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Table 2 The influence of multiple Tat amino acid substitutions on Tat-TAR binding affinity

From: HIV-1 Tat amino acid residues that influence Tat-TAR binding affinity: a scoping review

Tat amino acid region

Mutation

Binding affinity (Kd)

Percentage increase/decrease in binding affinity

Technique

References

30–46

C34S, C37W

7.16 × 10−8 M

19.7% decrease

Nuclear Magnetic Resonance Spectroscopy (NMR) and Fluorescence spectroscopy

[70]

47–58

R49A, Q54A

1.7 × 10−7 M

142% decrease

Fluorescence resonance energy transfer (FRET), MALDI-TOFMS and Fluorescence binding assay

[82]

R52A, R53A

 > 100 X 10−9 M

 > 1566% decrease

Electrophoretic mobility shift assay (EMSA)

[69]

R55A, R56A

 > 100 X 10−9 M

 > 1566% decrease

EMSA

[69]

R55K, R56K

4 × 10−9 M

33% increase

EMSA

[69]

R52K, R53K

13 X 10−9 M

116% decrease

EMSA

[69]

R52A, R55A

 > 100 X 10−9 M

 > 1566% decrease

EMSA

[69]

R52A, R56A

 > 100 X 10−9 M

 > 1566% decrease

EMSA

[69]

R53A, R55A

 > 100 X 10−9 M

 > 1566% decrease

EMSA

[69]

R53A, R56A

 > 100 X 10−9 M

 > 1566% decrease

EMSA

[69]

K50A, K51A, Q54A

2.9 × 10−6 M

4042% decrease

FRET, MALDI-TOFMS and Fluorescence binding assay

[82]

R49K, R55K, R56K, R57K

5 × 10−10 M

25% decrease

Gel electrophoresis and circular dichroism (CD)

[83]

R49A, K50A, K51A, Q54A

1.8 × 10−5 M

21,328.6% decrease

FRET, MALDI-TOFMS and Fluorescence binding assay

[82]

R49K, R53K, R55K, R56K, R57K

9 × 10−10 M

125% decrease

Gel electrophoresis and CD

[83]

R49K, Q54K, R55K, R56K, R57K

1.8 × 10−9 M

350% decrease

Gel electrophoresis and CD

[83]

R49K, R52K, R53K, R56K, R57K

 > 5 × 10−8 M

 > 12,400% decrease

Gel electrophoresis and CD

[83]

R49K, R52K, R53K, R55K, R57K

 > 1 × 10−7 M

 > 24,900% decrease

Gel electrophoresis and CD

[83]

R49K, R53K, Q54K, R55K, R56K, R57K

7 × 10−10 M

75% decrease

Gel electrophoresis and CD

[83]

R49K, R52K, R54K, R55K, R56K, R57K

3.5 × 10−9 M

775% decrease

Gel electrophoresis and CD

[83]

R49K, R52K, R53K, R55K, R56K, R57K

3.2 × 10–8

1428% decrease

EMSA and Anisotropy assay

[84]

R49A, K50A, Q54A, K51R, R53A, Q54R, R57A

6.6 × 10−5 M

94,185% decreased

FRET, MALDI-TOFMS and Fluorescence binding assay

[82]

R49A, K50A, R51R, R53A, Q54R, R56A, R57A

No binding

No binding

FRET, MALDI-TOFMS and Fluorescence binding assay

[82]

R49A, K50A, K51R, R53A, Q54R, R55A, R56A, R57A

No binding

No binding

FRET, MALDI-TOFMS and Fluorescence binding assay

[82]

G48K, R49K, R52K, R53K, Q54K, R55K, R56K, R57A

1.5 × 10–6 M

275% decrease

Electron paramagnetic resonance

spectroscopy (EPR)

[72]