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1. Li, Y.; Shen, Z.; Ratia, K.; Zhao, J.; Huang, F.; Dubrovyskyii, O.; Indukuri, D.; Fu, J.; Lozano Ramos, O.; Thatcher G.*, Xiong R.* Structure-Guided Design and Synthesis of Pyridinone-Based Selective Bromodomain and Extra-Terminal Domain (BET)-First Bromodomain (BD1) Inhibitors. J Med Chem, Published online, DOI: 10.1021/acs.jmedchem.3c01837
2. Shen Z., Ratia K., Krider I., Ackerman-Berrier M., Penton C., Musku S. R., Gordon-Blake J. M., Laham M. S., Christie, N. Ma, N., Fu, J., Xiong, R., Courey, J. M., Velma, G. R.,.Thatcher, G. R. J. Synthesis, Optimization, and Structure-Activity Relationships of Nicotinamide Phosphoribosyltransferase (NAMPT) Positive Allosteric Modulators (N-PAMs), J Med Chem. 2023, 66, 16704-16727. DOI: 10.1021/acs.jmedchem.3c01406.
3. Ratia K., Shen Z., Gordon-Blake J., Lee H., Laham M., Krider I., Christie N., Ackerman-Berrier M., Penton C., Knowles N., Musku S., Fu J., Velma G., Xiong R., Thatcher G. Biochemistry, 2023, 62, 923-933. DOI: 10.1021/acs.biochem.2c00655
4. Nair R. S., Kumar S., Das S., Singh S. K., Srivastava P., Sondarva G., Rao A., Sinha S. C., Xiong R., Bloem L., Hoskins K., Thatcher G., Rana B., Rana A. TrkA expression directs the anti-neoplastic activity of MLK3 inhibitors in triple-negative breast cancer. Oncogene 2023, 42 (14), 1132-1143. DOI: 10.1038/s41388-023-02633-6.
Prior to Arizona
Prior to Arizona
1. Principe D. #, Xiong R. #, Li Y., Pharm T., Kamath S., Dubrovskyi O., Ratia K., Huang F., Zhao J., Thummuri D., Zhou D., Underwood P., Trevino J., Munshi H., Thatcher G.*, and Rana A*. XP-524 is a Dual BET/EP300 Inhibitor that Represses Oncogenic KRAS and Potentiates Immune Checkpoint Inhibition in Pancreatic Cancer. Proc Natl Acad Sci U S A. 2022, 119(4):e2116764119. DOI: 10.1073/pnas.2116764119
2. Shen Z. #, Ratia K. #, Cooper L. #, Kong D., Kong D., Lee H., Kwon Y., Alqarni S., Huang F., Dubrovskyi O. Rong L., Thatcher G.*, Xiong R.* Potent, Design of SARS-Cov-2 Plpro Inhibitors for COVID-19 Antiviral Therapy Leveraging Binding Cooperativity. J Med Chem,, DOI: 10.1021/acs.jmedchem.1c01307
3. Schafer A.#, Xiong R.#*, Cooper L.#, Nowar R., Li Y., Thatcher G., Saphire E.O., Chen H., Rong L*. Distinct Mechanisms of Inhibition by Diverse Small Molecules Targeting Filoviral Glycoproteins. Plos Pathogens, 2021, 17(2):e1009312. DOI: 10.1371/journal.ppat.1009312
Cooper L. #, Schafer A. #, Li Y. #, Cheng H., Medegan Fagla B., Shen Z., Nowar R., Dye K., Anantpadama M., Davey R., Thatcher G, Rong L.*, Xiong R.* Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. J Med Chem, 2020, 63, 11085-11099. DOI: 10.1021/acs.jmedchem.0c01001
Li Y., Zhao J., Gutgesell L., Shen Z., Ratia K., Dye K., Dubrovyskyii O., Zhao H., Huang F., Tonetti D., Thatcher G.*, Xiong R.* Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors for ER+ Breast Cancer Resistant to Fulvestrant. J Med Chem, 2020, 63, 7186–7210. DOI: 10.1021/acs.jmedchem.0c00456
6. Xiong R.#, Zhao J.#, Gutgesell L., Wang Y., Lee S., Karumudi B., Zhao H., Lu Y., Tonetti D., Thatcher G.* Novel Benzothiophene-Based Selective Estrogen Receptor Downregulators for Advanced Breast Cancer. J Med Chem, 2017, 60, 1325-1342. DOI: 10.1021/acs.jmedchem.6b01355
7. Xiong R.#, Patel H.#, Gutgesell L., Zhao J., Delgado-Rivera L., Pham T., Zhao H., Carlson K., Martin T., Katzenellenbogen J., Moore T., Tonetti D., Thatcher G.* Selective Human Estrogen Receptor Partial Agonists (ShERPAs) for Tamoxifen-Resistant Breast Cancer. J Med Chem, 2016, 59, 219-237. DOI: 10.1021/acs.jmedchem.5b01276
8. Xiong R., Cai X., Wei J.*, Ren P. Some Insights into the Binding Mechanism of Aurora B Kinase Gained by Molecular Dynamics simulation. J Mol Model, 2012, 18, 4591-4601. DOI: 10.1007/s00894-012-1453-9
9. Chen H., Lu Y., Xiong R., Rosales C., Coles C., Hamada K., Asad N., Thatcher G., Lasek A. Effect of a brain‐penetrant selective estrogen receptor degrader (SERD) on binge drinking in female mice. Alcohol Clin Exp Res, 2022 Jul;46(7):1313-1320. DOI: 10.1111/acer.14874
10. Abderrahman B., Maximov P., Curpan R., Fanning S., Hanspal J., Fan P., Foulds C., Chen Y., Malovannaya A., Jain A., Xiong R., Greene G., Tonetti D., Thatcher G., and Jordan V.C. 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, 11-25. DOI: 10.1158/1535-7163.MCT-20-0563
11. Abderrahman b., Maximov P., Curpan R., Hanspal J., Fan P., Xiong R., Tonetti D., Thatcher G., Jordan V.C. 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, 94(4): 364-381. DOI: 10.1124/molpharm.120.000054
12. Andreano K., Wardell S., Baker J., Desautels T., Baldi R., Chao C., Heetderks K., Bae Y., Xiong R., Tonetti D., Gutgesell L., Zhao J.; Sorrentino J.; Thompson D.; Bisi J.; Strum J., Thatcher G., Norris J. 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):635-646. DOI: 10.1007/s10549-020-05575-9
13. Lu Y., Gutgesell L., Xiong R., Zhao J.; Li Y., Rosales C., Hollas M., Shen Z., Gordon-Blake J., Dye K., Wang Y., Lee S., Chen H., He D., Dubrovyskyii O., Zhao H., Huang F., Lasek A., Tonetti D., Thatcher G. Design and Synthesis of Basic Selective Estrogen Receptor Degraders (B-SERDs) for Endocrine Therapy Resistant Breast Cancer. J Med Chem, 2019, 62, 11301-11323. DOI: 10.1021/acs.jmedchem.9b01580
14. Cui Q., Cheng H., Xiong R., Zhang G., Du R., Anantpadma M., Davey R., Rong L. Identification of Diaryl-Quinoline Compounds as Entry Inhibitors of Ebola. Viruses, 2018, 10(12): 678. DOI: 10.3390/v10120678
15. 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 Res, 2018, 157:47-56. DOI: 10.1016/j.antiviral.2018.07.003
16. Molloy M., Perez-White B., Gherezghiher T., Michalsen B., Xiong R., Patel H., Maximov P., Jordan V., Thatcher G., Tonetti D. Novel Selective Estrogen Mimics for the Treatment of Tamoxifen-Resistant Breast Cancer. Mol Cancer Ther, 2014, 13, 2515-26. DOI: 10.1158/1535-7163.MCT-14-0319
17. Hemachandra L., Patel H., Chandrasena R., Choi J., Piyankarage S., Wang S., Wang Y., Thayer E., Scism R., Michalsen B., Xiong R., Siklos M., Bolton J., Thatcher G. SERMs Attenuate Estrogen-Induced Malignant Transformation of Human Mammary Epithelial Cells by Upregulating Detoxification of Oxidative Metabolites. Cancer Prev Res, 2014, 7, 505-515. DOI: 10.1158/1940-6207.CAPR-13-0296
18. Wang J., Yuan Y., Xiong R., Zhang-Negrerie D., Du Y., Zhao K. Phenyliodinebis(trifluoro- acetate)-Mediated Oxidative C-C Bond Formation: Synthesis of 3-hydroxy-2-oxindoles and Spirooxindoles from Anilides. Org Lett, 2012, 14, 2210-2213. DOI: 10.1021/ol300418h
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