Abstract

Public Health Relevance

Our study focuses on developing novel chemical probes specifically targeting an important signaling protein that has been implicated in many human diseases including pancreatic cancer. These new chemical probes can be used in studying disease mechanisms and in developing medications.

  Funding Agency

Agency
National Institute of Health (NIH)
Institute
National Institute of General Medical Sciences (NIGMS)
Type
Research Project (R01)
Project #
5R01GM106218-02
Application #
8869095
Study Section
Special Emphasis Panel (ZRG1-MDCN-C (58))
Program Officer
Fabian, Miles
Project Start
2013-04-01
Project End
2016-03-31
Budget Start
2014-04-01
Budget End
2015-03-31
Support Year
2
Fiscal Year
2014
Total Cost
$277,625
Indirect Cost
$24,767

  Institution

Name
University of Texas Medical Br Galveston
Department
Pharmacology
Type
Schools of Medicine
DUNS #
800771149
City
Galveston
State
TX
Country
United States
Zip Code
77555

  Publications

Wang, Pingyuan; Liu, Zhiqing; Chen, Haiying et al. (2017) Exchange proteins directly activated by cAMP (EPACs): Emerging therapeutic targets. Bioorg Med Chem Lett 27:1633-1639
Liu, Zhiqing; Zhu, Yingmin; Chen, Haiying et al. (2017) Structure-activity relationships of 2-substituted phenyl-N-phenyl-2-oxoacetohydrazonoyl cyanides as novel antagonists of exchange proteins directly activated by cAMP (EPACs). Bioorg Med Chem Lett 27:5163-5166
Ye, Na; Zhu, Yingmin; Liu, Zhiqing et al. (2017) Identification of novel 2-(benzo[d]isoxazol-3-yl)-2-oxo-N-phenylacetohydrazonoyl cyanide analoguesas potent EPAC antagonists. Eur J Med Chem 134:62-71
Wild, Christopher T; Zhu, Yingmin; Na, Ye et al. (2016) Functionalized N,N-Diphenylamines as Potent and Selective EPAC2 Inhibitors. ACS Med Chem Lett 7:460-4
Almahariq, Muayad; Mei, Fang C; Cheng, Xiaodong (2016) The pleiotropic role of exchange protein directly activated by cAMP 1 (EPAC1) in cancer: implications for therapeutic intervention. Acta Biochim Biophys Sin (Shanghai) 48:75-81
Singhmar, Pooja; Huo, XiaoJiao; Eijkelkamp, Niels et al. (2016) Critical role for Epac1 in inflammatory pain controlled by GRK2-mediated phosphorylation of Epac1. Proc Natl Acad Sci U S A 113:3036-41
Banerjee, Upasana; Cheng, Xiaodong (2015) Exchange protein directly activated by cAMP encoded by the mammalian rapgef3 gene: Structure, function and therapeutics. Gene 570:157-67
Zhu, Yingmin; Chen, Haijun; Boulton, Stephen et al. (2015) Biochemical and pharmacological characterizations of ESI-09 based EPAC inhibitors: defining the ESI-09 ""therapeutic window"". Sci Rep 5:9344
Ye, Na; Zhu, Yingmin; Chen, Haijun et al. (2015) Structure-Activity Relationship Studies of Substituted 2-(Isoxazol-3-yl)-2-oxo-N'-phenyl-acetohydrazonoyl Cyanide Analogues: Identification of Potent Exchange Proteins Directly Activated by cAMP (EPAC) Antagonists. J Med Chem 58:6033-47
Almahariq, Muayad; Chao, Celia; Mei, Fang C et al. (2015) Pharmacological inhibition and genetic knockdown of exchange protein directly activated by cAMP 1 reduce pancreatic cancer metastasis in vivo. Mol Pharmacol 87:142-9

Showing the most recent 10 out of 14 publications