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  • Jia Zhou
2020

A Bromodomain-Containing Protein 4 (BRD4) Inhibitor Suppresses Angiogenesis by Regulating AP-1 Expression

Zhou, Z., Li, X., Liu, Z., Huang, L., Yao, Y., Li, L., Chen, J., Zhang, R., Zhou, J., Wang, L. & Zhang, Q. Q., Jul 10 2020, In : Frontiers in Pharmacology. 11, 1043.

Research output: Contribution to journalArticle

Open Access

Bidirectional modulation of the voltage-gated sodium (Nav1.6) channel by rationally designed peptidomimetics

Dvorak, N. M., Wadsworth, P. A., Wang, P., Chen, H., Zhou, J. & Laezza, F., Aug 2020, In : Molecules. 25, 15, 3365.

Research output: Contribution to journalArticle

Open Access

Discovery of 4-Phenylpiperidine-2-Carboxamide Analogues as Serotonin 5-HT2CReceptor-Positive Allosteric Modulators with Enhanced Drug-like Properties

Wold, E. A., Garcia, E. J., Wild, C. T., Miszkiel, J. M., Soto, C. A., Chen, J., Pazdrak, K., Fox, R. G., Anastasio, N. C., Cunningham, K. A. & Zhou, J., Jul 23 2020, In : Journal of medicinal chemistry. 63, 14, p. 7529-7544 16 p.

Research output: Contribution to journalArticle

Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation

Liu, Z., Chen, H., Wang, P., Li, Y., Wold, E. A., Leonard, P. G., Joseph, S., Brasier, A. R., Tian, B., Tian, B., Zhou, J., Zhou, J. & Zhou, J., May 28 2020, In : Journal of medicinal chemistry. 63, 10, p. 5242-5256 15 p.

Research output: Contribution to journalArticle

2 Scopus citations

Epigenetic suppression of HIV in myeloid cells by the BRD4-selective small molecule modulator ZL0580

Alamer, E., Zhong, C., Liu, Z., Niu, Q., Long, F., Guo, L., Gelman, B. B., Soong, L., Zhou, J. & Hu, H., Jun 1 2020, In : Journal of virology. 94, 11, e01880-19.

Research output: Contribution to journalArticle

2 Scopus citations

HJC0152 suppresses human non–small-cell lung cancer by inhibiting STAT3 and modulating metabolism

Lu, L., Li, H., Wu, X., Rao, J., Zhou, J., Fan, S. & Shen, Q., Mar 1 2020, In : Cell Proliferation. 53, 3, e12777.

Research output: Contribution to journalArticle

Open Access

Mechanism of Action of an EPAC1-Selective Competitive Partial Agonist

Shao, H., Mohamed, H., Boulton, S., Huang, J., Wang, P., Chen, H., Zhou, J., Luchowska-Stańska, U., Jentsch, N. G., Armstrong, A. L., Magolan, J., Yarwood, S. & Melacini, G., May 14 2020, In : Journal of medicinal chemistry. 63, 9, p. 4762-4775 14 p.

Research output: Contribution to journalArticle

2 Scopus citations

Oridonin and its derivatives for cancer treatment and overcoming therapeutic resistance

Liu, X., Xu, J., Zhou, J. & Shen, Q., 2020, (Accepted/In press) In : Genes and Diseases.

Research output: Contribution to journalReview article

Open Access

Structure-Activity Relationship Studies on Diversified Salicylamide Derivatives as Potent Inhibitors of Human Adenovirus Infection

Xu, J., Berastegui-Cabrera, J., Chen, H., Pachón, J., Zhou, J. & Sánchez-Céspedes, J., Mar 26 2020, In : Journal of medicinal chemistry. 63, 6, p. 3142-3160 19 p.

Research output: Contribution to journalArticle

1 Scopus citations

Synthesis and Biochemical Evaluation of Noncyclic Nucleotide Exchange Proteins Directly Activated by cAMP 1 (EPAC1) Regulators

Wang, P., Luchowska-Stańska, U., Van Basten, B., Chen, H., Liu, Z., Wiejak, J., Whelan, P., Morgan, D., Lochhead, E., Barker, G., Rehmann, H., Yarwood, S. J. & Zhou, J., May 28 2020, In : Journal of medicinal chemistry. 63, 10, p. 5159-5184 26 p.

Research output: Contribution to journalArticle

Validation of the epigenetic reader bromodomain-containing protein 4 (BRD4) as a therapeutic target for treatment of airway remodeling

Brasier, A. R. & Zhou, J., Jan 2020, In : Drug Discovery Today. 25, 1, p. 126-132 7 p.

Research output: Contribution to journalReview article

4 Scopus citations
2019

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 journalArticle

18 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 journalArticle

7 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 journalArticle

Open Access
2 Scopus citations
5 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 journalArticle

11 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 journalArticle

4 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 journalArticle

4 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 journalArticle

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 journalArticle

11 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 journalArticle

2 Scopus citations

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 journalEditorial

Open Access
1 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 journalArticle

8 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 journalArticle

4 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 journalArticle

5 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 journalArticle

13 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 journalReview article

3 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 journalArticle

8 Scopus citations
5 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 journalReview article

2 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 journalArticle

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 journalArticle

Open Access
13 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 journalArticle

Open Access
3 Scopus citations

Targeting the 5-ht2c receptor in biological context and the current state of 5-ht2c 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 journalReview article

8 Scopus citations
2018

AMPA receptor positive allosteric modulators attenuate morphine tolerance and dependence

Hu, X., Tian, X., Guo, X., He, Y., Chen, H., Zhou, J. & Wang, Z. J., Jul 15 2018, In : Neuropharmacology. 137, p. 50-58 9 p.

Research output: Contribution to journalArticle

4 Scopus citations

Antifibrosis effect of novel oridonin analog CYD0618 via suppression of the NF-κB pathway

Cummins, C. B., Wang, X., Xu, J., Hughes, B. D., Ding, Y., Chen, H., Zhou, J. & Radhakrishnan, R. S., Dec 2018, In : Journal of Surgical Research. 232, p. 283-292 10 p.

Research output: Contribution to journalArticle

7 Scopus citations

Discovery of novel mifepristone derivatives via suppressing KLF5 expression for the treatment of triple-negative breast cancer

Lin, Y., Liu, R., Zhao, P., Ye, J., Zheng, Z., Huang, J., Zhang, Y., Gao, Y., Chen, H., Liu, S., Zhou, J., Chen, C. & Chen, H., Feb 25 2018, In : European Journal of Medicinal Chemistry. 146, p. 354-367 14 p.

Research output: Contribution to journalArticle

7 Scopus citations

Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation

Liu, Z., Tian, B., Chen, H., Wang, P., Brasier, A. R. & Zhou, J., May 10 2018, In : European journal of medicinal chemistry. 151, p. 450-461 12 p.

Research output: Contribution to journalArticle

21 Scopus citations

Erythrosin B is a potent and broad-spectrum orthosteric inhibitor of the flavivirus NS2B-NS3 protease

Li, Z., Sakamuru, S., Huang, R., Brecher, M., Koetzner, C. A., Zhang, J., Chen, H., Qin, C. F., Zhang, Q. Y., Zhou, J., Kramer, L. D., Xia, M. & Li, H., Feb 1 2018, In : Antiviral Research. 150, p. 217-225 9 p.

Research output: Contribution to journalArticle

17 Scopus citations

Exchange protein directly activated by cAMP modulates ebola virus uptake into vascular endothelial cells

Drelich, A., Judy, B., He, X., Chang, Q., Yu, S., Li, X., Lu, F., Wakamiya, M., Popov, V., Zhou, J., Ksiazek, T. & Gong, B., Oct 16 2018, In : Viruses. 10, 10, 563.

Research output: Contribution to journalArticle

4 Scopus citations

Exchange proteins directly activated by cAMP and their roles in respiratory syncytial virus infection

Choi, E. J., Ren, Y., Chen, Y., Liu, S., Wu, W., Ren, J., Wang, P., Garofalo, R. P., Zhou, J. & Bao, X., Nov 1 2018, In : Journal of virology. 92, 22, e01200-18.

Research output: Contribution to journalArticle

2 Scopus citations

Functional Modulation of Voltage-Gated Sodium Channels by a FGF14-Based Peptidomimetic

Ali, S. R., Liu, Z., Nenov, M. N., Folorunso, O., Singh, A., Scala, F., Chen, H., James, T. F., Alshammari, M., Panova-Elektronova, N. I., White, M. A., Zhou, J. & Laezza, F., May 16 2018, In : ACS chemical neuroscience. 9, 5, p. 976-987 12 p.

Research output: Contribution to journalArticle

11 Scopus citations

GPCR allosteric modulators: Mechanistic advantages and therapeutic applications

Wold, E. A. & Zhou, J., 2018, In : Current topics in medicinal chemistry. 18, 23, p. 2002-2006 5 p.

Research output: Contribution to journalArticle

3 Scopus citations

Luteolin-mediated inhibition of hepatic stellate cell activation via suppression of the STAT3 pathway

Cummins, C. B., Wang, X., Nunez Lopez, O., Graham, G., Tie, H. Y., Zhou, J. & Radhakrishnan, R. S., Jun 2018, In : International journal of molecular sciences. 19, 6, 1567.

Research output: Contribution to journalArticle

9 Scopus citations

Natural Compound Oridonin Inhibits Endotoxin-Induced Inflammatory Response of Activated Hepatic Stellate Cells

Cummins, C. B., Wang, X., Sommerhalder, C., Bohanon, F. J., Nunez Lopez, O., Tie, H. Y., Rontoyanni, V. G., Zhou, J. & Radhakrishnan, R. S., 2018, In : BioMed Research International. 2018, 6137420.

Research output: Contribution to journalArticle

6 Scopus citations

Proteolysis Targeting Chimera (PROTAC): A Paradigm-Shifting Approach in Small Molecule Drug Discovery

Wang, P. & Zhou, J., Jan 1 2018, In : Current Topics in Medicinal Chemistry. 18, 16, p. 1354-1356 3 p.

Research output: Contribution to journalReview article

19 Scopus citations

Regio- and Stereospecific Synthesis of Oridonin D-Ring Aziridinated Analogues for the Treatment of Triple-Negative Breast Cancer via Mediated Irreversible Covalent Warheads

Ding, Y., Li, D., Ding, C., Wang, P., Liu, Z., Wold, E. A., Ye, N., Chen, H., White, M. A., Shen, Q. & Zhou, J., Apr 12 2018, In : Journal of medicinal chemistry. 61, 7, p. 2737-2752 16 p.

Research output: Contribution to journalArticle

15 Scopus citations

Selective Antagonists of the Bronchiolar Epithelial NF-κB-Bromodomain-Containing Protein 4 Pathway in Viral-Induced Airway Inflammation

Tian, B., Liu, Z., Yang, J., Sun, H., Zhao, Y., Wakamiya, M., Chen, H., Rytting, E., Zhou, J. & Brasier, A. R., Apr 24 2018, In : Cell Reports. 23, 4, p. 1138-1151 14 p.

Research output: Contribution to journalArticle

16 Scopus citations