J. Synthesis and Characterization of an Aspirin-fumarate Prodrug that Inhibits NFkappaB Activity and Breast Cancer Stem Cells. Journal of visualized experiments : JoVE. 2017(119). Epub 2017/02/13. doi: 10.3791/54798. PubMed PMID: 28190074; PMCID: PMC5352264.

115. Bhattacharjee A, Sinha A, Ratia K, Yin L, Delgado-Rivera L, Petukhov PA, Thatcher GRJ, Wardrop DJ. 2-Arylidene Hydrazinecarbodithioates as Potent, Selective Inhibitors of Cystathionine gamma-Lyase (CSE). ACS Med Chem Lett. 2017;8(12):1241-5. Epub 2017/12/21. doi: 10.1021/acsmedchemlett.7b00313. PubMed PMID: 29259741; PMCID: PMC5733271.

116. Kastrati I, Siklos MI, Calderon-Gierszal EL, El-Shennawy L, Georgieva G, Thayer EN, Thatcher GR, Frasor J. Dimethyl Fumarate Inhibits the Nuclear Factor kappaB Pathway in Breast Cancer Cells by Covalent Modification of p65 Protein. J Biol Chem. 2016;291(7):3639-47. doi: 10.1074/jbc.M115.679704. PubMed PMID: 26683377; PMCID: 4751401.

117. Kastrati I, Litosh VA, Zhao S, Alvarez M, Thatcher GR, Frasor J. A novel aspirin prodrug inhibits NFkappaB activity and breast cancer stem cell properties. BMC Cancer. 2015;15:845. doi: 10.1186/s12885-015-1868-7. PubMed PMID: 26530254; PMCID: 4632459.