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• Article

  Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts

  Wold, E. A., Chen, J., Cunningham, K. A. & Zhou, J., Oct 1 2019, In: Journal of medicinal chemistry. 62, 1, p. 88-127 40 p.

  Research output: Contribution to journal › Article › peer-review

  • G-Protein-Coupled Receptors
  • Drug Discovery
  • Pharmaceutical Chemistry
  • Drug Delivery Systems
  • Clinical Trials
  28 Scopus citations

• An NPY Y1 receptor antagonist unmasks latent sensitization and reveals the contribution of protein kinase A and Epac to chronic inflammatory pain

  Fu, W., Nelson, T. S., Santos, D. F., Doolen, S., Gutierrez, J. J. P., Ye, N., Zhou, J. & Taylor, B. K., Aug 1 2019, In: Pain. 160, 8, p. 1754-1765 12 p.

  Research output: Contribution to journal › Article › peer-review

  • neuropeptide Y-Y1 receptor
  • Cyclic AMP-Dependent Protein Kinases
  • adenylyl cyclase 1
  • Chronic Pain
  • BIBO 3304
  9 Scopus citations

• Applications of bioorthogonal chemistry in tumor-targeted drug discovery

  Liu, G., Wold, E. A. & Zhou, J., Jan 1 2019, In: Current topics in medicinal chemistry. 19, 11, p. 892-897 6 p.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  • Cycloaddition Reaction
  • Drug Discovery
  • Alkynes
  • nitrones
  • Catalysis
  2 Scopus citations

• Design, Synthesis, and Biological Evaluation of Substituted 4,6-Dihydrospiro[[1,2,3]triazolo[4,5- b]pyridine-7,3′-indoline]-2′,5(3 H)-dione Analogues as Potent NS4B Inhibitors for the Treatment of Dengue Virus Infection

  Xu, J., Xie, X., Ye, N., Zou, J., Chen, H., White, M. A., Shi, P. Y. & Zhou, J., Sep 12 2019, In: Journal of medicinal chemistry. 62, 17, p. 7941-7960 20 p.

  Research output: Contribution to journal › Article › peer-review

  • indoline-2,3-dione
  • pyridine
  • Dengue Virus
  • indoline
  • Virus Diseases
  9 Scopus citations

• Design, Synthesis, and Characterization of 4-Undecylpiperidine-2-carboxamides as Positive Allosteric Modulators of the Serotonin (5-HT) 5-HT _2C Receptor

  Wild, C. T., Miszkiel, J. M., Wold, E. A., Soto, C. A., Ding, C., Hartley, R. M., White, M. A., Anastasio, N. C., Cunningham, K. A. & Zhou, J., Oct 1 2019, In: Journal of medicinal chemistry. 62, 1, p. 288-305 18 p.

  Research output: Contribution to journal › Article › peer-review

  • Receptor, Serotonin, 5-HT2C
  • Serotonin
  • 1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta(b)(1,4)diazepino(6,7,1hj)indole
  • Cocaine
  • Allosteric Site
  12 Scopus citations

• Discovery of niclosamide and its O-alkylamino-tethered derivatives as potent antibacterial agents against carbapenemase-producing and/or colistin resistant Enterobacteriaceae isolates

  Xu, J., Pachón-Ibáñez, M. E., Cebrero-Cangueiro, T., Chen, H., Sánchez-Céspedes, J. & Zhou, J., Jun 1 2019, In: Bioorganic and Medicinal Chemistry Letters. 29, 11, p. 1399-1402 4 p.

  Research output: Contribution to journal › Article › peer-review

  • Niclosamide
  • carbapenemase
  • Colistin
  • Enterobacteriaceae
  • Derivatives
  7 Scopus citations

• Dual activity of niclosamide to suppress replication of integrated HIV-1 and Mycobacterium tuberculosis (Beijing)

  Fan, X. Z., Xu, J., Files, M., Cirillo, J. D., Endsley, J. J., Zhou, J. & Endsley, M. A., May 2019, In: Tuberculosis. 116, p. S28-S33

  Research output: Contribution to journal › Article › peer-review

  • Niclosamide
  • Beijing
  • Mycobacterium tuberculosis
  • HIV-1
  • HIV
  7 Scopus citations

• Effect of N-(2-aminoethyl) ethanolamine on hypertrophic scarring changes in vitro: Finding novel anti-fibrotic therapies

  Chen, Z., Gu, J., El Ayadi, A., Oberhauser, A. F., Zhou, J., Sousse, L. E., Finnerty, C. C., Herndon, D. N. & Boor, P. J., Jan 1 2019, In: Toxicology and Applied Pharmacology. 362, p. 9-19 11 p.

  Research output: Contribution to journal › Article › peer-review

  • N-(2-hydroxyethyl)ethylenediamine
  • Ethanolamine
  • Hypertrophic Cicatrix
  • Cicatrix
  • Fibroblasts
  2 Scopus citations

• Efficacy of novel highly specific bromodomain-containing protein 4 inhibitors in innate inflammation–driven airway remodeling

  Tian, B., Liu, Z., Litvinov, J., Maroto, R., Jamaluddin, M., Rytting, E., Patrikeev, I., Ochoa, L., Vargas, G., Motamedi, M., Ameredes, B. T., Zhou, J. & Brasier, A. R., Jan 2019, In: American journal of respiratory cell and molecular biology. 60, 1, p. 68-83 16 p.

  Research output: Contribution to journal › Article › peer-review

  • Airway Remodeling
  • Toll-Like Receptor 3
  • Histone Acetyltransferases
  • Myofibroblasts
  • Proteins
  12 Scopus citations

• Exchange protein directly activated by cAMP plays a critical role in regulation of vascular fibrinolysis

  He, X., Drelich, A., Yu, S., Chang, Q., Gong, D., Zhou, Y., Qu, Y., Yuan, Y., Su, Z., Qiu, Y., Tang, S. J., Gaitas, A., Ksiazek, T., Xu, Z., Zhou, J., Feng, Z., Wakamiya, M., Lu, F. & Gong, B., Mar 15 2019, In: Life Sciences. 221, p. 1-12 12 p.

  Research output: Contribution to journal › Article › peer-review

  • Annexin A2
  • Endothelial cells
  • Fibrinolysis
  • Endothelial Cells
  • Blood Vessels
  2 Scopus citations

• Existing drugs as broad-spectrum and potent inhibitors for Zika virus by targeting NS2B-NS3 interaction

  Li, Z., Brecher, M., Deng, Y. Q., Zhang, J., Sakamuru, S., Liu, B., Huang, R., Koetzner, C. A., Allen, C. A., Jones, S. A., Chen, H., Zhang, N. N., Tian, M., Gao, F., Lin, Q., Banavali, N., Zhou, J., Boles, N., Xia, M., Kramer, L. D. & 2 others, Qin, C. F. & Li, H., Aug 1 2017, In: Cell Research. 27, 8, p. 1046-1064 19 p.

  Research output: Contribution to journal › Article › peer-review

  • temoporfin
  • Zika Virus
  • Flavivirus
  • Polyproteins
  • Niclosamide
  67 Scopus citations

• HFIP-promoted Michael reactions: direct para-selective C-H activation of anilines with maleimides

  Li, B., Mao, Q., Zhou, J., Liu, F. & Ye, N., Jan 1 2019, In: Organic and Biomolecular Chemistry. 17, 8, p. 2242-2246 5 p.

  Research output: Contribution to journal › Article › peer-review

  • Michael reaction
  • Maleimides
  • Aniline Compounds
  • aniline
  • Nucleophiles
  8 Scopus citations

• Identification of novel 2-(benzo[d]isoxazol-3-yl)-2-oxo-N-phenylacetohydrazonoyl cyanide analoguesas potent EPAC antagonists

  Ye, N., Zhu, Y., Liu, Z., Mei, F. C., Chen, H., Wang, P., Cheng, X. & Zhou, J., 2017, In: European journal of medicinal chemistry. 134, p. 62-71 10 p.

  Research output: Contribution to journal › Article › peer-review

  • erythromycin propionate-N-acetylcysteinate
  • azastene
  • Cyanides
  • 3-(5-tert-butylisoxazol-3-yl)-2-((3-chlorophenyl)hydrazono)-3-oxopropionitrile
  • Chemical modification
  3 Scopus citations

• Identification of peptidomimetics as novel chemical probes modulating fibroblast growth factor 14 (FGF14) and voltage-gated sodium channel 1.6 (Nav1.6) protein-protein interactions

  Liu, Z., Wadsworth, P., Singh, A. K., Chen, H., Wang, P., Folorunso, O., Scaduto, P., Ali, S. R., Laezza, F. & Zhou, J., Feb 1 2019, In: Bioorganic and Medicinal Chemistry Letters. 29, 3, p. 413-419 7 p.

  Research output: Contribution to journal › Article › peer-review

  • NAV1.6 Voltage-Gated Sodium Channel
  • fibroblast growth factor 14
  • Peptidomimetics
  • Voltage-Gated Sodium Channels
  • Proteins
  5 Scopus citations

• Methylglyoxal and a spinal TRPA1-AC1-Epac cascade facilitate pain in the db/db mouse model of type 2 diabetes

  Griggs, R. B., Santos, D. F., Laird, D. E., Doolen, S., Donahue, R. R., Wessel, C. R., Fu, W., Sinha, G. P., Wang, P., Zhou, J., Brings, S., Fleming, T., Nawroth, P. P., Susuki, K. & Taylor, B. K., Jul 2019, In: Neurobiology of Disease. 127, p. 76-86 11 p.

  Research output: Contribution to journal › Article › peer-review

  • adenylyl cyclase 1
  • Pyruvaldehyde
  • Ankyrins
  • Type 2 Diabetes Mellitus
  • Pain
  8 Scopus citations

• Modulation of Bax and mTOR for cancer therapeutics

  Li, R., Ding, C., Zhang, J., Xie, M., Park, D., Ding, Y., Chen, G., Zhang, G., Gilbert-Ross, M., Zhou, W., Marcus, A. I., Sun, S. Y., Chen, Z. G., Sica, G. L., Ramalingam, S. S., Magis, A. T., Fu, H., Khuri, F. R., Curran, W. J., Owonikoko, T. K. & 3 others, Shin, D. M., Zhou, J. & Deng, X., Jun 1 2017, In: Cancer Research. 77, 11, p. 3001-3012 12 p.

  Research output: Contribution to journal › Article › peer-review

  • Lung Neoplasms
  • Everolimus
  • Neoplasms
  • Phosphorylation
  • Mitochondrial Membranes
  11 Scopus citations

• Mucosal bromodomain-containing protein 4 mediates aeroallergen-induced inflammation and remodeling

  Tian, B., Hosoki, K., Liu, Z., Yang, J., Zhao, Y., Sun, H., Zhou, J., Rytting, E., Kaphalia, L., Calhoun, W. J., Sur, S. & Brasier, A. R., Apr 2019, In: Journal of Allergy and Clinical Immunology. 143, 4, p. 1380-1394.e9

  Research output: Contribution to journal › Article › peer-review

  • Dander
  • Cats
  • Myofibroblasts
  • Inflammation
  • Airway Remodeling
  13 Scopus citations

• Pharmacoproteomics reveal novel protective activity of bromodomain containing 4 inhibitors on vascular homeostasis in TLR3-mediated airway remodeling

  Zhao, Y., Tian, B., Sun, H., Zhang, J., Zhang, Y., Ivannikov, M., Motamedi, M., Liu, Z., Zhou, J., Kaphalia, L., Calhoun, W. J., Maroto, R. & Brasier, A. R., Aug 15 2019, In: Journal of Proteomics. 205, 103415.

  Research output: Contribution to journal › Article › peer-review

  • Airway Remodeling
  • Bronchoalveolar Lavage Fluid
  • Homeostasis
  • Pericytes
  • Blood Vessels
  9 Scopus citations

• Structure-activity relationships of 2-substituted phenyl-N-phenyl-2-oxoacetohydrazonoyl cyanides as novel antagonists of exchange proteins directly activated by cAMP (EPACs)

  Liu, Z., Zhu, Y., Chen, H., Wang, P., Mei, F. C., Ye, N., Cheng, X. & Zhou, J., Dec 1 2017, In: Bioorganic and Medicinal Chemistry Letters. 27, 23, p. 5163-5166 4 p.

  Research output: Contribution to journal › Article › peer-review

  • Cyanides
  • Structure-Activity Relationship
  • Proteins
  • 3-(5-tert-butylisoxazol-3-yl)-2-((3-chlorophenyl)hydrazono)-3-oxopropionitrile
  • erythromycin propionate-N-acetylcysteinate
  4 Scopus citations

• Structure-activity relationship studies on Bax activator SMBA1 for the treatment of ER-positive and triple-negative breast cancer

  Liu, G., Yin, T., Kim, H., Ding, C., Yu, Z., Wang, H., Chen, H., Yan, R., Wold, E. A., Zou, H., Liu, X., Ding, Y., Shen, Q. & Zhou, J., Sep 15 2019, In: European journal of medicinal chemistry. 178, p. 589-605 17 p.

  Research output: Contribution to journal › Article › peer-review

  • Triple Negative Breast Neoplasms
  • Structure-Activity Relationship
  • Tumors
  • Cells
  • fluorene
  1 Scopus citations

• Structure-guided drug design identifies a BRD4-selective small molecule that suppresses HIV

  Niu, Q., Liu, Z., Alamer, E., Fan, X., Chen, H., Endsley, J., Gelman, B. B., Tian, B., Kim, J. H., Michael, N. L., Robb, M. L., Ananworanich, J., Zhou, J. & Hu, H., Aug 1 2019, In: Journal of Clinical Investigation. 129, 8, p. 3361-3373 13 p.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  • Drug Design
  • HIV
  • Epigenomics
  • Proviruses
  • Therapeutics
  14 Scopus citations

• Suppression of the growth and invasion of human head and neck squamous cell carcinomas via regulating STAT3 signaling and the miR-21/β-catenin axis with HJC0152

  Wang, Y., Wang, S., Wu, Y., Ren, Y., Li, Z., Yao, X., Zhang, C., Ye, N., Jing, C., Dong, J., Zhang, K., Sun, S., Zhao, M., Guo, W., Qu, X., Qiao, Y., Chen, H., Kong, L., Jin, R., Wang, X. & 4 others, Zhang, L., Zhou, J., Shen, Q. & Zhou, X., Apr 2017, In: Molecular Cancer Therapeutics. 16, 4, p. 578-590 13 p.

  Research output: Contribution to journal › Article › peer-review

  • Catenins
  • STAT3 Transcription Factor
  • Squamous Cell Carcinoma of Head and Neck
  • Growth
  • Cell Cycle Resting Phase
  23 Scopus citations

• Synthesis and pharmacological evaluation of non-catechol G protein biased and unbiased dopamine D1 receptor agonists

  Wang, P., Felsing, D., Chen, H., Raval, S., Allen, J. & Zhou, J., May 9 2019, In: ACS Medicinal Chemistry Letters. 10.1021/acsmedchemlett.9b00050, p. 792-799 8 p., 10.1021/acsmedchemlett.9b00050.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  • Dopamine D1 Receptors
  • Dopamine Agonists
  • GTP-Binding Proteins
  • Arrestin
  • Dopamine
  3 Scopus citations

• Targeting 3-phosphoinositide-dependent protein kinase 1 associated with drug-resistant renal cell carcinoma using new oridonin analogs

  Zhou, J., Yun, E. J., Chen, W., Ding, Y., Wu, K., Wang, B., Ding, C., Hernandez, E., Santoyo, J., Pong, R. C., Chen, H., He, D., Zhou, J. & Hsieh, J. T., 2017, In: Cell Death and Disease. 8, 3, e2701.

  Research output: Contribution to journal › Article › peer-review

  • oridonin
  • 3-Phosphoinositide-Dependent Protein Kinases
  • Renal Cell Carcinoma
  • Diterpenes
  • Isodon
  14 Scopus citations

• YD277 suppresses triple-negative breast cancer partially through activating the endoplasmic reticulum stress pathway

  Chen, Z., Wu, Q., Ding, Y., Zhou, W., Liu, R., Chen, H., Zhou, J., Feng, J. & Chen, C., 2017, In: Theranostics. 7, 8, p. 2339-2349 11 p.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  • Triple Negative Breast Neoplasms
  • Endoplasmic Reticulum Stress
  • Factor V
  • G1 Phase Cell Cycle Checkpoints
  • Cyclin D1
  7 Scopus citations
• Chapter

  Chemistry and Bioactivity of ent-Kaurene Diterpenoids

  Ding, C., Ding, Y., Chen, H. & Zhou, J., 2017, Studies in Natural Products Chemistry. Elsevier B.V., Vol. 54. p. 141-197 57 p. (Studies in Natural Products Chemistry; vol. 54).

  Research output: Chapter in Book/Report/Conference proceeding › Chapter

  • Kaurane Diterpenes
  • Bioactivity
  • Diterpenes
  • geranylgeranyl pyrophosphate
  • Biosynthesis
  3 Scopus citations

• Fragment-based drug design: Strategic advances and lessons learned

  Chen, H., Zhou, X., Gao, Y., Chen, H. & Zhou, J., Jun 3 2017, Drug Discovery Technologies. Elsevier Inc., Vol. 2-8. p. 212-232 21 p.

  Research output: Chapter in Book/Report/Conference proceeding › Chapter

  • Screening
  • Drug Discovery
  • Pharmaceutical Preparations
  • Throughput
  • Assays
  3 Scopus citations

• Small-molecule inhibitors of protein-protein interactions

  Liu, Z., Chen, H., Wold, E. A. & Zhou, J., Jun 3 2017, Drug Discovery Technologies. Elsevier Inc., Vol. 2-8. p. 329-353 25 p.

  Research output: Chapter in Book/Report/Conference proceeding › Chapter

  • Molecules
  • Proteins
  • Modulators
  • Screening
  3 Scopus citations
• Comment/debate

  Positive-allosteric modulation of the 5-HT_2C receptor: implications for neuropsychopharmacology and neurotherapeutics

  Zhou, J. & Cunningham, K. A., Jan 1 2019, In: Neuropsychopharmacology. 44, 1, p. 230-231 2 p.

  Research output: Contribution to journal › Comment/debate › peer-review
  6 Scopus citations
• Editorial

  Gpcr drug discovery: Emerging targets, novel approaches and future trends

  Zhou, J. & Wild, C., 2019, In: Current topics in medicinal chemistry. 19, 16, p. 1363-1364 2 p.

  Research output: Contribution to journal › Editorial › peer-review

  Open Access
  2 Scopus citations
• Review article

  Drug Discovery Targeting Bromodomain-Containing Protein 4

  Liu, Z., Wang, P., Chen, H., Wold, E. A., Tian, B., Brasier, A. R. & Zhou, J., Jun 8 2017, In: Journal of medicinal chemistry. 60, 11, p. 4533-4558 26 p.

  Research output: Contribution to journal › Review article › peer-review

  • Drug Discovery
  • Drug Delivery Systems
  • Mediator Complex
  • Histone Acetyltransferases
  • RNA Polymerase II
  106 Scopus citations

• Exchange proteins directly activated by cAMP (EPACs): Emerging therapeutic targets

  Wang, P., Liu, Z., Chen, H., Ye, N., Cheng, X. & Zhou, J., 2017, In: Bioorganic and Medicinal Chemistry Letters. 27, 8, p. 1633-1639 7 p.

  Research output: Contribution to journal › Review article › peer-review

  • Proteins
  • Medical problems
  • Modulators
  • Molecules
  • Nervous System Diseases
  22 Scopus citations

• Orphan Receptor GPR88 as an Emerging Neurotherapeutic Target

  Ye, N., Li, B., Mao, Q., Wold, E. A., Tian, S., Allen, J. & Zhou, J., Jan 16 2019, In: ACS Chemical Neuroscience. 10, 1, p. 190-200 11 p., 10.1021/acschemneuro.8b00572.

  Research output: Contribution to journal › Review article › peer-review

  • G-Protein-Coupled Receptors
  • 2-(4-chlorophenyl)cyclopropylamine
  • N-phenylethanolamine
  • Ligands
  • Pharmaceutical Chemistry
  7 Scopus citations

• Recent advances in developing K-ras plasma membrane localization inhibitors

  Ye, N., Xu, Q., Li, W., Wang, P. & Zhou, J., Jan 1 2019, In: Current topics in medicinal chemistry. 19, 23, p. 2114-2127 14 p.

  Research output: Contribution to journal › Review article › peer-review

  • ras Proteins
  • Cell Membrane
  • Drug Repositioning
  • Drug Design
  • Biological Products
  2 Scopus citations

• Targeting the 5-ht_2c receptor in biological context and the current state of 5-ht_2c receptor ligand development

  Wold, E. A., Wild, C. T., Cunningham, K. A. & Zhou, J., 2019, In: Current topics in medicinal chemistry. 19, 16, p. 1381-1398 18 p.

  Research output: Contribution to journal › Review article › peer-review

  • lorcaserin
  • Serotonin
  • Artificial Receptors
  • Serotonin 5-HT2 Receptor Agonists
  • Receptor, Serotonin, 5-HT2C
  10 Scopus citations