Inhibition of telomerase by BIBR 1532 and related analogues.
BIBR 1532 has been reported to be a potent, small molecule inhibitor of human telomerase, suggesting it as a lead for the development of anti-telomerase therapy. We confirm the ability of BIBR 1532 to inhibit telomerase and report the discovery of an equally potent analogue. Importantly, IC(50) values in cell extract are considerably higher than those previously reported using assays for purified enzyme, indicating that substantial improvement may be necessary.
Barma
D K
DK
Department of Pharmacology, University of Texas Southwestern Medical Center at Dallas, 75390-9041, USA.
Elayadi
Anissa
A
Falck
J R
JR
Corey
David R
DR
D062365:Aminobenzoates; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D005784:Gene Amplification; D006367:HeLa Cells; D006801:Humans; D007202:Indicators and Reagents; D009281:Naphthalenes; D013329:Structure-Activity Relationship; D019098:Telomerase / Q000037:antagonists & inhibitors* / Q000235:genetics
D062365:Aminobenzoates; C458523:BIBR 1532; D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D009281:Naphthalenes; D019098:Telomerase