Pharmacology and Toxicology - Research

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Research Interests

Selected Publications

Mei, F. Young, T. W., and Cheng, X. RAS-mediated epigenetic inactivation of OPCML in oncogenic transformation of human ovarian surface epithelial cells. FASEB J., 20:497-499, 2006.

Yu, S., Fan, F., Mei, F., and Cheng, X. Investigating the mechanism of exchange protein directly activated by cAMP activation by FT-IR and structural modeling. Biochemistry. 45:15318-15326, 2006.

Young, T. W., Mei, F. C., Rosen, D. G., Yang, G., Li, N., Liu, J., and Cheng, X. Up-regulation of Tumor Susceptibility Gene 101 Protein in Human Epithelial Ovarian Cancer Revealed by functional proteomics. Molecular and Cellular Proteomics. 6:294-304, 2007.

Ji, Z., Mei, F. C., Xie. J. and Cheng, X. Oncogenic KRAS supresses GLI1 degradation and activates hedgehog signaling pathway in pancreatic cancer cells. J. Biol. Chem. 282:14048-14055, 2007.

Cheng, X., Young, T. W., and Mei, F. C. Proteomics analyses of ovarian cancer using genetically defined human ovarian cencer models. Frontiers in Bioscience. 12:5166-5176, 2007.

Li, J., O'Conner, K. L., Cheng, X., Mei, F. C., Uchida, T., Townsend, C. M., and Evers, B. M. Cyclic AMP-stimulated neurotensin secretion is mediated through Rap1 downstream of both Epac and PKA signaling pathways. Molecular Endocrinology. 21:159-171, 2007.

Wayne, C. W., Fan, H. Y., Cheng, X., and Richards, J. S. FSH induces multiple signaling cascades: evidence that activation RAS, SRC and the EGF receptor are critical for granulosa cell differentiation. Molecular Endocrinology. 21:1940-1957, 2007.

Brock, M., Fan, F., Mei, F., Li, S., Gessner, C., Woods Jr., V. L., and, Cheng, X. Conformational analysis of Epac activation revealed using amide hydrogen/deuterium exchange mass spectrometry (DXMS). J. Biol. Chem. 282:32256-32263, 2007.

Ji, Z., Mei, F. C., Johnson, B. H., Thompson, E. B., and Cheng, X. PKA, not Epac, suppresses hedgehog activity and regulates glucocorticoid sensitivity in acute lymphoblastic leukemia cells. J. Biol. Chem.282:37370-37377, 2007.

Young, T. W., Rosen, D. G., Mei, F., Li, N., Liu, J., and Cheng, X. Up-regulation of Tumor Susceptibility Gene 101 Conveys poor Prognosis through Suppression of p21 Expression in Ovarian Cancer. Clinical Cancer Research. 13:3848-3854, 2007.

Brock, M., Fan, F., Mei, F., Li, S., Gessner, C., Woods Jr., V. L., and Cheng, X. Conformational analysis of Epac activation revealed using amide hydrogen/deuterium exchange mass spectrometry (DXMS). J. Biol. Chem. 282:32256-32263, 2007.

Cheng, X. Silent assassin: Oncogenic Ras directs epigenetic inactivation of target genes. Science Signaling. 1:pe14, 2008.

Ji, Z., Mei, F. C., Miller, A. L., Thompson, E. B., and Cheng, X. Protein kinase A (PKA) isoform RIIβ mediates the synergistic killing effect of cAMP and glucocorticoid in acute lymphoblastic leukemia cells. J. Biol. Chem. 283:21920-21925, 2008.

Tsalkova, T., Blumenthal D. R., Mei, F. C., and Cheng, X. Mechanism of Epac activation: Structural and functional analyses of Epac2 hinge mutants with Constitutive and reduced activities. J. Biol. Chem. 284:23644-23651, 2009.

Ji, Z., Mei, F. C., and Cheng, X. Epac, not PKA catalytic subunit, is required for 3T3-L1 preadipocyte differentiation. Frontiers in Bioscience (Elite Ed). 2:392-398, 2010.

Tsalkova, T., Gribengo, A. V., and Cheng, X. Exchange protein directly activated by cAMP isoform 2 (Epac2) is not a direct target of sulfonylureas. Assay and Drug Development Technologies. 9:88-91, 2011. [Faculty1000 selected paper]

Li, S., Tsalkova, T., White, M. A., Mei, F. C., Liu, T., Wang, D., Woods Jr., V. L., and Cheng, X. Mechanism of intracellular cAMP sensor Epac2 activation: cAMP-induced conformational changes identified by amide hydrogen/deuterium exchange mass spectrometry (DXMS). J. Biol. Chem. 286:17889-17897, 2011. [JBC Paper of the Week, Cover Figure article]

Tsalkova, T.,Mei F.C., and Cheng, X. A Fluorescence-based High-throughput Assay for the discovery of Exchange Protein directly Activated by Cyclic AMP (EPAC) Antagonists. PLOS ONE> 7(1):e30441, 2012.

Chen, H., Tsalkova, T., Mei, F.C., Hu, Y., Cheng, X., and Zhou J. 5-Cyano-6-oxo-1, 6-dihydropyrimidines as Potent Antagonists Targeting Exchange Proteins Directly Activated by cAMP. Bioorganic & Medicinal Chemistry Letters. 22:4038-4043, 2012.

Lu, M., Huang, Y., White, M. A., Wu, X., Liu, N. Cheng, X.*, and Chen, Y.* Dual catalysis mode for the dicarbonyl reduction catalyzed by diketoreductase. Chemical Communication. 48:11352-11354, 2012.

Tsalkova, T., Mei, F. C., Li, Sheng, Chepurny, O. G., Liu, T., Woods, Jr., V. L., Holz, G.G., and Cheng, X. Isoform-specific antagonists of exchange protein directly activated by cAMP. Proc. Acad. Natl. Sci. USA. 109:18613-18618, 2012.

White, M. A., Li, S., Tsalkova, T., Mei, F. C., Liu, T., Woods Jr., V. L., and Cheng, X. Structural analyses of a constitutively active mutant of exchange protein directly activated by cAMP. PLOS ONE. 7(11):e49932, 2012.

Almahariq, M., Tsalkova, T., Mei, F. C., Chen, H., Zhou, J., Sastry, S. K., Schwede, F., and Cheng, X. A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion. Molecular Pharmacology. 83:122-128, 2013.

Yan, J., Mei, F. C., Cheng, H. Q., Lao, D. H., Hu, Y., Wei, J., Patrikeev, I., Hao, D., Stutz, S. J., Dineley, K. T., Motamedi, M., Hommel, J. D., Cunningham, K. A., Chen, J.*, and Cheng, X*. Enhanced leptin sensitivity, reduced adiposity and improved glucose homeostasis in mice lacking of exchange protein directly activated by cAMP isoform 1. Molecular Cellular Biology. In press.

Chen, H, Tsalkova, T., Mei, F. C., Cheng, X.*, and Zhou J.* Identification and characterization of small molecules as potent and specific EPAC antagonists. J. Med. Chem. In press.

Chen, H, Ding, C., Wild, C., Liu, H., Wang, T., White, M. A., Cheng, X., and Zhou J. Efficient Synthesis of ESI-09, A Novel Non-cyclic Nucleotide EPAC Antagonist. Submitted to Tetrahedron Lett. In press.