Jianyong Chen, Ph.D.
I was trained as an organic chemist and in medicinal chemistry. My major research interest is the design, synthesis, discovery and development of novel small-molecule inhibitors for the treatment of human cancer and other diseases. I have been working in Professor Shaomeng Wang’s laboratory in the Molecular Therapeutics Program at the University of Michigan Comprehensive Cancer Center since 2001. Through my research, I have collaborated extensively with computational chemists, biochemists, structural biologists, cell biologists and pharmacologists and have accumulated extensive research expertise in the design and discovery of novel small-molecule drugs. One of my small-molecule inhibitors I have discovered at the University of Michigan is now in Phase II clinical trials for the treatment of human cancer and additional compounds are in advanced preclinical development. I have served as co-investigators on several NIH R01 grants.
- Design, synthesis and biological evaluation of dopamine 3 agonists, partial agonists, and antagonists for the treatment of a variety of conditions, including drug abuse, restless legs syndrome, schizophrenia, and Parkinson’s disease.
- Design, synthesis and biological evaluation of STAT3 inhibitors for the treatment of cancers.
Education and Training
|1989||B.Sc., Medicinal Chemistry, China Pharmaceutical University, China|
|1992||M.Sc., Medicinal Chemistry, China Pharmaceutical University|
|1999||Ph.D., Organic Chemistry, Shanghai Institute of Materia Medica, China|
|1999-2001||Postdoctoral Research Fellow, Kyoto University, Japan|
|2001-2006||Postdoctoral Research Fellow, University of Michigan, Ann Arbor, MI|
Shangary S, Qin D, McEachern D, Liu M, Miller RS, Qiu S, Nikolovska-Coleska Z, Ding K, Wang G, Chen J, Bernard D, Zhang J, Lu Y, Gu Q, Shah RB, Pienta KJ, Ling X, Kang S, Guo M, Sun Y, Yang D, Wang S. Temporal activation of p53 by a specific MDM2 inhibitor is selectively toxic to tumors and leads to complete tumor growth inhibition. Proc Natl Acad Sci U S A, 2008 Mar 11; 105(10):3933-3938. (PMID 18316739) PMC 2268798.
Arnold AA, Aboukameel A, Chen J, Yang D, Wang S, Al-Katib A, Mohammad RM. Preclinical studies of Apogossypolone: a new nonpeptidic pan small-molecule inhibitor of Bcl-2, Bcl-XL and Mcl-1 proteins in Follicular Small Cleaved Cell Lymphoma model. Mol Cancer, 2008; 7:20. (PMID 18275607) PMC 2265299
Azmi AS, Wang Z, Burikhanov R, Rangnekar VM, Wang G, Chen J, Wang S, Sarkar FH, Mohammad RM. Critical role of prostate apoptosis response-4 in determining the sensitivity of pancreatic cancer cells to small-molecule inhibitor-induced apoptosis. Mol Cancer Ther, 2008 Sep; 7(9):2884-2893. (PMID 18790769).
Sun Y, Wu J, Aboukameel A, Banerjee S, Arnold AA, Chen J, Nikolovska-Coleska Z, Lin Y, Ling X, Yang D, Wang S, Al-Katib A, Mohammad RM. Apogossypolone, a nonpeptidic small molecule inhibitor targeting Bcl-2 family proteins, effectively inhibits growth of diffuse large cell lymphoma cells in vitro and in vivo. Cancer Biol Ther, 2008 Sep; 7(9):1418-1426. (PMID 18769131).
Chen J, Collins GT, Zhang J, Yang CY, Levant B, Woods J, Wang S. Design, synthesis, and evaluation of potent and selective ligands for the dopamine 3 (D3) receptor with a novel in vivo behavioral profile. J Med Chem, 2008 Oct 9; 51(19):5905-5908. (PMID 18785726) PMC 2662387.
Gomez C, Bai L, Zhang J, Nikolovska-Coleska Z, Chen J, Yi H, Wang S. Design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as STAT3 inhibitors. Bioorg Med Chem Lett, 2009 Mar 15; 19(6):1733-1736. (PMID 19243938).
Collins GT, Truccone A, Haji-Abdi F, Newman AH, Grundt P, Rice KC, Husbands SM, Greedy BM, Enguehard-Gueiffier C, Gueiffier A, Chen J, Wang S, Katz JL, Grandy DK, Sunahara RK, Woods JH. Proerectile effects of dopamine D2-like agonists are mediated by the D3 receptor in rats and mice. J Pharmacol Exp Ther, 2009 Apr; 329(1):210-217. (PMID 19136638) PMC 2670592.
Gomez C, Chen J, Wang S. Efficient synthesis of phosphotyrosine building blocks using imidazolium trifluoroacetate. Tetrahedron Letters, 2009; 50(48):6691-6692.
Yang CY, Sun H, Chen J, Nikolovska-Coleska Z, Wang S. Importance of ligand reorganization free energy in protein-ligand binding-affinity prediction. J Am Chem Soc, 2009 Sep 30; 131(38):13709-13721. (PMID 19736924) PMC 2773700.
Yu S, Qin D, Shangary S, Chen J, Wang G, Ding K, McEachern D, Qiu S, Nikolovska-Coleska Z, Miller R, Kang S, Yang D, Wang S. Potent and orally active small-molecule inhibitors of the MDM2-p53 interaction. J Med Chem, 2009 Dec 24; 52(24):7970-7973. (PMID 19928922) PMC 2795799.
Chen J, Bai L, Bernard D, Nikolovska-Coleska Z, Gomez C, Zhang J, Yi H, Wang S. Structure-Based Design of Conformationally Constrained, Cell-Permeable STAT3 Inhibitors. ACS Med Chem Lett, 2010 May 13; 1(2):85-89. (PMID 20596242) PMC 2892918.