Peptides having non-natural or modified amino acids

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

2078014

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

2078014

3

(w):D-Trp

(w)YDL

Synthetic

NA

12

µM

Protease inhibition

Enzyme inhibition assay

8783807

4

(w):D-Trp

(w)YEL

Synthetic

NA

27

µM

Protease inhibition

Enzyme inhibition assay

8783807

5

dimer

2x(LEAIPCSIPPEFLFGKPFVF)4

Human hemofiltrate

P4-CCR5

0.19±0.09

µM

Virus entry

ELISA

17448989

6

Ac:acetyl

Ac-EWYNQTKDLQQKFYEIIMDIEQNNVQGKKGIQQLQ-NH2

C-terminal HR2 domain of FIV gp45

CEM4/IIIb

>2.304

µM

Virus entry

Syncytial plaque-forming assay

12186891

7

Ac:acetyl

Ac-GEWYNQTKDLQQKFYEIIMDIEQNNVQGKKGIQQL-NH2

C-terminal HR2 domain of FIV gp44

CEM4/IIIb

>2.342

µM

Virus entry

Syncytial plaque-forming assay

12186891

8

Ac:acetyl

Ac-GNITLGEWYNQTKDLQQKFYEIIMDIEQNNVQG-NH2

C-terminal HR2 domain of FIV gp42

CEM4/IIIb

2.053

µM

Virus entry

Syncytial plaque-forming assay

12186891

9

Ac: acetyl

Ac-ISYNL

Synthetic

NA

70

µM

Protease inhibition

Enzyme inhibition assay

8783807

10

Ac:acetyl

Ac-ITLGEWYNQTKDLQQKFYEIIMDIEQNNVQGKKGI-NH2

C-terminal HR2 domain of FIV gp40

CEM4/IIIb

>2.365

µM

Virus entry

Syncytial plaque-forming assay

12186891

11

Ac: acetyl

Ac-LEAIPMSIPPEVKFNKPFVF

Human hemofiltrate

P4-CCR5

>100

µM

Virus entry

ELISA

17448989

12

Ac: acetyl, Am: amide

Ac-LEAIPMSIPPEVKFNKPFVF-Am

Human hemofiltrate

P4-CCR5

>100

µM

Virus entry

ELISA

17448989

13

Ac:acetyl

Ac-LGEWYNQTKDLQQKFYEIIMDIEQNNVQGKKGIQQ-NH2

C-terminal HR2 domain of FIV gp41

CEM4/IIIb

1.933

µM

Virus entry

Syncytial plaque-forming assay

12186891

14

Ac:acetyl

Ac-NITLGEWYNQTKDLQQKFYEIIMDIEQNNVQGK-NH2

C-terminal HR2 domain of FIV gp43

CEM4/IIIb

>2.473

µM

Virus entry

Syncytial plaque-forming assay

12186891

15

Ac:acetyl

Ac-NQTKDLQQKFYEIIMDIEQNNVQGKKGIQQLQKWE-NH2

C-terminal HR2 domain of FIV gp46

CEM4/IIIb

>2.322

µM

Virus entry

Syncytial plaque-forming assay

12186891

16

Ac: acetyl

Ac-NRGLAA

Synthetic

NA

>1000

µM

Protease inhibition

Enzyme inhibition assay

8783807

17

Ac:acetyl

Ac-QTKDLQQKFYEIIMDIEQNNVQGKKGIQQLQKWED-NH2

C-terminal HR2 domain of FIV gp47

CEM4/IIIb

>2.321

µM

Virus entry

Syncytial plaque-forming assay

12186891

18

Ac: acetyl

Ac-QVSQNY

Synthetic

NA

100

µM

Protease inhibition

Enzyme inhibition assay

8783807

19

Ac: acetyl

Ac-SYEL

Synthetic

NA

55

µM

Protease inhibition

Enzyme inhibition assay

8783807

20

Ac: acetyl

Ac-TVSFNF

Synthetic

NA

140

µM

Protease inhibition

Enzyme inhibition assay

8783807

21

Ac: acetyl

Ac-TVSYELN

Synthetic

NA

100

µM

Protease inhibition

Enzyme inhibition assay

8783807

22

Ac: acetyl

Ac-YDL

Synthetic

NA

9

µM

Protease inhibition

Enzyme inhibition assay

8783807

23

Ac: acetyl

Ac-YEL

Synthetic

NA

34

µM

Protease inhibition

Enzyme inhibition assay

8783807

24

Ac: acetyl

Ac-YEW

Synthetic

NA

21

µM

Protease inhibition

Enzyme inhibition assay

8783807

25

Amino group

AIGSILGALAKGLPTLISWIKNR-NH2

Rana tagoi

T cells

0

NA

Fusion inhibitor

GFP expression

16140737

26

Bio: biotinyl

Bio-CapTVSYEL

Synthetic

NA

3

µM

Protease inhibition

Enzyme inhibition assay

8783807

27

Bio: biotinyl

Bio-TVSYEL

Synthetic

NA

5

µM

Protease inhibition

Enzyme inhibition assay

8783807

28

Bio: biotinyl

Bio-YEL

Synthetic

NA

8

µM

Protease inhibition

Enzyme inhibition assay

8783807

29

Amino group

FFGKVLKLIRKIF-NH2

D76 (frog)

CEM-SS

0.63

µM

Multi-function

Formazan assay

20086159

30

Amino group

FISAIASMLGKFL-NH2

Rana catesbeiana

T cells

Low

NA

Fusion inhibitor

GFP expression

16140737

31

Amino group

GFGKAFHSVSNFAKKHKTA-NH2

Styelin A (tunicate)

CEM-SS

>48.5

µM

Multi-function

Formazan assay

20086159

32

Amino group

GFKDLLKGAAKALVKTVLF-NH2

Ascaphin-8 (frog)

CEM-SS

1.2

µM

Multi-function

Formazan assay

20086159

33

(I): D-Isoleucine, (L): D-Leucine

GFKRIVQR(I)KDF(L)RNLV

Cathelicidin

CEM-SS

47.5

µM

Multi-function

Cytopathic effect

18591279

34

(I): D-Isoleucine

GFKRIVQR(I)KDFLRNLV

Cathelicidin

CEM-SS

47.5

µM

Multi-function

Cytopathic effect

18591279

35

Amino group

GFKRIVQRIKDFLRNLV-NH2

NA

CEM-SS

0.76

µM

Multi-function

Formazan assay

20086159

36

Amino group

GFLSILKKVLPKVMAHMK-NH2

Melectin (insect)

CEM-SS

4.34

µM

Multi-function

Formazan assay

20086159

37

Amino group

GFNEIVQDIEDFLQNLV-NH2

NA

CEM-SS

>25.1

µM

Multi-function

Formazan assay

20086159

38

X: phenylglycine.

GIKEXKRIVQRIKDFLRNLV

Cathelicidin

CEM-SS

>40.6

µM

Multi-function

Cytopathic effect

18591279

39

Amino group

GIWDTIKSMGKVFAGKILQNL-NH2

Brevinin-2 related (frog)

CEM-SS

1.65

µM

Multi-function

Formazan assay

20086159

40

Amino group

GLADFLNKAVGKVVDFVKS-NH2

Desertcolin 1 (frog)

CEM-SS

>49.9

µM

Multi-function

Formazan assay

20086159

41

Amino group

GLFGVLAKVAAHVVPAIAEHF-NH2

Litoria genimaculata

T cells

80

%

Fusion inhibitor

GFP expression

16140737

42

Amino group

GLFGVLGSIAKHVLPHVVPVIAEKL-NH2

Litoria chloris

T cells

100

%

Fusion inhibitor

GFP expression

16140737

43

Amino group

GLLGLLGSVVSHVVPAIVGHF-NH2

Maculatin 1.3 (frog)

CEM-SS

4

µM

Multi-function

Formazan assay

20086159

44

Amino group

GLLSVLGSVAKHVLPHVVPVIAEHL-NH2

Litoria caerulea

T cells

95

%

Fusion inhibitor

GFP expression

16140737

45

Amino group

GLWQKIKSAAGDLASGIVEGIKS-NH2

Litoria caerulea

T cells

20

%

Fusion inhibitor

GFP expression

16140737

46

Amino group

GMASKAGAIAGKIAKVALKAL-NH2

PGLa (frog)

CEM-SS

>50.8

µM

Multi-function

Formazan assay

20086159

47

X: phenylglycine.

GRFKRXRKKXKKLFKKIS

Cathelicidin

CEM-SS

0.68

µM

Multi-function

Cytopathic effect

18591279

48

Fluorescein isothiocyanate

GTKWLTEWIPLTAEAEC-FITC

Pep-A/Synthetic

HeLa

2.7 ± 0.7

(Ki) µM

Reverse Transcriptase

RT-Polymerase Assay

18952602

49

Amino group

GVIDAAKKWNVLKNLF-NH2

Uperoleia mjobergii

T cells

20

%

Fusion inhibitor

GFP expression

16140737

50

Amino group

GWFDVVKHIAKRF-NH2

D70 (frog)

CEM-SS

2.99

µM

Multi-function

Formazan assay

20086159

51

Ibu: isobutyroyl

Ibu-TVSFNF

Synthetic

NA

<62

µM

Protease inhibition

Enzyme inhibition assay

8783807

52

Ibu: isobutyroyl

Ibu-TVSYEL

Synthetic

NA

6

µM

Protease inhibition

Enzyme inhibition assay

8783807

53

Ibu: isobutyroyl

Ibu-TVSYELNH

Synthetic

NA

175

µM

Protease inhibition

Enzyme inhibition assay

8783807

54

Amino group

IKWKKLLRAAKRIL-NH2

D74 (insect)

CEM-SS

>57.6

µM

Multi-function

Formazan assay

20086159

55

(b): benzyl

KEEIC(b)E(b)VEDQT(b)Y

V1J1 region of the CD4 molecule

CEM-SS

>500

µM

Fusion inhibitor

Cytopathic effect

2078014

56

p: D-proline

LEAIPCSIPpCFLFNKPFVF

Human hemofiltrate

P4-CCR5

0.20±0.04

µM

Virus entry

ELISA

17448989

57

p: D-proline

LEAIPCSIPpCFLFNKPFVF

Human hemofiltrate

P4-CCR5

High

NA

Virus entry

ELISA

17448989

58

p: D-proline

LEAIPCSIPpCVAFNKPFVF

Human hemofiltrate

P4-CCR5

0.94±0.54

µM

Virus entry

ELISA

17448989

59

p: D-proline

LEAIPCSIPpCVFFNKPFVF

Human hemofiltrate

P4-CCR5

0.33±0.07

µM

Virus entry

ELISA

17448989

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

17448989

61

p: D-proline

LEAIPMGIPpEVLFNKPFVF

Human hemofiltrate

P4-CCR5

High

NA

Virus entry

ELISA

17448989

62

Am: amide

LEAIPMSIPPEVKFNKPFVF-Am

Human hemofiltrate

P4-CCR5

>100

µM

Virus entry

ELISA

17448989

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

17448989

64

(Set): S-ethyl

LQITC(SEt)W

Synthetic

NA

12

µM

Protease inhibition

Enzyme inhibition assay

8783807

65

(w):D-Trp

LQITL(w)

Synthetic

NA

140

µM

Protease inhibition

Enzyme inhibition assay

8783807

66

Amino group

Natural mixture of peptides

Rana catesbeiana

T cells

25

%

Fusion inhibitor

GFP expression

16140737

67

Pam: palmitoyl

Pam-TVSFNF

Synthetic

NA

15

µM

Protease inhibition

Enzyme inhibition assay

8783807

68

Pam: palmitoyl

Pam-TVSYEL

Synthetic

NA

0.5

µM

Protease inhibition

Enzyme inhibition assay

8783807

69

Amino group

SLSRFLRFLKIVYRRAF-NH2

D98 (frog)

CEM-SS

0.83

µM

Multi-function

Formazan assay

20086159

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

2078014

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

2078014

72

(b): benzyl

T(b)EVE(b)lKC(b)QEDVE

V1J1 region of the CD4 molecule

CEM-SS

>500

µM

Fusion inhibitor

Cytopathic effect

2078014

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

2078014

74

(b): benzyl

T(b)Y(b)IC(b)EVEDQKEE

V1J1 region of the CD4 molecule

CEM-SS

63

µM

Fusion inhibitor

Cytopathic effect

2078014

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

2078014

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

2078014

77

(b): benzyl

T(b)YIC(b)E(b)VEDQKEE

V1J1 region of the CD4 molecule

CEM-SS

63

µM

Fusion inhibitor

Cytopathic effect

2078014

78

(b): benzyl

T(b)YIC(b)EVE(b)DOKEE

V1J1 region of the CD4 molecule

CEM-SS

>500

µM

Fusion inhibitor

Cytopathic effect

2078014

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

2078014

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

2078014

81

(b): benzyl

TYIC(b)E(b)VEDQKEE

V1J1 region of the CD4 molecule

CEM-SS

125

µM

Fusion inhibitor

Cytopathic effect

2078014

82

(b): benzyl

TYIC(b)EVEDQKEE

V1J1 region of the CD4 molecule

CEM-SS

>500

µM

Fusion inhibitor

Cytopathic effect

2078014

83

(Set): S-ethyl

VSYEC(SEt)G

Synthetic

NA

120

µM

Protease inhibition

Enzyme inhibition assay

8783807

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

22276994

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

22276994

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

22276994

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

22276994