Synthetic TAT peptides from LifeTein were used for fluorescence resonance energy transfer (FRET) assay. This arginine-rich TAT peptide contains two fluorophores with FAM at the N terminus and TAMRA at the C terminus.
Three alanines were used as a spacer to avoid potential interference on the binding affinity against TAR. The sequence used in this study is: (5‑FAM)‑ AAARKKRRQRRRAAA-K(TAMRA)‑C.
The Tat peptide causes two fluorophores to form a dimer, quenching the fluorescence of both fluorophores. When the Tat peptide is bound to the bulge of TAR, the peptide transitioned to the extended conformation.
In the study, researchers have identified 11 small molecule inhibitors of TAR‑Tat interaction from high throughput screening (HTS) and virtual screening (VS). One of the compounds showed promising anti‑HIV activity.
The hits from HTS and VS suggested that the HTS and VS are complimentary to each other. HTS and VS will boost the efficiency of the drug discovery.
http://scholar.google.com/scholar_url?hl=en&q=http://deepblue.lib.umich.edu/bitstream/handle/2027.42/108771/janghlee_1.pdf%3Fsequence%3D1%26isAllowed%3Dy&sa=X&scisig=AAGBfm20J8EkWT4LD8Rg3mQnJHE7mEZr_w&oi=scholaralrt
LifeTein, located in Somerset, New Jersey, was founded in 2008 with a simple vision: understanding life one protein at a time. This philosophy has formed the foundation of every peptide, antibody, protein, antibody, and chemical project that we have completed for our customers in the academic, biotechnology, agricultural, government institutions and pharmaceutical fields.
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