Dr. Lee, Te-Chang 's publons link picture

Dr. Lee, Te-Chang

Adjunct Research Fellow
  • 02-27899145 (Lab) (Room No: N247)
  • 02-26523055 (Office)
  • 02-27829142 (Fax)

  • Genetic and Molecular Toxicology
  • Cancer Biology
  • Pharmacology
  • Biobank

Education and Positions:
  • Ph.D. National Taiwan University

Highlight Detail

A Low-Toxicity DNA-Alkylating N-Mustard-Quinoline Conjugate with Preferential Sequence Specificity Exerts Potent Antitumor Activity Against Colorectal Cancer

Dr. Lee, Te-Chang
Neoplasia, Dec 13, 2017

Efficacy and safety are fundamental prerequisites for anticancer drug development. In the present study, we explored the anti–colorectal cancer (CRC) activity of SL-1, a DNA-directed N-mustard-quinoline conjugate. The N-mustard moiety in SL-1 induced DNA strand breaks, interstrand cross-links (ICLs), G2/M arrest, and apoptosis, whereas its quinoline moiety preferentially directed SL-1 to target the selective guanine sequence 5′-G-G/C-N-G-C/T-3′. Notably, SL-1 was highly cytotoxic to various CRC cell lines. Experiments using xenograft models revealed that SL-1 was more potent than 5-fluorouracil (5-FU) and oxaliplatin for suppressing the growth of RKO and RKO-E6 (oxaliplatin-resistant subline) cells as well as metastatic SW620 cells. In addition, SL-1 combined with 5-FU was more effective than oxaliplatin and 5-FU for suppressing RKO or SW620 cell growth in mice. Significantly, compared with cisplatin, oxaliplatin, or 5-FU, SL-1 alone or in combination with 5-FU did not cause obvious kidney or liver toxicity in ICR mice. In summary, SL-1, a DNA-directed alkylating agent, is established as an anti-CRC agent with high efficacy and low toxicity and thus warrants further development for the treatment of CRC patients.