DRAVP ID  DRAVPe00740

Peptide Name   SAH-gp41(626-662) A,B

Sequence  XTWXEWDXEINNYTSLIHSLIEESQNQXEKNXQELLE

Sequence Length  37

UniProt ID  P04582 

Source  Synthetic construct

Target Organism  HIV

Assay  luciferase assay

Activity 

• [Ref.20660316]HIV-1 HxB2:inhibition of virus infection in Cf2Th-CD4-CXCR4 cells(IC50=2.5±0.2 nM);
• HIV-1 YU2:inhibition of virus infection in Cf2Th-CD4-CCR5 cells(IC50=87±30 nM);
• HIV-1 V38A/N42T:inhibition of virus infection in Cf2Th-CD4-CXCR4 cells(IC50=10.7±2.2 nM);
• HIV-1 V38E/N42S:inhibition of virus infection in Cf2Th-CD4-CXCR4 cells(IC50=16.1±3.9 nM).

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

Cytotoxicity 

• No cytotoxicity information or data found in the reference(s) presented in this entry

Binding Target  Not found

Mechanism  The peptide disrupts assembly of the six-helix bundle viral fusion apparatus by mimicking the heptad repeat 2 (HR2) oligomerization domain of the gp41 envelope glycoprotein.

PDB ID  None

Predicted Structure Download  No predicted structure available

Linear/Cyclic  Cyclic

N-terminal Modification  Free

C-terminal Modification  Free

Other Modification  The 'X' at position 1 indicates Norleucine,the 'X' at position 4,8.28,32 indicates S-2-(4'-pentenyl) alanine. X(4) and X (5), X(28) and X (32) are cross-linked by hydrocarbon stapling.

Stereochemistry  L

Literature 1

Title   Hydrocarbon double-stapling remedies the proteolytic instability of a lengthy peptide therapeutic.

Pubmed ID   20660316

Reference   Proc Natl Acad Sci U S A. 2010 Aug 10;107(32):14093-8.

Author   Bird GH, Madani N, Perry AF, Princiotto AM, Supko JG, He X, Gavathiotis E, Sodroski JG, Walensky LD.

DOI   10.1073/pnas.1002713107