Qi-Yin Chen

Qi-Yin Chen, Ph.D.

Research Associate Professor

Department: Medicinal Chemistry
Business Phone: (352) 273-7739
Business Email: chenqyufl@ufl.edu

About Qi-Yin Chen

Qi-Yin Chen, Ph.D., serves as a research associate professor in Dr. Hendrik Luesch’s group in the department of Medicinal Chemistry. During his postdocs, he worked on the synthesis of bioprobes (natural product based), total synthesis of natural products, methodology of organic synthesis and the synthesis of pharmaceutical molecules. In 2008, he joined Dr. Luesch’s group where his research includes total synthesis and modification of (marine) natural products and the synthesis of pharmaceutical molecules.

Accomplishments

Research Service Incentive Award
2020 · College of Pharmacy University of Florida
Innovator Award
2016 · University of Florida
"Hai Yang Hua Gong” Prize
2004 · Institute of Chemistry, Chinese Academy of Sciences
“Head of Institute of Chemistry” Scholarship
2004 · Institute of Chemistry, Chinese Academy of Sciences

Research Profile

Total synthesis of natural products, synthesis of pharmaceutical compounds, synthesis of bioprobes, drug discovery and development.

Areas of Interest
  • Synthetic organic chemistry
Open Researcher and Contributor ID (ORCID)

0000-0002-4364-1057

Publications

2024
VCP/p97 mediates nuclear targeting of non-ER-imported prion protein to maintain proteostasis
Life Science Alliance. 7(6) [DOI] 10.26508/lsa.202302456. [PMID] 38570188.
2023
Heterologous Production of the C33–C45 Polyketide Fragment of Anticancer Apratoxins in a Cyanobacterial Host
Organic Letters. 25(13):2238-2242 [DOI] 10.1021/acs.orglett.3c00462. [PMID] 36961224.
2023
Nuclear quality control of non-imported secretory proteins attenuates proteostasis decline in the cytosol
BioRxiv. [DOI] 10.1101/2023.06.27.546668.
2023
Probing a distinct druggable tubulin binding site with gatorbulins 1–7, their metabolic and physicochemical properties, and pharmacological consequences
Bioorganic & Medicinal Chemistry. 95 [DOI] 10.1016/j.bmc.2023.117506.
2022
Discovery, Synthesis, and Biological Evaluation of Anaenamides C and D from a New Marine Cyanobacterium, Hormoscilla sp.
Journal of natural products. 85(3):581-589 [DOI] 10.1021/acs.jnatprod.1c01073. [PMID] 35167289.
2022
Sec61 Inhibitor Apratoxin S4 Potently Inhibits SARS-CoV-2 and Exhibits Broad-Spectrum Antiviral Activity.
ACS infectious diseases. 8(7):1265-1279 [DOI] 10.1021/acsinfecdis.2c00008. [PMID] 35766385.
2021
Bifunctional Doscadenamides Activate Quorum Sensing in Gram-Negative Bacteria and Synergize with TRAIL to Induce Apoptosis in Cancer Cells.
Journal of natural products. 84(3):779-789 [DOI] 10.1021/acs.jnatprod.0c01003. [PMID] 33480689.
2021
Gatorbulin-1, a distinct cyclodepsipeptide chemotype, targets a seventh tubulin pharmacological site.
Proceedings of the National Academy of Sciences of the United States of America. 118(9) [DOI] 10.1073/pnas.2021847118. [PMID] 33619102.
2021
Inhibition of cotranslational translocation by apratoxin S4: Effects on oncogenic receptor tyrosine kinases and the fate of transmembrane proteins produced in the cytoplasm.
Current research in pharmacology and drug discovery. 2 [DOI] 10.1016/j.crphar.2021.100053. [PMID] 34909679.
2021
Largazole Inhibits Ocular Angiogenesis by Modulating the Expression of VEGFR2 and p21.
Marine drugs. 19(8) [DOI] 10.3390/md19080471. [PMID] 34436310.
2020
Ahp-Cyclodepsipeptides as tunable inhibitors of human neutrophil elastase and kallikrein 7: Total synthesis of tutuilamide A, serine protease selectivity profile and comparison with lyngbyastatin 7.
Bioorganic & medicinal chemistry. 28(23) [DOI] 10.1016/j.bmc.2020.115756. [PMID] 33002682.
2020
Discovery, Total Synthesis, and SAR of Anaenamides A and B: Anticancer Cyanobacterial Depsipeptides with a Chlorinated Pharmacophore.
Organic letters. 22(11):4235-4239 [DOI] 10.1021/acs.orglett.0c01281. [PMID] 32418432.
2020
Largazole is a Brain-Penetrant Class I HDAC Inhibitor with Extended Applicability to Glioblastoma and CNS Diseases.
ACS chemical neuroscience. 11(13):1937-1943 [DOI] 10.1021/acschemneuro.0c00093. [PMID] 32559056.
2020
Seaweed natural products modify the host inflammatory response via Nrf2 signaling and alter colon microbiota composition and gene expression.
Free radical biology & medicine. 146:306-323 [DOI] 10.1016/j.freeradbiomed.2019.09.013. [PMID] 31536771.
2019
Apratoxin S4 Inspired by a Marine Natural Product, a New Treatment Option for Ocular Angiogenic Diseases.
Investigative ophthalmology & visual science. 60(8):3254-3263 [DOI] 10.1167/iovs.19-26936. [PMID] 31361305.
2019
Development of apratoxin S10 (Apra S10) as an anti-pancreatic cancer agent and its preliminary evaluation in an orthotopic patient-derived xenograft (PDX) model.
Investigational new drugs. 37(2):364-374 [DOI] 10.1007/s10637-018-0647-0. [PMID] 30073464.
2019
Discovery and Total Synthesis of Doscadenamide A: A Quorum Sensing Signaling Molecule from a Marine Cyanobacterium.
Organic letters. 21(18):7274-7278 [DOI] 10.1021/acs.orglett.9b02525. [PMID] 31414826.
2018
Apratyramide, a Marine-Derived Peptidic Stimulator of VEGF-A and Other Growth Factors with Potential Application in Wound Healing.
ACS chemical biology. 13(1):91-99 [DOI] 10.1021/acschembio.7b00827. [PMID] 29205032.
2018
Discovery of new A- and B-type laxaphycins with synergistic anticancer activity.
Bioorganic & medicinal chemistry. 26(9):2310-2319 [DOI] 10.1016/j.bmc.2018.03.022. [PMID] 29606488.
2018
Process Development and Scale-up Total Synthesis of Largazole, a Potent Class I Histone Deacetylase Inhibitor
Organic Process Research & Development. 22(2):190-199 [DOI] 10.1021/acs.oprd.7b00352.
2017
Apratoxin S10, a Dual Inhibitor of Angiogenesis and Cancer Cell Growth To Treat Highly Vascularized Tumors.
ACS medicinal chemistry letters. 8(10):1007-1012 [DOI] 10.1021/acsmedchemlett.7b00192. [PMID] 29057042.
2016
Total Synthesis and Biological Evaluation of Apratoxin E and Its C30 Epimer: Configurational Reassignment of the Natural Product.
Organic letters. 18(20):5400-5403 [DOI] 10.1021/acs.orglett.6b02780. [PMID] 27723359.
2016
Total Synthesis of the Potent Marine-Derived Elastase Inhibitor Lyngbyastatin 7 and in Vitro Biological Evaluation in Model Systems for Pulmonary Diseases.
The Journal of organic chemistry. 81(2):532-44 [DOI] 10.1021/acs.joc.5b02386. [PMID] 26709602.
2014
Evaluation of class I HDAC isoform selectivity of largazole analogues.
Bioorganic & medicinal chemistry letters. 24(16):3728-31 [DOI] 10.1016/j.bmcl.2014.07.006. [PMID] 25070421.
2014
Improved total synthesis and biological evaluation of potent apratoxin S4 based anticancer agents with differential stability and further enhanced activity.
Journal of medicinal chemistry. 57(7):3011-29 [DOI] 10.1021/jm4019965. [PMID] 24660812.
2014
Largazole pharmacokinetics in rats by LC-MS/MS.
Marine drugs. 12(3):1623-40 [DOI] 10.3390/md12031623. [PMID] 24658499.
2014
Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties.
ACS medicinal chemistry letters. 5(8):905-10 [DOI] 10.1021/ml500170r. [PMID] 25147612.
2011
Systematic Chemical Mutagenesis Identifies a Potent Novel Apratoxin A/E Hybrid with Improved in Vivo Antitumor Activity.
ACS medicinal chemistry letters. 2(11):861-865 [PMID] 22081789.
2009
Convenient and efficient preparations of azodye-labeled peptides.
Chemical biology & drug design. 73(6):611-7 [DOI] 10.1111/j.1747-0285.2009.00813.x. [PMID] 19635052.
2009
Design, synthesis, and structure-activity relationship of a novel series of 2-aryl 5-(4-oxo-3-phenethyl-2-thioxothiazolidinylidenemethyl)furans as HIV-1 entry inhibitors.
Journal of medicinal chemistry. 52(23):7631-9 [DOI] 10.1021/jm900450n. [PMID] 19746983.
2008
Convenient preparations of azo-dye labeled amino acids and amines.
Organic & biomolecular chemistry. 6(13):2400-4 [DOI] 10.1039/b802846j. [PMID] 18563275.
2008
Direct asymmetric alpha-amination of cyclic ketones catalyzed by siloxyproline.
Chemistry, an Asian journal. 3(2):225-32 [DOI] 10.1002/asia.200700307. [PMID] 18165948.
2006
Azocalix[4]arene-based chromogenic anion probes
New Journal of Chemistry. 30(2) [DOI] 10.1039/b513355f.
2005
A Highly Selective Fluorescent Chemosensor for H2PO4- Based on a Calix[4]arene Tetraamide Derivative
European Journal of Organic Chemistry. 2005(12):2468-2472 [DOI] 10.1002/ejoc.200400832.
2005
A new Hg2+-selective fluorescent sensor based on a dansyl amide-armed calix[4]-aza-crown
Tetrahedron Letters. 46(1):165-168 [DOI] 10.1016/j.tetlet.2004.10.169.
2004
A new fluorescent as well as chromogenic chemosensor for anions based on an anthracene carbamate derivative
Tetrahedron Letters. 45(34):6493-6496 [DOI] 10.1016/j.tetlet.2004.06.135.
2004
A tetra-sulfonamide derivative bearing two dansyl groups designed as a new fluoride selective fluorescent chemosensor
Tetrahedron Letters. 45(20):3957-3960 [DOI] 10.1016/j.tetlet.2004.03.108.
2003
A New Convenient Synthesis of Alkoxyanthracenes from Alkoxy-9,10-anthraquinones
Synthesis. (16):2464-2466 [DOI] 10.1055/s-2003-42408.

Grants

Dec 2015 – Mar 2017
Synthesis of Largazole
Role: Principal Investigator
Funding: OCEANYX PHARMACEUTICALS

Education

Ph.D.
2005 · Chinese Academy of Science Institute of Chemistry
M.S.
2000 · Central South University of Technology
B.S.
1997 · Henan Normal University

Contact Details

Phones:
Business:
(352) 273-7739
Emails:
Business:
chenqyufl@ufl.edu
Addresses:
Business Mailing:
Po Box 100485
GAINESVILLE FL 32610
Business Street:
MSB P5-26A
1345 Center Drive
GAINESVILLE FL 326110001