Drug Design

Functionally Selective Ligands for 7TM Receptors

Chemical Biology of Epigenetics

Small Molecule Cancer Therapy 

Jian is currently serving as an Associate Director of Medicinal Chemistry in the newly established Center for Integrative Chemical Biology & Drug Discovery, and a Research Associate Professor in the Division of Medicinal Chemistry & Natural Products in the Eshelman School of Pharmacy at The University of North Carolina at Chapel Hill (UNC – CH).  Prior to joining UNC - CH in August 2008, Jian had worked for GlaxoSmithKline (GSK and formerly SmithKline Beecham) as a medicinal chemist for over 10 years with extensive experience in multiple therapeutic areas and target classes, and expertise in the 7TM receptor (as known as GPCR) target class and 7TM system chemistry – he had led the U.S. 7TM system chemistry in GSK from 2001 to 2006.  Jian had led numerous multi-disciplinal drug discovery programs that successfully delivered high quality leads and pre-candidates that led to five clinical candidates.  Jian had been a research manager and team leader in Discovery Medicinal Chemistry and a manager of Medicinal Chemistry in the Cardiovascular and Urogenital Center of Excellence for Drug Discovery for five years (2003 – 2008).  In addition to leading drug discovery programs and managing a group of 5 – 10 medicinal chemists, he has managed research collaborations and chemistry outsourcing with a number of research institutes and contract research organizations from 2000 to 2008.  Jian has also been an Advisory Professor of Jilin University, Changchun, China since October 2005.         

Jian received a B.S. degree in chemistry from University of Science and Technology of China in 1991 and a Ph.D. degree in synthetic organic chemistry from the Pennsylvania State University in 1997 after completing enantioselective total syntheses of (-)-coccinine, (-)-montanine and (-)-pancracine.  He then completed a one-year post-doctoral training at the Ohio State University prior to joining GSK.  Jian has authored or co-authored 34 peer reviewed papers in leading scientific journals, has been an inventor or co-inventor of 38 issued patents and patent applications, and has presented a number of invited talks.

2008 Publications:

Jin, J.*; Wang, Y.; Shi, D.; Wang, F.; Davis, R. S.; Jin, Q.; Fu, W.; Foley, J. J.; Webb, E. F.; Dehaas, C. J.; Berlanga, M.; Burman, M.; Sarau, H. M.; Morrow, D. M.; Rao, P.; Kallal, L. A.; Moore, M. L; Rivero, R. A.; Palovich, M.; Salmon, M.; Belmonte, K. E.; Busch-Petersen, J.* “Discovery of Novel and Long Acting Muscarinic Acetylcholine Receptor Antagonists” J. Med. Chem. 2008, 51, 4866-4869.

Jin, J.*; Budzik, B. W.; Wang, Y.; Shi, D.; Wang, F.; Xie, H.; Wan, Z.; Zhu, C.; Foley, J. J.; Webb, E. F.; Berlanga, M.; Burman, M.; Sarau, H. M.; Morrow, D. M.; Moore, M. L; Rivero, R. A.; Palovich, M.; Salmon, M.; Belmonte, K. E.; Laine, D. I.* “Discovery of Bi-phenyl Piperazines as Novel and Long Acting Muscarinic Acetylcholine Receptor Antagonists” J. Med. Chem. 2008, 51, 5915-5918.

Jin, J.*; Wang, Y.; Wang, F.; Shi, D.; Erhard, K. F.; Wu, Z.; Guida, B. F.; Lawrence, S. K.; Behm, D. J.; Disa, J.; Vaidya, K. S.; Evans, C.; McMillan, L. J.; Rivero, R. A.; Neeb, M. J.; Douglas, S. A. “2-Aminomethyl Piperidines as Novel Urotensin-II Receptor Antagonists” Bioorg. Med. Chem. Lett. 2008, 18, 2860-2864.

McAtee, J. J.*; Dodson, J. W.; Dowdell, S. E.; Erhard, K. F.; Girard, G. R.; Goodman, K. B.; Hilfiker, M. A.; Jin, J.; Sehon, C. A.; Sha, D.; Shi, D.; Wang, F.; Wang, G. Z.; Wang, N.; Wang, Y.; Viet, A. Q.; Yuan, C. K.; Zhang, D.; Aiyar, N. V.; Behm, D. J.; Carballo, L. H.; Evans, C.; Fries, H. E.; Nagilla, R.; Roethke, T. J.; Xu, X.; Douglas, S. A.; Neeb, M. J. “Potent and Selective Small-Molecule Human Urotensin-II Antagonists with Improved Pharmacokinetic Profiles” Bioorg. Med. Chem. Lett. 2008, 18, 3716-3719.

Jin, J.*; An, M.; Sapienza, A.; Aiyar, N. V.; Naselsky, D.; Sarau, H. M.; Foley, J. J.; Salyers, K. L.; Knight, S. D.; Keenan, R. M.; Rivero, R. A.; Dhanak, D.; Douglas, S. A. “Urotensin-II Receptor Antagonists: Synthesis and SAR of N-cyclic Azaalkyl Benzamides” Bioorg. Med. Chem. Lett. 2008, 18, 3950-3954.

Wang, Y.*; Wu, Z.; Guida, B. F.; Lawrence, S. K.; Neeb, M. J.; Rivero, R. A.; Douglas, S. A.; Jin, J.*  “N-Alkyl-5H-pyrido[4,3-b]indol-1-amines and Derivatives as Novel Urotensin-II Receptor Antagonists” Bioorg. Med. Chem. Lett. 2008, 18, 4936-4939.

Su, X.*; Leon, L. A.; Wu, C. W.; Morrow, D. M.; Jaworski, J. P.; Heibler, J. P.; Lashinger, E. S. R.; Jin, J.; Edwards, R. M.; Laping, N. J. “Modulation of Bladder Function by Prostaglandin EP3 Receptors In the Central Nervous System” Am. J. Physiology – Renal Physiology 2008, 295, F984-F994.

Jin, J.*; Wang, Y.*; Shi, D.; Wang, F.; Fu, W.; Davis, R. S.; Jin, Q.; Foley, J. J.; Sarau, H. M.; Morrow, D. M.; Moore, M. L; Rivero, R. A.; Palovich, M.; Salmon, M.; Belmonte, K. E.; Busch-Petersen, J. “Muscarinic Acetylcholine Receptor Antagonists: SAR and Optimization of Tyrosine Ureas” Bioorg. Med. Chem. Lett. 2008, 18, 5481-5486.