-transparent.png){kind=logo}
Telomerase inhibitors--oligonucleotide phosphoramidates as potential therapeutic agents. 2001
S Gryaznov, and
K Pongracz, and
T Matray, and
R Schultz, and
R Pruzan, and
J Aimi, and
A Chin, and
C Harley, and
B Shea-Herbert, and
J Shay, and
Y Oshima, and
A Asai, and
Y Yamashita
Geron Corporation, 230 Constitution Drive, Menlo Park, California 94025, USA.
We have designed, synthesized, and evaluated using physical, chemical and biochemical assays various oligonucleotide N3'-->P5' phosphoramidates, as potential telomerase inhibitors. Among the prepared compounds were 2'-deoxy, 2'-hydroxy, 2'-methoxy, 2'-ribo-fluoro, and 2'-arabino-fluoro oligonucleotide phosphoramidates, as well as novel N3'-->P5' thio-phosphoramidates. The compounds demonstrated sequence specific and dose dependent activity with IC50 values in the sub-nM to pM concentration range.
Related Publications
S Gryaznov, and
K Pongracz, and
T Matray, and
R Schultz, and
R Pruzan, and
J Aimi, and
A Chin, and
C Harley, and
B Shea-Herbert, and
J Shay, and
Y Oshima, and
A Asai, and
Y Yamashita
December 1999,
Biochimica et biophysica acta,
S Gryaznov, and
K Pongracz, and
T Matray, and
R Schultz, and
R Pruzan, and
J Aimi, and
A Chin, and
C Harley, and
B Shea-Herbert, and
J Shay, and
Y Oshima, and
A Asai, and
Y Yamashita
March 2010,
Chemistry & biodiversity,
S Gryaznov, and
K Pongracz, and
T Matray, and
R Schultz, and
R Pruzan, and
J Aimi, and
A Chin, and
C Harley, and
B Shea-Herbert, and
J Shay, and
Y Oshima, and
A Asai, and
Y Yamashita
April 1996,
Nucleic acids research,
S Gryaznov, and
K Pongracz, and
T Matray, and
R Schultz, and
R Pruzan, and
J Aimi, and
A Chin, and
C Harley, and
B Shea-Herbert, and
J Shay, and
Y Oshima, and
A Asai, and
Y Yamashita
January 2002,
Methods in molecular biology (Clifton, N.J.),
S Gryaznov, and
K Pongracz, and
T Matray, and
R Schultz, and
R Pruzan, and
J Aimi, and
A Chin, and
C Harley, and
B Shea-Herbert, and
J Shay, and
Y Oshima, and
A Asai, and
Y Yamashita
May 2008,
Journal of cellular biochemistry,
S Gryaznov, and
K Pongracz, and
T Matray, and
R Schultz, and
R Pruzan, and
J Aimi, and
A Chin, and
C Harley, and
B Shea-Herbert, and
J Shay, and
Y Oshima, and
A Asai, and
Y Yamashita
January 1987,
Journal of enzyme inhibition,
S Gryaznov, and
K Pongracz, and
T Matray, and
R Schultz, and
R Pruzan, and
J Aimi, and
A Chin, and
C Harley, and
B Shea-Herbert, and
J Shay, and
Y Oshima, and
A Asai, and
Y Yamashita
September 1991,
Annals of Saudi medicine,
S Gryaznov, and
K Pongracz, and
T Matray, and
R Schultz, and
R Pruzan, and
J Aimi, and
A Chin, and
C Harley, and
B Shea-Herbert, and
J Shay, and
Y Oshima, and
A Asai, and
Y Yamashita
June 1995,
Proceedings of the National Academy of Sciences of the United States of America,
S Gryaznov, and
K Pongracz, and
T Matray, and
R Schultz, and
R Pruzan, and
J Aimi, and
A Chin, and
C Harley, and
B Shea-Herbert, and
J Shay, and
Y Oshima, and
A Asai, and
Y Yamashita
September 1988,
Pharmaceutical research,
S Gryaznov, and
K Pongracz, and
T Matray, and
R Schultz, and
R Pruzan, and
J Aimi, and
A Chin, and
C Harley, and
B Shea-Herbert, and
J Shay, and
Y Oshima, and
A Asai, and
Y Yamashita
June 2006,
Mini reviews in medicinal chemistry,
