Guangrong Zheng

Guangrong Zheng, Ph.D.

Associate Professor

Department: Medicinal Chemistry
Business Phone: (352) 294-8953
Business Email: zhengg@cop.ufl.edu

About Guangrong Zheng

Guangrong Zheng, Ph.D., is an associate professor in the department of medicinal chemistry at the University of Florida College of Pharmacy. He received his B.S. in medicinal chemistry from Fudan University and his Ph.D. in synthetic organic chemistry from Shanghai Institute of Materia Medica. He then completed his postdoc training in drug design and discovery at the University of Kentucky College of Pharmacy. Before he joined UF in March 2018, he was a faculty member at University of Arkansas for Medical Sciences College of Pharmacy.

Research Profile

Dr. Zheng’s lab focuses on the design, synthesis and structure-activity relationship study of both synthetically derived and natural product-based compounds for potential therapeutic uses or as molecular probes for biochemical/pharmacological research. His research also involves the development of efficient synthetic methodologies and strategies to facilitate the rapid construction of compound libraries. Ongoing projects in his lab include 1) development of small molecules that can induce targeted protein degradation as potential treatments for cancer; 2) development of senolytic agents, small molecules that can selectively kill senescent cells, as potential treatments for age-related diseases; and 3) development of radioprotective agents to improve the outcome of cancer radiotherapy or as radiation counter-measure agents.

Publications

2021
Concise Synthesis of (S)-δ-CEHC, a Metabolite of Vitamin E.
ACS omega. 6(6):4355-4361 [DOI] 10.1021/acsomega.0c05658. [PMID] 33623846.
2021
Proteolysis-targeting chimera against BCL-XL destroys tumor-infiltrating regulatory T cells.
Nature communications. 12(1) [DOI] 10.1038/s41467-021-21573-x. [PMID] 33627663.
2020
A Facile Semisynthesis and Evaluation of Garcinoic Acid and Its Analogs for the Inhibition of Human DNA Polymerase β.
Molecules (Basel, Switzerland). 25(24) [DOI] 10.3390/molecules25245847. [PMID] 33322249.
2020
Assays and technologies for developing proteolysis targeting chimera degraders.
Future medicinal chemistry. 12(12):1155-1179 [DOI] 10.4155/fmc-2020-0073. [PMID] 32431173.
2020
Deuteration of the farnesyl terminal methyl groups of δ-tocotrienol and its effects on the metabolic stability and ability of inducing G-CSF production.
Bioorganic & medicinal chemistry. 28(11) [DOI] 10.1016/j.bmc.2020.115498. [PMID] 32291146.
2020
Discovery of histone deacetylase 3 (HDAC3)-specific PROTACs.
Chemical communications (Cambridge, England). 56(68):9866-9869 [DOI] 10.1039/d0cc03243c. [PMID] 32840532.
2020
Discovery of IAP-recruiting BCL-XL PROTACs as potent degraders across multiple cancer cell lines.
European journal of medicinal chemistry. 199 [DOI] 10.1016/j.ejmech.2020.112397. [PMID] 32388279.
2020
Discovery of PROTAC BCL-XL degraders as potent anticancer agents with low on-target platelet toxicity.
European journal of medicinal chemistry. 192 [DOI] 10.1016/j.ejmech.2020.112186. [PMID] 32145645.
2020
DT2216-a Bcl-xL-specific degrader is highly active against Bcl-xL-dependent T cell lymphomas.
Journal of hematology & oncology. 13(1) [DOI] 10.1186/s13045-020-00928-9. [PMID] 32677976.
2020
Inhibition of USP7 activity selectively eliminates senescent cells in part via restoration of p53 activity.
Aging cell. 19(3) [DOI] 10.1111/acel.13117. [PMID] 32064756.
2020
Licochalcone A is a Natural Selective Inhibitor of Arginine Methyltransferase 6.
The Biochemical journal. [DOI] 10.1042/BCJ20200411. [PMID] 33245113.
2020
Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies.
Journal of hematology & oncology. 13(1) [DOI] 10.1186/s13045-020-00924-z. [PMID] 32718354.
2020
PROteolysis TArgeting Chimeras (PROTACs) as emerging anticancer therapeutics.
Oncogene. 39(26):4909-4924 [DOI] 10.1038/s41388-020-1336-y. [PMID] 32475992.
2020
Synthesis and liver microsomal metabolic stability studies of a fluoro-substituted δ-tocotrienol derivative
.
2020
Targeting anti-apoptotic BCL-2 family proteins for cancer treatment.
Future medicinal chemistry. 12(7):563-565 [DOI] 10.4155/fmc-2020-0004. [PMID] 32083493.
2020
Using proteolysis-targeting chimera technology to reduce navitoclax platelet toxicity and improve its senolytic activity.
Nature communications. 11(1) [DOI] 10.1038/s41467-020-15838-0. [PMID] 32332723.
2019
A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity.
Nature medicine. 25(12):1938-1947 [DOI] 10.1038/s41591-019-0668-z. [PMID] 31792461.
2019
Cellular senescence and radiation-induced pulmonary fibrosis.
Translational research : the journal of laboratory and clinical medicine. 209:14-21 [DOI] 10.1016/j.trsl.2019.03.006. [PMID] 30981698.
2019
GZ-11608, a Vesicular Monoamine Transporter-2 Inhibitor, Decreases the Neurochemical and Behavioral Effects of Methamphetamine.
The Journal of pharmacology and experimental therapeutics. 371(2):526-543 [DOI] 10.1124/jpet.119.258699. [PMID] 31413138.
2019
The curcumin analog EF24 is a novel senolytic agent.
Aging. 11(2):771-782 [DOI] 10.18632/aging.101787. [PMID] 30694217.
2019
Utilizing PROTAC technology to address the on-target platelet toxicity associated with inhibition of BCL-XL.
Chemical communications (Cambridge, England). 55(98):14765-14768 [DOI] 10.1039/c9cc07217a. [PMID] 31754664.
2018
An improved model of ethanol and nicotine co-use in female P rats: Effects of naltrexone, varenicline, and the selective nicotinic α6β2* antagonist r-bPiDI
Drug and Alcohol Dependence. 193:154-161
2018
Effects of the nicotinic agonist varenicline, nicotinic antagonist r-bPiDI, and DAT inhibitor (R)-modafinil on co-use of ethanol and nicotine in female P rats.
Psychopharmacology. 235(5):1439-1453 [DOI] 10.1007/s00213-018-4853-4. [PMID] 29455292.
2018
Muscarinic agonist, (±)-quinuclidin-3-yl-(4-fluorophenethyl)(phenyl)carbamate: High affinity, but low subtype selectivity for human M1 – M5 muscarinic acetylcholine receptors
Bioorganic & Medicinal Chemistry. 29(3):471-476 [DOI] 10.1016/j.bmcl.2018.12.022. [PMID] 30554957.
2018
New histone demethylase LSD1 inhibitor selectively targets teratocarcinoma cells by downregulating Sox2 expression
Bioorganic & Medicinal Chemistry. 26:1523-1537
2018
New Scaffold for Lead Compounds to Treat Methamphetamine Use Disorders.
The AAPS journal. 20(2) [DOI] 10.1208/s12248-018-0192-y. [PMID] 29427069.
2018
Oxidation resistance 1 is a novel senolytic target.
Aging cell. 17(4) [DOI] 10.1111/acel.12780. [PMID] 29766639.
2018
Senolytic activity of piperlongumine analogues: Synthesis and biological evaluation.
Bioorganic & medicinal chemistry. 26(14):3925-3938 [DOI] 10.1016/j.bmc.2018.06.013. [PMID] 29925484.
2018
Varenicline and GZ-793A differentially decrease methamphetamine self-administration under a multiple schedule of reinforcement in rats
. 29:87-97
2009
Selective inhibition of acetylcholine-evoked responses of alpha7 neuronal nicotinic acetylcholine receptors by novel tris- and tetrakis-azaaromatic quaternary ammonium antagonists.
Molecular pharmacology. 76(3):652-66 [DOI] 10.1124/mol.109.056176. [PMID] 19556356.
2008
Extending the analysis of nicotinic receptor antagonists with the study of alpha6 nicotinic receptor subunit chimeras.
Neuropharmacology. 54(8):1189-200 [DOI] 10.1016/j.neuropharm.2008.03.010. [PMID] 18448138.
2007
Contrast sensitivity and higher-order aberrations in patients with astigmatism.
Chinese medical journal. 120(10):882-5 [PMID] 17543177.
View on: PubMed
2005
The characterization of a novel rigid nicotine analog with alpha7-selective nAChR agonist activity and modulation of agonist properties by boron inclusion.
Bioorganic & medicinal chemistry letters. 15(17):3874-80 [PMID] 16005216.
View on: PubMed

Grants

Jan 2021 ACTIVE
Developing a Novel PROTAC-Based NR4A1 Degrader for Breast Cancer Therapy
Role: Principal Investigator
Funding: US ARMY MED RES ACQUISITION
Dec 2020 ACTIVE
Sanofi 2020 iAwards
Role: Co-Investigator
Funding: SANOFI
Sep 2020 ACTIVE
Identifying Novel Senolytic Agents and Molecular Targets
Role: Principal Investigator
Funding: NATL INST OF HLTH NIA
Jun 2020 ACTIVE
Intercollaborative Radiation Countermeasure (INTERACT) Consortium for Advanced Development of Medical Countermeasures to Mitigate/Treat Acute and Delayed Radiation Syndromes
Role: Co-Investigator
Funding: UNIV OF MARYLAND BALTIMORE via NATL INST OF HLTH NIAID
Apr 2020 ACTIVE
Inhibition of Bcl-xL by Targeted Degradation
Role: Principal Investigator
Funding: NATL INST OF HLTH NCI
Sep 2019 ACTIVE
Use of BCL-xL Proteolysis targeting chimeras to treat pancreatic cancer
Role: Principal Investigator
Funding: NATL INST OF HLTH NCI
Aug 2019 ACTIVE
Develop BCL-xL proteolysis targeting chimeras as safer and better senolytics
Role: Principal Investigator
Funding: NATL INST OF HLTH NIA
Sep 2018 – Aug 2020
NCI Clinical and Translational Exploratory/ Developmental Studies
Role: Principal Investigator
Funding: NATL INST OF HLTH NCI
Aug 2018 – Aug 2019
Discovery and Target Identification of Senolytic Agents
Role: Principal Investigator
Funding: NATL INST OF HLTH NIA
Jul 2018 ACTIVE
Role of Senescent Cells in Radiation-induced Pulmonary Fibrosis
Role: Co-Investigator
Funding: NATL INST OF HLTH NCI

Teaching Profile

Courses Taught
2018,2020-2021
PHA5878C Pt Care 3: Cv and Pulm
2019-2021
PHA6447 Drug Design
2019-2021
PHA7979 Advanced Research
2020
PHA7980 Research for Doctoral Dissertation
2020
PHA6971 Research for Master’s Thesis
2019-2021
PHA5782C Patient Care 2
2019-2020
PHA6910 Supervised Research
2019
PHA6934 Seminar in Medicinal Chemistry
2018,2020-2021
PHA5439 Prin Med Chem-Pcol I
2020-2021
PHA5930 Sem Pharm Research
2021
PHA6935 Selected Topics in Pharmacy

Contact Details

Phones:
Business:
(352) 294-8953
Emails:
Business:
zhengg@cop.ufl.edu