Table 2: Tat-based therapeutics.

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]