S.No. |
Modification |
Sequence |
Source |
Cell line |
Inhibition/IC50 |
Unit |
Target |
Assay |
Reference |
1 |
(ac):acetyl,
(b): benzyl, (K): D-lysine |
(ac)T(b)YIC(b)E(b)VEDQ(K)(ac)EE(a) |
V1J1
region of the CD4 molecule |
CEM-SS |
16 |
µM |
Fusion
inhibitor |
Cytopathic effect |
|
2 |
(ac):acetyl, (b): benzyl, (a): amide,
(ac): acetyl |
(ac)T(b)YIC(b)E(b)VEDQK(ac)EE(a) |
V1J1 region of the CD4 molecule |
CEM-SS |
16 |
µM |
Fusion inhibitor |
Cytopathic effect |
|
3 |
(w):D-Trp |
(w)YDL |
Synthetic |
NA |
12 |
µM |
Protease inhibition |
Enzyme
inhibition assay |
|
4 |
(w):D-Trp |
(w)YEL |
Synthetic |
NA |
27 |
µM |
Protease inhibition |
Enzyme inhibition assay |
|
5 |
dimer |
2x(LEAIPCSIPPEFLFGKPFVF)4 |
Human hemofiltrate |
P4-CCR5 |
0.19±0.09 |
µM |
Virus
entry |
ELISA |
|
6 |
Ac:acetyl |
Ac-EWYNQTKDLQQKFYEIIMDIEQNNVQGKKGIQQLQ-NH2 |
C-terminal HR2 domain of FIV gp45 |
CEM4/IIIb |
>2.304 |
µM |
Virus entry |
Syncytial plaque-forming assay |
|
7 |
Ac:acetyl |
Ac-GEWYNQTKDLQQKFYEIIMDIEQNNVQGKKGIQQL-NH2 |
C-terminal
HR2 domain of FIV gp44 |
CEM4/IIIb |
>2.342 |
µM |
Virus
entry |
Syncytial plaque-forming assay |
|
8 |
Ac:acetyl |
Ac-GNITLGEWYNQTKDLQQKFYEIIMDIEQNNVQG-NH2 |
C-terminal HR2 domain of FIV gp42 |
CEM4/IIIb |
2.053 |
µM |
Virus entry |
Syncytial plaque-forming assay |
|
9 |
Ac:
acetyl |
Ac-ISYNL |
Synthetic |
NA |
70 |
µM |
Protease inhibition |
Enzyme
inhibition assay |
|
10 |
Ac:acetyl |
Ac-ITLGEWYNQTKDLQQKFYEIIMDIEQNNVQGKKGI-NH2 |
C-terminal HR2 domain of FIV gp40 |
CEM4/IIIb |
>2.365 |
µM |
Virus entry |
Syncytial plaque-forming assay |
|
11 |
Ac:
acetyl |
Ac-LEAIPMSIPPEVKFNKPFVF |
Human hemofiltrate |
P4-CCR5 |
>100 |
µM |
Virus
entry |
ELISA |
|
12 |
Ac: acetyl, Am: amide |
Ac-LEAIPMSIPPEVKFNKPFVF-Am |
Human hemofiltrate |
P4-CCR5 |
>100 |
µM |
Virus entry |
ELISA |
|
13 |
Ac:acetyl |
Ac-LGEWYNQTKDLQQKFYEIIMDIEQNNVQGKKGIQQ-NH2 |
C-terminal
HR2 domain of FIV gp41 |
CEM4/IIIb |
1.933 |
µM |
Virus
entry |
Syncytial plaque-forming assay |
|
14 |
Ac:acetyl |
Ac-NITLGEWYNQTKDLQQKFYEIIMDIEQNNVQGK-NH2 |
C-terminal HR2 domain of FIV gp43 |
CEM4/IIIb |
>2.473 |
µM |
Virus entry |
Syncytial plaque-forming assay |
|
15 |
Ac:acetyl |
Ac-NQTKDLQQKFYEIIMDIEQNNVQGKKGIQQLQKWE-NH2 |
C-terminal
HR2 domain of FIV gp46 |
CEM4/IIIb |
>2.322 |
µM |
Virus
entry |
Syncytial plaque-forming assay |
|
16 |
Ac: acetyl |
Ac-NRGLAA |
Synthetic |
NA |
>1000 |
µM |
Protease inhibition |
Enzyme inhibition assay |
|
17 |
Ac:acetyl |
Ac-QTKDLQQKFYEIIMDIEQNNVQGKKGIQQLQKWED-NH2 |
C-terminal
HR2 domain of FIV gp47 |
CEM4/IIIb |
>2.321 |
µM |
Virus
entry |
Syncytial plaque-forming assay |
|
18 |
Ac: acetyl |
Ac-QVSQNY |
Synthetic |
NA |
100 |
µM |
Protease inhibition |
Enzyme inhibition assay |
|
19 |
Ac:
acetyl |
Ac-SYEL |
Synthetic |
NA |
55 |
µM |
Protease inhibition |
Enzyme
inhibition assay |
|
20 |
Ac: acetyl |
Ac-TVSFNF |
Synthetic |
NA |
140 |
µM |
Protease inhibition |
Enzyme inhibition assay |
|
21 |
Ac:
acetyl |
Ac-TVSYELN |
Synthetic |
NA |
100 |
µM |
Protease inhibition |
Enzyme
inhibition assay |
|
22 |
Ac: acetyl |
Ac-YDL |
Synthetic |
NA |
9 |
µM |
Protease inhibition |
Enzyme inhibition assay |
|
23 |
Ac:
acetyl |
Ac-YEL |
Synthetic |
NA |
34 |
µM |
Protease inhibition |
Enzyme
inhibition assay |
|
24 |
Ac: acetyl |
Ac-YEW |
Synthetic |
NA |
21 |
µM |
Protease inhibition |
Enzyme inhibition assay |
|
25 |
Amino
group |
AIGSILGALAKGLPTLISWIKNR-NH2 |
Rana tagoi |
T cells |
0 |
NA |
Fusion
inhibitor |
GFP
expression |
|
26 |
Bio: biotinyl |
Bio-CapTVSYEL |
Synthetic |
NA |
3 |
µM |
Protease inhibition |
Enzyme inhibition assay |
|
27 |
Bio: biotinyl |
Bio-TVSYEL |
Synthetic |
NA |
5 |
µM |
Protease inhibition |
Enzyme
inhibition assay |
|
28 |
Bio: biotinyl |
Bio-YEL |
Synthetic |
NA |
8 |
µM |
Protease inhibition |
Enzyme inhibition assay |
|
29 |
Amino
group |
FFGKVLKLIRKIF-NH2 |
D76
(frog) |
CEM-SS |
0.63 |
µM |
Multi-function |
Formazan assay |
|
30 |
Amino group |
FISAIASMLGKFL-NH2 |
Rana catesbeiana |
T cells |
Low |
NA |
Fusion inhibitor |
GFP expression |
|
31 |
Amino
group |
GFGKAFHSVSNFAKKHKTA-NH2 |
Styelin A (tunicate) |
CEM-SS |
>48.5 |
µM |
Multi-function |
Formazan assay |
|
32 |
Amino group |
GFKDLLKGAAKALVKTVLF-NH2 |
Ascaphin-8 (frog) |
CEM-SS |
1.2 |
µM |
Multi-function |
Formazan assay |
|
33 |
(I): D-Isoleucine, (L): D-Leucine |
GFKRIVQR(I)KDF(L)RNLV |
Cathelicidin |
CEM-SS |
47.5 |
µM |
Multi-function |
Cytopathic effect |
|
34 |
(I): D-Isoleucine |
GFKRIVQR(I)KDFLRNLV |
Cathelicidin |
CEM-SS |
47.5 |
µM |
Multi-function |
Cytopathic effect |
|
35 |
Amino
group |
GFKRIVQRIKDFLRNLV-NH2 |
NA |
CEM-SS |
0.76 |
µM |
Multi-function |
Formazan assay |
|
36 |
Amino group |
GFLSILKKVLPKVMAHMK-NH2 |
Melectin (insect) |
CEM-SS |
4.34 |
µM |
Multi-function |
Formazan assay |
|
37 |
Amino
group |
GFNEIVQDIEDFLQNLV-NH2 |
NA |
CEM-SS |
>25.1 |
µM |
Multi-function |
Formazan assay |
|
38 |
X: phenylglycine. |
GIKEXKRIVQRIKDFLRNLV |
Cathelicidin |
CEM-SS |
>40.6 |
µM |
Multi-function |
Cytopathic effect |
|
39 |
Amino
group |
GIWDTIKSMGKVFAGKILQNL-NH2 |
Brevinin-2
related (frog) |
CEM-SS |
1.65 |
µM |
Multi-function |
Formazan assay |
|
40 |
Amino group |
GLADFLNKAVGKVVDFVKS-NH2 |
Desertcolin 1 (frog) |
CEM-SS |
>49.9 |
µM |
Multi-function |
Formazan assay |
|
41 |
Amino
group |
GLFGVLAKVAAHVVPAIAEHF-NH2 |
Litoria genimaculata |
T cells |
80 |
% |
Fusion
inhibitor |
GFP
expression |
|
42 |
Amino group |
GLFGVLGSIAKHVLPHVVPVIAEKL-NH2 |
Litoria chloris |
T cells |
100 |
% |
Fusion inhibitor |
GFP expression |
|
43 |
Amino
group |
GLLGLLGSVVSHVVPAIVGHF-NH2 |
Maculatin 1.3 (frog) |
CEM-SS |
4 |
µM |
Multi-function |
Formazan assay |
|
44 |
Amino group |
GLLSVLGSVAKHVLPHVVPVIAEHL-NH2 |
Litoria caerulea |
T cells |
95 |
% |
Fusion inhibitor |
GFP expression |
|
45 |
Amino
group |
GLWQKIKSAAGDLASGIVEGIKS-NH2 |
Litoria caerulea |
T cells |
20 |
% |
Fusion
inhibitor |
GFP
expression |
|
46 |
Amino group |
GMASKAGAIAGKIAKVALKAL-NH2 |
PGLa (frog) |
CEM-SS |
>50.8 |
µM |
Multi-function |
Formazan assay |
|
47 |
X: phenylglycine. |
GRFKRXRKKXKKLFKKIS |
Cathelicidin |
CEM-SS |
0.68 |
µM |
Multi-function |
Cytopathic effect |
|
48 |
Fluorescein isothiocyanate |
GTKWLTEWIPLTAEAEC-FITC |
Pep-A/Synthetic |
HeLa |
2.7 ± 0.7 |
(Ki)
µM |
Reverse Transcriptase |
RT-Polymerase Assay |
|
49 |
Amino
group |
GVIDAAKKWNVLKNLF-NH2 |
Uperoleia mjobergii |
T cells |
20 |
% |
Fusion
inhibitor |
GFP
expression |
|
50 |
Amino group |
GWFDVVKHIAKRF-NH2 |
D70 (frog) |
CEM-SS |
2.99 |
µM |
Multi-function |
Formazan assay |
|
51 |
Ibu: isobutyroyl |
Ibu-TVSFNF |
Synthetic |
NA |
<62 |
µM |
Protease inhibition |
Enzyme
inhibition assay |
|
52 |
Ibu: isobutyroyl |
Ibu-TVSYEL |
Synthetic |
NA |
6 |
µM |
Protease inhibition |
Enzyme inhibition assay |
|
53 |
Ibu: isobutyroyl |
Ibu-TVSYELNH |
Synthetic |
NA |
175 |
µM |
Protease inhibition |
Enzyme
inhibition assay |
|
54 |
Amino group |
IKWKKLLRAAKRIL-NH2 |
D74 (insect) |
CEM-SS |
>57.6 |
µM |
Multi-function |
Formazan assay |
|
55 |
(b):
benzyl |
KEEIC(b)E(b)VEDQT(b)Y |
V1J1
region of the CD4 molecule |
CEM-SS |
>500 |
µM |
Fusion
inhibitor |
Cytopathic effect |
|
56 |
p: D-proline |
LEAIPCSIPpCFLFNKPFVF |
Human hemofiltrate |
P4-CCR5 |
0.20±0.04 |
µM |
Virus entry |
ELISA |
|
57 |
p: D-proline |
LEAIPCSIPpCFLFNKPFVF |
Human hemofiltrate |
P4-CCR5 |
High |
NA |
Virus
entry |
ELISA |
|
58 |
p: D-proline |
LEAIPCSIPpCVAFNKPFVF |
Human hemofiltrate |
P4-CCR5 |
0.94±0.54 |
µM |
Virus entry |
ELISA |
|
59 |
p: D-proline |
LEAIPCSIPpCVFFNKPFVF |
Human hemofiltrate |
P4-CCR5 |
0.33±0.07 |
µM |
Virus
entry |
ELISA |
|
60 |
p: D-proline,
Tic:tetrahydro-isoquinoline-3-carboxylic acid |
LEAIPMGIPpEV(L-Tic)FNKPFVF |
Human hemofiltrate |
P4-CCR5 |
0.28±0.08 |
µM |
Virus entry |
ELISA |
|
61 |
p: D-proline |
LEAIPMGIPpEVLFNKPFVF |
Human hemofiltrate |
P4-CCR5 |
High |
NA |
Virus
entry |
ELISA |
|
62 |
Am: amide |
LEAIPMSIPPEVKFNKPFVF-Am |
Human hemofiltrate |
P4-CCR5 |
>100 |
µM |
Virus entry |
ELISA |
|
63 |
p: D-proline, Tic:tetrahydro-isoquinoline-3-carboxylic acid |
LEKIPMSIPpEV(L-Tic)FNKPFVF |
Human hemofiltrate |
P4-CCR5 |
0.41±0.13 |
µM |
Virus
entry |
ELISA |
|
64 |
(Set): S-ethyl |
LQITC(SEt)W |
Synthetic |
NA |
12 |
µM |
Protease inhibition |
Enzyme inhibition assay |
|
65 |
(w):D-Trp |
LQITL(w) |
Synthetic |
NA |
140 |
µM |
Protease inhibition |
Enzyme
inhibition assay |
|
66 |
Amino group |
Natural mixture of peptides |
Rana catesbeiana |
T cells |
25 |
% |
Fusion inhibitor |
GFP expression |
|
67 |
Pam: palmitoyl |
Pam-TVSFNF |
Synthetic |
NA |
15 |
µM |
Protease inhibition |
Enzyme
inhibition assay |
|
68 |
Pam: palmitoyl |
Pam-TVSYEL |
Synthetic |
NA |
0.5 |
µM |
Protease inhibition |
Enzyme inhibition assay |
|
69 |
Amino
group |
SLSRFLRFLKIVYRRAF-NH2 |
D98
(frog) |
CEM-SS |
0.83 |
µM |
Multi-function |
Formazan assay |
|
70 |
(b): benzyl, (Y): D-tyrosine |
T(b)(Y)IC(b)EVE(b)DQKEE |
V1J1 region of the CD4 molecule |
CEM-SS |
125 |
µM |
Fusion inhibitor |
Cytopathic effect |
|
71 |
(b):
benzyl, (Y): D-tyrosine |
T(b)(Y)YIC(b)E(b)VEDQKEE |
V1J1
region of the CD4 molecule |
CEM-SS |
250 |
µM |
Fusion
inhibitor |
Cytopathic effect |
|
72 |
(b): benzyl |
T(b)EVE(b)lKC(b)QEDVE |
V1J1 region of the CD4 molecule |
CEM-SS |
>500 |
µM |
Fusion inhibitor |
Cytopathic effect |
|
73 |
(b):
benzyl |
T(b)EYE(b)lKC(b)QE(b)DVE |
V1J1
region of the CD4 molecule |
CEM-SS |
125-250 |
µM |
Fusion
inhibitor |
Cytopathic effect |
|
74 |
(b): benzyl |
T(b)Y(b)IC(b)EVEDQKEE |
V1J1 region of the CD4 molecule |
CEM-SS |
63 |
µM |
Fusion inhibitor |
Cytopathic effect |
|
75 |
(b):
benzyl |
T(b)YIC(b)E(b)KVQDE£E |
V1J1
region of the CD4 molecule |
CEM-SS |
63 |
µM |
Fusion
inhibitor |
Cytopathic effect |
|
76 |
(b): benzyl |
T(b)YIC(b)E(b)KVQDE£E |
V1J1 region of the CD4 molecule |
CEM-SS |
63-132 |
µM |
Fusion inhibitor |
Cytopathic effect |
|
77 |
(b):
benzyl |
T(b)YIC(b)E(b)VEDQKEE |
V1J1
region of the CD4 molecule |
CEM-SS |
63 |
µM |
Fusion
inhibitor |
Cytopathic effect |
|
78 |
(b): benzyl |
T(b)YIC(b)EVE(b)DOKEE |
V1J1 region of the CD4 molecule |
CEM-SS |
>500 |
µM |
Fusion inhibitor |
Cytopathic effect |
|
79 |
(b):
benzyl |
T(b)YIC(b)EVE(b)DQ(d)KEE |
V1J1
region of the CD4 molecule |
CEM-SS |
32 |
µM |
Fusion
inhibitor |
Cytopathic effect |
|
80 |
(b): benzyl (acm):
acetamidomethyl |
T(b)YlC(acm)E(b)VEDQKEE |
V1J1 region of the CD4 molecule |
CEM-SS |
>500 |
µM |
Fusion inhibitor |
Cytopathic effect |
|
81 |
(b):
benzyl |
TYIC(b)E(b)VEDQKEE |
V1J1
region of the CD4 molecule |
CEM-SS |
125 |
µM |
Fusion
inhibitor |
Cytopathic effect |
|
82 |
(b): benzyl |
TYIC(b)EVEDQKEE |
V1J1 region of the CD4 molecule |
CEM-SS |
>500 |
µM |
Fusion inhibitor |
Cytopathic effect |
|
83 |
(Set):
S-ethyl |
VSYEC(SEt)G |
Synthetic |
NA |
120 |
µM |
Protease inhibition |
Enzyme inhibition
assay |
|
84 |
Cyclic |
cyclo(d-Ala-d-Phe-d-Phe-Ile-Arg-Trp-d-Ala-d-Ala-d-Ala-Glu)-Lys |
Synthetic |
NA |
5.3± 0.8 |
µM |
Reverse transcription primer |
Fluorescence anisotropy |
|
85 |
Fpa: Fluorophenylalanine, Nle: Norleucine |
cyclo(d-Ala-Trp-Tyr-Gln-Fpa-Nle-d-Ala-d-Ala-d-Ala-Glu)-Lys |
Synthetic |
NA |
0.61± 0.04 |
µM |
Reverse
transcription primer |
Fluorescence
anisotropy |
|
86 |
Phg: Phenylglycine |
cyclo(d-Ala-Thr-Tyr-Tyr-Trp-Phg-d-Ala-d-Ala-d-Ala-Glu)-Lys |
Synthetic |
NA |
23± 3 |
µM |
Reverse transcription primer |
Fluorescence anisotropy |
|
87 |
Fpa: Fluorophenylalanine |
cyclo(d-Ala-Ile-Fpa-Arg-Tyr-Trp-d-Ala-d-Ala-Glu)-Lys |
Synthetic |
NA |
0.91± 0.1 |
µM |
Reverse
transcription primer |
Fluorescence
anisotropy |