General Information

General Information

DRAVP ID DRAVPe00785

Peptide Name LP-52

Sequence WEQKIEELLKKAEEQQKKNEEELKKLEX

Sequence Length 28

UniProt ID P03377

Source Synthetic construct

Activity Information

Target Organism HIV,SIV

Assay cell-fusion assay,single-cycle infection assay

Activity

[Ref.30089693]HIV-1 HXB2:inhibition of cell-cell fusion in TZM-bl cells(IC50=13±1 pM);
HIV-1 NL4-3:inhibition of pseudovirus infection in TZM-bl cells(IC50=4±0 pM);
HIV-1 JRCSF:inhibition of virus infection in TZM-bl cells(IC50=5±1 pM);
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=17 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=0.01-1.86 nM);
HIV-2(ROD,ST):inhibition of virus infection in TZM-bl cells(IC50=0.06-0.34 nM);
SIV(239,PBJ):inhibition of virus infection in TZM-bl cells(IC50=0.01-0.04 nM).

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

Cytotoxicity

[Ref.30089693]TZM-bl cell:CC50=112.9 ± 2.21 μM;
MT-4 cell:CC50=94.06± 4.97 μM;
HEK293T cell:CC50=88.86± 6.68μM;
PBMC:CC50=114.8± 12.68 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 28 is Lys-C16(palmitic acid)

Stereochemistry L

Physicochemical Information

Formula C150H247N39O49

Absent amino acids CDFGHMPRSTVY

Common amino acids E

Mass 3510.19

Pl 5

Basic residues 7

Acidic residues 9

Hydrophobic residues 7

Net charge -2

Boman Index -9466

Hydrophobicity -186.43

Aliphatic Index 73.21

Half Life

Mammalian:2.8 hour
Yeast:3 min
E.coli:2 min

Extinction Coefficient cystines 5500

Absorbance 280nm 203.7

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