Table 2: Tat-based therapeutics.

Compound/classMechanism of actionReference(s)

DRBPurine nucleoside analog; inhibits cyclin-dependent kinases[23]
Flavopiridol (flavonoids)Inhibits cyclin-dependent kinases[24]
SeliciclibInhibits cyclin-dependent kinases[25]
2-O-Methyl/LNA oligoribonucleotidesBinds TAR[26]
Phosphodiester/phophothiote oligonucleotidesBinds TAR[27]
PNA-(TAR-16)Polyamide nucleotide analog; binds TAR[28]
AcetylpromazineBinds 5 bulge of TAR[29]
O,O-Bismyristoyl thiamine disulfideInhibits nuclear translocation of Tan and NF-κB, via interaction with cysteine region[30]
Cyclic peptidesMimics basic region and binds TAR[31]
Tat 9-K-biotin peptideBinds TAR[32]
CGP64222Peptoid/peptide similar to Tat-basic domain; binds TAR[33]
CGP40336A (polyamine-acridine based)Binds TAR[34]
Aminoglycoside-arginine conjugatesBinds TAR in the major groove of the bulge and upper portion of the stem[35]
Transdominant Tat mutantsBinds TAR[36]
Biscationic diphenylfuran derivativesBinds TAR[35]
Neomycin (aminoglycoside)Binds TAR, CXCR4, and other Tat targets[37]
D-penicillamineBinds Tat stably through cysteine residues[38]
Stilbene (CGA137053)Binds Tat directly[39]
Suramin and derivativesCompetes with heparin/heparin sulfate for binding to the basic region of Tat; inhibits extracellular functions of Tat[40]
Benzodiazepine derivativesGeneral inhibition of HIV-1 transcription and Tat transactivation[41, 42]
Benzothiophene derivatives[43]
Temacrazine (bistriazolonoacridones)[44]
Fluoroquinolone derivatives[45, 46]