General Information


DRAVP ID  DRAVPe00835

Peptide Name   YIK-C16(625-656)

Sequence  EMTWEEWEKKIEEYIKKIEEILKKSQNQQIDLGSGX

Sequence Length  36

UniProt ID  No entry found 

Taxon ID  None

Source  Synthetic construct

Validation   Experimentally Validated



Origin Information


Gene Name/ID  Not Available

GenBank  Not Available

Amino Acid position  Not Available

Domain Accession ID  Not Available

Nucleotide sequence ID  Not Available

Molecular Type  Not Available

Chromosomal Position  Not Available



Activity Information


Target Organism  HIV

Assay  HIV-1-Mediated Cell-Cell Fusion Assay

Activity 

  • [Ref.30901967]HIV-1IIIB(X4 virus):inhibition of virus infection in MT-2 cells(IC50=76 pM);inhibition of cell-cell fusion between H9/IIIB cells and MT-2 cells(IC50=0.55 nM);
  • HIV-1Bal(R5 virus):inhibition of virus infection in MT-2 cells(IC50=61 pM);
  • HIV-1 NL4-3 D36G(6 T-20 resistant strains, WT,V38A,V38A/N42D,V38E/N42S,V38A/N42T,N42T/N43K):inhibition of virus infection in MT-2 cells(IC50=40-179 pM);
  • HIV-1 LAI (7 T2635-Resistant Strains,WT,A6V,Q66R,K90E,K154Q,Q79E/N126K,K90E/N126K):inhibition of virus infection in MT-2 cells(IC50=65-106 pM);
  • HIV-1 NL4-3 (5 HP23-Resistant Strains,WT,E49K,E49K/N126K,D36G/E49K/N126K,L34S/D36G/E49K/E136G):inhibition of virus infection in MT-2 cells(IC50=65-188 pM).

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

Cytotoxicity 

  • [Ref.30901967]No cytotoxicity against MT-2 or M7 cells at the concentrations as high as 8 μM.

Binding Target  membrane

Mechanism  It was a fusion inhibitor and inhibits cell-cell fusion



Structure Information


PDB ID  None

Predicted Structure Download  No predicted structure available

Linear/Cyclic  Linear

N-terminal Modification  Free

C-terminal Modification  Free

Other Modification  The 'X' at position 36 indicates PEG4-Lys-C16(Palmitic Acid).

Stereochemistry  L



Physicochemical Information


Formula  C191H301N47O61S

Absent amino acids  ACFHPRV

Common amino acids  E

Mass  4393.18

Pl  4.73

Basic residues  6

Acidic residues  9

Hydrophobic residues  9

Net charge  -3

Boman Index  -8594

Hydrophobicity  -119.72

Aliphatic Index  75.83

Half Life 

  •     Mammalian:1 hour
  •     Yeast:30 min
  •     E.coli:>10 hour

Extinction Coefficient cystines  12490

Absorbance 280nm  356.86

Polar residues  7



Literature Information


Literature 1

Title   A Peptide-Based HIV-1 Fusion Inhibitor with Two Tail-Anchors and Palmitic Acid Exhibits Substantially Improved In Vitro and Ex Vivo Anti-HIV-1 Activity and Prolonged In Vivo Half-Life.

Pubmed ID   30901967

Reference   Molecules. 2019 Mar 21;24(6):1134.

Author   Su S, Rasquinha G, Du L, Wang Q, Xu W, Li W, Lu L, Jiang S.

DOI   10.3390/molecules24061134