A novel pyrazolone, 4,4-dichloro-1-(2,4-dichlorophenyl)-3-methyl-5-pyrazolone, as a potent catalytic inhibitor of human telomerase

  • Kakiuchi Y
  • Sasaki N
  • Satoh-Masuoka M
 et al. 
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A new derivative of 1-phenyl-3-methyl-5-pyrazol one,
4,4-dichloro-1-(2,4-dichlorophenyl)-3-methyl-5-pyrazolone, named TELIN.
was chemically synthesized and identified as a potent inhibitor of human
telomerase in the cell-free telomeric repeat amplification protocol.
TELIN inhibited telomerase activity at submicromolar level with IC50 of
similar to0.3 muM. Kinetic studies revealed that TELIN does not bind to
DNA but to telomerase protein, and the mode of inhibition by this
substance was competitive-noncompetitive mixed-type with respect to the
TS primer, whereas it was uncompetitive or noncompetitive-uncompetitive
mixed-type with respect to the three deoxyribonucleosides. These results
demonstrate that TELIN is a specific potent catalytic blocker of
telomerase, and is considered to be a valuable substance for medical
treatment of cancer and related diseases. (C) 2004 Elsevier Inc. All
rights reserved.

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  • Yasutaka Kakiuchi

  • Narie Sasaki

  • Mieko Satoh-Masuoka

  • Hiromu Murofushi

  • Kimiko Murakami-Murofushi

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