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
2018,2020-2025
PHA7980 Research for Doctoral Dissertation
2018,2020-2025
PHA7979 Advanced Research
2017,2020-2024
PHA6447 Drug Design
2018-2024
PHA6935 Selected Topics in Pharmacy
2018,2020-2022,2022-2025
PHA6910 Supervised Research
2017,2020-2023,2023-2025,2025
PHA4913 Undergraduate Research in Medicinal Chemistry
2017-2019,2021-2025
PHA5784C Pt Care 4: GI and Renal
2019,2021-2025
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
2023-2025
GMS6065 Fundamentals of Cancer Biology
2023-2024
PHA6185 Life Cycle of a Drug
2024-2025
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
Publications
Academic Articles
2024
Flavokavains A- and B-Free Kava Enhances Resilience against the Adverse Health Effects of Tobacco Smoke in Mice.
ACS pharmacology & translational science.
7(11):3502-3517
[DOI] 10.1021/acsptsci.4c00415.
[PMID] 39539272.
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.
37(9):1515-1523
[DOI] 10.1021/acs.chemrestox.4c00109.
[PMID] 39001862.
2024
The potential of AB-free kava in enabling tobacco cessation via management of abstinence-related stress and insomnia: study protocol for a randomized clinical trial.
BMC complementary medicine and therapies.
24(1)
[DOI] 10.1186/s12906-024-04722-9.
[PMID] 39709468.
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
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.
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
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.
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 (Philadelphia, Pa.).
13(5):483-492
[DOI] 10.1158/1940-6207.CAPR-19-0501.
[PMID] 32102948.
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.
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
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
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.
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