DRAVP ID  DRAVPe00835

Peptide Name   YIK-C16(625-656)

Sequence  EMTWEEWEKKIEEYIKKIEEILKKSQNQQIDLGSGX

Sequence Length  36

UniProt ID  No entry found 

Source  Synthetic construct

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

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

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