General Information

General Information

DRAVP ID DRAVPe00660

Peptide Name LP-65

Sequence IEELLKKAEEQQKKNEEELKKLEX

Sequence Length 24

UniProt ID P03377

Source Synthetic construct

Activity Information

Target Organism HIV

Assay cell-fusion assay,single-cycle infection assay

Activity

[Ref.30089693]HIV-1 HXB2:inhibition of cell-cell fusion in TZM-bl cells(IC50=14±3 pM);
HIV-1 NL4-3:inhibition of pseudovirus infection in TZM-bl cells(IC50=8±3 pM);
HIV-1 JRCSF:inhibition of virus infection in TZM-bl cells(IC50=7±2 pM);
T-20 sensitive HIV-1(NL4-3D36G):inhibition of virus infection in TZM-bl cells(IC50<0.01 nM);
T-20 resistant HIV-1 NL4-3(WT,I37T,V38A,V38 M,Q40H,N43K,G36S/V38 M,I37T/N43K,V38A/N42T):inhibition of virus infection in TZM-bl cells(IC50=0.15-88.63 nM);
HIV-2(ROD,ST):inhibition of virus infection in TZM-bl cells(IC50=0.23-0.75 nM);
SIV(239,PBJ):inhibition of virus infection in TZM-bl cells(IC50=0.07-0.04 nM);
HIV-1(3 A, 13 B, 7 C, 1 G, 1 A/C, 5 A/E, 6 B/C pseudovirus subtypes):inhibition of pseudovirus infection in TZM-bl cells(IC50=35 pM).

Hemolytic Activity No hemolysis information or data found in the reference(s) presented in this entry

Cytotoxicity

[Ref.30089693]TZM-bl cell:CC50=256.23 ±14.58 μM;
MT-4 cell:CC50=213.4±59.59 μM;
HEK293T cell:CC50=208.43± 22.9μM;
PBMC:CC50=49.95± 2.97 μM.

Binding Target membrane

Mechanism The peptide acts by binding to the heptad repeat 1 (HR1) region of gp41 and preventing the interaction of the HR1 and HR2 domains, which is required for virus–cell fusion.(By similar)

Structure Information

PDB ID None

Predicted Structure Download No predicted structure available

Linear/Cyclic Linear

N-terminal Modification Acetylation

C-terminal Modification Amidation

Other Modification The 'X' at position 24 is Lys-C16(palmitic acid)

Stereochemistry L

Physicochemical Information

Formula C123H210N32O42

Absent amino acids CDFGHMPRSTVWY

Common amino acids E

Mass 2938.56

Pl 4.94

Basic residues 6

Acidic residues 8

Hydrophobic residues 6

Net charge -2

Boman Index -7909

Hydrophobicity -168.33

Aliphatic Index 85.42

Half Life

Mammalian:20 hour
Yeast:30 min
E.coli:>10 hour

Extinction Coefficient cystines 0

Absorbance 280nm 0

Polar residues 1

Literature Information

Literature 1

Title Structural and Functional Characterization of Membrane Fusion Inhibitors with Extremely Potent Activity against Human Immunodeficiency Virus Type 1 (HIV-1), HIV-2, and Simian Immunodeficiency Virus.

Pubmed ID 30089693

Reference J Virol. 2018 Sep 26;92(20):e01088-18.

Author Chong H, Zhu Y, Yu D, He Y.

DOI 10.1128/JVI.01088-18