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Medicinal Chemistry

Introduction of group leader

Kaapjoo Park, Ph.D.
Doctorate: Brown University, USA (1997)
Post-Doctorate: Texas A&M University, USA (1997-1998)
Research Scientist, Duke University, USA (1998-2001)
Project Leader, Pfizer Inc. USA (2001-2010)
Director, Yuhan Corp. S. Korea (2010-2015)
Instructor, Kyunghee University, S. Korea (2015)
CTO, Natural F&P (2016)
Hankuk University of Foreign Studies, S. Korea, Instructor (2016-2017)
Director, IPK Business Development & Medicinal Chemistry (2017-present)

Office phone: +82-31-8018-8009
Email: kaapjoo.park at ip-korea.org
Office location: R5.03

Research Interests

The Medicinal Chemistry group focuses on the optimization of compounds, which are identified through primary screening as being effective against target diseases. The optimization process is a multidisciplinary task to improve potential of becoming a new drug by optimizing biological activity, selectivity, physicochemical properties, in vivo properties and safety. Within the context of cell-based assays, optimization to create drug candidates is accelerated by eliminating unsatisfactory compounds, which have low cell permeability, as well as cytotoxicity, while evaluating biological activity. Additionally, integration of evaluating in vivo properties and toxicity make our drug discovery process faster and more efficient. Thereby qualified advanced molecules or preclinical candidates are created through lead optimization and our ample experience and creativity leads to successful research results.
Currently, we have entered into R&D agreement with Korea Drug Development Fund (KDDF) for ‘Discovery of novel anti-tubercular agent for the treatment of multidrug-resistant/extensively drug-resistant tuberculosis’, and have received funding for research and treatment from KDDF for 18 months.
IPK has established the PROTAC project as a new platform technology for developing new medicines. PROTAC is a new technology in the development of new medicines, which is a spotlighted as a molecule that degrades proteins, and it is been applied to areas such as anti-cancer.
The Medicinal Chemistry group’s area of expertise lies in diseases like tuberculosis, cancer, hepatitis C, influenza, antibiotics etc.

Our areas of activity include:

• Advancing and accelerating the optimization on drug discovery program
• Developing novel chemical platform technology for innovative drug discovery
• Developing probe molecules for identifying target and understanding the in vivo mechanism of drug candidates
• Developing tool compounds for monitoring drug localization in either the cell or living animal
• Providing open-analysis service and support to academia and pharmaceutical companies through collaboration as well as giving access to IPK’s well-equipped infrastructure
 

Recent Publications

Compound 19e, a Novel Glucokinase Activator, Protects against Cytokine-Induced Beta-Cell Apoptosis in INS-1 Cells.
Oh YS, Seo E, Park K, Jun HS
Front Pharmacol. 2017 Mar 29;8:169

Design and Synthesis of Acetylenyl Benzamide Derivatives as Novel Glucokinase Activators for the Treatment of T2DM.
Park K, Lee BM, Hyun KH, Han T, Lee DH, Choi HH
ACS Med Chem Lett. 2015 Jan 14;6(3):296-301

Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H-pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus.
Park K, Lee BM, Hyun KH, Lee DH, Choi HH, Kim H, Chong W, Kim KB, Nam SY
Bioorg Med Chem. 2014 Apr 1;22(7):2280-93

Synthesis and structure-activity relationships of novel fused ring analogues of Q203 as antitubercular agents
Kang S, Kim YM, Jeon H, Park S, Seo MJ, Lee S, Park D, Nam J, Lee S, Nam K, Kim S, Kim J
Eur J Med Chem. 2017 Aug 18;136:420-427

Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis
Pethe K, Bifani P, Jang J, Kang S, Park S, Ahn S, Jiricek J, Jung J, Jeon HK, Cechetto J, Christophe T, Lee H, Kempf M, Jackson M, Lenaerts AJ, Pham H, Jones V, Seo MJ, Kim YM, Seo M, Seo JJ, Park D, Ko Y, Choi I, Kim R, Kim SY, Lim S, Yim SA, Nam J, Kang H, Kwon H, Oh CT, Cho Y, Jang Y, Kim J, Chua A, Tan BH, Nanjundappa MB, Rao SP, Barnes WS, Wintjens R, Walker JR, Alonso S, Lee S, Kim J, Oh S, Oh T, Nehrbass U, Han SJ, No Z, Lee J, Brodin P, Cho SN, Nam K, Kim J
Nat Med. 2013 Sep;19(9):1157-60