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Publications

  • Structure-Guided Design and Synthesis of Pyridinone-Based Selective Bromodomain and Extra-Terminal Domain (BET)-First Bromodomain (BD1) Inhibitors.

    Authors:
    Yangfeng Li, Zhengnan Shen, Kiira Ratia, Jiong Zhao, Fei Huang, Oleksii Dubrovyskyii, Divakar Indukuri, Jiqiang Fu, Omar Lozano Ramos, Gregory R. J. Thatcher and Rui Xiong

    Journal:
    Journal of Medicinal Chemistry

    Citation/Links:
    J Med Chem. 2024 Feb 22;67(4):2712-2731.
    doi: 10.1021/acs.jmedchem.3c01837. Epub 2024 Jan 31.
    PMID: 38295759

  • Synthesis, Optimization, and Structure-Activity Relationships of Nicotinamide Phosphoribosyltransferase (NAMPT) Positive Allosteric Modulators (N-PAMs)

    Authors:
    Zhengnan Shen, Kiira Ratia, Isabella Krider, Martha Ackerman-Berrier, Christopher Penton, Soumya Reddy Musku, Jesse M. Gordon-Blake, Megan S. Laham, Nicholas Christie, Nina Ma, Jiqiang Fu, Rui Xiong, Jenna M. Courey, Ganga Reddy Velma and Gregory R. J. Thatcher

    Journal:
    Journal of Medicinal Chemistry

    Citation/Links:
    J Med Chem. 2023 Dec 28;66(24):16704-16727.
    doi: 10.1021/acs.jmedchem.3c01406. Epub 2023 Dec 14.
    PMID: 38096366    PMCID: PMC10758216 (available on 2024-12-14).

Publications List Heading link

ARTICLE CITATION (NLM)JOURNAL INFODATELINKS
Li Y, Shen Z, Ratia K, Zhao J, Huang F, Dubrovyskyii O, Indukuri D, Fu J, Lozano Ramos O, Thatcher GRJ, Xiong R. Structure-Guided Design and Synthesis of Pyridinone-Based Selective Bromodomain and Extra-Terminal Domain (BET)-First Bromodomain (BD1) Inhibitors. J Med Chem. 2024 Feb 22;67(4):2712-2731. doi: 10.1021/acs.jmedchem.3c01837. Epub 2024 Jan 31. PMID: 38295759.J Med Chem. 2024 Feb 22;67(4):2712-2731

2024-02-22

doi: 10.1021/acs.jmedchem.3c01837.

PMID: 38295759.
Shen Z, Ratia K, Krider I, Ackerman-Berrier M, Penton C, Musku SR, Gordon-Blake JM, Laham MS, Christie N, Ma N, Fu J, Xiong R, Courey JM, Velma GR, Thatcher GRJ. Synthesis, Optimization, and Structure-Activity Relationships of Nicotinamide Phosphoribosyltransferase (NAMPT) Positive Allosteric Modulators (N-PAMs). J Med Chem. 2023 Dec 28;66(24):16704-16727. doi: 10.1021/acs.jmedchem.3c01406. Epub 2023 Dec 14. PMID: 38096366; PMCID: PMC10758216  (available on 2024-12-14).J Med Chem. 2023 Dec 28;66(24):16704-167272023-12-28doi: 10.1021/acs.jmedchem.3c01406.

PMID: 38096366;

PMCID: PMC10758216  (available on 2024-12-14).
Petukhova VZ, Aboagye SY, Ardini M, Lullo RP, Fata F, Byrne ME, Gabriele F, Martin LM, Harding LNM, Gone V, Dangi B, Lantvit DD, Nikolic D, Ippoliti R, Effantin G, Ling WL, Johnson JJ, Thatcher GRJ, Angelucci F, Williams DL, Petukhov PA. Non-covalent inhibitors of thioredoxin glutathione reductase with schistosomicidal activity in vivo. Nat Commun. 2023 Jun 22;14(1):3737. doi: 10.1038/s41467-023-39444-y. PMID: 37349300; PMCID: PMC10287695.Nat Commun. 2023 Jun 22;14(1):37372023-06-22doi: 10.1038/s41467-023-39444-y.

PMID: 37349300;

PMCID: PMC10287695.
Nair RS, Kumar S, Das S, Singh SK, Srivastava P, Sondarva G, Rao A, Sinha SC, Xiong R, Bloem L, Hoskins K, Thatcher GRJ, Rana B, Rana A. TrkA expression directs the anti-neoplastic activity of MLK3 inhibitors in triple-negative breast cancer. Oncogene. 2023 Mar;42(14):1132-1143. doi: 10.1038/s41388-023-02633-6. Epub 2023 Feb 22. PMID: 36813855.Oncogene. 2023 Mar;42(14):1132-11432023-03doi: 10.1038/s41388-023-02633-6.

PMID: 36813855.
Ratia KM, Shen Z, Gordon-Blake J, Lee H, Laham MS, Krider IS, Christie N, Ackerman-Berrier M, Penton C, Knowles NG, Musku SR, Fu J, Velma GR, Xiong R, Thatcher GRJ. Mechanism of Allosteric Modulation of Nicotinamide Phosphoribosyltransferase to Elevate Cellular NAD. Biochemistry. 2023 Feb 21;62(4):923-933. doi: 10.1021/acs.biochem.2c00655. Epub 2023 Feb 6. PMID: 36746631; PMCID: PMC10935581.Biochemistry. 2023 Feb 21;62(4):923-9332023-02-21doi: 10.1021/acs.biochem.2c00655.

PMID: 36746631;

PMCID: PMC10935581.
Alqarni S, Cooper L, Galvan Achi J, Bott R, Sali VK, Brown A, Santarsiero BD, Krunic A, Manicassamy B, Peet NP, Zhang P, Thatcher GRJ, Gaisina IN, Rong L, Moore TW. Synthesis, Optimization, and Structure-Activity Relationships of Imidazo[1,2-a]pyrimidines as Inhibitors of Group 2 Influenza A Viruses. J Med Chem. 2022 Oct 27;65(20):14104-14120. doi: 10.1021/acs.jmedchem.2c01329. Epub 2022 Oct 19. PMID: 36260129.J Med Chem. 2022 Oct 27;65(20):14104-141202022-10-27doi: 10.1021/acs.jmedchem.2c01329.

PMID: 36260129.
Shen Z, Ratia K, Cooper L, Kong D, Lee H, Kwon Y, Li Y, Alqarni S, Huang F, Dubrovskyi O, Rong L, Thatcher GRJ, Xiong R. Design of SARS-CoV-2 PLpro Inhibitors for COVID-19 Antiviral Therapy Leveraging Binding Cooperativity. J Med Chem. 2022 Feb 24;65(4):2940-2955. doi: 10.1021/acs.jmedchem.1c01307. Epub 2021 Oct 19. PMID: 34665619; PMCID: PMC8547495.J Med Chem. 2022 Feb 24;65(4):2940-29552022-02-24doi: 10.1021/acs.jmedchem.1c01307.

PMID: 34665619;

PMCID: PMC8547495.
Principe DR, Xiong R, Li Y, Pham TND, Kamath SD, Dubrovskyi O, Ratia K, Huang F, Zhao J, Shen Z, Thummuri D, Daohong Z, Underwood PW, Trevino J, Munshi HG, Thatcher GRJ, 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 Jan 25;119(4):e2116764119. doi: 10.1073/pnas.2116764119. PMID: 35064087; PMCID: PMC8795568.Proc Natl Acad Sci U S A. 2022 Jan 25;119(4):e21167641192022-01-25doi: 10.1073/pnas.2116764119.

PMID: 35064087;

PMCID: PMC8795568.
Poloznikov AA, Nikulin SV, Hushpulian DM, Khristichenko AY, Osipyants AI, Asachenko AF, Shurupova OV, Savin SS, Lee SH, Gaisina IN, Thatcher GRJ, Narciso A, Chang EP, Kazakov SV, Krucher N, Tishkov VI, Thomas B, Gazaryan IG. Structure-Activity Relationships and Transcriptomic Analysis of Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors. Antioxidants (Basel). 2022 Jan 24;11(2):220. doi: 10.3390/antiox11020220. PMID: 35204103; PMCID: PMC8868400.Antioxidants (Basel). 2022 Jan 24;11(2):2202022-01-24doi: 10.3390/antiox11020220.

PMID: 35204103;

PMCID: PMC8868400.
Dubrovskyi O, Hasten E, Dudek SM, Flavin MT, Chan LL. Development of an Image-Based HCS-Compatible Method for Endothelial Barrier Function Assessment. SLAS Discov. 2021 Oct;26(9):1079-1090. doi: 10.1177/24725552211030900. Epub 2021 Jul 16. PMID: 34269109.SLAS Discov. 2021 Oct;26(9):1079-10902021-10doi: 10.1177/24725552211030900.

PMID: 34269109.
Amaya M, Cheng H, Borisevich V, Navaratnarajah CK, Cattaneo R, Cooper L, Moore TW, Gaisina IN, Geisbert TW, Rong L, Broder CC. A recombinant Cedar virus based high-throughput screening assay for henipavirus antiviral discovery. Antiviral Res. 2021 Sep;193:105084. doi: 10.1016/j.antiviral.2021.105084. Epub 2021 May 30. PMID: 34077807; PMCID: PMC8631057.Antiviral Res. 2021 Sep;193:1050842021-09doi: 10.1016/j.antiviral.2021.105084.

PMID: 34077807;

PMCID: PMC8631057.
Choi JV, Tchernookova BK, Kumar W, Kiedrowski L, Goeke C, Guizzetti M, Larson J, Kreitzer MA, Malchow RP. Extracellular ATP-Induced Alterations in Extracellular H+ Fluxes From Cultured Cortical and Hippocampal Astrocytes. Front Cell Neurosci. 2021 Apr 30;15:640217. doi: 10.3389/fncel.2021.640217. PMID: 33994945; PMCID: PMC8120152.Front Cell Neurosci. 2021 Apr 30;15:6402172021-04-30doi: 10.3389/fncel.2021.640217.

PMID: 33994945;

PMCID: PMC8120152.
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 Apr;66:103287. doi: 10.1016/j.ebiom.2021.103287. Epub 2021 Mar 19. PMID: 33752129; PMCID: PMC8010624.EBioMedicine. 2021 Apr;66:1032872021-04

doi: 10.1016/j.ebiom.2021.103287.

PMID: 33752129;

PMCID: PMC8010624.
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 [Preprint]. 2021 Feb 15:2021.02.13.431008. doi: 10.1101/2021.02.13.431008. Update in: J Med Chem. 2021 Oct 19;: PMID: 33594371; PMCID: PMC7885923.bioRxiv [Preprint]. 2021 Feb 15:2021.02.13.4310082021-02-15doi: 10.1101/2021.02.13.431008.

PMID: 33594371;

PMCID: PMC7885923.
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. Front Neurosci. 2021 Feb 10;15:628403. doi: 10.3389/fnins.2021.628403. PMID: 33642985; PMCID: PMC7902885.Front Neurosci. 2021 Feb 10;15:6284032021-02-10doi: 10.3389/fnins.2021.628403.

PMID: 33642985;

PMCID: PMC7902885.
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 Pathog. 2021 Feb 4;17(2):e1009312. doi: 10.1371/journal.ppat.1009312. PMID: 33539432; PMCID: PMC7888603.PLoS Pathog. 2021 Feb 4;17(2):e10093122021-02-04doi: 10.1371/journal.ppat.1009312.

PMID: 33539432;

PMCID: PMC7888603.
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 Feb 2;4(1):372-385. doi: 10.1021/acsptsci.0c00217. PMID: 33615187; PMCID: PMC7887848.ACS Pharmacol Transl Sci. 2021 Feb 2;4(1):372-3852021-02-02doi: 10.1021/acsptsci.0c00217.

PMID: 33615187;

PMCID: PMC7887848.
Du R, Cheng H, Cui Q, Peet NP, Gaisina IN, Rong L. Identification of a novel inhibitor targeting influenza A virus group 2 hemagglutinins. Antiviral Res. 2021 Feb;186:105013. doi: 10.1016/j.antiviral.2021.105013. Epub 2021 Jan 8. PMID: 33428962; PMCID: PMC8813174.Antiviral Res. 2021 Feb;186:1050132021-02doi: 10.1016/j.antiviral.2021.105013.

PMID: 33428962;

PMCID: PMC8813174.
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 Jan 5;4(1):143-154. doi: 10.1021/acsptsci.0c00149. PMID: 33615168; PMCID: PMC7887740.ACS Pharmacol Transl Sci. 2021 Jan 5;4(1):143-1542021-01-05doi: 10.1021/acsptsci.0c00149.

PMID: 33615168;

PMCID: PMC7887740.
Jastaniah A, Gaisina IN, Knopp RC, Thatcher GRJ. Synthesis of α-Ketoamide-Based Stereoselective Calpain-1 Inhibitors as Neuroprotective Agents. ChemMedChem. 2020 Dec 3;15(23):2280-2285. doi: 10.1002/cmdc.202000385. Epub 2020 Sep 18. PMID: 32840034; PMCID: PMC8583780.ChemMedChem. 2020 Dec 3;15(23):2280-22852020-12-03doi: 10.1002/cmdc.202000385.

PMID: 32840034;

PMCID: PMC8583780.
Cutler Lewandowski, Md. Wasim Khan, Manel Ben Aissa, Brian Layden and Gregory Thatcher. Discovery and Preclinical Optimization of Selective ABCA1 Inducers as Multifunctional Therapeutic Candidates. Circulation. 2020 Nov 12; doi: 10.1161/circ.142.suppl_3.15297. Circulation. 2020 Nov 122020-11-12doi: 10.1161/circ.142.suppl_3.15297.
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 Oct 8;63(19):11085-11099. doi: 10.1021/acs.jmedchem.0c01001. Epub 2020 Sep 22. PMID: 32886512; PMCID: PMC7904233.J Med Chem. 2020 Oct 8;63(19):11085-110992020-10-08doi: 10.1021/acs.jmedchem.0c01001.

PMID: 32886512;

PMCID: PMC7904233.
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 Oct;98(4):364-381. doi: 10.1124/molpharm.120.000054. Epub 2020 Aug 12. Erratum in: Mol Pharmacol. 2020 Oct;98(4):528. PMID: 32788222; PMCID: PMC7491312.Mol Pharmacol. 2020 Oct;98(4):364-381

Erratum in: Mol Pharmacol. 2020 Oct;98(4):528. 		2020-10doi: 10.1124/molpharm.120.000054.

PMID: 32788222;

PMCID: PMC7491312.
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 Jul 9;63(13):7211-7225. doi: 10.1021/acs.jmedchem.0c00463. Epub 2020 Jun 17. PMID: 32490678; PMCID: PMC7671190.J Med Chem. 2020 Jul 9;63(13):7211-72252020-07-09

doi: 10.1021/acs.jmedchem.0c00463.

PMID: 32490678;

PMCID: PMC7671190.
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 Jul 9;63(13):7186-7210. doi: 10.1021/acs.jmedchem.0c00456. Epub 2020 Jun 15. PMID: 32453591; PMCID: PMC8258866.J Med Chem. 2020 Jul 9;63(13):7186-72102020-07-09doi: 10.1021/acs.jmedchem.0c00456.

PMID: 32453591;

PMCID: PMC8258866.
Antanasijevic A, Durst MA, Cheng H, Gaisina IN, Perez JT, Manicassamy B, Rong L, Lavie A, Caffrey M. Structure of avian influenza hemagglutinin in complex with a small molecule entry inhibitor. Life Sci Alliance. 2020 Jul 1;3(8):e202000724. doi: 10.26508/lsa.202000724. PMID: 32611549; PMCID: PMC7335401.Life Sci Alliance. 2020 Jul 1;3(8):e2020007242020-07-01doi: 10.26508/lsa.202000724.

PMID: 32611549;

PMCID: PMC7335401.
Pavlinov I, Salkovski M, Aldrich LN. Beclin 1-ATG14L Protein-Protein Interaction Inhibitor Selectively Inhibits Autophagy through Disruption of VPS34 Complex I. J Am Chem Soc. 2020 May 6;142(18):8174-8182. doi: 10.1021/jacs.9b12705. Epub 2020 Apr 22. PMID: 32320221.J Am Chem Soc. 2020 May 6;142(18):8174-81822020-05-06doi: 10.1021/jacs.9b12705.

PMID: 32320221.
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 May;32:101486. doi: 10.1016/j.redox.2020.101486. Epub 2020 Mar 2. PMID: 32155582; PMCID: PMC7063127.Redox Biol. 2020 May;32:1014862020-05doi: 10.1016/j.redox.2020.101486.

PMID: 32155582;

PMCID: PMC7063127.
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 Mar 26;63(6):3120-3130. doi: 10.1021/acs.jmedchem.9b01900. Epub 2020 Mar 2. PMID: 32069052; PMCID: PMC8827112.J Med Chem. 2020 Mar 26;63(6):3120-31302020-03-26doi: 10.1021/acs.jmedchem.9b01900.

PMID: 32069052;

PMCID: PMC8827112.
Lyu H, Petukhov PA, Banta PR, Jadhav A, Lea WA, Cheng Q, Arnér 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 Mar 13;6(3):393-405. doi: 10.1021/acsinfecdis.9b00354. Epub 2020 Jan 24. PMID: 31939288; PMCID: PMC7072008.ACS Infect Dis. 2020 Mar 13;6(3):393-4052020-03-13doi: 10.1021/acsinfecdis.9b00354.

PMID: 31939288;

PMCID: PMC7072008.
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 Dec 26;62(24):11301-11323. doi: 10.1021/acs.jmedchem.9b01580. Epub 2019 Dec 10. PMID: 31746603; PMCID: PMC7261373.J Med Chem. 2019 Dec 26;62(24):11301-113232019-12-26doi: 10.1021/acs.jmedchem.9b01580.

PMID: 31746603;

PMCID: PMC7261373.
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 Jul;38(8):1471-1484. doi: 10.1177/0333102417737778. Epub 2017 Oct 12. PMID: 29022756; PMCID: PMC5916516.Cephalalgia. 2018 Jul;38(8):1471-14842018-07doi: 10.1177/0333102417737778.

PMID: 29022756;

PMCID: PMC5916516.
Pérez Morales TG, Ratia K, Wang DS, Gogos A, Bloem L, Driver TG, Federle MJ. A novel chemical inducer of Streptococcus quorum sensing acts by inhibiting the pheromone-degrading endopeptidase PepO. J Biol Chem. 2018 Jan 19;293(3):931-940. doi: 10.1074/jbc.M117.810994. Epub 2017 Dec 4. Erratum in: J Biol Chem. 2018 Mar 23;293(12 ):4580. Bloem, Laura [author added]; PMID: 29203527; PMCID: PMC5777264.J Biol Chem. 2018 Jan 19;293(3):931-940.

Erratum in: J Biol Chem. 2018 Mar 23;293(12 ):4580. Bloem, Laura [author added].		2018-01-19doi: 10.1074/jbc.M117.810994.

PMID: 29203527;

PMCID: PMC5777264.
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 γ-Lyase (CSE). ACS Med Chem Lett. 2017 Nov 21;8(12):1241-1245. doi: 10.1021/acsmedchemlett.7b00313. PMID: 29259741; PMCID: PMC5733271.ACS Med Chem Lett. 2017 Nov 21;8(12):1241-12452017-11-21doi: 10.1021/acsmedchemlett.7b00313.

PMID: 29259741;

PMCID: PMC5733271.
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 Feb 23;60(4):1325-1342. doi: 10.1021/acs.jmedchem.6b01355. Epub 2017 Feb 10. PMID: 28117994; PMCID: PMC5786431.J Med Chem. 2017 Feb 23;60(4):1325-13422017-02-23doi: 10.1021/acs.jmedchem.6b01355.

PMID: 28117994;

PMCID: PMC5786431.
Yao Y, Kong C, Yin L, Jain AD, Ratia K, Thatcher GR, Moore TW, Driver TG, Miller LW. Time-Gated Detection of Cystathionine γ-Lyase Activity and Inhibition with a Selective, Luminogenic Hydrogen Sulfide Sensor. Chemistry. 2017 Jan 18;23(4):752-756. doi: 10.1002/chem.201604786. Epub 2016 Nov 25. PMID: 27734530; PMCID: PMC5250566.Chemistry. 2017 Jan 18;23(4):752-7562017-01-18doi: 10.1002/chem.201604786.

PMID: 27734530;

PMCID: PMC5250566.
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 Apr 29;11:35. doi: 10.1186/s13024-016-0103-6. Erratum in: Mol Neurodegener. 2016;11(1):40. PMID: 27129593; PMCID: PMC4850651.Mol Neurodegener. 2016 Apr 29;11:35.

Erratum in: Mol Neurodegener. 2016;11(1):40		2016-04-29doi: 10.1186/s13024-016-0103-6.

PMID: 27129593;

PMCID: PMC4850651.
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 Jan 14;59(1):219-237. doi: 10.1021/acs.jmedchem.5b01276. Epub 2015 Dec 30. PMID: 26681208; PMCID: PMC4779956.J Med Chem. 2016 Jan 14;59(1):219-2372016-01-14doi: 10.1021/acs.jmedchem.5b01276.

PMID: 26681208;

PMCID: PMC4779956.