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KH Lee, PhD, is a UNC Lineberger Comprehensive Cancer Center member, Director of Natural Products Research Laboratories
and Kenan Distinguished Professor at UNC-Chapel Hill Eshelman School of Pharmacy.

School of Pharmacy
UNC-Chapel Hill
Molecular Therapeutics

Area of interest

Dr. K. H. Lee’s research has a substantial focus on investigation of novel plant cytotoxic antitumor principles, including those from traditional Chinese medicines (TCM), and their synthetic analogs as potential anticancer clinical trial candidates. This work has resulted in the discovery and development of numerous promising novel natural products and synthetic analogs as new anticancer drug candidates over the past 40 years. Research methodology involves a combination of (a) bioactivity-directed fractionation and isolation (BDFI) along with structural characterization of active principles from prioritized plant extracts, which show interesting and significant cytotoxicity against human tumor cell line panels and in supplemental bioassays, and (b) structural modification and synthesis of analogs of selected new active leads, in order to elucidate their structure-activity relationships (SAR) and mechanism of action (MOA), as well as to improve their pharmacological profiles as potential anticancer drugs. The scientific disciplines covered include natural products chemistry, molecular biology and biochemistry, pharmacology, and Chinese medicine, to discover promising new leads based on bioactivity- or MOA-directed approaches; medicinal chemistry and synthetic organic chemistry to achieve new leads optimization based on modern medicinal chemistry approaches; and analytical chemistry to apply state-of-the-art analytical instrumental chromatography technologies to support the above two tasks. MOA and in vivo evaluation studies are supported by collaborations with more than 60 active established researchers worldwide to enhance the programs of the NPRL. The quality and importance of Dr. Lee’s research are evidenced by over 295 publications entitled “Antitumor Agents” (see ref. 1), and briefly detailed in his recent review article “Antitumor Agents 275 and Anti-AIDS Agents 80. Discovery and Development of Natural Product-derived Chemotherapeutic Agents Based on a Medicinal Chemistry Approach, ” J. Nat. Prod., 73, 500-516 (2010) and literature cited therein, which was based on a talk given when Dr. Lee was presented with the 2009 Norman R. Farnsworth Research Achievement Award from the American Society of Pharmacognosy. Dr. Lee has been funded by NIH Grant CA-17625 entitled “Plant Antitumor Agents” for over 32 years. The isolated compounds and synthetic analogs come from many diverse chemical classes and have wide ranging novel structures with significant in vitro and in vivo anticancer activities and/or MOA. Table 1 highlights some of the current plant-derived modified analogs coming out of the NPRL, which are in clinical use, clinical trials, or preclinical studies as anticancer drugs. Notably, GL-331, an etoposide analog, progressed to anticancer Phase II clinical trials, and JC-9, a curcumin analog, has just successfully completed the Phase II clinical trials for treating acne and is in development for trials against prostate cancer. Many other compounds are currently under intensive preclinical evaluation.

Awards and Honors

1999 Outstanding Achievement Award, University of Minnesota at Minneapolis
2003 Taiwanese-American Foundation Achievement Award in Science & Engineering, USA
2005 Kitasato Microbial Chemistry Medal, Japan
2008 UNC Eshelman School of Pharmacy Established K.H. Lee Distinguished Professorship
2009 Norman R. Farnsworth Research Achievement Award from American Society of Pharmacognosy
2010 Fellow of the American Society of Pharmacognosy
2010 Chair Professor & Honorary Director, Chinese Medicine Research & Development Center, China Medical University & Hospital, Taiwan
2011 Chair Professor, College of Pharmacy, Kaohsiung Medical University, Taiwan
2011 Order of the Rising Sun, Gold Rays with Neck Ribbon, Government of Japan

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