Impact of Tat Genetic Variation on HIV-1 Disease

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]