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Chemical Compound Review:

CHEMBL289969 1H-indol-2-yl-[4-[3-(propan- 2...

Synonyms: AG-K-19621, SureCN14440008, CTK4C5892, AR-1C3594, U-88204, ...

Althaus, I.W. et al., Fan, N. et al., Vasudevachari, M.B. et al.

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Disease relevance of U-88204E

These data thus demonstrate the unique specificity of U-88204E for HIV-1 RT [1].

High impact information on U-88204E

The potency of U-88204E on the RNA-directed DNA polymerase activity depends on the base composition of the template:primer [1].
The bis(heteroaryl)piperazine U-88204E is a potent inhibitor of HIV-1 reverse transcriptase (RT) and possesses excellent anti-HIV activity in HIV-1-infected lymphocytes grown in tissue culture [1].
Three BHAPs (U-88204E, U-87201E, and U-90125S) and the pyridinone L-697,661 were selected to quantitatively assess the effects of these amino acid substitutions on sensitization to L-697,661 and resistance to the BHAPs [2].

Analytical, diagnostic and therapeutic context of U-88204E

Serial passage of a laboratory strain and a primary isolate of HIV-1 in cell culture in the presence of increasing concentrations of U-88204 yielded virus populations which were at least 100-fold resistant to the drug [3].

References

Kinetic studies with the non-nucleoside HIV-1 reverse transcriptase inhibitor U-88204E. Althaus, I.W., Chou, J.J., Gonzales, A.J., Deibel, M.R., Chou, K.C., Kezdy, F.J., Romero, D.L., Palmer, J.R., Thomas, R.C., Aristoff, P.A. Biochemistry (1993) [Pubmed]
Mechanism of resistance to U-90152S and sensitization to L-697,661 by a proline to leucine change at residue 236 of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. Fan, N., Evans, D.B., Rank, K.B., Thomas, R.C., Tarpley, W.G., Sharma, S.K. FEBS Lett. (1995) [Pubmed]
Prevention of the spread of HIV-1 infection with nonnucleoside reverse transcriptase inhibitors. Vasudevachari, M.B., Battista, C., Lane, H.C., Psallidopoulos, M.C., Zhao, B., Cook, J., Palmer, J.R., Romero, D.L., Tarpley, W.G., Salzman, N.P. Virology (1992) [Pubmed]

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