Chengguo (CX) Xing, Ph.D.
Professor And Associate Chair
About Chengguo (CX) Xing
Xing received his B.S. degree from the Dalian University of Technology and obtained his Ph.D. degree in organic chemistry from Arizona State University. He completed postdoctoral training in chemical biology at Harvard University. His independent research has been focusing on isolating, designing, and synthesizing biologically active small molecules as drug leads for translation and employing such candidates as probes to understand mechanism of drug action and related biology, with the long-term goal of developing solutions towards effectively managing human diseases. Another mission of our research is to train graduate students, post-doctoral fellows, undergraduate students, and other professionals the integration of different disciplines at the interface of chemistry and biology, including pharmacognosy, medicinal chemistry, chemical biology, molecular and cellular biology, and clinical bioanalytical chemistry.
Related Links:
Accomplishments
Teacher of the Year Award
2014-2015
·
University of Minnesota
Teacher of the Year Award
2006-2007
·
University of Minnesota
Young Investigator Award
2005-2006
·
AACP
Teaching Profile
Courses Taught
2020
PHA6971 Research for Master’s Thesis
2018,2020-2024
PHA7980 Research for Doctoral Dissertation
2018,2020-2024
PHA7979 Advanced Research
2017,2020-2023
PHA6447 Drug Design
2018-2024
PHA6935 Selected Topics in Pharmacy
2018,2020-2022,2022-2024
PHA6910 Supervised Research
2017,2020-2023,2023
PHA4913 Undergraduate Research in Medicinal Chemistry
2017-2019,2021-2024
PHA5784C Pt Care 4: GI and Renal
2019,2021-2024
PHA5789C Patient Care 7
2018
PHA6425 Drug Biotrans and Molecular Mechanisms of Toxicity
2018
CHM7979 Advanced Research
2017-2018
NGR7980 Research for Doctoral Dissertation
2017-2018
PHA6934 Seminar in Medicinal Chemistry
2017
PHA6905C Research Procedures in Medicinal Chemistry
2022
PHA6467C Drug Design II
2022-2023
PHA5439 Prin Med Chem-Pcol I
2023-2024
GMS6065 Fundamentals of Cancer Biology
2023-2024
PHA6185 Life Cycle of a Drug
2024
PHA6468 Biotransformation Considerations in Drug Design
Research Profile
Xing’s team’s research focuses on translational development with several indications, including novel therapies selective against multi-drug resistant malignancies, chemopreventive agents against primary carcinogenesis and a natural dietary supplement on neurological disorders with the goal to extend them in the clinical setting. There are currently three major independent directions: (i) To investigate the biology of the Bcl-2 family proteins, SERCA, Ca2+ homeostasis, and Notch in cancer multi-drug resistance, specifically their functions, interactions and regulations, and to develop novel small-molecule modulators as anticancer agents that will selectively eliminate multidrug-resistant malignancies and prevent drug resistance development in cancer therapies. (ii) To elucidate the molecular mechanisms underlying the beneficial (cancer preventive and anxiolytic) and adverse (hepatotoxic) effects of kava, to determine the responsible compound(s), to identify the cellular targets and to characterize their interactions, and to rationally develop structurally related lead candidates for drug discovery and development. (iii) To develop a panel of chalcone-based chemical probes with similar chemical structures but distinct biological activities, to employ such probes for target identification and mechanistic characterization, and to perform rational lead optimization and drug development.
Areas of Interest
- Cancer multi-drug resistance
- Cancer prevention
- Drug discovery
- Natural products
- Neurological disorders
Open Researcher and Contributor ID (ORCID)
0000-0002-4266-6236
Publications
2024
AB-free kava enhances resilience against the adverse health effects of tobacco smoke in mice.
bioRxiv : the preprint server for biology.
[DOI] 10.1101/2024.06.25.599576.
[PMID] 38979295.
2024
One-Week Kava Dietary Supplementation Increases Both Urinary N- and O-Glucuronides of NNAL, a Lung Carcinogen Major Metabolite, among Smokers
Chemical Research in Toxicology.
[DOI] 10.1021/acs.chemrestox.4c00109.
2023
A potent phosphodiester Keap1-Nrf2 protein-protein interaction inhibitor as the efficient treatment of Alzheimer’s disease
Redox Biology.
64
[DOI] 10.1016/j.redox.2023.102793.
[PMID] 37385075.
2023
Diallyl Disulfide Blocks Cigarette Carcinogen 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone-Induced Lung Tumorigenesis via Activation of the Nrf2 Antioxidant System and Suppression of NF-κB Inflammatory Response
Journal of Agricultural and Food Chemistry.
71(46):17763-17774
[DOI] 10.1021/acs.jafc.3c02007.
2023
Dietary Phytochemicals as Potential Chemopreventive Agents against Tobacco-Induced Lung Carcinogenesis
Nutrients.
15(3)
[DOI] 10.3390/nu15030491.
[PMID] 36771198.
2023
Fragment-Based Discovery of Azocyclic Alkyl Naphthalenesulfonamides as Keap1-Nrf2 Inhibitors for Acute Lung Injury Treatment
Journal of Medicinal Chemistry.
66(12):8267-8280
[DOI] 10.1021/acs.jmedchem.3c00686.
2023
Investigating miR-9 as a mediator in laryngeal cancer health disparities.
Frontiers in oncology.
13
[DOI] 10.3389/fonc.2023.1096882.
[PMID] 37081981.
2023
Opportunities and Challenges of Kava in Lung Cancer Prevention
International Journal of Molecular Sciences.
24(11)
[DOI] 10.3390/ijms24119539.
[PMID] 37298489.
2023
Profiling of the chemical space on the phenyl group of substituted benzothiazole RIPK3 inhibitors.
Bioorganic chemistry.
131
[DOI] 10.1016/j.bioorg.2022.106339.
[PMID] 36599218.
2023
Reducing tobacco-associated lung cancer risk: a study protocol for a randomized clinical trial of AB-free kava.
Trials.
24(1)
[DOI] 10.1186/s13063-023-07081-x.
[PMID] 36653872.
2023
ROS-mediated SRMS activation confers platinum resistance in ovarian cancer.
Oncogene.
42(20):1672-1684
[DOI] 10.1038/s41388-023-02679-6.
[PMID] 37020040.
2023
Targeting Receptor-Interacting Protein Kinase 1 by Novel Benzothiazole Derivatives: Treatment of Acute Lung Injury through the Necroptosis Pathway
Journal of Medicinal Chemistry.
66(7):5261-5278
[DOI] 10.1021/acs.jmedchem.3c00197.
2022
Angelica gigas: Signature Compounds, In Vivo Anticancer, Analgesic, Neuroprotective and Other Activities, and the Clinical Translation Challenges.
The American journal of Chinese medicine.
50(6):1475-1527
[DOI] 10.1142/S0192415X2250063X.
[PMID] 35876033.
2022
Characterization of adductomic totality of NNK, (R)-NNAL and (S)-NNAL in A/J mice, and their correlations with distinct lung carcinogenicity
Carcinogenesis.
43(2):170-181
[DOI] 10.1093/carcin/bgab113.
[PMID] 34919675.
2022
Characterization of Different Forms of Kava (Piper methysticum) Products by UPLC-MS/MS.
Planta medica.
88(14):1348-1359
[DOI] 10.1055/a-1708-1994.
[PMID] 34839465.
2022
Clinical pharmacokinetics of kavalactones after oral dosing of standardized kava extract in healthy volunteers.
Journal of ethnopharmacology.
297
[DOI] 10.1016/j.jep.2022.115514.
[PMID] 35777607.
2022
Crystallography-Guided Optimizations of the Keap1–Nrf2 Inhibitors on the Solvent Exposed Region: From Symmetric to Asymmetric Naphthalenesulfonamides
Journal of Medicinal Chemistry.
65(12):8289-8302
[DOI] 10.1021/acs.jmedchem.2c00170.
2022
Implementation strategies for integrating tobacco cessation treatment in cancer care: A qualitative study.
Implementation research and practice.
3
[DOI] 10.1177/26334895221112153.
[PMID] 36909717.
2022
In vitro inhibition of carboxylesterase 1 by Kava (Piper methysticum) Kavalactones.
Chemico-biological interactions.
357
[DOI] 10.1016/j.cbi.2022.109883.
[PMID] 35278473.
2022
In vivo Structure‐Activity Relationship of Dihydromethysticin in Reducing Nicotine‐Derived Nitrosamine Ketone (NNK)‐Induced Lung DNA Damage against Lung Carcinogenesis in A/J Mice
ChemMedChem.
17(7)
[DOI] 10.1002/cmdc.202100727.
[PMID] 35064644.
2022
LKB1 phosphorylation and deactivation in lung cancer by NNAL, a metabolite of tobacco-specific carcinogen, in an isomer-dependent manner.
Oncogene.
41(33):4042-4054
[DOI] 10.1038/s41388-022-02410-x.
[PMID] 35835853.
2022
Reducing Chemotherapy-Induced DNA Damage via nAChR-Mediated Redox Reprograming—A New Mechanism for SCLC Chemoresistance Boosted by Nicotine
Cancers.
14(9)
[DOI] 10.3390/cancers14092272.
[PMID] 35565402.
2022
Suppressing the activation of protein kinase A as a DNA damage-independent mechanistic lead for dihydromethysticin prophylaxis of NNK-induced lung carcinogenesis
Carcinogenesis.
43(7):659-670
[DOI] 10.1093/carcin/bgac031.
[PMID] 35353881.
2022
Targeting Necroptosis as a Promising Therapy for Alzheimer’s Disease
ACS Chemical Neuroscience.
13(12):1697-1713
[DOI] 10.1021/acschemneuro.2c00172.
2021
Structure-based molecular hybridization design of Keap1-Nrf2 inhibitors as novel protective agents of acute lung injury.
European journal of medicinal chemistry.
222
[DOI] 10.1016/j.ejmech.2021.113599.
[PMID] 34119834.
2020
CXL146, a Novel 4H-Chromene Derivative, Targets GRP78 to Selectively Eliminate Multidrug-Resistant Cancer Cells.
Molecular pharmacology.
97(6):402-408
[DOI] 10.1124/mol.119.118745.
[PMID] 32276963.
2020
Design, synthesis, and enzymatic characterization of quinazoline-based CYP1A2 inhibitors.
Bioorganic & medicinal chemistry letters.
30(2)
[DOI] 10.1016/j.bmcl.2019.126719.
[PMID] 31784319.
2020
Direct inhibition of Keap1-Nrf2 Protein-Protein interaction as a potential therapeutic strategy for Alzheimer’s disease.
Bioorganic chemistry.
103
[DOI] 10.1016/j.bioorg.2020.104172.
[PMID] 32890991.
2020
Erratum: Kava and its Kavalactones Inhibit Norepinephrine-induced Intracellular Calcium Influx in Lung Cancer Cells.
Planta medica.
86(1)
[DOI] 10.1055/a-1158-2228.
[PMID] 32316039.
2020
Kava and its Kavalactones Inhibit Norepinephrine-induced Intracellular Calcium Influx in Lung Cancer Cells.
Planta medica.
86(1):26-31
[DOI] 10.1055/a-1035-5183.
[PMID] 31711251.
2020
Kava as a Clinical Nutrient: Promises and Challenges.
Nutrients.
12(10)
[DOI] 10.3390/nu12103044.
[PMID] 33027883.
2020
Oral Dosing of Dihydromethysticin Ahead of Tobacco Carcinogen NNK Effectively Prevents Lung Tumorigenesis in A/J Mice
Chemical Research in Toxicology.
33(7):1980-1988
[DOI] 10.1021/acs.chemrestox.0c00161.
[PMID] 32476407.
2020
Smoking-Cessation Methods and Outcomes Among Cancer Survivors.
American journal of preventive medicine.
59(4):615-617
[DOI] 10.1016/j.amepre.2020.03.016.
[PMID] 32446750.
2020
The Impact of One-week Dietary Supplementation with Kava on Biomarkers of Tobacco Use and Nitrosamine-based Carcinogenesis Risk among Active Smokers
Cancer Prevention Research.
13(5):483-492
[DOI] 10.1158/1940-6207.capr-19-0501.
2019
Detection and quantification of 4-hydroxy-1-(3-pyridyl)-1-butanone (HPB) from smoker albumin and its potential as a surrogate biomarker of tobacco-specific nitrosamines exposure and bioactivation
Toxicology Letters.
311:11-16
[DOI] 10.1016/j.toxlet.2019.04.020.
[PMID] 31026483.
2019
Inhibitor of Apoptosis Protein (IAP) Antagonists in Anticancer Agent Discovery: Current Status and Perspectives
Journal of Medicinal Chemistry.
62(12):5750-5772
[DOI] 10.1021/acs.jmedchem.8b01668.
2018
A stable isotope dilution tandem mass spectrometry method of major kavalactones and its applications
PLOS ONE.
13(5)
[DOI] 10.1371/journal.pone.0197940.
[PMID] 29795658.
2018
An Indole–Chalcone Inhibits Multidrug-Resistant Cancer Cell Growth by Targeting Microtubules
Molecular Pharmaceutics.
15(9):3892-3900
[DOI] 10.1021/acs.molpharmaceut.8b00359.
[PMID] 30048137.
2018
Contribution of Tobacco Use and 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone to Three Methyl DNA Adducts in Urine
Chemical Research in Toxicology.
31(9):836-838
[DOI] 10.1021/acs.chemrestox.8b00155.
[PMID] 30136842.
2018
Exploring the Structure–Activity Relationship and Mechanism of a Chromene Scaffold (CXL Series) for Its Selective Antiproliferative Activity toward Multidrug-Resistant Cancer Cells
Journal of Medicinal Chemistry.
61(15):6892-6903
[DOI] 10.1021/acs.jmedchem.8b00813.
[PMID] 29995404.
2018
Quantitative profiling of cortisol metabolites in human urine by high-resolution accurate-mass MS.
Bioanalysis.
10(24):2015-2026
[DOI] 10.4155/bio-2018-0182.
[PMID] 30412681.
2018
The Effect of Tobacco Smoking on Musculoskeletal Health: A Systematic Review.
Journal of environmental and public health.
2018
[DOI] 10.1155/2018/4184190.
[PMID] 30112011.
2017
Chalcone: A Privileged Structure in Medicinal Chemistry
Chemical Reviews.
117(12):7762-7810
[DOI] 10.1021/acs.chemrev.7b00020.
[PMID] 28488435.
2017
Pilot in Vivo Structure–Activity Relationship of Dihydromethysticin in Blocking 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone-Induced O6-Methylguanine and Lung Tumor in A/J Mice
Journal of Medicinal Chemistry.
60(18):7935-7940
[DOI] 10.1021/acs.jmedchem.7b00921.
[PMID] 28806079.
2017
Prostate Cancer Xenograft Inhibitory Activity and Pharmacokinetics of Decursinol, a Metabolite of Angelica gigas Pyranocoumarins, in Mouse Models.
The American journal of Chinese medicine.
45(8):1773-1792
[DOI] 10.1142/S0192415X17500963.
[PMID] 29121805.
2017
Small molecules inhibiting Keap1-Nrf2 protein-protein interactions: a novel approach to activate Nrf2 function.
MedChemComm.
8(2):286-294
[DOI] 10.1039/c6md00500d.
[PMID] 30108745.
2016
4H-Chromene-based anticancer agents towards multi-drug resistant HL60/MX2 human leukemia: SAR at the 4th and 6th positions.
Bioorganic & medicinal chemistry.
24(6):1292-7
[DOI] 10.1016/j.bmc.2016.01.056.
[PMID] 26867486.
2016
Characterization of the Fluorescence Properties of 4-Dialkylaminochalcones and Investigation of the Cytotoxic Mechanism of Chalcones.
Archiv der Pharmazie.
349(7):539-52
[DOI] 10.1002/ardp.201500434.
[PMID] 27214789.
2016
Dietary Dihydromethysticin Increases Glucuronidation of 4-(Methylnitrosamino)-1-(3-Pyridyl)-1-Butanol in A/J Mice, Potentially Enhancing Its Detoxification.
Drug metabolism and disposition: the biological fate of chemicals.
44(3):422-7
[DOI] 10.1124/dmd.115.068387.
[PMID] 26744252.
2016
Dihydromethysticin (DHM) Blocks Tobacco Carcinogen 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK)-Induced O6-Methylguanine in a Manner Independent of the Aryl Hydrocarbon Receptor (AhR) Pathway in C57BL/6 Female Mice.
Chemical research in toxicology.
29(11):1828-1834
[PMID] 27728767.
2016
Direct detection of SERCA calcium transport and small-molecule inhibition in giant unilamellar vesicles.
Biochemical and biophysical research communications.
481(3-4):206-211
[DOI] 10.1016/j.bbrc.2016.10.096.
[PMID] 27815070.
2016
Gene expression signatures associated with suppression of TRAMP prostate carcinogenesis by a kavalactone-rich Kava fraction.
Molecular carcinogenesis.
55(12):2291-2303
[DOI] 10.1002/mc.22469.
[PMID] 26840761.
2016
Pyranocoumarin Tissue Distribution, Plasma Metabolome and Prostate Transcriptome Impacts of Sub-Chronic Exposure to Korean Angelica Supplement in Mice.
The American journal of Chinese medicine.
44(2):321-53
[DOI] 10.1142/S0192415X16500191.
[PMID] 27080944.
2016
Unambiguous Identification of β-Tubulin as the Direct Cellular Target Responsible for the Cytotoxicity of Chalcone by Photoaffinity Labeling.
ChemMedChem.
11(13):1436-45
[DOI] 10.1002/cmdc.201600150.
[PMID] 27203512.
2015
Cancer Chemoprevention with Korean Angelica: Active Compounds, Pharmacokinetics, and Human Translational Considerations.
Current pharmacology reports.
1(6):373-381
[PMID] 26623248.
2015
Chemopreventive effect of Korean Angelica root extract on TRAMP carcinogenesis and integrative “omic” profiling of affected neuroendocrine carcinomas.
Molecular carcinogenesis.
54(12):1567-83
[DOI] 10.1002/mc.22230.
[PMID] 25307620.
2015
Chemopreventive Effects of Korean Angelica versus Its Major Pyranocoumarins on Two Lineages of Transgenic Adenocarcinoma of Mouse Prostate Carcinogenesis.
Cancer prevention research (Philadelphia, Pa.).
8(9):835-44
[DOI] 10.1158/1940-6207.CAPR-15-0051.
[PMID] 26116406.
2015
Cytochrome P450 Isoforms in the Metabolism of Decursin and Decursinol Angelate from Korean Angelica.
The American journal of Chinese medicine.
43(6):1211-30
[DOI] 10.1142/S0192415X1550069X.
[PMID] 26394652.
2015
Diverse Molecular Targets for Chalcones with Varied Bioactivities.
Medicinal chemistry.
5(8):388-404
[PMID] 26798565.
2015
Kava for the treatment of generalised anxiety disorder (K-GAD): study protocol for a randomised controlled trial.
Trials.
16
[DOI] 10.1186/s13063-015-0986-5.
[PMID] 26527536.
2015
Single oral dose pharmacokinetics of decursin and decursinol angelate in healthy adult men and women.
PloS one.
10(2)
[DOI] 10.1371/journal.pone.0114992.
[PMID] 25695490.
2014
Dihydromethysticin from kava blocks tobacco carcinogen 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone-induced lung tumorigenesis and differentially reduces DNA damage in A/J mice.
Carcinogenesis.
35(10):2365-72
[DOI] 10.1093/carcin/bgu149.
[PMID] 25053626.
2014
Double-edged swords as cancer therapeutics: novel, orally active, small molecules simultaneously inhibit p53-MDM2 interaction and the NF-κB pathway.
Journal of medicinal chemistry.
57(3):567-77
[DOI] 10.1021/jm401800k.
[PMID] 24428757.
2014
Flavokawains a and B in kava, not dihydromethysticin, potentiate acetaminophen-induced hepatotoxicity in C57BL/6 mice.
Chemical research in toxicology.
27(10):1871-6
[DOI] 10.1021/tx5003194.
[PMID] 25185080.
2014
Kava blocks 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone-induced lung tumorigenesis in association with reducing O6-methylguanine DNA adduct in A/J mice.
Cancer prevention research (Philadelphia, Pa.).
7(1):86-96
[DOI] 10.1158/1940-6207.CAPR-13-0301.
[PMID] 24403291.
2014
Measuring the chemical and cytotoxic variability of commercially available kava (Piper methysticum G. Forster).
PloS one.
9(11)
[DOI] 10.1371/journal.pone.0111572.
[PMID] 25365244.
2014
Rapid identification of Keap1-Nrf2 small-molecule inhibitors through structure-based virtual screening and hit-based substructure search.
Journal of medicinal chemistry.
57(3):1121-6
[DOI] 10.1021/jm4017174.
[PMID] 24417449.
2013
A novel SERCA inhibitor demonstrates synergy with classic SERCA inhibitors and targets multidrug-resistant AML.
Molecular pharmaceutics.
10(11):4358-66
[DOI] 10.1021/mp400458u.
[PMID] 24079514.
2013
Ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (CXL017): a novel scaffold that resensitizes multidrug resistant leukemia cells to chemotherapy.
ACS chemical biology.
8(2):327-35
[DOI] 10.1021/cb300460f.
[PMID] 23102022.
2013
In vitro metabolism of pyranocoumarin isomers decursin and decursinol angelate by liver microsomes from man and rodents.
Planta medica.
79(16):1536-44
[DOI] 10.1055/s-0033-1350796.
[PMID] 24026903.
2013
Overexpression of Mcl-1 confers multidrug resistance, whereas topoisomerase IIβ downregulation introduces mitoxantrone-specific drug resistance in acute myeloid leukemia.
Molecular pharmacology.
84(2):236-43
[DOI] 10.1124/mol.113.086140.
[PMID] 23696245.
2013
Single oral dose pharmacokinetics of decursin, decursinol angelate, and decursinol in rats.
Planta medica.
79(3-4):275-80
[DOI] 10.1055/s-0032-1328202.
[PMID] 23364885.
2012
A new chalcone derivative (E)-3-(4-methoxyphenyl)-2-methyl-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one suppresses prostate cancer involving p53-mediated cell cycle arrests and apoptosis.
Anticancer research.
32(9):3689-98
[PMID] 22993307.
2012
A synthetic decursin analog with increased in vivo stability suppresses androgen receptor signaling in vitro and in vivo.
Investigational new drugs.
30(5):1820-9
[DOI] 10.1007/s10637-011-9738-x.
[PMID] 21870073.
2012
Anti-cancer and other bioactivities of Korean Angelica gigas Nakai (AGN) and its major pyranocoumarin compounds.
Anti-cancer agents in medicinal chemistry.
12(10):1239-54
[PMID] 22583405.
2012
Inhibition of mitogen activated protein kinases increases the sensitivity of A549 lung cancer cells to the cytotoxicity induced by a kava chalcone analog.
Biochemical and biophysical research communications.
424(3):488-92
[DOI] 10.1016/j.bbrc.2012.06.140.
[PMID] 22771807.
2012
Quantitative determination of decursin, decursinol angelate, and decursinol in mouse plasma and tumor tissue using liquid-liquid extraction and HPLC.
Planta medica.
78(3):252-9
[DOI] 10.1055/s-0031-1280384.
[PMID] 22116603.
2012
Reduction in colon cancer risk by consumption of kava or kava fractions in carcinogen-treated rats.
Nutrition and cancer.
64(6):838-46
[DOI] 10.1080/01635581.2012.689917.
[PMID] 22693990.
2012
Structure-activity relationship (SAR) study of ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (CXL017) and the potential of the lead against multidrug resistance in cancer treatment.
Journal of medicinal chemistry.
55(11):5566-81
[DOI] 10.1021/jm300515q.
[PMID] 22582991.
2011
A three-layer competition-based giant magnetoresistive assay for direct quantification of endoglin from human urine.
Analytical chemistry.
83(8):2996-3002
[DOI] 10.1021/ac2005229.
[PMID] 21417448.
2011
Chalcone-based inhibitors against hypoxia-inducible factor 1–structure activity relationship studies.
Bioorganic & medicinal chemistry letters.
21(1):555-7
[DOI] 10.1016/j.bmcl.2010.10.063.
[PMID] 21112783.
2011
Lung tumorigenesis suppressing effects of a commercial kava extract and its selected compounds in A/J mice.
The American journal of Chinese medicine.
39(4):727-42
[PMID] 21721153.
2011
Preparation of penta-O-galloyl-β-D-glucose from tannic acid and plasma pharmacokinetic analyses by liquid-liquid extraction and reverse-phase HPLC.
Journal of pharmaceutical and biomedical analysis.
54(3):545-50
[DOI] 10.1016/j.jpba.2010.09.028.
[PMID] 20970943.
2011
Structure-activity relationship and molecular mechanisms of ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (CXL017) and its analogues.
Journal of medicinal chemistry.
54(16):5937-48
[DOI] 10.1021/jm200764t.
[PMID] 21780800.
2010
A new and facile method for measurement of apparent density of monodisperse polymer beads.
Talanta.
80(5):1681-5
[DOI] 10.1016/j.talanta.2009.10.004.
[PMID] 20152396.
2010
Penta-O-galloyl-beta-D-glucose induces G1 arrest and DNA replicative S-phase arrest independently of cyclin-dependent kinase inhibitor 1A, cyclin-dependent kinase inhibitor 1B and P53 in human breast cancer cells and is orally active against triple negative xenograft growth.
Breast cancer research : BCR.
12(5)
[DOI] 10.1186/bcr2634.
[PMID] 20809980.
2009
A detection system based on giant magnetoresistive sensors and high-moment magnetic nanoparticles demonstrates zeptomole sensitivity: potential for personalized medicine.
Angewandte Chemie (International ed. in English).
48(15):2764-7
[DOI] 10.1002/anie.200806266.
[PMID] 19288507.
2009
Dual mechanisms of sHA 14-1 in inducing cell death through endoplasmic reticulum and mitochondria.
Molecular pharmacology.
76(3):667-78
[DOI] 10.1124/mol.109.055830.
[PMID] 19561125.
2009
Identification of methysticin as a potent and non-toxic NF-kappaB inhibitor from kava, potentially responsible for kava’s chemopreventive activity.
Bioorganic & medicinal chemistry letters.
19(19):5732-6
[DOI] 10.1016/j.bmcl.2009.08.003.
[PMID] 19716299.
2009
Structure-activity relationship and molecular mechanisms of ethyl 2-amino-4-(2-ethoxy-2-oxoethyl)-6-phenyl-4h-chromene-3-carboxylate (sha 14-1) and its analogues.
Journal of medicinal chemistry.
52(19):5937-49
[DOI] 10.1021/jm9005059.
[PMID] 19743858.
2009
Structure-activity relationship studies of chalcone leading to 3-hydroxy-4,3′,4′,5′-tetramethoxychalcone and its analogues as potent nuclear factor kappaB inhibitors and their anticancer activities.
Journal of medicinal chemistry.
52(22):7228-35
[DOI] 10.1021/jm901278z.
[PMID] 19883086.
2008
Chemopreventive effect of kava on 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone plus benzo[a]pyrene-induced lung tumorigenesis in A/J mice.
Cancer prevention research (Philadelphia, Pa.).
1(6):430-8
[DOI] 10.1158/1940-6207.CAPR-08-0027.
[PMID] 19138990.
2008
Development of dimeric modulators for anti-apoptotic Bcl-2 proteins.
Bioorganic & medicinal chemistry letters.
18(1):236-40
[PMID] 18023349.
2008
Diets, phytochemicals, and chemoprevention of tumorigenesis.
Journal of dietary supplements.
5(2):95-105
[DOI] 10.1080/19390210802332877.
[PMID] 22432428.
2008
Inhibition of siderophore biosynthesis by 2-triazole substituted analogues of 5′-O-[N-(salicyl)sulfamoyl]adenosine: antibacterial nucleosides effective against Mycobacterium tuberculosis.
Journal of medicinal chemistry.
51(23):7495-507
[DOI] 10.1021/jm8008037.
[PMID] 19053762.
2008
sHA 14-1, a stable and ROS-free antagonist against anti-apoptotic Bcl-2 proteins, bypasses drug resistances and synergizes cancer therapies in human leukemia cell.
Cancer letters.
259(2):198-208
[PMID] 18037229.
2008
WL-276, an antagonist against Bcl-2 proteins, overcomes drug resistance and suppresses prostate tumor growth.
Cancer research.
68(11):4377-83
[DOI] 10.1158/0008-5472.CAN-07-6590.
[PMID] 18519699.
2007
Development of selective inhibitors for anti-apoptotic Bcl-2 proteins from BHI-1.
Bioorganic & medicinal chemistry.
15(5):2167-76
[PMID] 17227711.
2007
Ethyl-2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H- chromene-3-carboxylate (HA 14-1), a prototype small-molecule antagonist against antiapoptotic Bcl-2 proteins, decomposes to generate reactive oxygen species that induce apoptosis.
Molecular pharmaceutics.
4(6):919-28
[PMID] 17874842.
2006
Structure-activity relationship studies of ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (HA 14-1), an antagonist for antiapoptotic Bcl-2 proteins to overcome drug resistance in cancer.
Journal of medicinal chemistry.
49(26):7731-9
[PMID] 17181155.
Grants
Aug 2023
ACTIVE
The potential of kava in enabling tobacco cessation – its holistic effects in managing stress and insomnia associated with abstinence
Role: Principal Investigator
Funding: NATL CTR FOR COMPLEM AND INTEGRATIVE HLT
Jun 2023
– May 2024
MGMT down-regulation in the carcinogenicity of hexavalent chromium
Role: Principal Investigator
Funding: STONY BROOK UNIVERSITY
via NATL INST OF HLTH NIEHS
Apr 2023
ACTIVE
AB-free kava in lung cancer chemoprevention
Role: Principal Investigator
Funding: FL DEPT OF HLTH BANKHEAD-COLEY CANCER RE
Aug 2022
ACTIVE
Quantifying NNK metabolites to facilitate Kava lung cancer prevention clinical translation
Role: Principal Investigator
Funding: NATL INST OF HLTH NCI
Jul 2022
– Jun 2024
Together: Transforming and Translating Discovery to Improve Health
Role: Project Manager
Funding: NATL INST OF HLTH NCATS
Sep 2021
– Feb 2023
MGMT down-regulation in the carcinogenicity of hexavalent chromium
Role: Principal Investigator
Funding: CASE WESTERN RESERVE UNIV
via NATL INST OF HLTH NIEHS
Jun 2021
ACTIVE
Reducing tobacco-associated lung cancer risk: A randomized clinical trial of AB-free kava
Role: Principal Investigator
Funding: FL DEPT OF HLTH BIOMED RES PGM/J&E KING
Dec 2020
– Nov 2022
Contributions of Tobacco use, NNK, and Stress to Lung Cancer Risk Disparities between AA and CA Male Smokers
Role: Principal Investigator
Funding: LUNG CANCER RESEARCH FOUNDATION
Jun 2020
– May 2023
Preclinical evaluation of the efficacy and mechanism of action for an alkylated polyamine analogue diethylnorspermine in treating pheochromocytoma/paraganglioma
Role: Project Manager
Funding: NATL INST OF HLTH NCATS
Sep 2019
– Feb 2021
MGMT down-regulation in the carcinogenicity of hexavalent chromium
Role: Principal Investigator
Funding: UNIV OF KENTUCKY
via NATL INST OF HLTH NIEHS
Sep 2019
– Aug 2023
A phased clinical trial of a dietary supplement kava: biomarker changes and anxiolytic effects
Role: Principal Investigator
Funding: NATL CTR FOR COMPLEM AND INTEGRATIVE HLT
Sep 2018
– Aug 2023
2/3 Florida-California Cancer Research, Education & Engagement (CaRE2) Health Equity Center
Role: Principal Investigator
Funding: NATL INST OF HLTH NCI
Nov 2017
– Oct 2022
The Harry T. Mangurian, Jr. Foundation – Support for the Study of Therapy Resistant Leukemia
Role: Co-Project Director/Principal Investigator
Funding: UF FOUNDATION
via HARRY T MANGURIAN JR FOU
Aug 2017
– Dec 2019
Research Core Scope of Work (Phase I Contract)
Role: Project Manager
Funding: FL STATE UNIV
via FL LEGISLATURE
Sep 2016
– Apr 2022
Dihydromethysticin (DHM) for Lung Cancer Chemoprevention
Role: Principal Investigator
Funding: NATL INST OF HLTH NCI
Sep 2016
– Jun 2018
Mechanisms of Anticancer Agents Selective against Drug Resistant Leukemia
Role: Principal Investigator
Funding: NATL INST OF HLTH NCI
Education
Ph.D. – Organic Chemistry
1996-2001
·
Arizona State University
B.S. – Chemical Engineering
1991-1996
·
Dalian University of Technology
Contact Details
Phones:
- Business:
- (352) 294-8511
Emails:
- Business:
- chengguoxing@ufl.edu
Addresses:
- Business Mailing:
-
PO Box 100485
GAINESVILLE FL 32610 - Business Street:
-
MSB P6-04
1345 Center Drive
GAINESVILLE FL 326103006