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Table 1 Summary of results

From: Inhibition of HIV-1 replication by P-TEFb inhibitors DRB, seliciclib and flavopiridol correlates with release of free P-TEFb from the large, inactive form of the complex

Assay

DRB (μM)

Seliciclib (μM)

Flavopiridol (nM)

IC50 of kinase inhibition:

0.9*

2.7

22

IC50 of loss of large form from HeLa cells:

   

Cyclin T1

5 +/- 3

2.7 +/- 1

12 +/- 4

Cdk9

4.2 +/- 1.6

3.2 +/- 1.4

26 +/- 6

IC50 of inhibition of HIV in HeLa 37 cells:

2.6

3

9.5

Hela37 cell cytotoxicity (LD50):

20

12.5

225

Hela37 therapeutic index:

7.7

4.2

23.7

PBL therapeutic index:

N/D

N/D

2.7

MDM therapeutic index:

N/D

N/D

1.7

  1. * as described in Peng et al (1998) Genes and Dev. 12: 755–762.
  2. N/D = not determined
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Retrovirology

ISSN: 1742-4690

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