|
Compound/class | Mechanism of action | Reference(s) |
|
DRB | Purine nucleoside analog; inhibits cyclin-dependent kinases | [23] |
Flavopiridol (flavonoids) | Inhibits cyclin-dependent kinases | [24] |
Seliciclib | Inhibits cyclin-dependent kinases | [25] |
2′-O-Methyl/LNA oligoribonucleotides | Binds TAR | [26] |
Phosphodiester/phophothiote oligonucleotides | Binds TAR | [27] |
PNA-(TAR-16) | Polyamide nucleotide analog; binds TAR | [28] |
Acetylpromazine | Binds 5′ bulge of TAR | [29] |
O,O′-Bismyristoyl thiamine disulfide | Inhibits nuclear translocation of Tan and NF-κB, via interaction with cysteine region | [30] |
Cyclic peptides | Mimics basic region and binds TAR | [31] |
Tat 9-K-biotin peptide | Binds TAR | [32] |
CGP64222 | Peptoid/peptide similar to Tat-basic domain; binds TAR | [33] |
CGP40336A (polyamine-acridine based) | Binds TAR | [34] |
Aminoglycoside-arginine conjugates | Binds TAR in the major groove of the bulge and upper portion of the stem | [35] |
Transdominant Tat mutants | Binds TAR | [36] |
Biscationic diphenylfuran derivatives | Binds TAR | [35] |
Neomycin (aminoglycoside) | Binds TAR, CXCR4, and other Tat targets | [37] |
D-penicillamine | Binds Tat stably through cysteine residues | [38] |
Stilbene (CGA137053) | Binds Tat directly | [39] |
Suramin and derivatives | Competes with heparin/heparin sulfate for binding to the basic region of Tat; inhibits extracellular functions of Tat | [40] |
Benzodiazepine derivatives | General inhibition of HIV-1 transcription and Tat transactivation | [41, 42] |
Benzothiophene derivatives | — | [43] |
Temacrazine (bistriazolonoacridones) | — | [44] |
Fluoroquinolone derivatives | — | [45, 46] |
|