Guangrong Zheng, Ph.D.
Professor
About Guangrong Zheng
Guangrong Zheng, Ph.D., is a 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.
Related Links:
Teaching Profile
Courses Taught
2018,2020-2024
PHA5878C Pt Care 3: Cv and Pulm
2019-2025
PHA6447 Drug Design
2019-2025
PHA7979 Advanced Research
2020,2022-2025
PHA7980 Research for Doctoral Dissertation
2020
PHA6971 Research for Master’s Thesis
2019-2025
PHA5782C Patient Care 2: Introduction to Infectious Disease and Oncology
2019-2023,2025
PHA6910 Supervised Research
2019
PHA6934 Seminar in Medicinal Chemistry
2018,2020-2024
PHA5439 Prin Med Chem-Pcol I
2020
PHA5930 Sem Pharm Research
2021,2023-2025
PHA6935 Selected Topics in 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
Academic Articles
2025
A BCL-xL/BCL-2 PROTAC effectively clears senescent cells in the liver and reduces MASH-driven hepatocellular carcinoma in mice
Nature Aging.
[DOI] 10.1038/s43587-025-00811-7.
2025
A novel regimen for pancreatic ductal adenocarcinoma targeting MEK, BCL-xL, and EGFR
Neoplasia.
59
[DOI] 10.1016/j.neo.2024.101070.
[PMID] 39541736.
2024
Design and optimization of piperlongumine analogs as potent senolytics
Bioorganic & Medicinal Chemistry Letters.
98
[DOI] 10.1016/j.bmcl.2023.129593.
2024
Development and crystal structures of a potent second-generation dual degrader of BCL-2 and BCL-xL
Nature Communications.
15(1)
[DOI] 10.1038/s41467-024-46922-4.
[PMID] 38548768.
2024
Discovery of a Highly Potent and Selective HDAC8 Degrader: Advancing the Functional Understanding and Therapeutic Potential of HDAC8
Journal of Medicinal Chemistry.
67(15):12784-12806
[DOI] 10.1021/acs.jmedchem.4c00761.
2024
GNAS knockout potentiates HDAC3 inhibition through viral mimicry-related interferon responses in lymphoma
Leukemia.
38(10):2210-2224
[DOI] 10.1038/s41375-024-02325-4.
[PMID] 39117798.
2024
Patent landscape of small molecule inhibitors of METTL3 (2020-present)
Expert Opinion on Therapeutic Patents.
1-16
[DOI] 10.1080/13543776.2024.2447056.
2024
Powering up targeted protein degradation through active and passive tumour-targeting strategies: Current and future scopes
Pharmacology & Therapeutics.
263
[DOI] 10.1016/j.pharmthera.2024.108725.
2024
PROTAC-Mediated Dual Degradation of BCL-xL and BCL-2 Is a Highly Effective Therapeutic Strategy in Small-Cell Lung Cancer
Cells.
13(6)
[DOI] 10.3390/cells13060528.
[PMID] 38534371.
2024
PROTAC-mediated NR4A1 degradation as a novel strategy for cancer immunotherapy
Journal of Experimental Medicine.
221(3)
[DOI] 10.1084/jem.20231519.
[PMID] 38334978.
2024
Targeted degradation of specific TEAD paralogs by small molecule degraders
Heliyon.
10(18)
[DOI] 10.1016/j.heliyon.2024.e37829.
[PMID] 39328531.
2024
Targeted Protein Degradation: Current and Emerging Approaches for E3 Ligase Deconvolution
Journal of Medicinal Chemistry.
67(14):11580-11596
[DOI] 10.1021/acs.jmedchem.4c00723.
2024
Targeting METTL3 protein by proteolysis-targeting chimeras: A novel therapeutic approach for acute myeloid leukemia
Genes & Diseases.
[DOI] 10.1016/j.gendis.2024.101452.
2023
Co-targeting BCL-XL and BCL-2 by PROTAC 753B eliminates leukemia cells and enhances efficacy of chemotherapy by targeting senescent cells.
Haematologica.
108(10):2626-2638
[DOI] 10.3324/haematol.2022.281915.
[PMID] 37078252.
2023
Co-targeting BCL-XL and MCL-1 with DT2216 and AZD8055 synergistically inhibit small-cell lung cancer growth without causing on-target toxicities in mice
Cell Death Discovery.
9(1)
[DOI] 10.1038/s41420-022-01296-8.
[PMID] 36588105.
2023
HDAC3 and HDAC8 PROTAC dual degrader reveals roles of histone acetylation in gene regulation.
Cell chemical biology.
30(11):1421-1435.e12
[DOI] 10.1016/j.chembiol.2023.07.010.
[PMID] 37572669.
2023
Piperlongumine conjugates induce targeted protein degradation.
Cell chemical biology.
30(2):203-213.e17
[DOI] 10.1016/j.chembiol.2023.01.004.
[PMID] 36750097.
2023
PROTAC therapy as a new targeted therapy for lung cancer
Molecular Therapy.
31(3):647-656
[DOI] 10.1016/j.ymthe.2022.11.011.
[PMID] 36415148.
2023
Resistance to the BCL-XL degrader DT2216 in T-cell acute lymphoblastic leukemia is rare and correlates with decreased BCL-XL proteolysis.
Cancer chemotherapy and pharmacology.
91(1):89-95
[DOI] 10.1007/s00280-022-04490-8.
[PMID] 36346454.
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 intracellular proteins with cell type-specific functions for cancer immunotherapy
Life Medicine.
2(3)
[DOI] 10.1093/lifemedi/lnad019.
[PMID] 39872303.
2023
YAP at the Crossroads of Biomechanics and Drug Resistance in Human Cancer
International Journal of Molecular Sciences.
24(15)
[DOI] 10.3390/ijms241512491.
[PMID] 37569866.
2022
BCL-XL PROTAC degrader DT2216 synergizes with sotorasib in preclinical models of KRASG12C-mutated cancers
Journal of Hematology & Oncology.
15(1)
[DOI] 10.1186/s13045-022-01241-3.
[PMID] 35260176.
2022
DyScore: A Boosting Scoring Method with Dynamic Properties for Identifying True Binders and Nonbinders in Structure-Based Drug Discovery
Journal of Chemical Information and Modeling.
62(22):5550-5567
[DOI] 10.1021/acs.jcim.2c00926.
[PMID] 36327102.
2022
Overcoming Cancer Drug Resistance Utilizing PROTAC Technology
Frontiers in Cell and Developmental Biology.
10
[DOI] 10.3389/fcell.2022.872729.
[PMID] 35547806.
2022
Overcoming Gemcitabine Resistance in Pancreatic Cancer Using the BCL-XL–Specific Degrader DT2216
Molecular Cancer Therapeutics.
21(1):184-192
[DOI] 10.1158/1535-7163.mct-21-0474.
2022
Patent landscape of inhibitors and PROTACs of the anti-apoptotic BCL-2 family proteins.
Expert opinion on therapeutic patents.
32(9):1003-1026
[DOI] 10.1080/13543776.2022.2116311.
[PMID] 35993382.
2022
Targeting BCL-XL in fibrolamellar hepatocellular carcinoma
JCI Insight.
7(17)
[DOI] 10.1172/jci.insight.161820.
[PMID] 36073545.
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
Development of a BCL-xL and BCL-2 dual degrader with improved anti-leukemic activity,
Nature Communications.
12(1)
[DOI] 10.1038/s41467-021-27210-x.
[PMID] 34824248.
2021
Discovery of a Novel BCL-XL PROTAC Degrader with Enhanced BCL-2 Inhibition
Journal of Medicinal Chemistry.
64(19):14230-14246
[DOI] 10.1021/acs.jmedchem.1c00517.
[PMID] 34533954.
2021
Mitigation of late cardiovascular effects of oxygen ion radiation by gamma-tocotrienol in a mouse model
Life Sciences in Space Research.
31:43-50
[DOI] 10.1016/j.lssr.2021.07.006.
[PMID] 34689949.
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.
2021
Therapy-Induced Senescence: Opportunities to Improve Anti-Cancer Therapy
JNCI: Journal of the National Cancer Institute.
[DOI] 10.1093/jnci/djab064.
[PMID] 33792717.
2020
A Facile Semisynthesis and Evaluation of Garcinoic Acid and Its Analogs for the Inhibition of Human DNA Polymerase β
Molecules.
25(24)
[DOI] 10.3390/molecules25245847.
[PMID] 33322249.
2020
Assays and technologies for developing proteolysis targeting chimera degraders
Future Medicinal Chemistry.
[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.
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
Biochemical Journal.
[DOI] 10.1042/BCJ20200411.
[PMID] 33245113.
2020
PROTACs are effective in addressing the platelet toxicity associated with BCL-XL inhibitors
Exploration of Targeted Anti-tumor Therapy.
1(4):259-272
[DOI] 10.37349/etat.2020.00017.
[PMID] 34296214.
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
Senolytic Drug Development
Healthy Ageing and Longevity.
3-20
[DOI] 10.1007/978-3-030-44903-2_1.
2020
Synthesis and Liver Microsomal Metabolic Stability Studies of a Fluorine‐Substituted δ‐Tocotrienol Derivative
ChemMedChem.
15(6):506-516
[DOI] 10.1002/cmdc.201900676.
[PMID] 31957223.
2020
Targeting Anti-Apoptotic BCL-2 Family Proteins for Cancer Treatment
Future Medicinal Chemistry.
12(7):563-565
[DOI] 10.4155/fmc-2020-0004.
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.
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
Journal of Pharmacology and Experimental Therapeutics.
371(2):526-543
[DOI] 10.1124/jpet.119.258699.
[PMID] 31413138.
2019
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 Letters.
29(3):471-476
[DOI] 10.1016/j.bmcl.2018.12.022.
[PMID] 30554957.
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.
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
New histone demethylase LSD1 inhibitor selectively targets teratocarcinoma cells by downregulating Sox2 expression
Bioorganic & Medicinal Chemistry.
26:1523-1537
2018
Novel scaffold for lead compounds to treat methamphetamine use disorders
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
Behavioural Pharmacology.
29(1):87-97
[DOI] 10.1097/fbp.0000000000000340.
2017
GZ-793A inhibits the neurochemical effects of methamphetamine via a selective interaction with the vesicular monoamine transporter-2
European Journal of Pharmacology.
795:143-149
[DOI] 10.1016/j.ejphar.2016.12.016.
[PMID] 27986625.
2017
Novel Linear Lipopeptide Paenipeptins with Potential for Eradicating Biofilms and Sensitizing Gram-Negative Bacteria to Rifampicin and Clarithromycin
Journal of Medicinal Chemistry.
60(23):9630-9640
[DOI] 10.1021/acs.jmedchem.7b01064.
2016
1,4-Diphenalkylpiperidines: A new scaffold for the design of potent inhibitors of the vesicular monoamine transporter-2
Bioorganic & Medicinal Chemistry Letters.
26(13):2997-3000
[DOI] 10.1016/j.bmcl.2016.05.025.
[PMID] 27212067.
2016
Discovery of piperlongumine as a potential novel lead for the development of senolytic agents
Aging.
8(11):2915-2926
[DOI] 10.18632/aging.101100.
[PMID] 27913811.
2016
Lobelane analogues containing 4-hydroxy and 4-(2-fluoroethoxy) aromatic substituents: Potent and selective inhibitors of [3H]dopamine uptake at the vesicular monoamine transporter-2
Bioorganic & Medicinal Chemistry Letters.
26(10):2422-2427
[DOI] 10.1016/j.bmcl.2016.03.119.
[PMID] 27080180.
2016
Synthesis and in vitro evaluation of water-soluble 1,4-diphenethylpiperazine analogs as novel inhibitors of the vesicular monoamine transporter-2
Bioorganic & Medicinal Chemistry Letters.
26(18):4441-4445
[DOI] 10.1016/j.bmcl.2016.08.001.
[PMID] 27524311.
2016
Synthesis of (2 R ,8′ S ,3′ E )-δ-tocodienol, a tocoflexol family member designed to have a superior pharmacokinetic profile compared to δ-tocotrienol
Tetrahedron.
72(27-28):4001-4006
[DOI] 10.1016/j.tet.2016.05.028.
[PMID] 27773949.
2015
AgSbF6-catalyzed efficient propargylation/cycloisomerization tandem reaction for the synthesis of fully substituted furans and new insights into the reaction mechanism
Tetrahedron.
71(36):6183-6188
[DOI] 10.1016/j.tet.2015.06.090.
2015
Asymmetric synthesis of (S)- and (R)-norketamine via Sharpless asymmetric dihydroxylation/Ritter amination sequence
Tetrahedron Letters.
56(20):2608-2610
[DOI] 10.1016/j.tetlet.2015.04.050.
2015
Muscarinic acetylcholine receptor binding affinities of pethidine analogs
Bioorganic & Medicinal Chemistry Letters.
25(22):5032-5035
[DOI] 10.1016/j.bmcl.2015.10.029.
[PMID] 26494260.
2015
r-bPiDI, an α6β2* Nicotinic Receptor Antagonist, Decreases Nicotine-Evoked Dopamine Release and Nicotine Reinforcement
Neurochemical Research.
40(10):2121-2130
[DOI] 10.1007/s11064-015-1680-4.
[PMID] 26227997.
2015
Synthesis of Lobeline, Lobelane and their Analogues. A Review
Organic Preparations and Procedures International.
47(5):317-337
[DOI] 10.1080/00304948.2015.1066642.
[PMID] 26858465.
2015
Synthesis of O- and N-alkylated products of 1,2,3,4-tetrahydrobenzo[c][2,7]naphthyrin-5(6H)-one
Tetrahedron Letters.
56(46):6472-6474
[DOI] 10.1016/j.tetlet.2015.09.156.
[PMID] 26663991.
2014
A mild and efficient AgSbF6-catalyzed synthesis of fully substituted pyrroles through a sequential propargylation/amination/cycloisomerization reaction
Tetrahedron.
70(34):5267-5273
[DOI] 10.1016/j.tet.2014.05.073.
[PMID] 25061238.
2014
Molecular Dynamics Guided Design of Tocoflexol: A New Radioprotectant Tocotrienol with Enhanced Bioavailability
Drug Development Research.
75(1):10-22
[DOI] 10.1002/ddr.21162.
[PMID] 24648045.
2013
Amberlite IR-120H as an efficient and versatile solid phase catalyst for nucleophilic substitution of propargylic alcohols
Tetrahedron Letters.
54(27):3550-3553
[DOI] 10.1016/j.tetlet.2013.04.120.
2013
Effects of VMAT2 inhibitors lobeline and GZ-793A on methamphetamine-induced changes in dopamine release, metabolism and synthesis in vivo
Journal of Neurochemistry.
127(2):187-198
[DOI] 10.1111/jnc.12373.
[PMID] 23875705.
2013
Exploring the effect of N-substitution in nor-lobelane on the interaction with VMAT2: discovery of a potential clinical candidate for treatment of methamphetamine abuse
MedChemComm.
4(3)
[DOI] 10.1039/c3md20374c.
2013
GZ-793A, a lobelane analog, interacts with the vesicular monoamine transporter-2 to inhibit the effect of methamphetamine
Journal of Neurochemistry.
127(2):177-186
[DOI] 10.1111/jnc.12371.
[PMID] 23875622.
2013
Oral administration of GZ-793A, a VMAT2 inhibitor, decreases methamphetamine self-administration in rats
Pharmacology Biochemistry and Behavior.
112:29-33
[DOI] 10.1016/j.pbb.2013.09.006.
[PMID] 24075974.
2013
Structural Modifications to Tetrahydropyridine-3-carboxylate Esters en Route to the Discovery of M5-Preferring Muscarinic Receptor Orthosteric Antagonists
Journal of Medicinal Chemistry.
56(4):1693-1703
[DOI] 10.1021/jm301774u.
[PMID] 23379472.
2012
Microscopic Binding of M5 Muscarinic Acetylcholine Receptor with Antagonists by Homology Modeling, Molecular Docking, and Molecular Dynamics Simulation
The Journal of Physical Chemistry B.
116(1):532-541
[DOI] 10.1021/jp210579b.
[PMID] 22185605.
2012
The effect of a novel VMAT2 inhibitor, GZ-793A, on methamphetamine reward in rats
Psychopharmacology.
220(2):395-403
[DOI] 10.1007/s00213-011-2488-9.
[PMID] 21938414.
2012
The effect of VMAT2 inhibitor GZ-793A on the reinstatement of methamphetamine-seeking in rats
Psychopharmacology.
224(2):255-262
[DOI] 10.1007/s00213-012-2748-3.
[PMID] 22638813.
2011
(S)-1-(2-Chlorophenyl)-2-oxocyclohexan-1-aminiumD-tartrate
Acta Crystallographica Section E Structure Reports Online.
67(3):o736-o736
[DOI] 10.1107/s1600536811006131.
2011
Design, Synthesis and Interaction at the Vesicular Monoamine Transporter-2 of Lobeline Analogs: Potential Pharmacotherapies for the Treatment of Psychostimulant Abuse
Current Topics in Medicinal Chemistry.
11(9):1103-1127
[DOI] 10.2174/156802611795371332.
2011
Discovery of non-peptide, small molecule antagonists of α9α10 nicotinic acetylcholine receptors as novel analgesics for the treatment of neuropathic and tonic inflammatory pain
Bioorganic & Medicinal Chemistry Letters.
21(8):2476-2479
[DOI] 10.1016/j.bmcl.2011.02.043.
[PMID] 21397497.
2011
Novel bis-, tris-, and tetrakis-tertiary amino analogs as antagonists at neuronal nicotinic receptors that mediate nicotine-evoked dopamine release
Bioorganic & Medicinal Chemistry Letters.
21(1):88-91
[DOI] 10.1016/j.bmcl.2010.11.070.
[PMID] 21147530.
2011
Novel N-1,2-Dihydroxypropyl Analogs of Lobelane Inhibit Vesicular Monoamine Transporter-2 Function and Methamphetamine-Evoked Dopamine Release
Journal of Pharmacology and Experimental Therapeutics.
339(1):286-297
[DOI] 10.1124/jpet.111.184770.
[PMID] 21778282.
2011
Phenyl Ring-Substituted Lobelane Analogs: Inhibition of [3H]Dopamine Uptake at the Vesicular Monoamine Transporter-2
Journal of Pharmacology and Experimental Therapeutics.
336(3):724-733
[DOI] 10.1124/jpet.110.172882.
[PMID] 20876747.
2010
(2S,6S)-1-Methyl-2,6-trans-distyrylpiperidinium chloride
Acta Crystallographica Section E Structure Reports Online.
66(1):o78-o78
[DOI] 10.1107/s1600536809049587.
2010
1-Methyl-2,6-cis-distyrylpiperidine
Acta Crystallographica Section E Structure Reports Online.
66(1):o77-o77
[DOI] 10.1107/s1600536809049617.
2010
Bis-azaaromatic quaternary ammonium salts as ligands for the blood–brain barrier choline transporter
Bioorganic & Medicinal Chemistry Letters.
20(11):3208-3210
[DOI] 10.1016/j.bmcl.2010.04.098.
[PMID] 20462759.
2010
ChemInform Abstract: Absolute Configuration of Falcarinol, a Potent Antitumor Agent Commonly Occurring in Plants.
ChemInform.
30(25):no-no
[DOI] 10.1002/chin.199925224.
2010
ChemInform Abstract: First Total Synthesis of Optically Active Panaxydol, a Potential Antitumor Agent Isolated from Panax ginseng.
ChemInform.
30(12):no-no
[DOI] 10.1002/chin.199912252.
2010
Lobelane Inhibits Methamphetamine-Evoked Dopamine Release via Inhibition of the Vesicular Monoamine Transporter-2
Journal of Pharmacology and Experimental Therapeutics.
332(2):612-621
[DOI] 10.1124/jpet.109.160275.
[PMID] 19855096.
2010
Repeated nicotine administration robustly increases bPiDDB inhibitory potency at α6β2-containing nicotinic receptors mediating nicotine-evoked dopamine release
Biochemical Pharmacology.
80(3):402-409
[DOI] 10.1016/j.bcp.2010.03.018.
[PMID] 20346923.
2009
Computational neural network analysis of the affinity of N-n-alkylnicotinium salts for the α4β2* nicotinic acetylcholine receptor
Journal of Enzyme Inhibition and Medicinal Chemistry.
24(1):157-168
[DOI] 10.1080/14756360801945648.
[PMID] 18629679.
2009
Selective Inhibition of Acetylcholine-Evoked Responses of α7 Neuronal Nicotinic Acetylcholine Receptors by Novel tris- and tetrakis-Azaaromatic Quaternary Ammonium Antagonists
Molecular Pharmacology.
76(3):652-666
[DOI] 10.1124/mol.109.056176.
[PMID] 19556356.
2009
Stereocontrolled Synthesis and Pharmacological Evaluation ofcis-2,6-Diphenethyl-1-azabicyclo[2.2.2]octanes as Lobelane Analogues
The Journal of Organic Chemistry.
74(16):6072-6076
[DOI] 10.1021/jo901082r.
[PMID] 20560567.
2008
Extending the analysis of nicotinic receptor antagonists with the study of α6 nicotinic receptor subunit chimeras
Neuropharmacology.
54(8):1189-1200
[DOI] 10.1016/j.neuropharm.2008.03.010.
[PMID] 18448138.
2008
Synthesis and evaluation of a series of homologues of lobelane at the vesicular monoamine transporter-2
Bioorganic & Medicinal Chemistry Letters.
18(24):6509-6512
[DOI] 10.1016/j.bmcl.2008.10.042.
[PMID] 18976906.
2008
Tetrakis-azaaromatic quaternary ammonium salts: Novel subtype-selective antagonists at neuronal nicotinic receptors that mediate nicotine-evoked dopamine release
Bioorganic & Medicinal Chemistry Letters.
18(21):5753-5757
[DOI] 10.1016/j.bmcl.2008.09.084.
[PMID] 18851914.
2007
Bis-azaaromatic quaternary ammonium salts as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release: An investigation of binding conformation
Bioorganic & Medicinal Chemistry Letters.
17(24):6734-6738
[DOI] 10.1016/j.bmcl.2007.10.052.
[PMID] 18029180.
2007
Computational neural network analysis of the affinity of lobeline and tetrabenazine analogs for the vesicular monoamine transporter-2
Bioorganic & Medicinal Chemistry.
15(8):2975-2992
[DOI] 10.1016/j.bmc.2007.02.013.
[PMID] 17331733.
2007
Discovery of a novel nicotinic receptor antagonist for the treatment of nicotine addiction: 1-(3-Picolinium)-12-triethylammonium-dodecane dibromide (TMPD)
Biochemical Pharmacology.
74(8):1271-1282
[DOI] 10.1016/j.bcp.2007.07.021.
[PMID] 17727820.
2007
tris-Azaaromatic quaternary ammonium salts: Novel templates as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release
Bioorganic & Medicinal Chemistry Letters.
17(24):6701-6706
[DOI] 10.1016/j.bmcl.2007.10.062.
[PMID] 17977723.
2006
Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters
Bioorganic & Medicinal Chemistry Letters.
16(19):5018-5021
[DOI] 10.1016/j.bmcl.2006.07.070.
[PMID] 16905316.
2006
Vesicular monoamine transporter 2: Role as a novel target for drug development
The AAPS Journal.
8(4):E682-E692
[DOI] 10.1208/aapsj080478.
[PMID] 17233532.
2005
Defunctionalized Lobeline Analogues: Structure−Activity of Novel Ligands for the Vesicular Monoamine Transporter
Journal of Medicinal Chemistry.
48(17):5551-5560
[DOI] 10.1021/jm0501228.
[PMID] 16107155.
2005
Lobelane analogues as novel ligands for the vesicular monoamine transporter-2
Bioorganic & Medicinal Chemistry.
13(12):3899-3909
[DOI] 10.1016/j.bmc.2005.04.013.
[PMID] 15911306.
2005
Synthesis and evaluation of a series of tropane analogues as novel vesicular monoamine transporter-2 ligands
Bioorganic & Medicinal Chemistry Letters.
15(20):4463-4466
[DOI] 10.1016/j.bmcl.2005.07.032.
[PMID] 16112864.
2005
The characterization of a novel rigid nicotine analog with α7-selective nAChR agonist activity and modulation of agonist properties by boron inclusion
Bioorganic & Medicinal Chemistry Letters.
15(17):3874-3880
[DOI] 10.1016/j.bmcl.2005.05.118.
[PMID] 16005216.
2004
Indirect Trapping of the Retroconjugate Addition Reaction Intermediate Involved in the Epimerization of Lobeline: Application to the Synthesis of (−)-Sedamine
The Journal of Organic Chemistry.
69(24):8514-8517
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2004
Lobeline Analogs with Enhanced Affinity and Selectivity for Plasmalemma and Vesicular Monoamine Transporters
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The Preparation of 2‐Arylmethylidene‐8‐methyl‐8‐azabicyclo[3.2.1]octan‐3‐ones
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Two isomers of 2,4-dibenzyl-8-azabicyclo[3.2.1]octan-3-ol
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1999
Syntheses of two diastereoisomers of panaxytriol, a potent antitumor agent isolated from panax ginseng
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Syntheses of two enantiomers of eicos-(4E)-en-1-yn-3-ol, a bioactive component of the marine sponge Cribrochalina vasculum
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Grants
Aug 2024
ACTIVE
Hijacking Post-translational Arginylation for Targeted Protein Degradation
Role: Project Manager
Funding: WASHINGTON UNIV SAINT LOUIS
via NATL INST OF HLTH NCI
Jun 2024
– Jun 2024
Proteolysis targeting chimera against nuclear receptor NR4A1 for melanoma therapy
Role: Principal Investigator
Funding: FL DEPT OF HLTH BANKHEAD-COLEY CANCER RE
Apr 2024
ACTIVE
Proteolysis targeting chimera against nuclear receptor NR4A1 for melanoma therapy
Role: Principal Investigator
Funding: NATL INST OF HLTH NCI
Apr 2024
ACTIVE
UF Health Cancer Center Bridge Seed Grant (Continued)
Role: Project Manager
Funding: UF HEALTH SHANDS HOSPITAL
Dec 2023
ACTIVE
Development of Caspase Cleavage Targeting Chimeras (CACTACs) for Targeted Protein Cleavage
Role: Principal Investigator
Funding: UNIV OF TEXAS HLTH SCI CTR SAN ANTONIO
via NATL INST OF HLTH NCI
Jan 2023
ACTIVE
Exploring novel therapeutic strategies for combinatory therapy to treat renal clear cell carcinomas
Role: Co-Investigator
Funding: NATL INST OF HLTH NCI
Sep 2022
ACTIVE
Synthetic lethal targeting of EBV-positive diffuse large B cell lymphomas in persons living with HIV
Role: Project Manager
Funding: NATL INST OF HLTH NCI
Apr 2022
ACTIVE
Development of first-in-class HDAC3-selective degraders for breast cancer therapy
Role: Co-Project Director/Principal Investigator
Funding: FL DEPT OF HLTH BIOMED RES PGM/J&E KING
Apr 2022
– Jun 2022
The Role of Immune Microenvironment in Small Cell Lung Cancer
Role: Principal Investigator
Funding: FL DEPT OF HLTH BANKHEAD-COLEY CANCER RE
Apr 2021
ACTIVE
Proteolysis-targeting chimera against BCL-XL inhibits breast cancer metastasis
Role: Principal Investigator
Funding: NATL INST OF HLTH NCI
Apr 2021
– Dec 2023
Selecting a Drug Development Candidate for Cancer Treatment
Role: Principal Investigator
Funding: DIALECTIC THERAPEUTICS
Jan 2021
– Dec 2024
Developing a Novel PROTAC-Based NR4A1 Degrader for Breast Cancer Therapy
Role: Principal Investigator
Funding: US ARMY MED RES ACQUISITION
Dec 2020
– Nov 2021
Sanofi 2020 iAwards
Role: Co-Investigator
Funding: SANOFI
Sep 2020
– Aug 2022
Identifying Novel Senolytic Agents and Molecular Targets
Role: Principal Investigator
Funding: NATL INST OF HLTH NIA
Jun 2020
– May 2022
Intercollaborative Radiation Countermeasure (INTERACT) Consortium for Advanced Development of Medical Countermeasures to Mitigate/Treat Acute and Delayed Radiation Syndromes
Role: Co-Project Director/Principal 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
– Aug 2024
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
– May 2022
Role of Senescent Cells in Radiation-induced Pulmonary Fibrosis
Role: Co-Investigator
Funding: NATL INST OF HLTH NCI
Contact Details
Phones:
- Business:
- (352) 294-8953
Emails:
- Business:
- zhengg@ufl.edu
Addresses:
- Business Mailing:
-
PO Box 100485
GAINESVILLE FL 32610 - Business Street:
-
1333 CENTER DR
BSB BG-022C
GAINESVILLE FL 326112025